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Chemistry

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Also known as: 518048-05-0, Mk-0518, Isentress, Raltegravir (mk-0518), Mk0518, Raltegravir (inn)
Molecular Formula
C20H21FN6O5
Molecular Weight
444.4  g/mol
InChI Key
CZFFBEXEKNGXKS-UHFFFAOYSA-N
FDA UNII
22VKV8053U

Raltegravir Potassium
A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.
Raltegravir is a Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor. The mechanism of action of raltegravir is as a HIV Integrase Inhibitor.
1 2D Structure

Raltegravir Potassium

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide
2.1.2 InChI
InChI=1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30)
2.1.3 InChI Key
CZFFBEXEKNGXKS-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC1=NN=C(O1)C(=O)NC(C)(C)C2=NC(=C(C(=O)N2C)O)C(=O)NCC3=CC=C(C=C3)F
2.2 Other Identifiers
2.2.1 UNII
22VKV8053U
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 0518, Mk

2. Isentress

3. Mk 0518

4. Mk-0518

5. Mk0518

6. Potassium, Raltegravir

7. Raltegravir Potassium

2.3.2 Depositor-Supplied Synonyms

1. 518048-05-0

2. Mk-0518

3. Isentress

4. Raltegravir (mk-0518)

5. Mk0518

6. Raltegravir (inn)

7. Mk 0518

8. N-(2-(4-((4-fluorobenzyl)carbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide

9. 22vkv8053u

10. 518048-05-0 (free)

11. 4-pyrimidinecarboxamide, N-((4-fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo-

12. N-(2-(4-(4-fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide

13. Ncgc00184997-01

14. Raltegravir [inn]

15. Dsstox_cid_28586

16. Dsstox_rid_82857

17. Dsstox_gsid_48660

18. N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-2-{2-[(5-methyl-1,3,4-oxadiazol-2-yl)formamido]propan-2-yl}-6-oxo-1,6-dihydropyrimidine-4-carboxamide

19. Isentress(tm)

20. N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide

21. Cas-518048-05-0

22. Raltegravir [usan:inn]

23. Raltegravirum

24. Unii-22vkv8053u

25. Hsdb 8124

26. N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide

27. N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(1-methyl-1-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}ethyl)-6-oxo-1,6-di Hydropyrimidine-4-carboxamide

28. N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(1-methyl-1-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}ethyl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide

29. Rlt

30. Raltegravir- Bio-x

31. Raltegravir [mi]

32. N-[1-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxo-pyrimidin-2-yl]-1-methyl-ethyl]-5-methyl-1,3,4-oxadiazole-2-carboxamide

33. Raltegravir; Mk-0518

34. K-0518

35. Raltegravir [vandf]

36. Raltegravir - Mk-0518

37. Raltegravir [mart.]

38. Hydropyrimidine-4-carboxamide

39. Schembl51817

40. Raltegravir [who-dd]

41. Mls006011985

42. Schembl996804

43. Raltegravir [ema Epar]

44. Chembl254316

45. Schembl2112870

46. Dtxsid2048660

47. Bdbm25351

48. Chebi:82960

49. Gtpl11571

50. Bcpp000093

51. Hms3655b09

52. Bcp01394

53. Ex-a2147

54. Tox21_113019

55. Mfcd10698872

56. Nsc762522

57. S2005

58. Zinc13831130

59. Akos015902444

60. Akos025149884

61. Akos032960305

62. Tox21_113019_1

63. Zinc114994525

64. Ac-5261

65. Ccg-269170

66. Db06817

67. Nsc-762522

68. Pb13312

69. Sb20935

70. Ncgc00274066-01

71. Ncgc00274066-05

72. As-16992

73. Br164312

74. Hy-10353

75. Smr003601806

76. Ft-0649660

77. Sw220138-1

78. A25486

79. D06676

80. Mk-0518;mk 0518;mk0518

81. Yl}-6-oxo-1,6-dihydropyrimidine-4-carboxamide

82. Ab01566833_01

83. 038r721

84. 048r050

85. A828788

86. Q421552

87. Brd-k05658747-237-01-1

88. [(5-methyl-1,3,4-oxadiazol-2-yl)formamido]propan-2-

89. N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-2-{2-

90. Z1551429745

91. (z)-n-(2-(4-(((4-fluorophenyl)(methyl)amino)(hydroxy)methylene)-1-methyl-5,6-dioxo-1,4,5,6-tetrahydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide

92. Mk-0518;n-[(4-fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-4-pyrimidinecarboxamide Potassium Salt

93. N-(2-(4-(4-fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2-yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- Carboxamide

94. N-(2-(4-(4-fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6- Dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide

95. N-(2-(4-(4-fluorobenzylcarbamoyl)-5-oh-1-me-6-oxo-pyrimidin-2-yl)propan-2-yl)-5-me-1,3,4-oxadiazole-2-carboxamide

96. N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(1-methyl-1-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}ethyl)-6-oxo-1,6-di

97. N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(2-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}propan-2-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide

98. N-[2-(4-{[(4-fluorophenyl)methyl]carbamoyl}-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide

2.4 Create Date
2011-12-26
3 Chemical and Physical Properties
Molecular Weight 444.4 g/mol
Molecular Formula C20H21FN6O5
XLogP31.1
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count9
Rotatable Bond Count6
Exact Mass444.15574595 g/mol
Monoisotopic Mass444.15574595 g/mol
Topological Polar Surface Area150 Ų
Heavy Atom Count32
Formal Charge0
Complexity836
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 4  
Drug NameIsentress
PubMed HealthRaltegravir (By mouth)
Drug ClassesAntiretroviral Agent
Drug LabelISENTRESS contains raltegravir potassium, a human immunodeficiency virus integrase strand transfer inhibitor. The chemical name for raltegravir potassium is N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxa...
Active IngredientRaltegravir potassium
Dosage FormTablet; Powder; Tablet, chewable
RouteOral
Strengtheq 100mg base; eq 400mg base; eq 100mg base/packet; eq 25mg base
Market StatusPrescription
CompanyMerck Sharp Dohme

2 of 4  
Drug NameRaltegravir
PubMed HealthRaltegravir (By mouth)
Drug ClassesAntiretroviral Agent
Drug LabelISENTRESS contains raltegravir potassium, a human immunodeficiency virus integrase strand transfer inhibitor. The chemical name for raltegravir potassium is N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxa...
Active IngredientRaltegravir
Dosage FormTablet
RouteOral
Strength400mg
Market StatusTentative Approval
CompanyHetero Labs Ltd Iii

3 of 4  
Drug NameIsentress
PubMed HealthRaltegravir (By mouth)
Drug ClassesAntiretroviral Agent
Drug LabelISENTRESS contains raltegravir potassium, a human immunodeficiency virus integrase strand transfer inhibitor. The chemical name for raltegravir potassium is N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxa...
Active IngredientRaltegravir potassium
Dosage FormTablet; Powder; Tablet, chewable
RouteOral
Strengtheq 100mg base; eq 400mg base; eq 100mg base/packet; eq 25mg base
Market StatusPrescription
CompanyMerck Sharp Dohme

4 of 4  
Drug NameRaltegravir
PubMed HealthRaltegravir (By mouth)
Drug ClassesAntiretroviral Agent
Drug LabelISENTRESS contains raltegravir potassium, a human immunodeficiency virus integrase strand transfer inhibitor. The chemical name for raltegravir potassium is N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxa...
Active IngredientRaltegravir
Dosage FormTablet
RouteOral
Strength400mg
Market StatusTentative Approval
CompanyHetero Labs Ltd Iii

4.2 Therapeutic Uses

Pyrrolidinones

National Library of Medicine's Medical Subject Headings online file (MeSH, 2009)


ISENTRESS (raltegravir) is indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection. /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


ISENTRESS (raltegravir) is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in children and adolescents 2 years of age and older and weighing at least 10 kg. /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


/EXPERIMENTAL THER/ /Investigators/ describe five patients with HIV-2 infection (four antiretroviral-experienced and one antiretroviral-naive) treated with a regimen containing raltegravir. All responded to treatment as demonstrated by viral load and CD4(+) T-cell count monitoring. /This/ series confirms the clinical effectiveness of raltegravir in HIV-2-infected patients when given with other antiretrovirals to which the virus is susceptible.

PMID:22892365 Peterson K et al; Antivir Ther.17 (6):1097-100 (2012)


/EXPERIMENTALTHER VET/ Feline leukemia virus (FeLV) is a gammaretrovirus that is a significant cause of neoplastic-related disorders affecting cats worldwide. Treatment options for FeLV are limited, associated with serious side effects, and can be cost-prohibitive. The development of drugs used to treat a related retrovirus, human immunodeficiency virus type 1 (HIV-1), has been rapid, leading to the approval of five drug classes. Although structural differences affect the susceptibility of gammaretroviruses to anti-HIV drugs, the similarities in mechanism of replication suggest that some anti-HIV-1 drugs may also inhibit FeLV. This study demonstrates the anti-FeLV activity of four drugs approved by the US FDA (Food and Drug Administration) at non-toxic concentrations. Of these, tenofovir and raltegravir are anti-HIV-1 drugs, while decitabine and gemcitabine are approved to treat myelodysplastic syndromes and pancreatic cancer, respectively, but also have anti-HIV-1 activity in cell culture. Our results indicate that these drugs may be useful for FeLV treatment and should be investigated for mechanism of action and suitability for veterinary use.

PMID:22258856 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3542715 Greggs WM 3rd et al; J Gen Virol. 93 (Pt 4): 900-5 (2012)


4.3 Drug Warning

Severe, potentially life-threatening skin reactions have been reported, including some fatalities. Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity reactions characterized by rash, constitutional findings, and organ dysfunction (including hepatic failure) have occurred.

American Society of Health-System Pharmacists 2012; Drug Information 2012. Bethesda, MD. 2012


Raltegravir and any other suspect agents should be discontinued immediately if signs or symptoms of severe skin or hypersensitivity reactions occur, including (but not limited to) severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, or angioedema. Clinical status, including liver aminotransferases, should be monitored and appropriate therapy initiated. A life-threatening reaction could occur if there is a delay in discontinuing raltegravir or other suspect agents after the onset of severe rash.

American Society of Health-System Pharmacists 2012; Drug Information 2012. Bethesda, MD. 2012


During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium, M. tuberculosis, cytomegalovirus (CMV), Pneumocystis jiroveci (formerly P. carinii), varicella-zoster virus (VZV)); this may necessitate further evaluation and treatment. Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barre syndrome) have been reported to occur in the setting of immune reconstitution; the time to onset is more variable and can occur many months after initiation of antiretroviral therapy.

American Society of Health-System Pharmacists 2012; Drug Information 2012. Bethesda, MD. 2012, p. 691


Individuals with phenylketonuria (i.e., homozygous genetic deficiency of phenylalanine hydroxylase) and other individuals who must restrict their intake of phenylalanine should be advised that raltegravir chewable tablets contain aspartame (NutraSweet), which is metabolized in the GI tract to phenylalanine. Each 25-mg chewable tablet provides approximately 0.05 mg of phenylalanine and each 100-mg chewable tablet provides approximately 0.1 mg of phenylalanine.

American Society of Health-System Pharmacists 2012; Drug Information 2012. Bethesda, MD. 2012


For more Drug Warnings (Complete) data for Raltegravir (12 total), please visit the HSDB record page.


4.4 Drug Indication

For the treatment of HIV-1 infection in conjunction with other antiretrovirals.


FDA Label


Isentress is indicated in combination with other anti-retroviral medicinal products for the treatment of human immunodeficiency virus (HIV 1) infection.


Treatment of human immunodeficiency virus (HIV-1) infection


5 Pharmacology and Biochemistry
5.1 MeSH Pharmacological Classification

Anti-HIV Agents

Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. (See all compounds classified as Anti-HIV Agents.)


HIV Integrase Inhibitors

Inhibitors of HIV INTEGRASE, an enzyme required for integration of viral DNA into cellular DNA. (See all compounds classified as HIV Integrase Inhibitors.)


5.2 FDA Pharmacological Classification
5.2.1 Active Moiety
RALTEGRAVIR
5.2.2 FDA UNII
22VKV8053U
5.2.3 Pharmacological Classes
Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor [EPC]; HIV Integrase Inhibitors [MoA]
5.3 ATC Code

J05AJ01


J05AX08

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


J - Antiinfectives for systemic use

J05 - Antivirals for systemic use

J05A - Direct acting antivirals

J05AJ - Integrase inhibitors

J05AJ01 - Raltegravir


5.4 Absorption, Distribution and Excretion

Absorption

Absorbed from the gastrointestinal tract.


Route of Elimination

Feces and urine


Volume of Distribution

Approximately 83% bound to human plasma protein and is minimally distributed into red blood cells (blood-to-plasma partitioning ratio of 0.6).


Clearance

The major mechanism of clearance of raltegravir in humans is glucuronidation mediated by UGT1A1, the renal clearance of unchanged drug is a minor pathway of elimination of raltegravir (9% of total dose).


Raltegravir (film-coated tablet) is absorbed with a Tmax of approximately 3 hours postdose in the fasted state. Raltegravir AUC and Cmax increase dose proportionally over the dose range 100 mg to 1600 mg. Raltegravir C12hr increases dose proportionally over the dose range of 100 to 800 mg and increases slightly less than dose proportionally over the dose range 100 mg to 1600 mg.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


With twice-daily dosing, pharmacokinetic steady state is achieved within approximately the first 2 days of dosing. There is little to no accumulation in AUC and Cmax. The average accumulation ratio for C12hr ranged from approximately 1.2 to 1.6.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


The absolute bioavailability of raltegravir has not been established. Based on a formulation comparison study in healthy adult volunteers, the chewable tablet has higher oral bioavailability compared to the 400 mg film-coated tablet.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


In subjects who received 400 mg twice daily alone, raltegravir drug exposures were characterized by a geometric mean AUC0-12hr of 14.3 uM.hr and C12hr of 142 nM.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


For more Absorption, Distribution and Excretion (Complete) data for Raltegravir (13 total), please visit the HSDB record page.


5.5 Metabolism/Metabolites

Hepatic (UGT1A1)


In feces, only raltegravir was present, most of which is likely derived from hydrolysis of raltegravir-glucuronide secreted in bile as observed in preclinical species. Two components, namely raltegravir and raltegravir-glucuronide, were detected in urine and accounted for approximately 9 and 23% of the dose, respectively. The major circulating entity was raltegravir and represented approximately 70% of the total radioactivity; the remaining radioactivity in plasma was accounted for by raltegravir-glucuronide.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


Studies using isoform-selective chemical inhibitors and cDNA-expressed UDP-glucuronosyltransferases (UGT) show that UGT1A1 is the main enzyme responsible for the formation of raltegravir-glucuronide. Thus, the data indicate that the major mechanism of clearance of raltegravir in humans is UGT1A1-mediated glucuronidation.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


5.6 Biological Half-Life

9 hours


The apparent terminal half-life of raltegravir is approximately 9 hours, with a shorter alpha-phase half-life (approximetly1 hour) accounting for much of the AUC.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


5.7 Mechanism of Action

Raltegravir inhibits HIV integrase to prevent the viral genome being incorporated into the human genome. Raltegravir is primarily metabolized by glucuronidation.


Raltegravir inhibits the catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of unintegrated linear HIV-1 DNA into the host cell genome preventing the formation of the HIV-1 provirus. The provirus is required to direct the production of progeny virus, so inhibiting integration prevents propagation of the viral infection. Raltegravir did not significantly inhibit human phosphoryltransferases including DNA polymerases alpha, beta, and gamma.

US Natl Inst Health; DailyMed. Current Medication Information for ISENTRESS (raltegravir) tablet, film coated; tablet, chewable (Janurary 2013). Available from, as of March 14, 2013: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3


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Hetero Drugs

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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06

Maithri Drugs

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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Maithri Drugs

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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07

Viatris

U.S.A

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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Viatris

U.S.A

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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08

Viatris

U.S.A

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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Viatris

U.S.A

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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09

Lupin Ltd

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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Lupin Ltd

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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10

Emcure Pharmaceuticals

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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Emcure Pharmaceuticals

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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USDMF

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01

Discovery on Target
Not Confirmed

01

Discovery on Target
Not Confirmed

GDUFA

DMF Review : Complete

Rev. Date : 2024-02-14

Pay. Date : 2023-12-22

DMF Number : 39315

Submission : 2023-12-30

Status : Active

Type : II

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02

Discovery on Target
Not Confirmed

03

Hetero Drugs Ltd

India

USDMF

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Discovery on Target
Not Confirmed

03

Discovery on Target
Not Confirmed

GDUFA

DMF Review : N/A

Rev. Date :

Pay. Date :

DMF Number : 25261

Submission : 2011-09-06

Status : Active

Type : II

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04

Hetero Drugs Ltd

India

USDMF

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Discovery on Target
Not Confirmed

04

Discovery on Target
Not Confirmed

GDUFA

DMF Review : Complete

Rev. Date : 2023-02-08

Pay. Date : 2023-01-10

DMF Number : 37182

Submission : 2022-12-10

Status : Active

Type : II

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05

Lee Pharma Ltd

India

USDMF

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Discovery on Target
Not Confirmed

06

Discovery on Target
Not Confirmed

07

Lupin Ltd

India

USDMF

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Discovery on Target
Not Confirmed

08

Discovery on Target
Not Confirmed

09

Discovery on Target
Not Confirmed

09

Discovery on Target
Not Confirmed

GDUFA

DMF Review : Complete

Rev. Date : 2014-03-31

Pay. Date : 2013-12-09

DMF Number : 27728

Submission : 2013-12-24

Status : Active

Type : II

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10

Discovery on Target
Not Confirmed

10

Discovery on Target
Not Confirmed

GDUFA

DMF Review : Complete

Rev. Date : 2016-09-02

Pay. Date : 2016-06-21

DMF Number : 30595

Submission : 2016-06-24

Status : Active

Type : II

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CEP/COS

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TIANISH LABORATORIES PRIVATE LIMITE...

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CEP 2020-216 - Rev 01
Valid
Chemical
2024-07-25
2887
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01

TIANISH LABORATORIES PRIVATE LIMITE...

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Luxepack
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TIANISH LABORATORIES PRIVATE LIMITE...

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Certificate Number : CEP 2020-216 - Rev 01

Status : Valid

Issue Date : 2024-07-25

Type : Chemical

Substance Number : 2887

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Listed Suppliers

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01

LGM Pharma

U.S.A
  • fda
  • EDQM
  • WHO-GMP

Virtual BoothLGM Pharma accelerates & optimizes the new product pathway from early development through commercialization.

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Raltegravir Potassium

About the Company : LGM Pharma is a global leader in sourcing hard-to-find APIs and intermediates for the pharmaceutical and biotech industries. LGM is also a full service CDMO providing formulation, ...

LGM Pharma is a global leader in sourcing hard-to-find APIs and intermediates for the pharmaceutical and biotech industries. LGM is also a full service CDMO providing formulation, analytical method development and testing, and commercial manufacturing. LGM Pharma offers custom API synthesis, analytical development, and regulatory services. With a network of over 300 accredited CGMP manufacturing partners, LGM provides unparalleled supply chain security. And, with over 100,000 square feet of FDA-inspected cGMP manufacturing and warehouse capacity, LGM Pharma provides a one-stop solution for solid dose, powder, semi-solid and liquid drugs.
LGM Pharma CB

02

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothHRV Global Life Sciences - Market Expansion Leader in Pharmaceuticals.

Flag India
Digital Content Digital Content

Raltegravir Potassium

About the Company : HRV Global is a leading global manufacturer, seller & exporter of a wide range of APIs, advanced intermediates, pellets, food grade chemicals, food additives & food ingredients. It...

HRV Global is a leading global manufacturer, seller & exporter of a wide range of APIs, advanced intermediates, pellets, food grade chemicals, food additives & food ingredients. It offers services such as sourcing, manufacturing and supply, helping partners enter new markets worldwide. Its strong partnerships with major players in the pharma and food additive industries help HRV Global effectively promote projects and products. HRV Global represents over 30 large Indian drugmakers, primarily targeting Europe, the US and the Middle East markets. Headquartered in India, HRV Global has offices in the US, Switzerland, Dubai, Lithuania & Turkey.
HRV Global Life Sciences

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Raltegravir Potassium

About the Company : Since 2004, Arene Lifesciences Private Limited is committed to a cause to deliver the best and to aim for continuous improvement in order to transform new knowledge into innovative...

Since 2004, Arene Lifesciences Private Limited is committed to a cause to deliver the best and to aim for continuous improvement in order to transform new knowledge into innovative synthetic processes, designed to ensure quality, efficiency and sustainability. Our leaders step outside to do things that symbolize our vision “to be recognized as a one of the leading Global manufacturers of Quality API and their intermediates”.Our expert teams maintain the highest global standards of quality and regulatory compliance, while our unparalleled customer support and attention will help our customers to maintain a competitive edge in the market.
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Lee Pharma

India
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Lee Pharma

India
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Raltegravir Potassium

About the Company : Lee helps you focus on the business results that matter to your company. Over the years, we have leveraged our position in the global market with an enviable list of clients and a ...

Lee helps you focus on the business results that matter to your company. Over the years, we have leveraged our position in the global market with an enviable list of clients and a phenomenal growth rate achieved through product innovation, dedicated teams and timely implementation of solutions. Our success is based on providing a value-added service by adopting a customer-orientated approach. Our corporate independence allows us to respond as fast as possible, gives us a greater flexibility, and enables us to invest in plant and processes.
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05

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Raltegravir Potassium

About the Company : Maithri Drugs is one of India's fast-growing pharmaceutical companies. Maithri's strategic focus is on active pharma ingredients (APIs). The company is widely recognized for its ex...

Maithri Drugs is one of India's fast-growing pharmaceutical companies. Maithri's strategic focus is on active pharma ingredients (APIs). The company is widely recognized for its excellent research & development and aggressive growth strategies. Our 32 US DMFs and 9 CEPs in a short span attest to our R&D excellence. Maithri's manufacturing facility is located in Hyderabad. This facility is audited and approved by the US FDA. In addition, our facility is certified according to the standards of DCGI, WHO GMP, and ISO 9001:2015 We have a portfolio of 65 products and are continually expanding.
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06

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Raltegravir Potassium

About the Company : Prajna is an innovation driven pharmaceutical company. We dedicated to Research, Process development and Manufacturing APIs and Advanced Intermediates for Active Pharmaceutical Ing...

Prajna is an innovation driven pharmaceutical company. We dedicated to Research, Process development and Manufacturing APIs and Advanced Intermediates for Active Pharmaceutical Ingredients (APIs) for the global pharmaceutical companies. It provides value-added services in Contract Research, Custom Synthesis, and Specialties Scientific technology (Green Process, APIs Process Development, Polymorphism, Crystallisation and Purification) for Pharmaceutical and Life Sciences industry.
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07

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Raltegravir

About the Company : SAINTSUN PHARMA, we are engaging mainly in the manufacturing and distributing APIs, Pharmaceutical Intermediates, Chemicals, Formulations, Medical supplies, etc... With a self-owne...

SAINTSUN PHARMA, we are engaging mainly in the manufacturing and distributing APIs, Pharmaceutical Intermediates, Chemicals, Formulations, Medical supplies, etc... With a self-owned brand of "SAINTSUN PHARMA", after more than 12 years efforts, our products are successfully expanded to different continents like Asia, South America, Africa more than 35 countries and regions.
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Raltegravir

About the Company : Founded in 1995, Shenzhen Oriental Pharma focussed on the production of Active Pharma Ingredients (APIs), Now the main product is Phenylephrine Hcl (PE), Doxylamine succinate.We ha...

Founded in 1995, Shenzhen Oriental Pharma focussed on the production of Active Pharma Ingredients (APIs), Now the main product is Phenylephrine Hcl (PE), Doxylamine succinate.We have 14 years production experience for Phenylephrine Hcl, granted the GMP for PE in 2004,re-certified in 2009. A DMF has been submitted to FDA in 2005 (DMF # 18799), this product passed the US FDA inspection in March 2014. According to the customer’s needs, we can supply the APIs conforming to the current standard of USP, EP and CP .At the same time, we can supply various particle sizes product.
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Raltegravir

About the Company : SMS Pharmaceuticals Ltd. is a global player in API manufacturing having a strong research and manufacturing team supported by state of the art facilities. What started off as a sin...

SMS Pharmaceuticals Ltd. is a global player in API manufacturing having a strong research and manufacturing team supported by state of the art facilities. What started off as a single facility - single product manufacturing company in 1990 grew to be a multi-location group having product list spreading across an array of therapeutic segments. SMS was given the export house status in the year 1997-98. SMS is currently a listed company having ever appreciating international and domestic customer base.
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10

Viatris

U.S.A
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Viatris

U.S.A
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Raltegravir Potassium

About the Company : In November 2020, Viatris was formed through the combination of Mylan and Upjohn, with a mission of empowering people worldwide to live healthier at every stage of life. Viatris (N...

In November 2020, Viatris was formed through the combination of Mylan and Upjohn, with a mission of empowering people worldwide to live healthier at every stage of life. Viatris (NASDAQ: VTRS) is a global healthcare company empowering people worldwide to live healthier at every stage of life. We provide access to medicines, advance sustainable operations, develop innovative solutions and leverage our collective expertise to connect more people to more products and services through our one-of-a-kind Global Healthcare Gateway®. Formed in November 2020.
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API Reference Price

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DIST.AP","customerAddress":""},{"dataSource":"API Export","activeIngredients":"RALTEGRAVIR POTASSIUM","year":"2021","qtr":"Q1","strtotime":1614018600,"product":"RALTEGRAVIR POTASSIUM (MILLED)","address":"7.1.77\/E\/1\/303, DHARAM KARAM ROAD","city":"HYDERABAD,A.P.","supplier":"DIVIS LABORATORIES","supplierCountry":"INDIA","foreign_port":"SINGAPORE","customer":"MERCK & CO","customerCountry":"SINGAPORE","quantity":"425.00","actualQuantity":"425","unit":"KGS","unitRateFc":"767.1","totalValueFC":"322403.7","currency":"USD","unitRateINR":55230.945882352942,"date":"23-Feb-2021","totalValueINR":"23473152","totalValueInUsd":"322403.7","indian_port":"Vizag-DLL SEZ","hs_no":"29349990","bill_no":"4000261","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"SINGAPORE","selfForZScoreResived":"Pharma Grade","supplierPort":"Vizag-DLL SEZ","supplierAddress":"7.1.77\/E\/1\/303, DHARAM KARAM ROAD, HYDERABAD,A.P.","customerAddress":""},{"dataSource":"API 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HILLS,","city":"HYDEABAD.AP","supplier":"LAURUS LABS","supplierCountry":"INDIA","foreign_port":"PHILADELPHIA METROP","customer":"SIGMAPHARM LABORATORIES, LLC","customerCountry":"UNITED STATES","quantity":"5.00","actualQuantity":"5","unit":"KGS","unitRateFc":"2279","totalValueFC":"11277.6","currency":"USD","unitRateINR":164204.576,"date":"19-Mar-2021","totalValueINR":"821022.88","totalValueInUsd":"11277.6","indian_port":"HYDERABAD AIR","hs_no":"29349990","bill_no":"9495746","productDescription":"API","marketType":"REGULATED MARKET","country":"UNITED STATES","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"2ND FLOOR, SERENE CHAMBERS,ROAD NO. 7, BANJARA HILLS,, HYDEABAD.AP","customerAddress":""},{"dataSource":"API Export","activeIngredients":"RALTEGRAVIR POTASSIUM","year":"2021","qtr":"Q1","strtotime":1616351400,"product":"RALTEGRAVIR POTASSIUM","address":"2ND FLOOR, SERENE CHAMBERS,ROAD NO. 7, BANJARA HILLS,","city":"HYDEABAD.AP","supplier":"LAURUS LABS","supplierCountry":"INDIA","foreign_port":"ZAGREB","customer":"A2B EXPRESS LIGISTIKA ","customerCountry":"CROATIA","quantity":"4.00","actualQuantity":"4","unit":"KGS","unitRateFc":"3332.5","totalValueFC":"13192.3","currency":"USD","unitRateINR":240105.23000000001,"date":"22-Mar-2021","totalValueINR":"960420.92","totalValueInUsd":"13192.3","indian_port":"HYDERABAD AIR","hs_no":"29349990","bill_no":"9537658","productDescription":"API","marketType":"REGULATED MARKET","country":"CROATIA","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"2ND FLOOR, SERENE CHAMBERS,ROAD NO. 7, BANJARA HILLS,, HYDEABAD.AP","customerAddress":""},{"dataSource":"API Export","activeIngredients":"RALTEGRAVIR POTASSIUM","year":"2021","qtr":"Q1","strtotime":1616524200,"product":"RALTEGRAVIR POTASSIUM","address":"7.1.77\/E\/1\/303, DHARAM KARAM ROAD","city":"HYDERABAD,A.P.","supplier":"DIVIS LABORATORIES","supplierCountry":"INDIA","foreign_port":"SINGAPORE","customer":"MERCK 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ROAD,KALINA, SANTACRUZ (E)","city":"MUMBAI,MAHARASHTRA","supplier":"LUPIN LTD","supplierCountry":"INDIA","foreign_port":"MOSCOW","customer":"ALPHARMA LLC","customerCountry":"RUSSIA","quantity":"5.00","actualQuantity":"5","unit":"KGS","unitRateFc":"2859.7","totalValueFC":"14064.5","currency":"USD","unitRateINR":206042.61000000002,"date":"28-May-2021","totalValueINR":"1030213.05","totalValueInUsd":"14064.5","indian_port":"BOMBAY AIR","hs_no":"29420090","bill_no":"2057747","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"RUSSIA","selfForZScoreResived":"Crystalline","supplierPort":"BOMBAY AIR","supplierAddress":"159, C.S.T. ROAD,KALINA, SANTACRUZ (E), MUMBAI,MAHARASHTRA","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2021","qtr":"Q2","strtotime":1623609000,"product":"RALTEGRAVIR POTASSIUM","address":"7.1.77\/E\/1\/303, DHARAM KARAM ROAD","city":"HYDERABAD,A.P.","supplier":"DIVIS LABORATORIES","supplierCountry":"INDIA","foreign_port":"SHANGHAI","customer":"MERCK & CO","customerCountry":"CHINA","quantity":"500.00","actualQuantity":"500","unit":"KGS","unitRateFc":"728","totalValueFC":"357587.5","currency":"USD","unitRateINR":52598,"date":"14-Jun-2021","totalValueINR":"26299000","totalValueInUsd":"357587.5","indian_port":"Vizag-DLL SEZ","hs_no":"29349990","bill_no":"4000843","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"Vizag-DLL SEZ","supplierAddress":"7.1.77\/E\/1\/303, DHARAM KARAM ROAD, HYDERABAD,A.P.","customerAddress":""},{"dataSource":"API 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16-Feb-2021
01-Aug-2024
KGS
overview
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Average Price (USD/KGS)

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Total Quantity (KGS)

Total Value (USD)

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

API Imports and Exports

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(USD/KGS)
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DOSAGE - TABLET;ORAL - EQ 400MG BASE

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DOSAGE - TABLET;ORAL - EQ 600MG BASE

USFDA APPLICATION NUMBER - 22145

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