Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites.
Frontiers in pharmacology January 1, 2022 Margarida L F Martins, Paniz Heydari, Wenlong Li et al. 9 citations
Ibogaine, a psychedelic alkaloid used orally for substance use disorders despite being unlicensed, is rapidly converted to noribogaine and noribogaine glucuronide in mice. The drug efflux transporters ABCB1 and ABCG2 modestly restrict ibogaine's oral availability, possibly through hepatobiliary or intestinal excretion, and ABCB1 limits its brain penetration. In wild-type mice, the brain-to-plasma ratio was 3.4, increasing 1.5-fold in mice lacking both transporters. Human OATP transporters and CYP3A4 had no major impact on ibogaine pharmacokinetics, suggesting low risk of drug interactions or interindividual variation from these pathways.