J05AX07 - Enfuvirtide |
Propably not porphyrinogenic |
PNP |
Side effects
Common side effects are decreased appetite and weight, anorexia, peripheral neuropathy and myalgia.
Rationale
Enfuvirtide is not an inhibitor of CYP3A4 or CYP1A2 in vivo.
Therapeutic characteristics
Enfuvirtide is indicated in combination with other antiretroviral medicinal products for the treatment of HIV-1 infected patients.
Metabolism and pharmakokinetics
Enfuvirtide is a peptide and is expected to undergo catabolism to its constituent amino acids (SPC and Patel 2005). Elimination half-life is 3-4 hours.
It is listed as a weak inhibitor of CYP3A4 (Isoherranen 2009), but in vivo studies has shown that enfuvirtide insignificantly inhibited CYP3A4 and that it has minimal inhibitory effect on CYP1A2. This indicates that it is has no or little influence on CYP3A4 and CYP1A2 (Patel 2005, SPC and Zhang 2004).
References
- Scientific articles
- Isoherranen, N., H. Hachad, et al. (2009). "Qualitative analysis of the role of metabolites in inhibitory drug-drug interactions: literature evaluation based on the metabolism and transport drug interaction database." Chem Res Toxicol 22(2): 294-298. #1799
- Patel, I. H., X. Zhang, et al. (2005). "Pharmacokinetics, pharmacodynamics and drug interaction potential of enfuvirtide." Clin Pharmacokinet 44(2): 175-186. #1846
- Zhang, X., J. P. Lalezari, et al. (2004). "Assessment of drug-drug interaction potential of enfuvirtide in human immunodeficiency virus type 1-infected patients." Clin Pharmacol Ther 75(6): 558-568. #1848
- Summary of Product Characteristics
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Enfuvirtide. #1847
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