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Maraviroc

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TABLET;ORAL - 300MG
TABLET;ORAL - 75MG

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Chemistry

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Also known as: 376348-65-1, Selzentry, Celsentri, Uk-427857, Uk-427,857, Uk 427857

Molecular Formula

C₂₉H₄₁F₂N₅O

Molecular Weight

513.7 g/mol

InChI Key

GSNHKUDZZFZSJB-HLMSNRGBSA-N

FDA UNII

MD6P741W8A

A cyclohexane and triazole derivative that acts as an antagonist of the CCR5 RECEPTOR. It prevents infection by HIV-1 virus strains which use CCR5 as a co-receptor for membrane fusion and cellular entry.

Maraviroc is a CCR5 Co-receptor Antagonist. The mechanism of action of maraviroc is as a Chemokine Co-receptor 5 Antagonist.

1 2D Structure

Maraviroc

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

4,4-difluoro-N-[(1S)-3-[(1S,5R)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide

2.1.2 InChI

InChI=1S/C29H41F2N5O/c1-19(2)27-34-33-20(3)36(27)25-17-23-9-10-24(18-25)35(23)16-13-26(21-7-5-4-6-8-21)32-28(37)22-11-14-29(30,31)15-12-22/h4-8,19,22-26H,9-18H2,1-3H3,(H,32,37)/t23-,24+,25?,26-/m0/s1

2.1.3 InChI Key

GSNHKUDZZFZSJB-HLMSNRGBSA-N

2.1.4 Canonical SMILES

CC1=NN=C(N1C2CC3CCC(C2)N3CCC(C4=CC=CC=C4)NC(=O)C5CCC(CC5)(F)F)C(C)C

2.1.5 Isomeric SMILES

CC1=NN=C(N1C2C[C@H]3CC[C@@H](C2)N3CC[C@@H](C4=CC=CC=C4)NC(=O)C5CCC(CC5)(F)F)C(C)C

2.2 Other Identifiers

2.2.1 UNII

MD6P741W8A

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 4,4-difluoro-n-((1s)-3-(exo-3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo(3.2.1)oct-8-yl)-1-phenylpropyl)cyclohexanecarboxamide

2. Selzentry

3. Uk 427,857

4. Uk 427857

5. Uk-427,857

6. Uk-427857

7. Uk427,857

8. Uk427857

2.3.2 Depositor-Supplied Synonyms

1. 376348-65-1

2. Selzentry

3. Celsentri

4. Uk-427857

5. Uk-427,857

6. Uk 427857

7. Md6p741w8a

8. Chembl256907

9. 4,4-difluoro-n-[(1s)-3-[(1r,5s)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide

10. Mvc

11. Chembl1201187

12. Chebi:63608

13. Ncgc00183109-02

14. 4,4-difluoro-n-((1s)-3-((1r,5s)-3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexane-1-carboxamide

15. Celsentri(tm)

16. Selzentry(tm)

17. [3h]maraviroc

18. 4,4-difluoro-n-((1s)-3-((1r,5s)-3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide

19. 4,4-difluoro-n-[(1s)-3-{(3-exo)-3-[3-methyl-5-(propan-2-yl)-4h-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]oct-8-yl}-1-phenylpropyl]cyclohexanecarboxamide

20. Pro 140 & Maraviroc

21. Maravirocum

22. Maraviroc [inn:ban:jan]

23. Unii-md6p741w8a

24. Rel-maraviroc

25. Hsdb 8021

26. 4,4-difluoro-n-[(1s)-3-[(1s,5r)-3-(3-isopropyl-5-methyl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenyl-propyl]cyclohexanecarboxamide

27. Uk-427,857 Maraviroc (mvc)

28. Maraviroc [inn]

29. Maraviroc [jan]

30. Maraviroc [mi]

31. [3h]uk 427,857

32. [3h]uk-427,857

33. Maraviroc [vandf]

34. Maraviroc [mart.]

35. (non-labelled)maraviroc-d6

36. Maraviroc [who-dd]

37. Dsstox_cid_28875

38. Dsstox_rid_83144

39. Dsstox_gsid_48949

40. Schembl51991

41. Gtpl803

42. Gtpl806

43. Maraviroc [ema Epar]

44. Cyclohexanecarboxamide, 4,4-difluoro-n-((1s)-3-((3-exo)-3-(3-methyl-5-(1-methylethyl)-4h-1,2,4-triazol-4-yl)-8-azabicyclo(3.2.1)oct-8-yl)-1-phenylpropyl)-

45. Isopropyl, 4,4-difluoro-n-((1s)-3-{(1r,3s,5s)-3-(3-methyl-5-(propan-2-yl)-4h-1,2,4-triazol-4-yl)-8-azabicyclo(3.2.1)octan-8-yl}-1-phenylpropyl)cyclohexanecarboxamide

46. Mls006011960

47. Chembl584744

48. Schembl2177194

49. Schembl4576508

50. Maraviroc [orange Book]

51. Dtxsid8048949

52. Maraviroc, >=98% (hplc)

53. Ex-a200

54. Chebi:184662

55. Amy12578

56. Zinc3817234

57. Tox21_113369

58. Ac-558

59. Bdbm50334986

60. Bdbm50464147

61. Akos025402143

62. Akos032960315

63. Zinc100003902

64. Zinc101160855

65. Cs-0366

66. Db04835

67. Ncgc00183109-01

68. As-75265

69. Exo-4,4-difluoro-n-[3-[3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1(s)-phenylpropyl]cyclohexanecarboxamide

70. Hy-13004

71. Pro 140 (anti-ccr5 Monoclonal Antibody) & Exo-4,4-difluoro-n-[3-[3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1(s)-phenylpropyl]cyclohexanecarboxamide

72. Smr004703532

73. Cas-376348-65-1

74. 348m651

75. Q421369

76. Sr-01000942244

77. J-521678

78. Sr-01000942244-1

79. Brd-a23284911-001-02-4

80. Z1618161028

81. 4,4-difluoro-cyclohexanecarboxylic Acid {(s)-3-[(1s,5s)-3-(3-isopropyl-5-methyl-[1,2,4]triazol-4-yl)-8-aza-bicyclo[3.2.1]oct-8-yl]-1-phenyl-propyl}-amide

82. 4,4-difluoro-n-((1s)-3-((1r,3s,5s)-3-(3-methyl-5-(propan-2-yl)-4h-1,2,4-triazol-4-yl)-8-azabicyclo(3.2.1)octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide

83. 4,4-difluoro-n-((1s)-3-(3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide

84. 4,4-difluoro-n-((s)-3-((1r,3r,5s)-3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexane-1-carboxamide

85. 4,4-difluoro-n-((s)-3-((1s,3r,5r)-3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-aza-bicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide

86. 4,4-difluoro-n-((s)-3-((1s,3s,5r)-3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-aza-bicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide

87. 4,4-difluoro-n-((s)-3-(3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-aza-bicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide

88. 4,4-difluoro-n-[(1s)-3-[(1r,3s,5s)-3-[3-methyl-5-(propan-2-yl)-4h-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide

89. 4,4-difluoro-n-[(1s)-3-[(1r,5s)-3-(3-isopropyl-5-methyl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenyl-propyl]cyclohexanecarboxamide

90. 4,4-difluoro-n-[(1s)-3-[(1r,5s)-3-[3-methyl-5-(propan-2-yl)-4h-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide

91. 4,4-difluoro-n-[(1s)-3-[(1r,5s)-3-[3-methyl-5-(propan-2-yl)-4h-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboximidic Acid

92. 4,4-difluoro-n-{(1s)-3-[(3-exo)-3-(3-isopropyl-5-methyl-4h-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl}cyclohexanecarboxamide

93. 4,4-diluoro-n-[(1s)-3-[(1s,5r)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide

94. Cyclohexanecarboxamide,4,4-difluoro-n-[(1s)-3-[(3-exo)-3-[3-methyl-5-(1-methylethyl)-4h-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl]-

95. Mrv

2.4 Create Date

2005-08-01

3 Chemical and Physical Properties

Molecular Formula	C₂₉H₄₁F₂N₅O
Molecular Weight	513.7 g/mol
XLogP3	5.1
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	8
Exact Mass	513.32791727 g/mol
Monoisotopic Mass	513.32791727 g/mol
Topological Polar Surface Area	63 Å²
Heavy Atom Count	37
Formal Charge	0
Complexity	751
Isotope Atom Count	0
Defined Atom Stereocenter Count	3
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Selzentry
PubMed Health	Maraviroc (By mouth)
Drug Classes	Antiretroviral Agent
Drug Label	SELZENTRY (maraviroc) is a selective, slowly reversible, small molecule antagonist of the interaction between human CCR5 and HIV-1 gp120. Blocking this interaction prevents CCR5-tropic HIV-1 entry into cells.SELZENTRY is available as film-coated tabl...
Active Ingredient	Maraviroc
Dosage Form	Tablet
Route	Oral
Strength	150mg; 300mg
Market Status	Prescription
Company	Viiv Hlthcare

2 of 2
Drug Name	Selzentry
PubMed Health	Maraviroc (By mouth)
Drug Classes	Antiretroviral Agent
Drug Label	SELZENTRY (maraviroc) is a selective, slowly reversible, small molecule antagonist of the interaction between human CCR5 and HIV-1 gp120. Blocking this interaction prevents CCR5-tropic HIV-1 entry into cells.SELZENTRY is available as film-coated tabl...
Active Ingredient	Maraviroc
Dosage Form	Tablet
Route	Oral
Strength	150mg; 300mg
Market Status	Prescription
Company	Viiv Hlthcare

4.2 Therapeutic Uses

Receptors, CCR5/antagonists & inhibitors; HIV Fusion Inhibitors

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

Maraviroc, in combination with other antiretroviral agents, is indicated for adult patients infected with only CCR5-tropic HIV-1. This indication is based on analyses of plasma HIV-1 RNA levels in two controlled studies of maraviroc in treatment-experienced subjects and one study in treatment-naive subjects. Both studies in treatment-experienced subjects were conducted in clinically advanced, 3-class antiretroviral-experienced (NRTI, NNRTI, PI, or enfuvirtide) adults with evidence of HIV-1 replication despite ongoing antiretroviral therapy. /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for SELZENTRY (maraviroc) tablet, film coated (May 2010). Available from, as of February 21, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a94a9a2b-337b-4c13-8622-fc392194dc21

4.3 Drug Warning

/BOXED WARNING/ Hepatotoxicity has been reported with maraviroc use. Evidence of a systemic allergic reaction (e.g., pruritic rash, eosinophilia or elevated IgE) prior to the development of hepatotoxicity may occur. Patients with signs or symptoms of hepatitis or allergic reaction following use of maraviroc should be evaluated immediately.

Adult patients infected with only CCR5-tropic HIV-1 should use Maraviroc.

Tropism testing must be conducted with a highly sensitive tropism assay that has demonstrated the ability to identify patients appropriate for Maraviroc use. Outgrowth of pre-existing low-level CXCR4- or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on Maraviroc.

Use of Maraviroc is not recommended in subjects with dual/mixed or CXCR4-tropic HIV-1 as efficacy was not demonstrated in a phase 2 study of this patient group.

For more Drug Warnings (Complete) data for Maraviroc (26 total), please visit the HSDB record page.

4.4 Drug Indication

For treatment-experienced adult patients infected with only CCR5-tropic HIV-1 detectable, who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.

FDA Label

Celsentri, in combination with other antiretroviral medicinal products, is indicated for treatment experienced adults, adolescents and children of 2 years of age and older and weighing at least 10 kg infected with only CCR5-tropic HIV-1 detectable

5 Pharmacology and Biochemistry

5.1 Pharmacology

Maraviroc is a chemokine receptor antagonist drug developed by the drug company Pfizer that is designed to act against HIV by interfering with the interaction between HIV and CCR5.

5.2 MeSH Pharmacological Classification

CCR5 Receptor Antagonists

Compounds and drugs that inhibit or block the activity of CCR5 RECEPTORS. (See all compounds classified as CCR5 Receptor Antagonists.)

HIV Fusion Inhibitors

Inhibitors of the fusion of HIV to host cells, preventing viral entry. This includes compounds that block attachment of HIV ENVELOPE PROTEIN GP120 to CD4 RECEPTORS. (See all compounds classified as HIV Fusion Inhibitors.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

MARAVIROC

5.3.2 FDA UNII

MD6P741W8A

5.3.3 Pharmacological Classes

Chemokine Co-receptor 5 Antagonists [MoA]; CCR5 Co-receptor Antagonist [EPC]

5.4 ATC Code

J05AX09

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

J05AX - Other antivirals

J05AX09 - Maraviroc

5.5 Absorption, Distribution and Excretion

Absorption

The absolute oral bioavailability of a 100 mg dose is 23% and is predicted to be 33% at 300 mg. Coadministration of a 300mg tablet with a high fat breakfast reduced maraviroc Cmax and AUC by 33% in healthy volunteers.

Volume of Distribution

194 L

... Maraviroc (Celsentri) is an orally administered drug ... Maraviroc plasma exposure is not dose proportional. After a rapid (but moderate) intestinal absorption, several inactive oxidized metabolites are produced via cytochrome P450 3A4 pathway. ...

PMID:18455057 Peytavin G; Med Mal Infect 38 Suppl 1: S12-6 (2008)

Peak maraviroc plasma concentrations are attained 0.5-4 hr following single oral doses of 1-1200 mg administered to uninfected volunteers.

The absolute bioavailability of a 100 mg dose is 23% and is predicted to be 33% at 300 mg. Maraviroc is a substrate for the efflux transporter P-glycoprotein.

Coadministration of a 300mg tablet with a high fat breakfast reduced maraviroc Cmax and AUC by 33% in healthy volunteers. There were no food restrictions in the studies that demonstrated the efficacy and safety of maraviroc. Therefore, maraviroc can be taken with or without food at the recommended dose.

For more Absorption, Distribution and Excretion (Complete) data for Maraviroc (12 total), please visit the HSDB record page.

5.6 Metabolism/Metabolites

In vitro studies indicate that CYP3A is the major enzyme responsible for maraviroc metabolism.

Maraviroc is the major circulating component ( approximately 42% drug-related radioactivity) following a single oral dose of 300 mg(14)C-maraviroc. The most significant circulating metabolite in humans is a secondary amine (approximately 22% radioactivity) formed by N-dealkylation. This polar metabolite has no significant pharmacological activity. Other metabolites are products of mono-oxidation and are only minor components of plasma drug-related radioactivity.

Studies in humans and in vitro studies using human liver microsomes and expressed enzymes have demonstrated that maraviroc is principally metabolized by the cytochrome P450 system to metabolites that are essentially inactive against HIV-1. In vitro studies indicate that CYP3A is the major enzyme responsible for maraviroc metabolism. In vitro studies also indicate that polymorphic enzymes CYP2C9, CYP2D6 and CYP2C19 do not contribute significantly to the metabolism of maraviroc.

... Maraviroc is extensively metabolized by CYP3A4, with renal clearance accounting for approximately 23% of total clearance. ...

PMID:19704163 Abel S et al; Antivir Ther 14 (5): 607-18 (2009)

5.7 Biological Half-Life

14-18 hours

The terminal half-life of maraviroc following oral dosing to steady state in healthy subjects was 14-18 hours.

... The half-life of maraviroc is approximately 16 hr. ...

PMID:19704163 Abel S et al; Antivir Ther 14 (5): 607-18 (2009)

5.8 Mechanism of Action

Maraviroc is an entry inhibitor and works by blocking HIV from entering human cells. Specifically maraviroc is a selective, slowly reversible, small molecule antagonist of the interaction between human CCR5 and HIV-1 gp120. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the membrane of CD4 cells (T-cells), preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells.

Maraviroc, a synthetic antiretroviral agent, is an HIV entry inhibitor. The drug is a small molecule CCR5 antagonist. HIV enters host cells by attaching to the CD4+ T-cell receptor using 1 of 2 chemokine co-receptors, CCR5 or CXCR4. Maraviroc selectively binds to CCR5 on the cell membrane and prevents the interaction of HIV-1 glycoprotein 120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. Maraviroc does not inhibit entry of CXCR4-tropic and dual/mixed-tropic HIV-1 into cells. CCR5 is a co-receptor for the most commonly transmitted HIV-1 strains that predominate during the early stages of infection; this form remains the dominant form in many patients with late-stage infection. Maraviroc is active against some strains of HIV-1 resistant to nucleoside reverse transcriptase inhibitors (NRTIs), nonnucleoside reverse transcriptase inhibitors (NNRTIs), HIV protease inhibitors (PIs), and HIV entry and fusion inhibitors (enfuvirtide). HIV-1 strains with reduced susceptibility to maraviroc have been produced in vitro and have emerged during maraviroc therapy.

American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 654

Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc.

Maraviroc inhibits the replication of CCR5-tropic laboratory strains and primary isolates of HIV-1 in models of acute peripheral blood leukocyte infection. The mean EC50 value (50% effective concentration) for maraviroc against HIV-1 group M isolates (subtypes A to J and circulating recombinant form AE) and group O isolates ranged from 0.1 to 4.5 nM (0.05 to 2.3 ng/mL) in cell culture. ... Maraviroc was not active against CXCR4-tropic and dual-tropic viruses (EC50 value >10 uM). The antiviral activity of maraviroc against HIV-2 has not been evaluated.

Maraviroc (MVC, Celsentri) is an allosteric and reversible inhibitor of the CCR5 chemokine coreceptor. ... MVC exclusively inhibits the replication of R5- tropic HIV-1 variants after binding to the transmembrane CCR5 receptor cavity.

PMID:19133216 Soriano V, Poveda E; Enferm Infecc Microbiol Clin 26 Suppl 11: 12-6 (2008)

For more Mechanism of Action (Complete) data for Maraviroc (6 total), please visit the HSDB record page.

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