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Chemistry

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Also known as: 5-fluorouracil, 51-21-8, 5-fu, Fluoroplex, Efudex, Adrucil
Molecular Formula
C4H3FN2O2
Molecular Weight
130.08  g/mol
InChI Key
GHASVSINZRGABV-UHFFFAOYSA-N
FDA UNII
U3P01618RT

Fluorouracil
A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.
Fluorouracil is a Nucleoside Metabolic Inhibitor. The mechanism of action of fluorouracil is as a Nucleic Acid Synthesis Inhibitor.
1 2D Structure

Fluorouracil

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
5-fluoro-1H-pyrimidine-2,4-dione
2.1.2 InChI
InChI=1S/C4H3FN2O2/c5-2-1-6-4(9)7-3(2)8/h1H,(H2,6,7,8,9)
2.1.3 InChI Key
GHASVSINZRGABV-UHFFFAOYSA-N
2.1.4 Canonical SMILES
C1=C(C(=O)NC(=O)N1)F
2.2 Other Identifiers
2.2.1 UNII
U3P01618RT
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 5 Fluorouracil

2. 5 Fluorouracil Biosyn

3. 5 Fu Lederle

4. 5 Fu Medac

5. 5 Hu Hexal

6. 5-fluorouracil

7. 5-fluorouracil-biosyn

8. 5-fu

9. 5-fu Lederle

10. 5-fu Medac

11. 5-hu Hexal

12. 5fu

13. Adrucil

14. Carac

15. Dakota, Fluorouracile

16. Efudex

17. Efudix

18. Fluoro Uracile Icn

19. Fluoro-uracile Icn

20. Fluoroplex

21. Fluorouracil Gry

22. Fluorouracil Mononitrate

23. Fluorouracil Monopotassium Salt

24. Fluorouracil Monosodium Salt

25. Fluorouracil Potassium Salt

26. Fluorouracil-gry

27. Fluorouracile Dakota

28. Fluorouracilo Ferrer Far

29. Fluoruracil

30. Fluracedyl

31. Flurodex

32. Haemato Fu

33. Haemato-fu

34. Neofluor

35. Onkofluor

36. Ribofluor

2.3.2 Depositor-Supplied Synonyms

1. 5-fluorouracil

2. 51-21-8

3. 5-fu

4. Fluoroplex

5. Efudex

6. Adrucil

7. Carac

8. 5-fluoropyrimidine-2,4(1h,3h)-dione

9. Fluracil

10. Fluoroblastin

11. Queroplex

12. Kecimeton

13. Phthoruracil

14. Carzonal

15. Timazin

16. Arumel

17. Efudix

18. Fluril

19. 5-fluoracil

20. Fluracilum

21. Ulup

22. 5-fluoro-1h-pyrimidine-2,4-dione

23. Fluorouracilum

24. Fluro Uracil

25. 5 Fluorouracil

26. 5-fluoruracil

27. Ftoruracil

28. Efurix

29. Fluri

30. 5-fluoro-2,4(1h,3h)-pyrimidinedione

31. 5-fluoropyrimidine-2,4-dione

32. Effluderm (free Base)

33. Fluorouracilo

34. 2,4(1h,3h)-pyrimidinedione, 5-fluoro-

35. 2,4-dihydroxy-5-fluoropyrimidine

36. Ro 2-9757

37. Uracil, 5-fluoro-

38. 5-fluoropyrimidine-2,4-diol

39. 5-fluor-2,4-pyrimidindiol

40. 5-fluoro Uracil

41. 5-fluoro-uracil

42. 5-ftouracyl

43. 2,4-dioxo-5-fluoropyrimidine

44. Nsc 19893

45. Nsc-19893

46. Fluorouracil, 5-

47. 5-fluoro-2,4-pyrimidinedione

48. Fluorouracil (adrucil)

49. Fluorouricil

50. Ro-2-9757

51. Tolak

52. 5-fluor-2,4-dihydroxypyrimidin

53. U-8953

54. 191047-65-1

55. Fu

56. Chembl185

57. 2,4-pyrimidinediol, 5-fluoro- (9ci)

58. Mls000069498

59. 5 Fu

60. 5fu

61. Fluroblastin

62. Phtoruracil

63. Chebi:46345

64. Fluoro-uracile

65. Fluoro-uracilo

66. U3p01618rt

67. Nsc19893

68. 5-fluoro-1,2,3,4-tetrahydropyrimidine-2,4-dione

69. 5-faracil

70. Cinco Fu

71. Ro-29757

72. 191047-64-0

73. 191115-88-5

74. Urf

75. Ncgc00015442-02

76. Fluorouracile

77. Effluderm

78. Smr000038082

79. Dsstox_cid_634

80. Fluorouracile [dcit]

81. 5-fluoracil [german]

82. 5-fluoracyl

83. 5-fluoruracil [german]

84. Dsstox_rid_75705

85. Dsstox_gsid_20634

86. Fluorouracilum [inn-latin]

87. Fluorouracilo [inn-spanish]

88. 5-fluoropyrimidin-2,4-diol

89. Fluorouracil Cream

90. Cas-51-21-8

91. Fluoroplex (tn)

92. 5-fluor-2,4-pyrimidindiol [czech]

93. Adrucil (tn)

94. Ccris 2582

95. Carac (tn)

96. 5-fluor-2,4-dihydroxypyrimidin [czech]

97. Hsdb 3228

98. Sr-01000075881

99. 5-fluor-2,4(1h,3h)-pyrimidindion [czech]

100. Einecs 200-085-6

101. 5-fluor-2,4(1h,3h)-pyrimidindion

102. Fluouracil

103. Inhibits Thymilidate Synthetase

104. Unii-u3p01618rt

105. 2,4-dioxo-5-fluoropryimidine

106. 5-fluorourasil

107. Ai3-25297

108. Fluoro Uracil

109. 5-florouracil

110. 5-fluorouacil

111. 5-fu (tn)

112. 5-fluracil

113. 1upf

114. 5f-uracil

115. U 8953

116. 1-fluoro-1h-pyrimidine-2,4-dione

117. Adrucil (icn)

118. Mfcd00006018

119. Adrucil (fluorouracil)

120. Fluorouracil - Adrucil

121. Fluorouracil [usan:usp:inn:ban:jan]

122. Spectrum_000841

123. Opera_id_134

124. 5-fluorouracil, 99%

125. Spectrum2_000076

126. Spectrum3_000434

127. Spectrum4_000557

128. Spectrum5_000718

129. Wln: T6mvmvj Ef

130. Fluorouracil [mi]

131. Lopac-f-6627

132. F0151

133. Fluorouracil [inn]

134. Fluorouracil [jan]

135. Upcmld-dp130

136. Ec 200-085-6

137. F 6627

138. Fluorouracil [hsdb]

139. Fluorouracil [usan]

140. Schembl3646

141. 5-fluorpyrimidin-2,4-diol

142. Fluorouracil [vandf]

143. Lopac0_000536

144. Bspbio_002048

145. Fluorouracil [mart.]

146. Kbiogr_001253

147. Kbioss_001321

148. 2(1h)-pyrimidinone, 5-fluoro-4-hydroxy- (9ci)

149. 4(3h)-pyrimidinone, 5-fluoro-2-hydroxy- (9ci)

150. Mls002415705

151. Divk1c_000054

152. Fluorouracil [usp-rs]

153. Fluorouracil [who-dd]

154. Fluorouracil [who-ip]

155. Spectrum1500305

156. Spbio_000291

157. 5-fluorouracil [iarc]

158. 5-fluoro-2,4-dioxo-pyrimidin

159. 5-fluoro-pyrimidine-2,4-diol

160. Gtpl4789

161. Dtxsid2020634

162. Upcmld-dp130:001

163. Fluorouracil (jp17/usp/inn)

164. Hms500c16

165. Kbio1_000054

166. Kbio2_001321

167. Kbio2_003889

168. Kbio2_006457

169. Kbio3_001268

170. 5-fluoro-2,3h)-pyrimidinedione

171. 5-fluorouracil [who-ip]

172. 2,4-pyrimidinedione, 5-fluoro-

173. Ninds_000054

174. Bcpp000428

175. Fluorouracil [orange Book]

176. Hms1920o18

177. Hms2090i04

178. Hms2091f19

179. Hms3259o03

180. Hms3261l13

181. Hms3654k22

182. Hms3715h03

183. Hms3865l03

184. Pharmakon1600-01500305

185. Fluorouracil [ep Monograph]

186. 5-fluorouracil, Analytical Standard

187. Bcp02083

188. 2,3h)-pyrimidinedione, 5-fluoro-

189. Fluorouracil (5-fluoracil, 5-fu)

190. Fluorouracil (5-fluoracil; 5-fu)

191. Fluorouracil [usp Monograph]

192. Tox21_110150

193. Tox21_202335

194. Tox21_300112

195. Tox21_500536

196. Bdbm50340677

197. Ccg-39879

198. Dl-399

199. Nsc757036

200. Nsc816997

201. S1209

202. Stk297802

203. Stl367375

204. Zinc38212689

205. Fluorouracilum [who-ip Latin]

206. Akos000119162

207. Akos003237897

208. Akos008044307

209. Tox21_110150_1

210. Bcp9000239

211. Cs-0993

212. Db00544

213. Ks-5129

214. Lp00536

215. Nc00454

216. Nsc-757036

217. Nsc-816997

218. Sdccgsbi-0050519.p005

219. Flucytosine Impurity A [who-ip]

220. Idi1_000054

221. Ncgc00015442-01

222. Ncgc00015442-03

223. Ncgc00015442-04

224. Ncgc00015442-05

225. Ncgc00015442-06

226. Ncgc00015442-07

227. Ncgc00015442-08

228. Ncgc00015442-09

229. Ncgc00015442-10

230. Ncgc00015442-11

231. Ncgc00015442-12

232. Ncgc00015442-15

233. Ncgc00015442-16

234. Ncgc00015442-24

235. Ncgc00015442-30

236. Ncgc00091349-01

237. Ncgc00091349-02

238. Ncgc00091349-03

239. Ncgc00091349-04

240. Ncgc00091349-05

241. Ncgc00091349-07

242. Ncgc00091349-08

243. Ncgc00254023-01

244. Ncgc00259884-01

245. Ncgc00261221-01

246. 1004-03-1

247. 5-fluoro-2,4-(1h,3h)-pyrimidinedione

248. Ac-11201

249. Bf166014

250. Emtricitabine Impurity F [who-ip]

251. Hy-90006

252. Nci60_001652

253. Sri-10792-04

254. Sri-10792-05

255. Sri-10792-06

256. Sri-10792_07

257. Sri-10792_08

258. 5-fluoro-1h-pyrimidine-2,4-dione(5fu)

259. 5-fluorouracil, >=99% (hplc), Powder

260. Sbi-0050519.p004

261. 5-fluoro-1h-pyrimidine-2,4-dione(5-fu)

262. Db-051923

263. Db-065735

264. 5-fluoro-1h-pyrimidine-2,4-dione (5-fu)

265. Am20100252

266. Eu-0100536

267. Flucytosine Impurity A [ep Impurity]

268. Ft-0601511

269. Ft-0668745

270. Ft-0695666

271. Ft-0695667

272. Ft-0707652

273. Sw199617-3

274. 5-fluoro-1h-pyrimidine-2,4-dione(5-fura)

275. Fluorouracil, Meets Usp Testing Specifications

276. 51f218

277. C07649

278. D00584

279. 5-fluorouracil, Vetec(tm) Reagent Grade, >=99%

280. Q238512

281. W-60379

282. (5-fluorouracil)5-fluoro-1h-pyrimidine-2,4-dione

283. 5-fluoro-1h-pyrimidine-2,4-dione(5-fluoro Uracil)

284. Sr-01000075881-1

285. Sr-01000075881-3

286. Sr-01000075881-5

287. W-202929

288. 5-fluoro-1h-pyrimidine-2,4-dione (5-fluorouracil)

289. Brd-k24844714-001-02-1

290. 5-fluoropyrimidin-2,4(1h,3h)-dione [who-ip]

291. Z275128052

292. 5-fluoro-1h-pyrimidine-2,4-dione(5-fluorouracil)(5-fu)

293. 5-fluorouracil, Certified Reference Material, Tracecert(r)

294. Fluorouracil, British Pharmacopoeia (bp) Reference Standard

295. Fluorouracil, European Pharmacopoeia (ep) Reference Standard

296. Fluorouracil, United States Pharmacopeia (usp) Reference Standard

297. Pyrimidine Antimetabolite: Inhibits Nucleic Acid Replication; Tetratogen

298. Fluorouracil, Pharmaceutical Secondary Standard; Certified Reference Material

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 130.08 g/mol
Molecular Formula C4H3FN2O2
XLogP3-0.9
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count3
Rotatable Bond Count0
Exact Mass130.01785550 g/mol
Monoisotopic Mass130.01785550 g/mol
Topological Polar Surface Area58.2 Ų
Heavy Atom Count9
Formal Charge0
Complexity199
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 8  
Drug NameCarac
PubMed HealthFluorouracil
Drug ClassesAntineoplastic Agent, Antineoplastic, Dermatological
Drug LabelCarac (fluorouracil cream) Cream, 0.5%, contains fluorouracil for topical dermatologic use. Chemically, fluorouracil is 5-fluoro-2,4(1H, 3H)-pyrimidinedione. The molecular formula is C4H3FN2O2. Fluorouracil has a molecular weight of 130.08.Carac Cr...
Active IngredientFluorouracil
Dosage FormCream
RouteTopical
Strength0.5%
Market StatusPrescription
CompanyValeant Bermuda

2 of 8  
Drug NameEfudex
PubMed HealthFluorouracil
Drug ClassesAntineoplastic Agent, Antineoplastic, Dermatological
Drug LabelEfudex Solutions and Cream are topical preparations containing the fluorinated pyrimidine 5-fluorouracil, an antineoplastic antimetabolite.Efudex Solution consists of 2% or 5% fluorouracil on a weight/weight basis, compounded with propylene glycol, t...
Active IngredientFluorouracil
Dosage FormCream; Solution
RouteTopical
Strength5%; 2%
Market StatusPrescription
CompanyValeant Pharm Intl

3 of 8  
Drug NameFluoroplex
PubMed HealthFluorouracil
Drug ClassesAntineoplastic Agent, Antineoplastic, Dermatological
Drug LabelFLUOROPLEX (fluorouracil) 1% Topical Cream is an antineoplastic/antimetabolite product for dermatological use. Fluorouracil has the empirical formula C4H3FN2O2 and a molecular weight of 130.08. It is sparingly soluble in water and slightly soluble...
Active IngredientFluorouracil
Dosage FormCream
RouteTopical
Strength1%
Market StatusPrescription
CompanyAqua Pharms

4 of 8  
Drug NameFluorouracil
Drug LabelFluorouracil Injection, USP an antineoplastic antimetabolite, is a sterile, nonpyrogenic injectable solution for intravenous administration. Each mL contains 50 mg of fluorouracil and water for injection. Sodium hydroxide may be added to adjust pH to...
Active IngredientFluorouracil
Dosage FormCream; Injectable; Solution
RouteInjection; Topical
Strength5gm/100ml (50mg/ml); 1gm/20ml (50mg/ml); 500mg/10ml (50mg/ml); 5%; 2%; 2.5gm/50ml (50mg/ml)
Market StatusPrescription
CompanyAccord Hlthcare; Spear Pharms; Teva Pharms Usa; Taro; Sandoz; Fresenius Kabi Usa; Ebewe Pharma; Onco Therapies

5 of 8  
Drug NameCarac
PubMed HealthFluorouracil
Drug ClassesAntineoplastic Agent, Antineoplastic, Dermatological
Drug LabelCarac (fluorouracil cream) Cream, 0.5%, contains fluorouracil for topical dermatologic use. Chemically, fluorouracil is 5-fluoro-2,4(1H, 3H)-pyrimidinedione. The molecular formula is C4H3FN2O2. Fluorouracil has a molecular weight of 130.08.Carac Cr...
Active IngredientFluorouracil
Dosage FormCream
RouteTopical
Strength0.5%
Market StatusPrescription
CompanyValeant Bermuda

6 of 8  
Drug NameEfudex
PubMed HealthFluorouracil
Drug ClassesAntineoplastic Agent, Antineoplastic, Dermatological
Drug LabelEfudex Solutions and Cream are topical preparations containing the fluorinated pyrimidine 5-fluorouracil, an antineoplastic antimetabolite.Efudex Solution consists of 2% or 5% fluorouracil on a weight/weight basis, compounded with propylene glycol, t...
Active IngredientFluorouracil
Dosage FormCream; Solution
RouteTopical
Strength5%; 2%
Market StatusPrescription
CompanyValeant Pharm Intl

7 of 8  
Drug NameFluoroplex
PubMed HealthFluorouracil
Drug ClassesAntineoplastic Agent, Antineoplastic, Dermatological
Drug LabelFLUOROPLEX (fluorouracil) 1% Topical Cream is an antineoplastic/antimetabolite product for dermatological use. Fluorouracil has the empirical formula C4H3FN2O2 and a molecular weight of 130.08. It is sparingly soluble in water and slightly soluble...
Active IngredientFluorouracil
Dosage FormCream
RouteTopical
Strength1%
Market StatusPrescription
CompanyAqua Pharms

8 of 8  
Drug NameFluorouracil
Drug LabelFluorouracil Injection, USP an antineoplastic antimetabolite, is a sterile, nonpyrogenic injectable solution for intravenous administration. Each mL contains 50 mg of fluorouracil and water for injection. Sodium hydroxide may be added to adjust pH to...
Active IngredientFluorouracil
Dosage FormCream; Injectable; Solution
RouteInjection; Topical
Strength5gm/100ml (50mg/ml); 1gm/20ml (50mg/ml); 500mg/10ml (50mg/ml); 5%; 2%; 2.5gm/50ml (50mg/ml)
Market StatusPrescription
CompanyAccord Hlthcare; Spear Pharms; Teva Pharms Usa; Taro; Sandoz; Fresenius Kabi Usa; Ebewe Pharma; Onco Therapies

4.2 Therapeutic Uses

Antimetabolites; Antimetabolites, Antineoplastic; Immunosuppressive Agents

National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)


Fluorouracil is indicated for palliative treatment of carcinoma of the colon, rectum, breast, stomach, and pancreas in patients considered to be incurable by surgery or other means. /Included in US product update/

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1430


Fluorouracil is also indicated for treatment of bladder carcinoma, prostatic carcinoma, epithelial ovarian carcinoma, cervical carcinoma, endometrial carcinoma, anal carcinoma, esophageal carcinoma,metastatic tumors of skin carcinoma, and hepatoblastoma, and is used by intra-arterial injection for treatment of hepatic tumors and head and neck tumors. /Not included in US product label/

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1430


Fluorouracil, in combination therapy, is reasonable medical therapy at some point in the management of adrenocortical carcinoma, vulvar carcinoma, penile carcinoma and carcinoid tumors (gastrointestinal and neuroendocrine tumors). /Not included in US product label/

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1430


For more Therapeutic Uses (Complete) data for FLUOROURACIL (12 total), please visit the HSDB record page.


4.3 Drug Warning

Anorexia and nausea are common adverse effects of fluorouracil, and vomiting occurs frequently. These reactions generally occur during the first week of therapy, can often be alleviated by antiemetics, and generally subside within 2 or 3 days following therapy. Stomatitis is one of the most common and often the earliest sign of specific toxicity, appearing as early as the fourth day but more commonly on the fifth to eighth day of therapy. Diarrhea, which also occurs frequently, usually appears slightly later than stomatitis, but may occur concurrently or even in the absence of stomatitis. Esophagitis, proctitis, and GI ulceration and bleeding have been reported, and paralytic ileus occurred in two patients who received excessive dosage. Patients must be closely monitored for adverse GI effects.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1046


Leukopenia, predominantly of the granulocytopenic type, thrombocytopenia, and anemia occur commonly with fluorouracil therapy; leukopenia usually occurs after an adequate course of fluorouracil therapy. Pancytopenia and agranulocytosis also have occurred. The patient's hematologic status must be carefully monitored. The nadir of the white blood cell count usually occurs from the ninth to the fourteenth day after therapy is initiated but may occur as late as the 25th day after the first dose of fluorouracil. Maximum thrombocytopenia has been reported to occur from the seventh to seventeenth day of therapy. Hematopoietic recovery is usually rapid and by the thirtieth day, blood cell counts have usually reached the normal range.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1047


Hair loss occurs frequently with fluorouracil therapy, and cosmetically significant alopecia has occurred in a substantial number of patients. Regrowth of hair has been reported even in patients receiving repeated courses of the drug. Partial loss of nails has occurred rarely, and diffuse melanosis of the nails has been reported. The most common type of dermatologic toxicity is a pruritic maculopapular rash which usually appears on the extremities and less frequently on the trunk. This rash is generally reversible and usually responsive to symptomatic treatment.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1047


An erythematous, desquamative rash involving the hands and feet has been reported in patients receiving fluorouracil (in some cases, prolonged infusions of high dosages of the drug were administered). The rash may be accompanied by tingling or painful hands and feet, swollen palms and soles, and phalangeal tenderness. These adverse effects, referred to as palmar-plantar erythrodysesthesia or hand-foot syndrome, may gradually disappear over 5-7 days after discontinuance of fluorouracil therapy.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1047


For more Drug Warnings (Complete) data for FLUOROURACIL (31 total), please visit the HSDB record page.


4.4 Drug Indication

For the topical treatment of multiple actinic or solar keratoses. In the 5% strength it is also useful in the treatment of superficial basal cell carcinomas when conventional methods are impractical, such as with multiple lesions or difficult treatment sites. Fluorouracil injection is indicated in the palliative management of some types of cancer, including colon, esophageal, gastric, rectum, breast, biliary tract, stomach, head and neck, cervical, pancreas, renal cell, and carcinoid.


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Fluorouracil is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances from becoming incorporated into DNA during the "S" phase (of the cell cycle), stopping normal development and division. Fluorouracil blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Fluorouracil blocks the incorporation of the thymidine nucleotide into the DNA strand.


5.2 MeSH Pharmacological Classification

Antimetabolites, Antineoplastic

Antimetabolites that are useful in cancer chemotherapy. (See all compounds classified as Antimetabolites, Antineoplastic.)


Immunosuppressive Agents

Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging. (See all compounds classified as Immunosuppressive Agents.)


Antimetabolites

Drugs that are chemically similar to naturally occurring metabolites, but differ enough to interfere with normal metabolic pathways. (From AMA Drug Evaluations Annual, 1994, p2033) (See all compounds classified as Antimetabolites.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
FLUOROURACIL
5.3.2 FDA UNII
U3P01618RT
5.3.3 Pharmacological Classes
Nucleoside Metabolic Inhibitor [EPC]; Nucleic Acid Synthesis Inhibitors [MoA]
5.4 ATC Code

L01BC02

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355


L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01B - Antimetabolites

L01BC - Pyrimidine analogues

L01BC02 - Fluorouracil


5.5 Absorption, Distribution and Excretion

Absorption

28-100%


Route of Elimination

Seven percent to 20% of the parent drug is excreted unchanged in the urine in 6 hours; of this over 90% is excreted in the first hour. The remaining percentage of the administered dose is metabolized, primarily in the liver.


Given by continuous iv infusion for 24 hr, plasma concn in range of 0.5 to 3.0 uM are obtained and urinary excretion of fluorouracil is only 4%.

Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 1229


Fluorouracil readily enters cerebrospinal fluid, and concn of about 7 uM are reached within 30 min after iv admin; values are sustained for approx 3 hr and subside slowly during period of 9 hr.

Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 1229


Fluorouracil crosses the placenta in rats.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1048


Following iv administration of fluorouracil, no intact drug is detected in plasma after 3 hours.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1048


For more Absorption, Distribution and Excretion (Complete) data for FLUOROURACIL (7 total), please visit the HSDB record page.


5.6 Metabolism/Metabolites

Hepatic. The catabolic metabolism of fluorouracil results in degradation products ( e.g., CO2, urea and -fluoro--alanine) which are inactive.


A small portion of fluorouracil is anabolized in the tissues to 5-fluoro-2'-deoxyuridine and then to 5-fluoro-2'-deoxyuridine-5'-monophosphate, the active metabolite of the drug. The major portion of the drug is degraded in the liver. The metabolites are excreted as respiratory carbon dioxide and as urea, alpha-fluoro-beta-alanine, alpha-fluoro-beta-guanidopropionic acid, and alpha-fluoro-beta-ureidopropionic acid in urine. Following a single iv dose of fluorouracil, approximately 15% of the dose is excreted in urine as intact drug within 6 hours; over 90% of this is excreted in the first hour.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1048


... Dihydropyrimidine dehydrogenase /is/ an NADPH-requiring homodimeric protein (Mr ~210 kDa) containing FMN/FAD, and an iron-sulfur cluster in each subunit. The enzyme is located mainly in liver cytosol, where it catalyzes the reduction of 5-fluorouracil and related pyrimidines ...

Klaassen, C.D. (ed). Casarett and Doull's Toxicology. The Basic Science of Poisons. 6th ed. New York, NY: McGraw-Hill, 2001., p. 149


... Several routes are available for the formation of the 5'-monophosphate nucleotide (F-UMP) in animal cells. 5-FU may be converted to fluorouridine by uridine phosphorylase and then to F-UMP by uridine kinase, or it may react directly with 5-phosphoribosyl-1-pyrophosphate (PRPP), in a reaction catalyzed by ... orotate phosphoribosyl transferase, to form F-UMP. Many metabolic pathways are available to F-UMP, including incorporation into RNA. A reaction sequence crucial for antineoplastic activity involves reduction of the diphosphate nucleotide by the enzyme ribonucleoside diphosphate reductase to the deoxynucleotide level and the eventual formation of 5-fluoro-2'-deoxyuridine-5'-phosphate (F-dUMP). 5-FU also may be converted directly to the deoxyriboside 5-FUdR by the enzyme thymidine phosphorylase and further to F-dUMP, a potent inhibitor of thymidylate synthesis, by thymidine kinase ... The folate cofactor, 5,10-methylenetetrahydrofolate, and F-dUMP form a covalently bound ternary complex with the enzyme /thymidylate synthase/ ...

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 1405


... Metabolic degradation /of 5-FU and floxuridine/ occurs in many tissues, particularly in liver. Floxuridine is converted by thymidine or deoxyuridine phosphorylases into 5-FU. 5-FU is inactivated by reduction of the pyrimidine ring; this reaction is carried out by dihydropyrimidine dehydrogenase (DPD), which is found in liver, intestinal mucosa, tumor cells, and other tissues ... Its metabolite, 5-fluoro-5,6-dihydrouracil ... is ultimately degraded to alpha-fluoro-beta-alanine ... Although the liver contains high concn of DPD, dosage does not have to be modified in patients with hepatic dysfunction, presumably because of degradation of the drug at extrahepatic sites or by vast excess of this enzyme in the liver ...

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 1407


5-Fluorouracil is a known human metabolite of Tegafur.

S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560


5.7 Biological Half-Life

10-20 minutes


Following iv administration, the plasma elimination half-life averages about 16 minutes (range: 8-20 minutes) and is dose dependent.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1048


Rapid iv admin of 5-FU produces plasma concn of 0.1 to 1.0 mM; plasma clearance is rapid (half-life 10 to 20 min) ...

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 1407


5.8 Mechanism of Action

The precise mechanism of action has not been fully determined, but the main mechanism of fluorouracil is thought to be the binding of the deoxyribonucleotide of the drug (FdUMP) and the folate cofactor, N510-methylenetetrahydrofolate, to thymidylate synthase (TS) to form a covalently bound ternary complex. This results in the inhibition of the formation of thymidylate from uracil, which leads to the inhibition of DNA and RNA synthesis and cell death. Fluorouracil can also be incorporated into RNA in place of uridine triphosphate (UTP), producing a fraudulent RNA and interfering with RNA processing and protein synthesis.


5-FU requires enzymatic conversion to the nucleotide (ribosylation and phosphorylation) in order to exert its cytotoxic activity. Several routes are available for the formation of the 5'-monophosphate nucleotide (F-UMP) in animal cells. 5-FU may be converted to fluorouridine by uridine phosphorylase and then to F-UMP by uridine kinase, or it may react directly with 5-phosphoribosyl-1-pyrophosphate (PRPP), in a reaction catalyzed by ... orotate phosphoribosyl transferase, to form F-UMP. Many metabolic pathways are available to F-UMP, including incorporation in to RNA. A reaction sequence crucial for antineoplastic activity involves reduction of the diphosphate nucleotide by the enzyme ribonucleoside diphosphate reductase to the deoxynucleotide level and the eventual formation of 5-fluoro-2'-deoxyuridine-5'-phosphate (F-dUMP). 5-FU also may be converted directly to the deoxyriboside 5-FUdR by the enzyme thymidine phosphorylase and further to F-dUMP, a potent inhibitor of thymidylate synthesis, by thymidine kinase ... The interaction between F-dUMP and the enzyme thymidylate synthase leads to depletion of TTP, a necessary constituent of DNA ... The folate cofactor, 5,10-methylenetetrahydrofolate, and F-dUMP form a covalently bound ternary complex with the enzyme. The inhibitory complex resembles the transition state formed during the normal enzymatic reaction when dUMP is converted to thymidylate. Although the physiological complex progresses to the synthesis of thymidylate by transfer of the methylene group and 2 hydrogen atoms from folate to dUMP, this reaction is blocked in the inhibitory complex by the stability of the fluorine carbon bond on F-dUMP; sustained inhibition of the enzyme results ...

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 1405


Although the precise mechanisms of action of fluorouracil have not been fully elucidated, the main mechanism is thought to be the binding of the deoxyribonucleotide of the drug (FdUMP) and the folate cofactor, N5-10-methylenetetrahydrofolate, to thymidylate synthase (TS) to form a covalently bound ternary complex, which inhibits the formation of thymidylate from uracil, thereby interfering with DNA synthesis. In addition, FUTP can be incorporated into RNA in place of uridine triphosphate (UTP), producing a fraudulent RNA and interfering with RNA processing and protein synthesis.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1048


Fluorouracil is an antimetabolite of the pyrimidine analog type. Fluorouracil is considered to be cell cycle-specific for the S phase of cell division. Activity results from its conversion to an active metabolite in the tissues, and includes inhibition of DNA and RNA synthesis.

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1430


There is evidence that the metabolism of fluorouracil in the anabolic pathway blocks the methylation reaction of deoxyuridylic acid to thymidylic acid. In this manner fluorouracil interferes with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibits the formation of ribonucleic acid (RNA). Since DNA and RNA are essential for cell division and growth, the effect of fluorouracil may be to create a thymine deficiency which provokes unbalanced growth and death of the cell. The effects of DNA and RNA deprivation are most marked on those cells which grow more rapidly and take up fluorouracil at a more rapid rate. The catabolic metabolism of fluorouracil results in degradation products (eg, CO2 , urea, (alpha)-fluoro-(beta)-alanine) which are inactive. /Efudex Solutions/

Physicians Desk Reference 61st ed, Thomson PDR, Montvale, NJ 2007., p. 3363


For more Mechanism of Action (Complete) data for FLUOROURACIL (7 total), please visit the HSDB record page.


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EST.","city":"ANDHERI WEST MUMBAI","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"GUANGZHOU","customer":"KETAN PHARMA","customerCountry":"INDIA","quantity":"110.00","actualQuantity":"110","unit":"KGS","unitRateFc":"229","totalValueFC":"25490.9","currency":"USD","unitRateINR":"19316.2","date":"27-May-2024","totalValueINR":"2124776.5","totalValueInUsd":"25490.9","indian_port":"Bombay Air","hs_no":"29339990","bill_no":"3684792","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"GUANGZHOU","supplierAddress":"NO.20 3 HAIBIN ROAD YANHAI ECONOMICDEVELOPMENT ZONE RUDONG NANTONG JIANGSU , , CHINA CHINA","customerAddress":"646, LAXMI PLAZA,LAXMI INDL. EST."},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q2","strtotime":1719340200,"product":"FLUOROURACIL BP\/IP (5-FLUOROURACIL) (LIST 3 SR NO.52) (IGSTLIST NO.1 SR NO.52)","address":"646, LAXMI PLAZA,LAXMI INDL. EST.","city":"ANDHERI WEST MUMBAI","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"SHANGHAI - PU DONG","customer":"KETAN PHARMA","customerCountry":"INDIA","quantity":"50.95","actualQuantity":"50.95","unit":"KGS","unitRateFc":"229","totalValueFC":"11782.2","currency":"USD","unitRateINR":"19304.7","date":"26-Jun-2024","totalValueINR":"983574.47","totalValueInUsd":"11782.2","indian_port":"Bombay Air","hs_no":"29339990","bill_no":"4185949","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI - PU DONG","supplierAddress":"NO.20 3 HAIBIN ROAD YANHAI ECONOMICDEVELOPMENT ZONE RUDONG NANTONG JIANGSU , , CHINA CHINA","customerAddress":"646, LAXMI PLAZA,LAXMI INDL. EST."},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1719772200,"product":"FLUOROURACIL USP","address":"PLOT NO.2, MAITHRIVIHAR,","city":"HYDERABAD, AP.","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"SHANGHAI","customer":"EUGIA PHARMA SPECIALITIES ","customerCountry":"INDIA","quantity":"60.01","actualQuantity":"60.01","unit":"KGS","unitRateFc":"295","totalValueFC":"17853.1","currency":"USD","unitRateINR":"24868.5","date":"01-Jul-2024","totalValueINR":"1492358.69","totalValueInUsd":"17853.1","indian_port":"Hyderabad Air","hs_no":"29335990","bill_no":"4266103","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"NO.20, 3 HAIBIN ROAD, YANHAI ECONOMIC DEVELOPMENT ZONE,RUDONG, NANTONG, JIANGSU, CHINA ,226407 China","customerAddress":"PLOT NO.2, MAITHRIVIHAR,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1719772200,"product":"FLUOROURACIL USP","address":"PLOT NO.2, MAITHRIVIHAR,","city":"HYDERABAD, AP.","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"SHANGHAI","customer":"EUGIA PHARMA SPECIALITIES ","customerCountry":"INDIA","quantity":"89.99","actualQuantity":"89.99","unit":"KGS","unitRateFc":"295","totalValueFC":"26772.2","currency":"USD","unitRateINR":"24868.5","date":"01-Jul-2024","totalValueINR":"2237916.32","totalValueInUsd":"26772.2","indian_port":"Hyderabad Air","hs_no":"29335990","bill_no":"4266103","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"NO.20, 3 HAIBIN ROAD, YANHAI ECONOMIC DEVELOPMENT ZONE,RUDONG, NANTONG, JIANGSU, CHINA ,226407 China","customerAddress":"PLOT NO.2, MAITHRIVIHAR,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1721845800,"product":"5-FLUOROURACIL USP","address":"UNIT NO.24 STEEL MADE INDL.ESTATE","city":"MUMBAI","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"SHANGHAI","customer":"ENCUBE ETHICALS PRIVATE LIMITED","customerCountry":"INDIA","quantity":"1.70","actualQuantity":"1.7","unit":"KGS","unitRateFc":"900","totalValueFC":"1547.6","currency":"USD","unitRateINR":"76095","date":"25-Jul-2024","totalValueINR":"129361.5","totalValueInUsd":"1547.6","indian_port":"Bombay Air","hs_no":"29335990","bill_no":"4686693","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"LTD. NO.20, 3 HAIBIN ROAD, YANHAIECONOMIC DEVELOPMENT ZONERUDONG, NANTONG, JIANGSU CN","customerAddress":"UNIT NO.24 STEEL MADE INDL.ESTATE"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1722623400,"product":"2-METHOXY-5-FLUOROURACIL (INTERMEDIATE PRODUCTS)","address":"8-2-293\/82\/2\/76A, MLA COLONY,","city":"HILLS, HYDERABAD, TS","supplier":"S AND Y BIOCHEM CO., LTD","supplierCountry":"CHINA","foreign_port":"BEIJING","customer":"SESA CHEM INDIA ","customerCountry":"INDIA","quantity":"150.00","actualQuantity":"150","unit":"KGS","unitRateFc":"74","totalValueFC":"11195.5","currency":"USD","unitRateINR":"6260.4","date":"03-Aug-2024","totalValueINR":"939060","totalValueInUsd":"11195.5","indian_port":"Delhi Air","hs_no":"29349990","bill_no":"4873096","productDescription":"Intermediate","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"BEIJING","supplierAddress":"BUILDING 1-710, SHANDONG DESIGN ANDCREATIVE INDUSTRY PARK, NO. 868 TANGYE WEST ROAD JINAN CITY SHANDONG CHINA","customerAddress":"8-2-293\/82\/2\/76A, MLA COLONY,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1723573800,"product":"FLUOROURACIL PH. EUR. 11 (CEP) BATCH NO. FLU2024096 MFG. DATE 16.07.2024 RETEST DATE 15.07.2029","address":"CORPORATE HOUSE, NR. SOLA BRIDGE,,","city":"AHMEDABAD,GUJARAT","supplier":"WELDING GMBH & CO.KG","supplierCountry":"CHINA","foreign_port":"SHANGHAI - PU DONG","customer":"INTAS PHARMACEUTICALS","customerCountry":"INDIA","quantity":"40.00","actualQuantity":"40","unit":"KGS","unitRateFc":"294","totalValueFC":"11861.2","currency":"USD","unitRateINR":"24872.4","date":"14-Aug-2024","totalValueINR":"994896","totalValueInUsd":"11861.2","indian_port":"Ahmedabad Air","hs_no":"29335990","bill_no":"5043938","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI - PU DONG","supplierAddress":"ESPLANADE 39 20354 HAMBURG ,GERMANYHamburg, Hamburg, GERMANYSDNF GERMANY","customerAddress":"CORPORATE HOUSE, NR. SOLA BRIDGE,,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1723573800,"product":"FLUOROURACIL PH. EUR. 11 (CEP) BATCH NO. FLU2024096 MFG. DATE 16.07.2024 RETEST DATE 15.07.2029","address":"CORPORATE HOUSE, NR. SOLA BRIDGE,,","city":"AHMEDABAD,GUJARAT","supplier":"WELDING GMBH & CO.KG","supplierCountry":"CHINA","foreign_port":"SHANGHAI - PU DONG","customer":"INTAS PHARMACEUTICALS","customerCountry":"INDIA","quantity":"60.00","actualQuantity":"60","unit":"KGS","unitRateFc":"294","totalValueFC":"17791.7","currency":"USD","unitRateINR":"24872.4","date":"14-Aug-2024","totalValueINR":"1492344","totalValueInUsd":"17791.7","indian_port":"Ahmedabad Air","hs_no":"29335990","bill_no":"5043938","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI - PU DONG","supplierAddress":"ESPLANADE 39 20354 HAMBURG ,GERMANYHamburg, Hamburg, GERMANYSDNF GERMANY","customerAddress":"CORPORATE HOUSE, NR. SOLA BRIDGE,,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1727116200,"product":"FLUOROURACIL BP\/IP (5-FLUOROURACIL) (LIST 3 SR NO.52) (IGSTLIST NO.1 SR NO.52)","address":"646, LAXMI PLAZA,LAXMI INDL. EST.","city":"ANDHERI WEST MUMBAI","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"SHANGHAI","customer":"KETAN PHARMA","customerCountry":"INDIA","quantity":"30.00","actualQuantity":"30","unit":"KGS","unitRateFc":"227","totalValueFC":"6874.9","currency":"USD","unitRateINR":"19204.2","date":"24-Sep-2024","totalValueINR":"576126","totalValueInUsd":"6874.9","indian_port":"Bombay Air","hs_no":"29339990","bill_no":"5765569","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"NO.20 3 HAIBIN ROAD YANHAI ECONOMIC DEVELOPMENT ZONE RUDONG NANTONG JI ANGSU , , CHINA CHINA","customerAddress":"646, LAXMI PLAZA,LAXMI INDL. EST."},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1727116200,"product":"FLUOROURACIL BP\/IP (5-FLUOROURACIL) (LIST 3 SR NO.52) (IGSTLIST NO.1 SR NO.52)","address":"646, LAXMI PLAZA,LAXMI INDL. EST.","city":"ANDHERI WEST MUMBAI","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"SHANGHAI","customer":"KETAN PHARMA","customerCountry":"INDIA","quantity":"125.50","actualQuantity":"125.5","unit":"KGS","unitRateFc":"227","totalValueFC":"28760","currency":"USD","unitRateINR":"19204.2","date":"24-Sep-2024","totalValueINR":"2410127.1","totalValueInUsd":"28760","indian_port":"Bombay Air","hs_no":"29339990","bill_no":"5765569","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"NO.20 3 HAIBIN ROAD YANHAI ECONOMIC DEVELOPMENT ZONE RUDONG NANTONG JI ANGSU , , CHINA CHINA","customerAddress":"646, LAXMI PLAZA,LAXMI INDL. EST."},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1727634600,"product":"5-FLUOROURACIL USP","address":"UNIT NO.24 STEEL MADE INDL.ESTATE","city":"MUMBAI","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"SHANGHAI","customer":"ENCUBE ETHICALS PRIVATE LIMITED","customerCountry":"INDIA","quantity":"1.00","actualQuantity":"1","unit":"KGS","unitRateFc":"600","totalValueFC":"605.7","currency":"USD","unitRateINR":"50760","date":"30-Sep-2024","totalValueINR":"50760","totalValueInUsd":"605.7","indian_port":"Bombay Air","hs_no":"29335990","bill_no":"5878787","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"LTD. NO.20, 3 HAIBIN ROAD, YANHAI ECONOMIC DEVELOPMENT ZONE RUDONG, NANTONG, JIANGSU CN","customerAddress":"UNIT NO.24 STEEL MADE INDL.ESTATE"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q4","strtotime":1730053800,"product":"5-FLUOROURACIL USP","address":"UNIT NO.24 STEEL MADE INDL.ESTATE","city":"MUMBAI","supplier":"NANTONG JINGHUA PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"BEIJING","customer":"ENCUBE ETHICALS PRIVATE LIMITED","customerCountry":"INDIA","quantity":"5.00","actualQuantity":"5","unit":"KGS","unitRateFc":"600","totalValueFC":"3033","currency":"USD","unitRateINR":"50970","date":"28-Oct-2024","totalValueINR":"254850","totalValueInUsd":"3033","indian_port":"Bombay Air","hs_no":"29335990","bill_no":"6370080","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"BEIJING","supplierAddress":"LTD. NO.20, 3 HAIBIN ROAD, YANHAI ECONOMIC DEVELOPMENT ZONE RUDONG, NANTONG, JIANGSU CN","customerAddress":"UNIT NO.24 STEEL MADE INDL.ESTATE"}]
15-Jan-2021
28-Oct-2024
KGS
overview
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Average Price (USD/KGS)

Number of Transactions

Total Quantity (KGS)

Total Value (USD)

Quantity (KGS) & Unit rate (USD/KGS) over time

API Imports and Exports

Importing Country Total Quantity
(KGS)
Average Price
(USD/KGS)
Number of Transactions

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INTERMEDIATES SUPPLIERS

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01

The Pharmacy Technology
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The Pharmacy Technology
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CAS Number : 56177-80-1

End Use API : Fluorouracil

About The Company : Nantong Jinghua Pharmaceutical is a public pharmaceutical company that was established in 1957, owns about 302 staff, located in No. 20, 3 Haibin Road, Yanhai E...

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02

The Pharmacy Technology
Not Confirmed
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The Pharmacy Technology
Not Confirmed
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CAS Number : 1480-96-2

End Use API : Fluorouracil

About The Company : Nantong Jinghua Pharmaceutical is a public pharmaceutical company that was established in 1957, owns about 302 staff, located in No. 20, 3 Haibin Road, Yanhai E...

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FDA Orange Book

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01

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothDRL offers a portfolio of products & services, including APIs, CMO services, generics, biosimilars & differentiated formulations.

Flag India
Digital Content Digital Content

RLD : No

TE Code : AB

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : CREAM;TOPICAL

Dosage Strength : 5%

Approval Date : 2008-04-11

Application Number : 77524

RX/OTC/DISCN : RX

RLD : No

TE Code : AB

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02

TARO

U.S.A
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : SOLUTION;TOPICAL

Dosage Strength : 2%

Approval Date : 2003-11-05

Application Number : 76526

RX/OTC/DISCN : RX

RLD : No

TE Code : AT

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03

TARO

U.S.A
arrow
BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : SOLUTION;TOPICAL

Dosage Strength : 5%

Approval Date : 2003-11-05

Application Number : 76526

RX/OTC/DISCN : RX

RLD : No

TE Code : AT

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04

TARO

U.S.A
arrow
BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : CREAM;TOPICAL

Dosage Strength : 5%

Approval Date : 2010-03-05

Application Number : 90368

RX/OTC/DISCN : RX

RLD : No

TE Code : AB

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05

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 50MG/ML

Approval Date : 1987-01-12

Application Number : 89428

RX/OTC/DISCN : DISCN

RLD : No

TE Code :

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06

BAUSCH

Canada
BioFlorida Conference
Not Confirmed
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BAUSCH

Canada
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : EFUDEX

Dosage Form : SOLUTION;TOPICAL

Dosage Strength : 2%

Approval Date : 1982-01-01

Application Number : 16831

RX/OTC/DISCN : RX

RLD : Yes

TE Code : AT

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07

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 2.5GM/50ML (50MG/ML)

Approval Date : 1998-09-30

Application Number : 40278

RX/OTC/DISCN : RX

RLD : No

TE Code : AP

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08

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 1GM/20ML (50MG/ML)

Approval Date : 2017-10-27

Application Number : 210123

RX/OTC/DISCN : RX

RLD : No

TE Code : AP

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09

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 1GM/20ML (50MG/ML)

Approval Date : 2017-05-11

Application Number : 203608

RX/OTC/DISCN : RX

RLD : No

TE Code : AP

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10

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 5GM/100ML (50MG/ML)

Approval Date : 2000-02-25

Application Number : 40334

RX/OTC/DISCN : DISCN

RLD : No

TE Code :

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Europe

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01

Accord Healthcare Ltd.

United Kingdom
BioFlorida Conference
Not Confirmed
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Accord Healthcare Ltd.

United Kingdom
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil Accord

Dosage Form : Injection/infusion fluid, resolution

Dosage Strength : 50 mg/ml

Packaging : Hood glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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02

Accord Healthcare AG

United Kingdom
BioFlorida Conference
Not Confirmed
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Accord Healthcare AG

United Kingdom
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil Accord

Dosage Form : Inj. Solution

Dosage Strength : 2500mg/50ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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03

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil Hospira

Dosage Form : Injection fluid, resolution

Dosage Strength : 50 mg/ml

Packaging : Hood glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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04

Labatec Pharma SA

Switzerland
BioFlorida Conference
Not Confirmed
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Labatec Pharma SA

Switzerland
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil Labatec

Dosage Form : Inj. Solution

Dosage Strength : 250mg/5ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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05

Labatec Pharma SA

Switzerland
BioFlorida Conference
Not Confirmed
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Labatec Pharma SA

Switzerland
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil Labatec

Dosage Form : Inj. Solution

Dosage Strength : 500mg/10ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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06

Orifarm AS

Denmark
BioFlorida Conference
Not Confirmed
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Orifarm AS

Denmark
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Tolak

Dosage Form : Cream

Dosage Strength : 40mg/g

Packaging : Tube 20g

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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07

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil Sandoz

Dosage Form : Inj. Solution

Dosage Strength : 5000mg/100ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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08

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil Sandoz

Dosage Form : Inj. Solution

Dosage Strength : 500mg/10ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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09

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

fluorouracil

Brand Name : fluorouracil Teva

Dosage Form : SOLUTION FOR INJECTION

Dosage Strength : 50 MG / ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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10

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

Fluorouracil

Brand Name : Fluorouracil

Dosage Form : Fluorouracil 5.000Mg 100Ml 1 Units Parenteral Use

Dosage Strength : 1 vial EV 5 g 100 ml 50 mg/ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

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Canada

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01

ACCORD HEALTHCARE INC

United Kingdom
BioFlorida Conference
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ACCORD HEALTHCARE INC

United Kingdom
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL INJECTION USP

Dosage Form : SOLUTION

Dosage Strength : 50MG/ML

Packaging : 100ML

Approval Date :

Application Number : 2413450

Regulatory Info : Prescription

Registration Country : Canada

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02

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : EFUDEX

Dosage Form : CREAM

Dosage Strength : 5%/W/W

Packaging : 40G

Approval Date :

Application Number : 330582

Regulatory Info : Prescription

Registration Country : Canada

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03

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL INJECTION

Dosage Form : SOLUTION

Dosage Strength : 0.5G/10ML

Packaging : 10ML

Approval Date :

Application Number : 2473763

Regulatory Info : Prescription

Registration Country : Canada

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04

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : FLUOROURACIL INJECTION

Dosage Form : SOLUTION

Dosage Strength : 5G/100ML

Packaging : 100ML

Approval Date :

Application Number : 2473771

Regulatory Info : Prescription

Registration Country : Canada

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05

BioFlorida Conference
Not Confirmed
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BioFlorida Conference
Not Confirmed

FLUOROURACIL

Brand Name : ACTIKERALL

Dosage Form : SOLUTION

Dosage Strength : 0.5%/W/W

Packaging : 25ML

Approval Date :

Application Number : 2428946

Regulatory Info : Prescription

Registration Country : Canada

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BioFlorida Conference
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BioFlorida Conference
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FLUOROURACIL

Brand Name : FLUOROURACIL INJECTION

Dosage Form : SOLUTION

Dosage Strength : 50MG/ML

Packaging : 10ML

Approval Date :

Application Number : 12882

Regulatory Info : Prescription

Registration Country : Canada

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Listed Dossiers

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NanoAlvand

Iran
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  • fda
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Virtual BoothNanoAlvand is the entrance to Global Markets as a trusted Highly Potent Products manufacturer.

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Regulatory Info :

Registration Country : Iran

Fluorouracil

Brand Name : Fiverna

Dosage Form : Vial

Dosage Strength : 250MG/5ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Iran

NanoAlvand

01

NanoAlvand

Iran
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Virtual BoothNanoAlvand is the entrance to Global Markets as a trusted Highly Potent Products manufacturer.

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Packaging :

Regulatory Info :

Fluorouracil

Dosage : Vial

Dosage Strength : 250MG/5ML

Brand Name : Fiverna

Approval Date :

Application Number :

Registration Country : Iran

NanoAlvand

02

NanoAlvand

Iran
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  • fda
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Virtual BoothNanoAlvand is the entrance to Global Markets as a trusted Highly Potent Products manufacturer.

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Regulatory Info :

Registration Country : Iran

Fluorouracil

Brand Name : Fiverna

Dosage Form : Vial

Dosage Strength : 1000MG/20ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Iran

NanoAlvand

02

NanoAlvand

Iran
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  • fda
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Virtual BoothNanoAlvand is the entrance to Global Markets as a trusted Highly Potent Products manufacturer.

Flag Iran
Digital Content Digital Content

Packaging :

Regulatory Info :

Fluorouracil

Dosage : Vial

Dosage Strength : 1000MG/20ML

Brand Name : Fiverna

Approval Date :

Application Number :

Registration Country : Iran

NanoAlvand

03

  • fda
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Virtual BoothNaprod is a top player in Oncology & Anesthesia FDF through excellent innovation, discovery of new processes & high-quality production.

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Regulatory Info :

Registration Country : India

Fluorouracil

Brand Name :

Dosage Form : Liquid Injection

Dosage Strength : 50MG/ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : India

Naprod Life Sciences

03

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothNaprod is a top player in Oncology & Anesthesia FDF through excellent innovation, discovery of new processes & high-quality production.

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Packaging :

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Fluorouracil

Dosage : Liquid Injection

Dosage Strength : 50MG/ML

Brand Name :

Approval Date :

Application Number :

Registration Country : India

Naprod Life Sciences

04

The Pharmacy Technology
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Fluorouracil

Brand Name :

Dosage Form : INJECTION

Dosage Strength : 250MG

Packaging :

Approval Date :

Application Number :

Regulatory Info : Generic

Registration Country : India

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The Pharmacy Technology
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Fluorouracil

Dosage : INJECTION

Dosage Strength : 250MG

Brand Name :

Approval Date :

Application Number :

Registration Country : India

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05

The Pharmacy Technology
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Fluorouracil

Brand Name :

Dosage Form : INJECTION

Dosage Strength : 500MG

Packaging :

Approval Date :

Application Number :

Regulatory Info : Generic

Registration Country : India

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The Pharmacy Technology
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Fluorouracil

Dosage : INJECTION

Dosage Strength : 500MG

Brand Name :

Approval Date :

Application Number :

Registration Country : India

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Belco Pharma

India
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Belco Pharma

India
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Fluorouracil

Brand Name :

Dosage Form : Injection

Dosage Strength : 50MG

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : India

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Belco Pharma

India
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Belco Pharma

India
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Fluorouracil

Dosage : Injection

Dosage Strength : 50MG

Brand Name :

Approval Date :

Application Number :

Registration Country : India

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07

The Pharmacy Technology
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Fluorouracil

Brand Name : RACIWEL

Dosage Form : Injection

Dosage Strength : 250MG/5ML

Packaging : 5 Ampoules , 1 Vial

Approval Date :

Application Number :

Regulatory Info :

Registration Country : India

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The Pharmacy Technology
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Fluorouracil

Dosage : Injection

Dosage Strength : 250MG/5ML

Brand Name : RACIWEL

Approval Date :

Application Number :

Registration Country : India

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Fluorouracil

Brand Name : RACIWEL

Dosage Form : Injection

Dosage Strength : 1G/20ML

Packaging : 5 Ampoules , 1 Vial

Approval Date :

Application Number :

Regulatory Info :

Registration Country : India

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The Pharmacy Technology
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Fluorouracil

Dosage : Injection

Dosage Strength : 1G/20ML

Brand Name : RACIWEL

Approval Date :

Application Number :

Registration Country : India

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09

JW Pharmaceutical

South Korea
The Pharmacy Technology
Not Confirmed
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JW Pharmaceutical

South Korea
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Fluorouracil

Brand Name : 5-Fu

Dosage Form : Injection

Dosage Strength : 500MG

Packaging : 5ml × 10 Vials

Approval Date :

Application Number :

Regulatory Info : Generic

Registration Country : South Korea

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09

JW Pharmaceutical

South Korea
The Pharmacy Technology
Not Confirmed
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JW Pharmaceutical

South Korea
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Fluorouracil

Dosage : Injection

Dosage Strength : 500MG

Brand Name : 5-Fu

Approval Date :

Application Number :

Registration Country : South Korea

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10

JW Pharmaceutical

South Korea
The Pharmacy Technology
Not Confirmed
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JW Pharmaceutical

South Korea
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Fluorouracil

Brand Name : 5-Fu

Dosage Form : Injection

Dosage Strength : 250MG

Packaging : 10ml × 10 Vials

Approval Date :

Application Number :

Regulatory Info : Generic

Registration Country : South Korea

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10

JW Pharmaceutical

South Korea
The Pharmacy Technology
Not Confirmed
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JW Pharmaceutical

South Korea
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Fluorouracil

Dosage : Injection

Dosage Strength : 250MG

Brand Name : 5-Fu

Approval Date :

Application Number :

Registration Country : South Korea

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DRUG PRODUCT COMPOSITIONS

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DOSAGE - SOLUTION;TOPICAL - 2%

USFDA APPLICATION NUMBER - 16831

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DOSAGE - SOLUTION;TOPICAL - 5% **Federal Regi...DOSAGE - SOLUTION;TOPICAL - 5% **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

USFDA APPLICATION NUMBER - 16831

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DOSAGE - CREAM;TOPICAL - 0.5%

USFDA APPLICATION NUMBER - 20985

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DOSAGE - CREAM;TOPICAL - 4%

USFDA APPLICATION NUMBER - 22259

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DKSH

Switzerland
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Virtual BoothDKSH is your trusted partner for companies looking to grow their business in Asia & beyond.

Grade : Topical, Parenteral

Category : Solubilizers, Topical

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DKSH

Switzerland
  • fda
  • EDQM
  • WHO-GMP

Virtual BoothDKSH is your trusted partner for companies looking to grow their business in Asia & beyond.

Grade : Topical

Category : Topical

06

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  • fda
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Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

Grade : Parenteral, Oral, Topical

Category : Parenteral, Solubilizers, Topical

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Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

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Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

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Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

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