DIRA 1.0: Atlas of Drug-induced Rhabdomyolysis

MARAVIROC

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Less-DIR concern

Severity Score:1

Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF

OVERDOSAGE
The highest single dose administered in clinical trials was 1,200 mg. The dose-limiting adverse event was postural hypotension, which was observed at 600 mg. While the recommended dose for SELZENTRY in patients receiving a CYP3A inducer without a CYP3A inhibitor is 600 mg twice daily, this dose is appropriate due to enhanced metabolism.
Prolongation of the QT interval was seen in dogs and monkeys at plasma concentrations 6 and 12 times, respectively, those expected in humans at the intended exposure of 300-mg equivalents twice daily. However, no significant QT prolongation was seen in the trials in treatment-experienced subjects with HIV using the recommended doses of maraviroc, or in a specific pharmacokinetic trial to evaluate the potential of maraviroc to prolong the QT interval [see Clinical Pharmacology (12.2)].
CLINICAL PHARMACOLOGY
Pharmacodynamics
Effects on Electrocardiogram
A placebo-controlled, randomized, crossover trial to evaluate the effect on the QT interval of healthy male and female volunteers was conducted with 3 single oral doses of maraviroc and moxifloxacin. The placebo-adjusted mean maximum (upper 1-sided 95% CI) increases in QTc from baseline after 100, 300, and 900 mg of maraviroc were –2 (0), -1 (1), and 1 (3) msec, respectively, and 13 (15) msec for moxifloxacin 400 mg. No subject in any group had an increase in QTc of greater than or equal to 60 msec from baseline. No subject experienced an interval exceeding the potentially clinically relevant threshold of 500 msec.

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

Rhabdomyolysis

42909

Other ADRs

1465

14115814

Odds Ratio = 0.674

Drug Property Information

ATC Code(s):

J05AX09 - maraviroc

J05AX - Other antivirals
J05A - DIRECT ACTING ANTIVIRALS
J05 - ANTIVIRALS FOR SYSTEMIC USE
J - ANTIINFECTIVES FOR SYSTEMIC USE

Active Ingredient:maraviroc

Active Ingredient UNII:MD6P741W8A

Drugbank ID:DB04835

PubChem Compound:3002977

CAS Number:376348-65-1

Dosage Form(s):tablet, film coated

Route(s) Of Administrator:oral

Daily Dose:

600.0 mg/day J05AX09

Chemical Structure:

SMILE Code:
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

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MARAVIROC

DIR Classification

Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF

Postmarketing Surveillance

Contingency Table:

Drug Property Information

Reference

COHORT STUDY:

OTHER REFERENCE(S):

1: Common adverse effects of antiretroviral therapy for HIV disease.