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Accession NumberDB04835
TypeSmall Molecule
GroupsApproved, Investigational

Maraviroc (brand-named Selzentry, or Celsentri outside the U.S.) 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. It was originally labelled as UK-427857 during development but was assigned the Maraviroc name as it entered trials. It was approved for use by the FDA in August, 2007.

SynonymsNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Selzentrytablet, film coated150 mgoralPfizer Laboratories Div Pfizer Inc2007-08-06Not AvailableUs
Selzentrytablet, film coated300 mgoralPfizer Laboratories Div Pfizer Inc2007-08-06Not AvailableUs
Selzentrytablet, film coated300 mgoralVii V Healthcare Company2010-09-012015-03-31Us
Selzentrytablet, film coated150 mgoralVii V Healthcare Company2011-05-16Not AvailableUs
Selzentrytablet, film coated300 mgoralVii V Healthcare Company2011-05-16Not AvailableUs
Selzentrytablet, film coated150 mgoralREMEDYREPACK INC.2013-02-18Not AvailableUs
Selzentrytablet, film coated300 mgoralPhysicians Total Care, Inc.2007-12-19Not AvailableUs
Celsentritablet150 mgoralViiv Healthcare UlcNot AvailableNot AvailableCanada
Celsentritablet300 mgoralViiv Healthcare UlcNot AvailableNot AvailableCanada
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
CAS number376348-65-1
WeightAverage: 513.6655
Monoisotopic: 513.327917369
Chemical FormulaC29H41F2N5O
DescriptionThis compound belongs to the class of organic compounds known as phenylpropylamines. These are compounds containing a phenylpropylamine moiety, which consists of a phenyl group substituted at the third carbon by an propan-1-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylpropylamines
Direct ParentPhenylpropylamines
Alternative Parents
  • Phenylpropylamine
  • Tropane alkaloid
  • Aralkylamine
  • 4-aminopiperidine
  • N-alkylpyrrolidine
  • Piperidine
  • Heteroaromatic compound
  • 1,2,4-triazole
  • Pyrrolidine
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
IndicationFor 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.
PharmacodynamicsMaraviroc 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.
Mechanism of actionMaraviroc 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.
AbsorptionThe 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
Protein bindingApproximately 76% bound to human plasma proteins, with moderate affinity for albumin and alpha-1 acid glycoprotein.

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

Route of eliminationNot Available
Half life14-18 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Human Immunodeficiency Virus
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Predicted ADMET features
Human Intestinal Absorption+0.997
Blood Brain Barrier+0.8329
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.6716
P-glycoprotein inhibitor IInhibitor0.8931
P-glycoprotein inhibitor IIInhibitor0.9431
Renal organic cation transporterNon-inhibitor0.5695
CYP450 2C9 substrateNon-substrate0.8308
CYP450 2D6 substrateNon-substrate0.7344
CYP450 3A4 substrateSubstrate0.8199
CYP450 1A2 substrateNon-inhibitor0.8616
CYP450 2C9 substrateInhibitor0.6028
CYP450 2D6 substrateNon-inhibitor0.8331
CYP450 2C19 substrateInhibitor0.5684
CYP450 3A4 substrateInhibitor0.6066
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7814
Ames testNon AMES toxic0.63
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7115 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9864
hERG inhibition (predictor II)Inhibitor0.8971
ManufacturersNot Available
Dosage forms
Tabletoral150 mg
Tabletoral300 mg
Tablet, film coatedoral150 mg
Tablet, film coatedoral300 mg
Unit descriptionCostUnit
Selzentry 150 mg tablet18.36USD tablet
Selzentry 300 mg tablet18.36USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
CountryPatent NumberApprovedExpires (estimated)
United States65864301999-12-012019-12-01
United States73684602002-11-252022-11-25
Experimental PropertiesNot Available
Predicted Properties
Water Solubility0.0106 mg/mLALOGPS
pKa (Strongest Acidic)14.5ChemAxon
pKa (Strongest Basic)9.38ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area63.05 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity142.88 m3·mol-1ChemAxon
Polarizability55.59 Å3ChemAxon
Number of Rings5ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Mass Spec (NIST)Not Available
SpectraNot Available
Synthesis Reference

General ReferenceNot Available
External Links
ATC CodesJ05AX09
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (241 KB)
MSDSNot Available
Drug Interactions
Azilsartan medoxomilPharmacodynamic synergist- increases effects.
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Maraviroc. When used with a strong CYP3A4 inhibitor, the adult dose of maraviroc should be decreased to 150 mg twice daily. Maraviroc is contraindicated in patients with severe renal impairment (creatinine clearance less than 30 mL/min) receiving a strong CYP3A4 inhibitor. Maraviroc may be administered at a dose of 300 mg twice daily with concomitant tipranavir/ritonavir but not with other ritonavir combinations.
EtravirineMaraviroc, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
TelithromycinTelithromycin may reduce clearance of Maraviroc. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Maraviroc if Telithromycin is initiated, discontinued or dose changed.
TopiramateTopiramate, a CYP3A4 inducer, may decrease the serum concentration of Maraviroc by increasing Maraviroc metabolism and clearance. A dose adjustment of Maraviroc may be required. Monitor for changes in Maraviroc therapeutic and adverse effects if Topiramate is initiated, discontinued or dose changed.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of maraviroc by decreasing its metabolism. A dose reduction in maraviroc is warranted. Monitor for changes in the therapeutic and adverse effects of maraviroc if voriconazole is initiated, discontinued or dose changed.
Food InteractionsNot Available


1. C-C chemokine receptor type 5

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist


Name UniProt ID Details
C-C chemokine receptor type 5 P51681 Details


  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  4. Levy JA: HIV pathogenesis: 25 years of progress and persistent challenges. AIDS. 2009 Jan 14;23(2):147-60. Pubmed
  5. Agrawal-Gamse C, Lee FH, Haggarty B, Jordan AP, Yi Y, Lee B, Collman RG, Hoxie JA, Doms RW, Laakso MM: Adaptive mutations in a human immunodeficiency virus type 1 envelope protein with a truncated V3 loop restore function by improving interactions with CD4. J Virol. 2009 Nov;83(21):11005-15. Epub 2009 Aug 19. Pubmed
  6. Napier C, Sale H, Mosley M, Rickett G, Dorr P, Mansfield R, Holbrook M: Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human. Biochem Pharmacol. 2005 Dec 19;71(1-2):163-72. Epub 2005 Nov 18. Pubmed


1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate


Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details


  1. Abel S, Back DJ, Vourvahis M: Maraviroc: pharmacokinetics and drug interactions. Antivir Ther. 2009;14(5):607-18. Pubmed
  2. Abel S, Jenkins TM, Whitlock LA, Ridgway CE, Muirhead GJ: Effects of CYP3A4 inducers with and without CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers. Br J Clin Pharmacol. 2008 Apr;65 Suppl 1:38-46. Pubmed
  3. Mannu J, Jenardhanan P, Mathur PP: A computational study of CYP3A4 mediated drug interaction profiles for anti-HIV drugs. J Mol Model. 2010 Nov 16. Pubmed

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Drug created on September 11, 2007 19:14 / Updated on October 08, 2013 14:24