Acute Porphyria Drug Database

J05AX09 - Maraviroc
Propably not porphyrinogenic
PNP

Rationale
Maraviroc is a substrate of CYP3A4. Data indicates that it does not induce CYP3A4, or inhibit CYP3A4 and other CYP enzymes. Side effects that can be potentially porphyrinogenic are nausea and insomnia. Abdominal pain, another common side effect, can be confused with an acute porphyria attack.
Therapeutic characteristics
Maraviroc is used in combination with other antiretroviral medicinal products, indicated for treatment-experienced adult patients infected with only CCR5-tropic HIV-1 detectable. Common side effects that can be confused with an acute porphyria attack are abdominal pain and nausea. Other common side effects are anorexia, depression and insomnia.
Metabolism and pharmacokinetics
Maraviroc is a substrate of CYP3A4 (Abel 2008, SPC). In vitro studies have shown that CYP3A4 is the major enzyme responsible for the metabolism of maraviroc and that CYP2C9, CYP2D6 and CYP2C19 do not contribute significantly to the metabolism of maraviroc (SPC). The half-life elimination is 14-18 hours. In vitro studies have shown that maraviroc do not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 at clinically relevant concentrations (Hyland 2008, SPC). In vivo studies showed that maraviroc have no clinically relevant effect on the pharmacokinetics of midazolam, ethinylestradiol and levonorgestrel or urinary 6β-hydroxycortisol/cortisol ratio. This indicates that maraviroc has low potential to inhibit or induce CYP3A4 in vivo (Abel 2008, SPC).

References

  1. Scientific articles
  2. Abel S, Russell D, et al. Effect of maraviroc on the pharmacokinetics of midazolam, lamivudine/zidovudine, and ethinyloestradiol/levonorgestrel in healthy volunteers. Br J Clin Pharmacol. 2008 Apr;65 Suppl 1:19-26. PMID 18333862. #4554
  3. Hyland R, Dickins M, et al. Maraviroc: in vitro assessment of drug-drug interaction potential. Br J Clin Pharmacol. 2008 Oct;66(4):498-507. PMID 18647303. #4555
  4. Drug reference publications
  5. Up to date. Maraviroc. #1856
  6. Summary of Product Characteristics
  7. Norwegian medicines agency. Summary of Product Characteristics (SPC). Maraviroc. #1854
  8. The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Maraviroc. #1855

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