Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites

Martins, Margarida L. F., Heydari, Paniz, Li, Wenlong, Martínez-Chávez, Alejandra, Venekamp, Nikkie, Lebre, Maria C., Lucas, Luc, Beijnen, Jos H., Schinkel, Alfred H. · 2022 · Frontiers in Pharmacology

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ABCB1/ABCG2 modestly restrict ibogaine oral availability (2.3× AUC) and brain penetration (1.5×). Human OATP1B1/1B3 and CYP3A4 have minimal impact — reducing drug interaction risk.

Dosing: 10 mg/kg oral (ibogaine HCl in DMSO:saline 1:9, v/v) — mouse study (oral)