Maraviroc

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Celsentri; Belgium: Celsentri; Bulgaria: Celsentri; Cyprus: Celsentri; Czech Republic: Celsentri; Denmark: Celsentri; Estonia: Celsentri; Finland: Celsentri; France: Celsentri; Germany: Celsentri; Greece: Celsentri; Hungary: Celsentri; Ireland: Celsentri; Italy: Celsentri; Latvia: Celsentri; Lithuania: Celsentri; Luxembourg: Celsentri; Malta: Celsentri; Netherlands: Celsentri; Poland: Celsentri; Portugal: Celsentri; Romania: Celsentri; Slovakia: Celsentri; Slovenia: Celsentri; Spain: Celsentri; Sweden: Celsentri; UK: Celsentri.

North America

Canada: Celsentri; USA: Selzentry.

Latin America

Argentina: Celsentri.

Drug combinations

Chemistry

Maraviroc: C~29~H~41~F~2~N~5~O. Mw: 513.67. 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. CAS-376348-65-1.

Pharmacologic Category

Antiretrovirals; HIV Entry and Fusion Inhibitors. CCR5 Antagonist Antiretroviral Agent. (ATC-Code: J05AX09).

Mechanism of action

Selectively binds to CCR5 on cell membrane and prevents interaction of HIV-1 glycoprotein 120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells.

Therapeutic use

Treatment of CCR5-tropic HIV-1 infection, in combination with other antiretroviral agents.

Pregnancy and lactiation implications

Adverse fetal effects not observed in animal studies. There are no adequate, well-controlled studies in pregnant women; available data insufficient to recommend use in pregnancy. HIV-infected mothers are discouraged from breast-feeding to decrease potential transmission of HIV.

Unlabeled use

Contraindications

Hypersensitivity to maraviroc or any component of the formulation.

Warnings and precautions

Possible hepatotoxicity (might be preceded by allergic type reactions and/or hepatic adverse events). Patients might develop immune reconstitution syndrome. Infections might develop. Symptomatic postural hypotension occurred. Use with caution in cardiovascular disease or cardiac risk factors. Use caution in hepatic dysfunction or concomitant viral hepatitis B or C. Renal impairment might increase maraviroc concentrations. Avoid concomitant therapy with CYP3A inhibitors in presence of renal impairment unless potential benefit outweighs potential risk. High potential for interactions (use with caution in patients taking strong CYP3A4/ABCB1 inhibitors and moderate or strong CYP3A4/ABCB1 inducers). Therapy not recommended for use in CXCR4- or dual/mixed tropic HIV-1 infection. High potential for drug-drug interactions.

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