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Class: Diarylquinoline
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Mechanism: Inhibits mycobacterial ATP synthase, depleting the organism's energy supply. It is active against replicating and nonreplicating Mycobacterium tuberculosis.
Katzung's Basic and Clinical Pharmacology, 16th Edition, p. 1320
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Usual adult schedule: 400 mg orally once daily for 2 weeks, then 200 mg three times weekly for 22 weeks, taken with food. Exact use, duration, and companion drugs must follow susceptibility results and a TB specialist or national program protocol.
Katzung's Basic and Clinical Pharmacology, 16th Edition, p. 1320
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Role in current treatment: WHO includes bedaquiline in recommended MDR/RR-TB regimens, including shorter all-oral regimens in eligible patients. The 2025 WHO guidance also describes 6-month regimens containing bedaquiline, such as BPaLM for suitable patients and BDLLfxC as a conditional option. See the
WHO TB treatment guidance.
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Important adverse effects: QT-interval prolongation, hepatotoxicity or raised liver enzymes, nausea, arthralgia, headache, and dizziness. ECG and liver-function monitoring are generally required.
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Major interactions: It is metabolized mainly by CYP3A4. Avoid strong CYP3A4 inducers, particularly rifampicin/rifampin, which markedly lowers bedaquiline concentrations. Use caution with CYP3A4 inhibitors and with other QT-prolonging drugs such as clofazimine, fluoroquinolones, delamanid, and certain antiarrhythmics or antipsychotics.
Goodman & Gilman’s The Pharmacological Basis of Therapeutics, newer anti-TB drugs section.
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Pharmacokinetic point: It has a very long terminal half-life, about 5.5 months, so adverse effects and interactions can persist after treatment stops.
Katzung's Basic and Clinical Pharmacology, 16th Edition, p. 1320
Recent systematic reviews address its pharmacokinetics and safety monitoring, including
a 2025 pharmacokinetic review and
a safety-monitoring review.