Synopsis
Synopsis
0
VMF
DRUG PRODUCT COMPOSITIONS0
Stock Recap #PipelineProspector
0
Weekly News Recap #Phispers
1. Anhydrous Tacrolimus
2. Anhydrous, Tacrolimus
3. Fk 506
4. Fk-506
5. Fk506
6. Fr 900506
7. Fr-900506
8. Fr900506
9. Prograf
10. Prograft
11. Tacrolimus Anhydrous
12. Tacrolimus, Anhydrous
1. Fujimycin
2. 104987-11-3
3. Prograf
4. Tsukubaenolide
5. Protopic
6. Fk506
7. Tacrolimus Anhydrous
8. Anhydrous Tacrolimus
9. Modigraf
10. Fk-506
11. Protopy
12. Lcp-tacro
13. Advagraf
14. Tacrolimus (fk506)
15. Fk 506
16. Fr-900506
17. Tacrolimus, Anhydrous
18. 8-deethyl-8-[but-3-enyl]-ascomycin
19. Tacrolimus (inn)
20. Fr900506
21. Astagraf Xl
22. Envarsus Xr
23. (-)-fk 506
24. Prograf (tn)
25. Tacrolimus [usan]
26. Chembl269732
27. Chebi:61049
28. Y5l2157c4j
29. Nsc-758659
30. K506
31. Ncgc00163470-03
32. Prograft
33. Tacrolimus [inn]
34. Avagraf
35. Envarsus
36. Graceptor
37. (3s,4r,5s,8r,9e,12s,14s,15r,16s,18r,19r,26as)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[(1e)-2-[(1r,3r,4r)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-epoxy-3h-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4h,23h)tetrone
38. Fk-506 (tacrolimus)
39. Tacrolimus (anhydrous)
40. Sr-05000001879
41. Tacrolimus [usan:inn]
42. Hecoria
43. Talymus
44. Unii-y5l2157c4j
45. Ccris 7124
46. Mfcd00869853
47. Hsdb 8195
48. L 679934
49. Prograph
50. Tacro
51. Envarsus-xr
52. Tacrolimus [mi]
53. Schembl3088
54. Tacrolimus [mart.]
55. Dsstox_cid_26354
56. Dsstox_rid_81557
57. Tacrolimus [who-dd]
58. Dsstox_gsid_46354
59. Bspbio_001279
60. Chembl66247
61. L-679934
62. Gtpl6784
63. Dtxsid5046354
64. Chebi:93221
65. Hms503o21
66. Hms1792o21
67. Hms1990o21
68. Hms2093m19
69. Hms3403o21
70. Pharmakon1600-01503968
71. Ex-a1677
72. Tox21_112056
73. Bdbm50030448
74. Bdbm50079777
75. Lmpk04000003
76. Nsc758659
77. S5003
78. Akos005145901
79. Zinc169289411
80. Ac-1182
81. Am81227
82. Ccg-270494
83. Cs-1507
84. Db00864
85. Idi1_001040
86. Ncgc00163470-01
87. Ncgc00163470-02
88. Ncgc00163470-04
89. Ncgc00163470-05
90. Ncgc00163470-06
91. Ncgc00163470-07
92. Ncgc00163470-27
93. (3s,4r,5s,8r,9e,12s,14s,15r,16s,18r,19r,26as)-5,19-dihydroxy-3-{(1e)-1-[(1r,3r,4r)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl}-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(prop-2-en-1-yl)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3h-15,19-epoxypyrido[2,1-c][1,4]oxazacyclotricosine-1,7,20,21(4h,23h)-tetrone
94. Hy-13756
95. Sbi-0052894.p002
96. Cas-104987-11-3
97. M2258
98. C01375
99. D08556
100. Ab01209746-01
101. Ab01209746_03
102. 581t933
103. Q411648
104. Q-201775
105. Sr-05000001879-1
106. Sr-05000001879-2
107. Sr-05000001879-5
108. Brd-k35452788-001-02-1
109. Brd-k69608737-001-03-7
110. Brd-k69608737-001-10-2
111. [(e)-2-[(1r,3r,4r)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-
112. 15,19-epoxy-3h-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(23h)-tetrone,
113. (1r,9s,12s,13r,14s,17r,18e,21s,23s,24r,25s,27r)-1,14-dihydroxy-12-[(e)-1-[(1r,3r,4r)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone
114. (3s,4r,5s,8r,9e,12s,14s,15r,16s,18r,19r,26as)-5,19-dihydroxy-3-{(e)-2-[(1r,3r,4r)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl}-14,16-dimethoxy-4,10,12,18-tetramethyl-8-prop-2-en-1-yl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3h-15,19-epoxypyrido[2,1-c][1,4]oxazacyclotricosine-1,7,20,21(4h,23h)-tetrone
115. (3s,4r,5s,8r,9e,12s,14s,15r,16s,18r,19r,26as)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[(1e)-2-[(1r,3r,4r)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19
116. (e)-(1r,9s,12s,13r,14r,21s,23s,24r,25s,27r)-17-allyl-1,14-dihydroxy-12-[(e)-2-((3r,4r)-4-hydroxy-3-methoxy-cyclohexyl)-1-methyl-vinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-aza-tricyclo[22.3.1.0*4,9*]octacos-18-ene-2,3,10,16-tetraone
117. 15,19-epoxy-3h-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4h,23h)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-((1e)-2-((1r,3r,4r)-4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl)-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-, (3s,4r,5s,8r,9e,12s,14s,15r,16s,18r,19r,26as)-
118. 15,19-epoxy-3h-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4h,23h)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-(2-(4-hydroxy-3-methoxycyclohexyl)-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-, (3s-(3r*(e(1s*,3s*,4s*)),4s*,5r*,8s*,9e,12r*,14r*,15s*,16r*,18s*,19s*,26ar*))-
119. 15,19-epoxy-3h-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4h,23h)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[(1e)-2-[(1r,3r,4r)-4-hydroxy-3-methoxycyc
120. 15,19-epoxy-3h-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4h,23h)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[(e)-2-[(1r,3r,4r)-4-hydroxy-3-methoxycycl Ohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-, (3s,4r,5s,8r,9e,12s,14s,15r,16s,18r,19r,26as)-
121. 4,5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-heptadecahydro-5,19-dihydroxy-3-
122. Dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-,(3s,4r,5s,8r,12s,14s,15r,16s,18r,19r,26as)-
123. Lohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-, (3s,4r,5s,8r,9e,12s,14s,15r,16s,18r,19r,26as)-
124. Tacrolimus Solution, 1.0 Mg/ml In Acetonitrile, Ampule Of 1 Ml, Certified Reference Material
| Molecular Weight | 804.0 g/mol |
|---|---|
| Molecular Formula | C44H69NO12 |
| XLogP3 | 2.7 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 12 |
| Rotatable Bond Count | 7 |
| Exact Mass | 803.48197664 g/mol |
| Monoisotopic Mass | 803.48197664 g/mol |
| Topological Polar Surface Area | 178 Ų |
| Heavy Atom Count | 57 |
| Formal Charge | 0 |
| Complexity | 1480 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 14 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 2 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
| 1 of 8 | |
|---|---|
| Drug Name | Astagraf xl |
| PubMed Health | Tacrolimus |
| Drug Classes | Antipsoriatic, Immune Suppressant |
| Drug Label | ASTAGRAF XL is available for oral administration as hard gelatin capsules (tacrolimus extended-release capsules) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include ethylcellulose NF, hypromello... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Capsule, extended release |
| Route | Oral |
| Strength | eq 5mg base; eq 0.5mg base; eq 1mg base |
| Market Status | Prescription |
| Company | Astellas |
| 2 of 8 | |
|---|---|
| Drug Name | Prograf |
| PubMed Health | Tacrolimus |
| Drug Classes | Antipsoriatic, Immune Suppressant |
| Drug Label | Prograf is available for oral administration as capsules (tacrolimus capsules USP) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include lactose monohydrate NF, hypromellose USP, croscarmellose so... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Capsule; Injectable |
| Route | Injection; Oral |
| Strength | eq 0.5mg base; eq 5mg base; eq 1mg base; eq 5mg base/ml |
| Market Status | Prescription |
| Company | Astellas |
| 3 of 8 | |
|---|---|
| Drug Name | Protopic |
| PubMed Health | Tacrolimus (On the skin) |
| Drug Classes | Antipsoriatic |
| Drug Label | PROTOPIC (tacrolimus) Ointment contains tacrolimus, a macrolide immunosuppressant produced by Streptomyces tsukubaensis. It is for topical dermatologic use only. Chemically, tacrolimus is designated as [3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Ointment |
| Route | Topical |
| Strength | 0.1%; 0.03% |
| Market Status | Prescription |
| Company | Astellas |
| 4 of 8 | |
|---|---|
| Drug Name | Tacrolimus |
| PubMed Health | Tacrolimus |
| Drug Classes | Antipsoriatic, Immune Suppressant |
| Drug Label | Prograf is available for oral administration as capsules (tacrolimus capsules USP) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include lactose monohydrate NF, hypromellose USP, croscarmellose so... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Ointment; Capsule |
| Route | Oral; Topical |
| Strength | eq 5mg base; eq 0.5mg base; 0.1%; eq 1mg base; 0.03% |
| Market Status | Prescription |
| Company | Panacea Biotec; Accord Hlthcare; Sandoz; Strides Pharma; Fougera Pharms; Dr Reddys Labs; Mylan |
| 5 of 8 | |
|---|---|
| Drug Name | Astagraf xl |
| PubMed Health | Tacrolimus |
| Drug Classes | Antipsoriatic, Immune Suppressant |
| Drug Label | ASTAGRAF XL is available for oral administration as hard gelatin capsules (tacrolimus extended-release capsules) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include ethylcellulose NF, hypromello... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Capsule, extended release |
| Route | Oral |
| Strength | eq 5mg base; eq 0.5mg base; eq 1mg base |
| Market Status | Prescription |
| Company | Astellas |
| 6 of 8 | |
|---|---|
| Drug Name | Prograf |
| PubMed Health | Tacrolimus |
| Drug Classes | Antipsoriatic, Immune Suppressant |
| Drug Label | Prograf is available for oral administration as capsules (tacrolimus capsules USP) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include lactose monohydrate NF, hypromellose USP, croscarmellose so... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Capsule; Injectable |
| Route | Injection; Oral |
| Strength | eq 0.5mg base; eq 5mg base; eq 1mg base; eq 5mg base/ml |
| Market Status | Prescription |
| Company | Astellas |
| 7 of 8 | |
|---|---|
| Drug Name | Protopic |
| PubMed Health | Tacrolimus (On the skin) |
| Drug Classes | Antipsoriatic |
| Drug Label | PROTOPIC (tacrolimus) Ointment contains tacrolimus, a macrolide immunosuppressant produced by Streptomyces tsukubaensis. It is for topical dermatologic use only. Chemically, tacrolimus is designated as [3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Ointment |
| Route | Topical |
| Strength | 0.1%; 0.03% |
| Market Status | Prescription |
| Company | Astellas |
| 8 of 8 | |
|---|---|
| Drug Name | Tacrolimus |
| PubMed Health | Tacrolimus |
| Drug Classes | Antipsoriatic, Immune Suppressant |
| Drug Label | Prograf is available for oral administration as capsules (tacrolimus capsules USP) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include lactose monohydrate NF, hypromellose USP, croscarmellose so... |
| Active Ingredient | Tacrolimus |
| Dosage Form | Ointment; Capsule |
| Route | Oral; Topical |
| Strength | eq 5mg base; eq 0.5mg base; 0.1%; eq 1mg base; 0.03% |
| Market Status | Prescription |
| Company | Panacea Biotec; Accord Hlthcare; Sandoz; Strides Pharma; Fougera Pharms; Dr Reddys Labs; Mylan |
Immunosuppressive Agents
National Library of Medicine's Medical Subject Headings. Tacrolimus. Online file (MeSH, 2014). Available from, as of April 30 2014: https://www.nlm.nih.gov/mesh/2014/mesh_browser/MBrowser.html
Prograf is indicated for the prophylaxis of organ rejection in patients receiving allogeneic kidney transplants. It is recommended that Prograf be used concomitantly with azathioprine or mycophenolate mofetil (MMF) and adrenal corticosteroids. /Included in US product label/
NIH; DailyMed. Current Medication Information for Prograf (Tacrolimus) Capsule, Gelatin Coated; Prograf (Tacrolimus) Injection, Solution (Revised: September 2013). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7f667de1-9dfa-4bd6-8ba0-15ee2d78873b
Prograf is indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver transplants. It is recommended that Prograf be used concomitantly with adrenal corticosteroids. Therapeutic drug monitoring is recommended for all patients receiving Prograf. /Included in US product label/
NIH; DailyMed. Current Medication Information for Prograf (Tacrolimus) Capsule, Gelatin Coated; Prograf (Tacrolimus) Injection, Solution (Revised: September 2013). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7f667de1-9dfa-4bd6-8ba0-15ee2d78873b
Prograf is indicated for the prophylaxis of organ rejection in patients receiving allogeneic heart transplants. It is recommended that Prograf be used concomitantly with azathioprine or mycophenolate mofetil (MMF) and adrenal corticosteroids. /Included in US product label/
NIH; DailyMed. Current Medication Information for Prograf (Tacrolimus) Capsule, Gelatin Coated; Prograf (Tacrolimus) Injection, Solution (Revised: September 2013). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7f667de1-9dfa-4bd6-8ba0-15ee2d78873b
For more Therapeutic Uses (Complete) data for Tacrolimus (13 total), please visit the HSDB record page.
/BOXED WARNING/ MALIGNANCIES AND SERIOUS INFECTIONS. Increased risk of development of lymphoma and other malignancies, particularly of the skin, due to immunosuppression. Increased susceptibility to bacterial, viral, fungal, and protozoal infections, including opportunistic infections. Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe Prograf. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient.
NIH; DailyMed. Current Medication Information for Prograf (Tacrolimus) Capsule, Gelatin Coated; Prograf (Tacrolimus) Injection, Solution (Revised: September 2013). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7f667de1-9dfa-4bd6-8ba0-15ee2d78873b
/BOXED WARNING/ WARNING: Long-term Safety of Topical Calcineurin Inhibitors Has Not Been Established Although a causal relationship has not been established, rare cases of malignancy (e.g., skin and lymphoma) have been reported in patients treated with topical calcineurin inhibitors, including Protopic Ointment. Therefore: Continuous long-term use of topical calcineurin inhibitors, including Protopic Ointment, in any age group should be avoided, and application limited to areas of involvement with atopic dermatitis; Protopic Ointment is not indicated for use in children less than 2 years of age; Only 0.03% Protopic Ointment is indicated for use in children 2-15 years of age.
NIH; DailyMed. DailyMed. Current Medication Information for Protopic (Tacrolimus) Ointment (Revised: May 2012). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=8c2e5036-5f1b-4e71-bf87-5faef295fa96
Topical tacrolimus therapy should be avoided for malignant or premalignant skin conditions (e.g., cutaneous T-cell lymphoma (CTCL)), which may appear clinically similar to dermatitis.
American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014
Because of a potential increased risk for skin cancer, patients /using topical tacrolimus/ should be advised to limit exposure to sunlight or other UV light by wearing protective clothing and using a broad-spectrum sunscreen with a high protection factor.
American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014
For more Drug Warnings (Complete) data for Tacrolimus (42 total), please visit the HSDB record page.
For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was given FDA approval in 1994 for use in liver transplantation. Since then, this indication has expanded to kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.
FDA Label
Prophylaxis of transplant rejection in adult kidney or liver allograft recipients.
Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult patients.
Prophylaxis of transplant rejection in adult kidney or liver allograft recipients. Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult patients.
Prophylaxis of transplant rejection in adult and paediatric, kidney, liver or heart allograft recipients.
Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult and paediatric patients.
Prophylaxis of transplant rejection in adult kidney or liver allograft recipients.
Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult patients.
* Flare treatment:
Adults and adolescents (16 years of age and above)
Treatment of moderate to severe atopic dermatitis in adults who are not adequately responsive to or are intolerant of conventional therapies such as topical corticosteroids.
Children (two years of age and above)
Treatment of moderate to severe atopic dermatitis in children (two years of age and above) who failed to respond adequately to conventional therapies such as topical corticosteroids.
* Maintenance treatment:
Maintenance treatment of moderate to severe atopic dermatitis for the prevention of flares and the prolongation of flare-free intervals in patients experiencing a high frequency of disease exacerbations (i. e. occurring four or more times per year) who have had an initial response to a maximum of six weeks treatment of twice daily tacrolimus ointment (lesions cleared, almost cleared or mildly affected).
Treatment of moderate to severe atopic dermatitis in adults who are not adequately responsive to or are intolerant of conventional therapies such as topical corticosteroids. Treatment of moderate to severe atopic dermatitis in children (2 years of age and above) who failed to respond adequately to conventional therapies such as topical corticosteroids.
Maintenance treatment of moderate to severe atopic dermatitis for the prevention of flares and the prolongation of flare-free intervals in patients experiencing a high frequency of disease exacerbations (i. e. occurring 4 or more times per year) who have had an initial response to a maximum of 6 weeks treatment of twice daily tacrolimus ointment (lesions cleared, almost cleared or mildly affected).
Prevention of solid organ transplant rejection, Treatment of solid organ transplant rejection
Tacrolimus acts by reducing peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This inhibits both T-lymphocyte signal transduction and IL-2 transcription. Tacrolimus has similar activity to cyclosporine but rates of rejection are lower with tacrolimus. Tacrolimus has also been shown to be effective in the topical treatment of eczema, particularly atopic eczema. It suppresses inflammation in a similar way to steroids, but is not as powerful. An important dermatological advantage of tacrolimus is that it can be used directly on the face; topical steroids cannot be used on the face, as they thin the skin dramatically there. On other parts of the body, topical steroid are generally a better treatment.
Calcineurin Inhibitors
Compounds that inhibit or block the PHOSPHATASE activity of CALCINEURIN. (See all compounds classified as Calcineurin Inhibitors.)
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.)
L04AD02
L04AD02
L04AD02
L04AD02
D11AH01
D11AX14
L04AD02
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
D - Dermatologicals
D11 - Other dermatological preparations
D11A - Other dermatological preparations
D11AH - Agents for dermatitis, excluding corticosteroids
D11AH01 - Tacrolimus
L - Antineoplastic and immunomodulating agents
L04 - Immunosuppressants
L04A - Immunosuppressants
L04AD - Calcineurin inhibitors
L04AD02 - Tacrolimus
Absorption
Absorption of tacrolimus from the gastrointestinal tract after oral administration is incomplete and variable. The absolute bioavailability in adult kidney transplant patients is 1710%; in adults liver transplant patients is 226%; in healthy subjects is 185%. The absolute bioavailability in pediatric liver transplant patients was 3124%. Tacrolimus maximum blood concentrations (Cmax) and area under the curve (AUC) appeared to increase in a dose-proportional fashion in 18 fasted healthy volunteers receiving a single oral dose of 3, 7, and 10 mg. When given without food, the rate and extent of absorption were the greatest. The time of the meal also affected bioavailability. When given immediately after a meal, mean Cmax was reduced 71%, and mean AUC was reduced 39%, relative to the fasted condition. When administered 1.5 hours following the meal, mean Cmax was reduced 63%, and mean AUC was reduced 39%, relative to the fasted condition.
Route of Elimination
In man, less than 1% of the dose administered is excreted unchanged in urine. When administered IV, fecal elimination accounted for 92.630.7%, urinary elimination accounted for 2.31.1%.
Volume of Distribution
2.6 2.1 L/kg [pediatric liver transplant patients]
1.07 0.20 L/kg [patients with renal impairment, 0.02 mg/kg/4 hr dose, IV]
3.1 1.6 L/kg [Mild Hepatic Impairment, 0.02 mg/kg/4 hr dose, IV]
3.7 4.7 L/kg [Mild Hepatic Impairment, 7.7 mg dose, PO]
3.9 1.0 L/kg [Severe hepatic impairment, 0.02 mg/kg/4 hr dose, IV]
3.1 3.4 L/kg [Severe hepatic impairment, 8 mg dose, PO]
Clearance
0.040 L/hr/kg [healthy subjects, IV]
0.172 0.088 L/hr/kg [healthy subjects, oral]
0.083 L/hr/kg [adult kidney transplant patients, IV]
0.053 L/hr/kg [adult liver transplant patients, IV]
0.051 L/hr/kg [adult heart transplant patients, IV]
0.138 0.071 L/hr/kg [pediatric liver transplant patients]
0.12 0.04 (range 0.06-0.17) L/hr/kg [pediatric kidney transplant patients]
0.038 0.014 L/hr/kg [patients with renal impairment, 0.02 mg/kg/4 hr dose, IV]
0.042 0.02 L/hr/kg [Mild Hepatic Impairment, 0.02 mg/kg/4 hr dose, IV]
0.034 0.019 L/hr/kg [Mild Hepatic Impairment, 7.7 mg dose, PO]
0.017 0.013 L/hr/kg [Severe hepatic impairment, 0.02 mg/kg/4 hr dose, IV]
0.016 0.011 L/hr/kg [Severe hepatic impairment, 8 mg dose, PO]
The aim of this study was to assess tacrolimus levels in breast milk and neonatal exposure during breastfeeding. An observational cohort study was performed in two tertiary referral high-risk obstetric medicine clinics. Fourteen women taking tacrolimus during pregnancy and lactation, and their 15 infants, 11 of whom were exclusively breast-fed, were assessed. Tacrolimus levels were analyzed by liquid chromatography-tandem mass spectrometry. Samples from mothers and cord blood were collected at delivery and from mothers, infants, and breast milk postnatally where possible. All infants with serial sampling had a decline in tacrolimus level, which was approximately 15% per day (ratio of geometric mean concentrations 0.85; 95% confidence interval, 0.82-0.88; P<0.001). Breast-fed infants did not have higher tacrolimus levels compared with bottle-fed infants (median 1.3 ug/L [range, 0.0-4.0] versus 1.0 ug/L (range, 0.0-2.3), respectively; P=0.91). Maximum estimated absorption from breast milk is 0.23% of maternal dose (weight-adjusted). Ingestion of tacrolimus by infants via breast milk is negligible. Breastfeeding does not appear to slow the decline of infant tacrolimus levels from higher levels present at birth.
PMID:23349333 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3613954 Bramham K et al; Clin J Am Soc Nephrol 8 (4): 563-7 (2013)
Maternal and umbilical cord (venous and arterial) samples were obtained at delivery from eight solid organ allograft recipients to measure tacrolimus and metabolite bound and unbound concentrations in blood and plasma. Tacrolimus pharmacokinetics in breast milk were assessed in one subject. Mean (+ or - SD) tacrolimus concentrations at the time of delivery in umbilical cord venous blood (6.6 + or - 1.8 ng ml(-1)) were 71 + or - 18% (range 45-99%) of maternal concentrations (9.0 + or - 3.4 ng ml(-1)). The mean umbilical cord venous plasma (0.09 + or - 0.04 ng ml(-1)) and unbound drug concentrations (0.003 + or - 0.001 ng ml(-1)) were approximately one fifth of the respective maternal concentrations. Arterial umbilical cord blood concentrations of tacrolimus were 100 + or - 12% of umbilical venous concentrations. In addition, infant exposure to tacrolimus through the breast milk was less than 0.3% of the mother's weight-adjusted dose. Differences between maternal and umbilical cord tacrolimus concentrations may be explained in part by placental P-gp function, greater red blood cell partitioning and higher haematocrit levels in venous cord blood.
PMID:23528073 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3845323 Zheng S et al; Br J Clin Pharmacol 76 (6): 988-96 (2013)
Ten colostrum samples were obtained from six women in the immediate postpartum period (0-3 days) with a mean drug concentration of 0.79 ng/mL (range 0.3-1.9 ng/mL). The median milk:maternal plasma ratio was 0.5.
Briggs, G.G., Freeman, R.K., Yaffee, S.J.; Drugs in Pregancy and Lactation Nineth Edition. Wolters Kluwer/Lippincott Williams & Wilkins, Philadelphia, PA. 2011, p. 1385
The plasma protein binding of tacrolimus is approximately 99% and is independent of concentration over a range of 5-50 ng/mL. Tacrolimus is bound mainly to albumin and alpha-1-acid glycoprotein, and has a high level of association with erythrocytes. The distribution of tacrolimus between whole blood and plasma depends on several factors, such as hematocrit, temperature at the time of plasma separation, drug concentration, and plasma protein concentration. In a US study, the ratio of whole blood concentration to plasma concentration averaged 35 (range 12 to 67). There was no evidence based on blood concentrations that tacrolimus accumulates systemically upon intermittent topical application for periods of up to 1 year. As with other topical calcineurin inhibitors, it is not known whether tacrolimus is distributed into the lymphatic system.
NIH; DailyMed. DailyMed. Current Medication Information for Protopic (Tacrolimus) Ointment (Revised: May 2012). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=8c2e5036-5f1b-4e71-bf87-5faef295fa96
For more Absorption, Distribution and Excretion (Complete) data for Tacrolimus (9 total), please visit the HSDB record page.
The metabolism of tacrolimus is predominantly mediated by CYP3A4 and secondarily by CYP3A5. Tacrolimus is metabolized into 8 metabolites: 13-demethyl tacrolimus, 31-demethyl tacrolimus, 15-demethyl tacrolimus, 12-hydroxy tacrolimus, 15,31-didemethyl tacrolimus, 13,31-didemethyl tacrolimus, 13,15-didemethyl tacrolimus, and a final metabolite involving O-demethylation and the formation of a fused ring. The major metabolite identified in incubations with human liver microsomes is 13-demethyl tacrolimus. In in vitro studies, a 31-demethyl metabolite has been reported to have the same activity as tacrolimus.
Tacrolimus is extensively metabolized by the mixed-function oxidase system, primarily the cytochrome P-450 system (CYP3A). A metabolic pathway leading to the formation of 8 possible metabolites has been proposed. Demethylation and hydroxylation were identified as the primary mechanisms of biotransformation in vitro. The major metabolite identified in incubations with human liver microsomes is 13-demethyl tacrolimus. In in vitro studies, a 31-demethyl metabolite has been reported to have the same activity as tacrolimus.
NIH; DailyMed. Current Medication Information for Prograf (Tacrolimus) Capsule, Gelatin Coated; Prograf (Tacrolimus) Injection, Solution (Revised: September 2013). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7f667de1-9dfa-4bd6-8ba0-15ee2d78873b
Fk_506 has known human metabolites that include 13-O-Desmethyltacrolimus and 15-O-Desmethyltacrolimus.
S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560
The elimination half life in adult healthy volunteers, kidney transplant patients, liver transplants patients, and heart transplant patients are approximately 35, 19, 12, 24 hours, respectively. The elimination half life in pediatric liver transplant patients was 11.53.8 hours, in pediatric kidney transplant patients was 10.25.0 (range 3.4-25) hours.
In a mass balance study of IV administered radiolabeled tacrolimus to 6 healthy volunteers, ... the elimination half-life based on radioactivity was 48.1+ or - 15.9 hours whereas it was 43.5 + or- 11.6 hours based on tacrolimus concentrations. ... When administered PO, the elimination half-life based on radioactivity was 31.9 + or- 10.5 hours whereas it was 48.4 + or - 12.3 hours based on tacrolimus concentrations ... .
NIH; DailyMed. Current Medication Information for Prograf (Tacrolimus) Capsule, Gelatin Coated; Prograf (Tacrolimus) Injection, Solution (Revised: September 2013). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7f667de1-9dfa-4bd6-8ba0-15ee2d78873b
... A case of tacrolimus toxicity in a non-transplant patient /is presented/. ... /The/ patient's tacrolimus dose was 2.1 mg/kg/day for 4 days (therapeutic 0.03 to 0.05 mg/kg/day). Her tacrolimus elimination half-life was 16.5 hours, compared to a mean half-life in healthy volunteers of 34.2 +/- 7.7 hours. ...
PMID:18608277 O'Connor AD et al; Clin Toxicol (Phila) 46 (9): 838-40 (2008)
The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This prevents the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines. Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-, all of which are involved in the early stages of T-cell activation. Additionally, tacrolimus has been shown to inhibit the release of pre-formed mediators from skin mast cells and basophils, and to downregulate the expression of FceRI on Langerhans cells.
Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. Tacrolimus is commercially available for topical use as a 0.03 or 0.1% ointment. The exact mechanism(s) of action of tacrolimus in the treatment of atopic dermatitis has not been elucidated but appears to involve inhibition of the activation of T cells. Tacrolimus also has been shown to inhibit release of mediators from skin mast cells and basophils and to downregulate the expression of high-affinity receptors for immunoglobulin E (IgE) on Langerhans cells. Although tacrolimus is not genotoxic and does not interact directly with DNA, the drug may impair local immunosurveillance.
American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014
Tacrolimus inhibits T-lymphocyte activation, although the exact mechanism of action is not known. Experimental evidence suggests that tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin inhibited. This effect may prevent the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines (such as interleukin-2, gamma interferon). The net result is the inhibition of T-lymphocyte activation (i.e., immunosuppression).
NIH; DailyMed. Current Medication Information for Prograf (Tacrolimus) Capsule, Gelatin Coated; Prograf (Tacrolimus) Injection, Solution (Revised: September 2013). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7f667de1-9dfa-4bd6-8ba0-15ee2d78873b
The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This effect has been shown to prevent the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines (such as interleukin-2, gamma interferon). Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-a, all of which are involved in the early stages of T-cell activation. Additionally, tacrolimus has been shown to inhibit the release of pre-formed mediators from skin mast cells and basophils, and to down regulate the expression of FceRI on Langerhans cells.
NIH; DailyMed. DailyMed. Current Medication Information for Protopic (Tacrolimus) Ointment (Revised: May 2012). Available from, as of June 17, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=8c2e5036-5f1b-4e71-bf87-5faef295fa96
Tacrolimus, formerly known as FK506, is a macrolide antibiotic with immunosuppressive properties. Although structurally unrelated to cyclosporin A (CsA), its mode of action is similar. It exerts its effects principally through impairment of gene expression in target cells. Tacrolimus bonds to an immunophilin, FK506 binding protein (FKBP). This complex inhibits calcineurin phosphatase. The drug inhibits calcium-dependent events, such as interleukin-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the transforming growth factor beta-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by tacrolimus. Type 1 T helper cells appear to be preferentially suppressed compared with type 2 T helper cells. T cell-mediated cytotoxicity is impaired. B cell growth and antibody production are affected indirectly by the suppression of T cell-derived growth factors necessary for these functions. Antigen presentation appears to be spared. ...
PMID:8588225 Thomson AW et al; Ther Drug Monit 17 (6): 584-91 (1995)
API SUPPLIERS
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]
USDMF
Fishfa Biogenics: Renowned Manufacturer, & Exporter of Tacrolimus & Mupirocin API.
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 39667
Submission : 2024-03-19
Status : Active
Type : II
Farmhispania Group, a leading European CDMO in HPAPI Technologies & High Potency Fermentation.
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 35852
Submission : 2021-04-23
Status : Active
Type : II
Chunghwa provides cost-effective APIs & advanced intermediates with complete DMF or COS, ensuring quality & reliable production.
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 23213
Submission : 2009-10-26
Status : Active
Type : II
Chunghwa provides cost-effective APIs & advanced intermediates with complete DMF or COS, ensuring quality & reliable production.
GDUFA
DMF Review : Complete
Rev. Date : 2016-04-01
Pay. Date : 2016-03-09
DMF Number : 18985
Submission : 2005-11-28
Status : Active
Type : II
Chunghwa provides cost-effective APIs & advanced intermediates with complete DMF or COS, ensuring quality & reliable production.
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 38310
Submission : 2023-04-26
Status : Active
Type : II
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 16833
Submission : 2003-09-12
Status : Active
Type : II
GDUFA
DMF Review : Complete
Rev. Date : 2013-05-30
Pay. Date : 2013-05-17
DMF Number : 18442
Submission : 2005-06-21
Status : Active
Type : II
GDUFA
DMF Review : Complete
Rev. Date : 2013-08-28
Pay. Date : 2013-08-16
DMF Number : 18908
Submission : 2005-10-24
Status : Active
Type : II
GDUFA
DMF Review : Complete
Rev. Date : 2015-05-28
Pay. Date : 2015-05-05
DMF Number : 19979
Submission : 2006-11-20
Status : Active
Type : II
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 19072
Submission : 2005-12-22
Status : Inactive
Type : II
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]CEP/COS
Chunghwa provides cost-effective APIs & advanced intermediates with complete DMF or COS, ensuring quality & reliable production.
Chunghwa provides cost-effective APIs & advanced intermediates with complete DMF or COS, ensuring quality & reliable production.
Tacrolimus monohydrate, Process B
Certificate Number : CEP 2023-345 - Rev 00
Status : Valid
Issue Date : 2024-03-28
Type : Chemical
Substance Number : 2244
Chunghwa provides cost-effective APIs & advanced intermediates with complete DMF or COS, ensuring quality & reliable production.
Chunghwa provides cost-effective APIs & advanced intermediates with complete DMF or COS, ensuring quality & reliable production.
Certificate Number : R0-CEP 2018-241 - Rev 01
Status : Valid
Issue Date : 2023-03-30
Type : Chemical
Substance Number : 2244
Certificate Number : CEP 2017-257 - Rev 01
Status : Valid
Issue Date : 2023-11-29
Type : Chemical
Substance Number : 2244
Tacrolimus monohydrate, Process II
Certificate Number : R0-CEP 2020-227 - Rev 01
Status : Valid
Issue Date : 2022-12-19
Type : Chemical
Substance Number : 2244
Certificate Number : R0-CEP 2018-216 - Rev 00
Status : Valid
Issue Date : 2020-06-02
Type : Chemical
Substance Number : 2244
Certificate Number : CEP 2021-210 - Rev 01
Status : Valid
Issue Date : 2024-07-22
Type : Chemical and TSE
Substance Number : 2244
Certificate Number : R0-CEP 2021-204 - Rev 01
Status : Valid
Issue Date : 2023-08-07
Type : Chemical
Substance Number : 2244
Certificate Number : R0-CEP 2021-180 - Rev 01
Status : Valid
Issue Date : 2023-06-19
Type : Chemical
Substance Number : 2244
Certificate Number : CEP 2018-233 - Rev 04
Status : Valid
Issue Date : 2024-08-05
Type : Chemical
Substance Number : 2244
Certificate Number : CEP 2023-051 - Rev 00
Status : Valid
Issue Date : 2024-09-26
Type : Chemical
Substance Number : 2244
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results] EU WC
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]NDC API
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Listed Suppliers
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]API Reference Price
API Imports and Exports
| Importing Country | Total Quantity (KGS) |
Average Price (USD/KGS) |
Number of Transactions |
|---|
Upgrade, download data, analyse, strategize, subscribe with us 
Drugs in Development
Details:
The company’s lead product candidate TFF TAC (tacrolimus) inhalation powder, is undergoing Phase 2 trial studies for the prevention of lung transplant rejection.
Lead Product(s): Tacrolimus
Therapeutic Area: Immunology Brand Name: TFF TAC
Study Phase: Phase IIProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable August 06, 2024
Lead Product(s) : Tacrolimus
Therapeutic Area : Immunology
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
TFF Reports Positive Phase 2 Data for Tacrolimus Powder in Lung Transplant Rejection
Details : The company’s lead product candidate TFF TAC (tacrolimus) inhalation powder, is undergoing Phase 2 trial studies for the prevention of lung transplant rejection.
Brand Name : TFF TAC
Molecule Type : Small molecule
Upfront Cash : Not Applicable
August 06, 2024
Details:
The company’s lead product candidate TFF TAC (tacrolimus) inhalation powder, is undergoing Phase 2 trial studies for the prevention of lung transplant rejection.
Lead Product(s): Tacrolimus
Therapeutic Area: Immunology Brand Name: TFF TAC
Study Phase: Phase IIProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable June 24, 2024
Lead Product(s) : Tacrolimus
Therapeutic Area : Immunology
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
TFF Pharmaceuticals Provides Update on Tacrolimus Inhalation Powder for Lung Transplant
Details : The company’s lead product candidate TFF TAC (tacrolimus) inhalation powder, is undergoing Phase 2 trial studies for the prevention of lung transplant rejection.
Brand Name : TFF TAC
Molecule Type : Small molecule
Upfront Cash : Not Applicable
June 24, 2024
Details:
The company’s lead product candidate TFF TAC (tacrolimus) inhalation powder, is undergoing Phase 2 trial studies for the prevention of lung transplant rejection.
Lead Product(s): Tacrolimus
Therapeutic Area: Immunology Brand Name: TFF TAC
Study Phase: Phase IIProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable May 15, 2024
Lead Product(s) : Tacrolimus
Therapeutic Area : Immunology
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
TFF Pharmaceuticals Updates on Tacrolimus Inhalation Powder Phase 2 Trial
Details : The company’s lead product candidate TFF TAC (tacrolimus) inhalation powder, is undergoing Phase 2 trial studies for the prevention of lung transplant rejection.
Brand Name : TFF TAC
Molecule Type : Small molecule
Upfront Cash : Not Applicable
May 15, 2024
Details:
Tacrograf (tacrolimus) is a next-generation, capsule formulation immunosuppressent for the treatment and prevention of prophylaxis of organ rejection after transplant.
Lead Product(s): Tacrolimus
Therapeutic Area: Immunology Brand Name: Tacrograf
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable April 20, 2024
Lead Product(s) : Tacrolimus
Therapeutic Area : Immunology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Biocon Receives Approval for Tacrolimus Capsules from SAHPRA
Details : Tacrograf (tacrolimus) is a next-generation, capsule formulation immunosuppressent for the treatment and prevention of prophylaxis of organ rejection after transplant.
Brand Name : Tacrograf
Molecule Type : Small molecule
Upfront Cash : Not Applicable
April 20, 2024
Details:
TFF TAC (tacrolimus) is a next-generation, direct-to-lung, inhaled dry powder formulation of tacrolimus for the treatment and prevention of prophylaxis of organ rejection in lung transplant.
Lead Product(s): Tacrolimus
Therapeutic Area: Immunology Brand Name: TFF TAC
Study Phase: Phase IIProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable March 25, 2024
Lead Product(s) : Tacrolimus
Therapeutic Area : Immunology
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
TFF Pharmaceuticals Presents Interim Data from Phase 2 Study of Tacrolimu
Details : TFF TAC (tacrolimus) is a next-generation, direct-to-lung, inhaled dry powder formulation of tacrolimus for the treatment and prevention of prophylaxis of organ rejection in lung transplant.
Brand Name : TFF TAC
Molecule Type : Small molecule
Upfront Cash : Not Applicable
March 25, 2024
Details:
TFF TAC (tacrolimus) is a next-generation, direct-to-lung, inhaled dry powder formulation of tacrolimus for the treatment and prevention of prophylaxis of organ rejection in lung transplant.
Lead Product(s): Tacrolimus
Therapeutic Area: Immunology Brand Name: TFF-TAC
Study Phase: Phase IIProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable December 19, 2023
Lead Product(s) : Tacrolimus
Therapeutic Area : Immunology
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : TFF TAC (tacrolimus) is a next-generation, direct-to-lung, inhaled dry powder formulation of tacrolimus for the treatment and prevention of prophylaxis of organ rejection in lung transplant.
Brand Name : TFF-TAC
Molecule Type : Small molecule
Upfront Cash : Not Applicable
December 19, 2023
Details:
BNSO will develop, manufacture and commercialize a range of innovative ophthalmic pharmaceutical products developed by BioNanoSim, including BNSO-1, a Tacrolimus ocular emulsion developed by its proprietary nano-technology platform to address serious ophthalmic unmet needs.
Lead Product(s): Tacrolimus
Therapeutic Area: Ophthalmology Brand Name: BNSO-1
Study Phase: PreclinicalProduct Type: Small molecule
Sponsor: BioNanoSim
Deal Size: Undisclosed Upfront Cash: Undisclosed
Deal Type: Agreement May 30, 2023
Lead Product(s) : Tacrolimus
Therapeutic Area : Ophthalmology
Highest Development Status : Preclinical
Partner/Sponsor/Collaborator : BioNanoSim
Deal Size : Undisclosed
Deal Type : Agreement
Details : BNSO will develop, manufacture and commercialize a range of innovative ophthalmic pharmaceutical products developed by BioNanoSim, including BNSO-1, a Tacrolimus ocular emulsion developed by its proprietary nano-technology platform to address serious oph...
Brand Name : BNSO-1
Molecule Type : Small molecule
Upfront Cash : Undisclosed
May 30, 2023
Details:
The collaboration aims to facilitate Chemistry, Manufacturing, and Control documentation for Lipella's drug candidate LP-10 (liposomal tacrolimus), aimed at treating hemorrhagic cystitis. LP-10 has been granted Orphan Drug Designation by the FDA.
Lead Product(s): Tacrolimus
Therapeutic Area: Urology Brand Name: LP-10
Study Phase: Phase IIProduct Type: Small molecule
Sponsor: Lipella Pharmaceuticals
Deal Size: Undisclosed Upfront Cash: Undisclosed
Deal Type: Collaboration April 17, 2023
Lead Product(s) : Tacrolimus
Therapeutic Area : Urology
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Lipella Pharmaceuticals
Deal Size : Undisclosed
Deal Type : Collaboration
Lipella Pharmaceuticals Enters Manufacturing Collaboration Agreement with Cook MyoSite
Details : The collaboration aims to facilitate Chemistry, Manufacturing, and Control documentation for Lipella's drug candidate LP-10 (liposomal tacrolimus), aimed at treating hemorrhagic cystitis. LP-10 has been granted Orphan Drug Designation by the FDA.
Brand Name : LP-10
Molecule Type : Small molecule
Upfront Cash : Undisclosed
April 17, 2023
Details:
LP-10 is a proprietary liposomal formulation of tacrolimus that is currently being evaluated as a treatment for moderate to severe hemorrhagic cystitis. The product candidate is currently in Phase 2a clinical trial.
Lead Product(s): Tacrolimus
Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: LP-10
Study Phase: Phase IIProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable January 11, 2023
Lead Product(s) : Tacrolimus
Therapeutic Area : Obstetrics/Gynecology (Women’s Health)
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Lipella Pharmaceuticals Announces Successful Top Line Results of Phase 2A Clinical Trial of LP-10
Details : LP-10 is a proprietary liposomal formulation of tacrolimus that is currently being evaluated as a treatment for moderate to severe hemorrhagic cystitis. The product candidate is currently in Phase 2a clinical trial.
Brand Name : LP-10
Molecule Type : Small molecule
Upfront Cash : Not Applicable
January 11, 2023
Details:
Study demonstrated that NK cells when stimulated with a cytokine cocktail developed a memory-like phenotype with increased expansion and persistence in vivo, as a treatment for cancer of its m-ceNK platform combined with IL-15 superagonist cytokine fusion protein Anktiva™.
Lead Product(s): Inbakicept,Tacrolimus,Mycophenolate Mofetil
Therapeutic Area: Oncology Brand Name: Anktiva
Study Phase: Phase IIProduct Type: Cell and Gene therapy
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable March 02, 2022
Lead Product(s) : Inbakicept,Tacrolimus,Mycophenolate Mofetil
Therapeutic Area : Oncology
Highest Development Status : Phase II
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : Study demonstrated that NK cells when stimulated with a cytokine cocktail developed a memory-like phenotype with increased expansion and persistence in vivo, as a treatment for cancer of its m-ceNK platform combined with IL-15 superagonist cytokine fusio...
Brand Name : Anktiva
Molecule Type : Cell and Gene therapy
Upfront Cash : Not Applicable
March 02, 2022
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]INTERMEDIATES SUPPLIERS
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]FDF Dossiers
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]FDA Orange Book
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Europe
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Canada
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Australia
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]DRUG PRODUCT COMPOSITIONS
DOSAGE - TABLET, EXTENDED RELEASE;ORAL - EQ 0...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - EQ 0.75MG BASE
USFDA APPLICATION NUMBER - 206406
DOSAGE - TABLET, EXTENDED RELEASE;ORAL - EQ 1...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - EQ 1MG BASE
USFDA APPLICATION NUMBER - 206406
DOSAGE - TABLET, EXTENDED RELEASE;ORAL - EQ 4...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - EQ 4MG BASE
USFDA APPLICATION NUMBER - 206406
DOSAGE - CAPSULE;ORAL - EQ 0.5MG BASE
USFDA APPLICATION NUMBER - 50708
DOSAGE - CAPSULE;ORAL - EQ 1MG BASE
USFDA APPLICATION NUMBER - 50708
DOSAGE - CAPSULE;ORAL - EQ 5MG BASE
USFDA APPLICATION NUMBER - 50708
Related Excipient Companies
SPI Pharma
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Faran Shimi Pharmaceutical
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Gangwal Healthcare
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Nanjing Well Pharmaceutical
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Capital Farma
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]ACG Worldwide
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Anhui Sunhere Pharmaceutical Excipients Co.,Ltd
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Corel Pharma Chem
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]DFE Pharma
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Finar
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Gangwal Chemicals
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Ideal Cures Pvt Ltd
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Ingredion Pharma Solutions
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Kerry
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Kima Chemical
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Lonza Capsugel
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Microlex e.U
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Nanjing Bold Chemical
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Novo Excipients
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Pluviaendo
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Prachin Chemical
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Qianhao Chemical (Hebei) Co., Ltd
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Qualicaps
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Roquette
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Seppic
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Shanghai Shenmei Pharmaceutical Technology Co., Ltd
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Sigachi Industries
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]The Dow Chemical Company
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Excipients by Applications
Coating Systems & Additives
Fillers, Diluents & Binders
Controlled & Modified Release
Gangwal Healthcare is powered by innovation, driving health, wellness & healing.
Grade : Oral
Category : Co-Processed Excipients, Controlled & Modified Release, Direct Compression
Application : Co-Processed Excipients, Controlled & Modified Release, Direct Compression
Excipient Details : DiCOM-DC SR300 is used as a directly compressible, rate-controlling, and co-processed excipient in sustained-release tablets and capsules.
Grade : Not Available
Category : Coating Systems & Additives, Controlled & Modified Release
Application : Coating Systems & Additives, Controlled & Modified Release
Excipient Details : Film Forming Agent, Wet/Dry Granulation- Binder,Thickening & Suspension Agent, Non-Gelatin Capsule Manufacturing & Enteric Film Coating Systems
Pharmacopoeia Ref : USP, EP, and JP
Technical Specs : Not Available
Ingredient(s) : Hydroxypropyl Methylcellulose
Grade : Not Available
Category : Coating Systems & Additives, Controlled & Modified Release
Application : Coating Systems & Additives, Controlled & Modified Release
Excipient Details : Sustained Release Tablet Matrix
Pharmacopoeia Ref : USP, EP, and JP
Technical Specs : Not Available
Ingredient(s) : Hydroxypropyl Methylcellulose
Application : Controlled & Modified Release
Excipient Details : Instamodel Blend is used to provide Extended Release from the dosage form.
Dosage Form : Tablet
Grade : Not Available
Category : Coating Systems & Additives, Controlled & Modified Release
Application : Coating Systems & Additives, Controlled & Modified Release
Excipient Details : Immediate Release
Pharmacopoeia Ref : Customized per requirements
Technical Specs : Not Available
Ingredient(s) : Starch
Grade : Not Available
Category : API Stability Enhancers, Coating Systems & Additives, Controlled & Modified Release, Direct Compression, Granulation, Rheology Modifiers, Vegetarian Capsules
Application : API Stability Enhancers, Coating Systems & Additives, Controlled & Modified Release, Direct Compression, Granulation, Rheology Modifiers, Vegetarian Capsules
Excipient Details : Controlled Release, Direct Compression,Wet Granulation,Tablet Coating, Liquid Solutions and Suspensions
Pharmacopoeia Ref : Not Available
Technical Specs : Not Available
Ingredient(s) : Hydroxypropyl Methylcellulose
Dosage Form : Tablet
Grade : Not Available
Category : Coating Systems & Additives, Controlled & Modified Release
Brand Name : SheffCoat™Enhance
Application : Coating Systems & Additives, Controlled & Modified Release
Excipient Details : Immediate Release
Pharmacopoeia Ref : Customized per requirements
Technical Specs : Not Available
Ingredient(s) : Hydroxypropyl Methylcellulose
Brand Name : Hydroxypropyl Methyl Cellulose (75K100)
Application : Controlled & Modified Release
Excipient Details : Hydroxypropyl Methyl Cellulose (75K100) is used in the production of controlled-release tablets.
Dosage Form : Tablet
Grade : Not Available
Category : Coating Systems & Additives, Controlled & Modified Release
Application : Coating Systems & Additives, Controlled & Modified Release
Excipient Details : Immediate Release
Pharmacopoeia Ref : Customized per requirements
Technical Specs : Not Available
Ingredient(s) : Hydroxypropyl Methylcellulose
Dosage Form : Tablet
Grade : Not Available
Category : Coating Systems & Additives, Controlled & Modified Release
Application : Coating Systems & Additives, Controlled & Modified Release
Excipient Details : Immediate Release
Pharmacopoeia Ref : Customized per requirements
Technical Specs : Not Available
Ingredient(s) : Hydroxypropyl Methylcellulose
Direct Compression
Lubricants & Glidants
Granulation
Faran Shimi: Leading producer of high-quality APIs & alkaloid opiates, serving major pharmaceutical companies across the Middle East.
Brand Name : Sodium Dodecyl Sulfate
Application : Granulation
Excipient Details : Sodium dodecyl sulfate is used in wet granulation tableting applications for the production of antacid tablets and digestive aids.
Dosage Form : Tablet
Grade : Oral
Category : Granulation, Lubricants & Glidants, Surfactant & Foaming Agents
Brand Name : Sodium Dodecyl Sulfate
Application : Granulation, Lubricants & Glidants, Surfactant & Foaming Agents
Excipient Details : Sodium Dodecyl Sulfate is used as an ionic surfactant, lubricant, and granulating agent in the solid dosage forms such as tablets.
Dosage Form : Tablet
Grade : Oral
Category : Direct Compression, Disintegrants & Superdisintegrants, Granulation
Application : Direct Compression, Disintegrants & Superdisintegrants, Granulation
Excipient Details : Croscarmellose sodium, a cellulose-based super disintegrant, provides excellent results in tablet disintegration. It is used in both wet granulation and direct compression.
Application : Fillers, Diluents & Binders, Granulation
Pharmacopoeia Ref : Conforms to USP-NF, Ph.Eur., J...
Technical Specs : Density- Tapped density- 857 g/l, Bulk density- 589 g/l; Particle...
Ingredient(s) : Lactose Monohydrate
Grade : Not Available
Category : API Stability Enhancers, Coating Systems & Additives, Controlled & Modified Release, Direct Compression, Granulation, Rheology Modifiers, Vegetarian Capsules
Application : API Stability Enhancers, Coating Systems & Additives, Controlled & Modified Release, Direct Compression, Granulation, Rheology Modifiers, Vegetarian Capsules
Excipient Details : Controlled Release, Direct Compression,Wet Granulation,Tablet Coating, Liquid Solutions and Suspensions
Pharmacopoeia Ref : Not Available
Technical Specs : Not Available
Ingredient(s) : Hydroxypropyl Methylcellulose
Dosage Form : Tablet
Grade : Oral
Category : Coating Systems & Additives, Fillers, Diluents & Binders, Granulation
Brand Name : Hydroxypropyl Methyl Cellulose (60E3)
Application : Coating Systems & Additives, Fillers, Diluents & Binders, Granulation
Excipient Details : Hydroxypropyl Methyl Cellulose (60E3) is used as a binding, coating, and granulating agent for the production of tablets.
Application : Granulation
Excipient Details : Wetting agent, reduces disintegration time, Ionic solubilizer, high HLB anionic emulsifier for semi-solids and foams.
Pharmacopoeia Ref : Ph. Eur.: Sodium Laurilsulfate...
Technical Specs : Not Available
Ingredient(s) : Sodium Lauryl Sulfate
Grade : Not Available
Category : Direct Compression, Granulation, Lubricants & Glidants
Brand Name : Kolliphor SLS Fine
Application : Direct Compression, Granulation, Lubricants & Glidants
Excipient Details : Wetting agent, reducing disintegration time, direct compression, Hydrophilic lubricant, effervescent tablets.
Pharmacopoeia Ref : Ph. Eur.: Sodium Laurilsulfate...
Technical Specs : Not Available
Ingredient(s) : Sodium Lauryl Sulfate
Application : Disintegrants & Superdisintegrants, Granulation
Pharmacopoeia Ref : Not Available
Technical Specs : Not Available
Ingredient(s) : Croscarmellose Sodium
Application : Direct Compression, Granulation
Pharmacopoeia Ref : Not Available
Technical Specs : Not Available
Ingredient(s) : Lactose Monohydrate
Film Formers & Plasticizers
Disintegrants & Superdisintegrants
Thickeners and Stabilizers
Empty Capsules
Solubilizers
Topical
Co-Processed Excipients
Emulsifying Agents
Taste Masking
Coloring Agents
Vegetarian Capsules
API Stability Enhancers
Parenteral
Rheology Modifiers
Chewable & Orodispersible Aids
Surfactant & Foaming Agents
Digital Content
DATA COMPILATION #PharmaFlow
NEWS #PharmaBuzz
Global Sales Information
US Medicaid Prescriptions
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Market Place
Patents & EXCLUSIVITIES
US Patents
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]REF. STANDARDS & IMPURITIES
USP
ANALYTICAL
BioAnalytical Methods
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Analytical Methods
ABOUT THIS PAGE
LOOKING FOR A SUPPLIER?
