The effect of antacid and mineral supplements on bictegravir pharmacokinetics: results from a Phase 1, open-label, drug-drug interaction study.

ABSTRACT: The mechanism of action of integrase strand transfer inhibitors involves binding to magnesium ions in the active site of the HIV integrase enzyme, making them susceptible to chelation-type drug-drug interactions with metal cation-containing medications. This study evaluated the potential of metal cation-containing antacids and mineral supplements to impact bictegravir (BIC) exposure and assessed alternative approaches for combined use. This was an open-label, single-dose, Phase 1 study in adult participants without HIV. The pharmacokinetics and safety of BIC (administered as part of a single-tablet combination with emtricitabine [F] and tenofovir alafenamide [TAF; B/F/TAF]) were assessed when co-administered with maximum-strength aluminum/magnesium-containing antacid (referred to as "alumi

SUBMITTER: Arora P 

PROVIDER: S-EPMC12777568 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature