Description

Simple

A medication used to treat human immunodeficiency virus (HIV) infections.

Clinical

A CCR5 co-receptor antagonist used with other antiretroviral medications to treat CCR5-tropic HIV-1 infection.

Overview

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.

Pharmacology

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.

Pharmacodynamic

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.

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... Read more

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.

Protein binding

Approximately 76% bound to human plasma proteins, with moderate affinity for albumin and alpha-1 acid glycoprotein.

Volume of distribution

194 L

Clearance

Information currently not available.

Half life

14-18 hours

Route of elimination

Information currently not available.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Hypersensitivity:
    • false
  • Lab Values:
    • CrCl < 30 mL/min
  • Regions: US
  • Patient Conditions:
      • Name: Severe Renal Impairment
      • Drugbank Id: DBCOND0045819
      • Modification Of:
        • Base:
          • Name: Renal Impairment
          • Drugbank Id: DBCOND0031781
        • Severity:
          • Includes:
            • severe
  • With Categories:
      • Name: Cytochrome P-450 CYP3A Inhibitors
      • Drugbank Id: DBCAT000934
      • Mesh Id: D065692
  • Hypersensitivity:
    • false
  • Lab Values:
    • CrCl < 30 mL/min
  • Regions: US
  • Patient Conditions:
      • Name: End-Stage Renal Disease
      • Drugbank Id: DBCOND0028021
  • With Categories:
      • Name: Cytochrome P-450 CYP3A Inhibitors
      • Drugbank Id: DBCAT000934
      • Mesh Id: D065692
  • Hypersensitivity:
    • false
  • Lab Values:
    • CrCl < 30 mL/min
  • Regions: US
  • Patient Conditions:
      • Name: End-Stage Renal Disease
      • Drugbank Id: DBCOND0028021
  • With Categories:
      • Name: Cytochrome P-450 CYP3A Inducers
      • Drugbank Id: DBCAT000492
      • Mesh Id: D065701
  • Hypersensitivity:
    • false
  • Lab Values:
    • CrCl < 30 mL/min
  • Regions: US
  • Patient Conditions:
      • Name: Severe Renal Impairment
      • Drugbank Id: DBCOND0045819
      • Modification Of:
        • Base:
          • Name: Renal Impairment
          • Drugbank Id: DBCOND0031781
        • Severity:
          • Includes:
            • severe
  • With Categories:
      • Name: Cytochrome P-450 CYP3A Inducers
      • Drugbank Id: DBCAT000492
      • Mesh Id: D065701

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Maraviroc
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
6-Deoxyerythronolide B
The metabolism of Maraviroc can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecin
The metabolism of Maraviroc can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
9-aminocamptothecin
The metabolism of Maraviroc can be decreased when combined with 9-aminocamptothecin.
Abatacept
The metabolism of Maraviroc can be increased when combined with Abatacept.
Acalabrutinib
The metabolism of Maraviroc can be decreased when combined with Acalabrutinib.
Acetaminophen
The metabolism of Maraviroc can be increased when combined with Acetaminophen.
Acetazolamide
The metabolism of Maraviroc can be decreased when combined with Acetazolamide.
Adalimumab
The metabolism of Maraviroc can be increased when combined with Adalimumab.
Adenovirus type 7 vaccine live
The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Maraviroc.
Afelimomab
The metabolism of Maraviroc can be increased when combined with Afelimomab.
Albendazole
The metabolism of Maraviroc can be decreased when combined with Albendazole.
Aldesleukin
The metabolism of Maraviroc can be decreased when combined with Aldesleukin.
Allylestrenol
The metabolism of Maraviroc can be decreased when combined with Allylestrenol.
Alpelisib
The metabolism of Maraviroc can be increased when combined with Alpelisib.
Aminoglutethimide
The metabolism of Maraviroc can be increased when combined with Aminoglutethimide.
Amiodarone
The metabolism of Maraviroc can be decreased when combined with Amiodarone.
Amobarbital
The metabolism of Maraviroc can be increased when combined with Amobarbital.
Amphotericin B
The metabolism of Maraviroc can be decreased when combined with Amphotericin B.
Amprenavir
The metabolism of Maraviroc can be decreased when combined with Amprenavir.
Anakinra
The metabolism of Maraviroc can be increased when combined with Anakinra.