Bedaquiline: a review of human pharmacokinetics and drug-drug interactions.
Article Details
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van Heeswijk RP, Dannemann B, Hoetelmans RM
Bedaquiline: a review of human pharmacokinetics and drug-drug interactions.
J Antimicrob Chemother. 2014 Sep;69(9):2310-8. doi: 10.1093/jac/dku171. Epub 2014 May 23.
- PubMed ID
- 24860154 [ View in PubMed]
- Abstract
Bedaquiline has recently been approved for the treatment of pulmonary multidrug-resistant tuberculosis (TB) as part of combination therapy in adults. It is metabolized primarily by the cytochrome P450 isoenzyme 3A4 (CYP3A4) to a less-active N-monodesmethyl metabolite. Phase I and Phase II studies in healthy subjects and patients with drug-susceptible or multidrug-resistant TB have assessed the pharmacokinetics and drug-drug interaction profile of bedaquiline. Potential interactions have been assessed between bedaquiline and first- and second-line anti-TB drugs (rifampicin, rifapentine, isoniazid, pyrazinamide, ethambutol, kanamycin, ofloxacin and cycloserine), commonly used antiretroviral agents (lopinavir/ritonavir, nevirapine and efavirenz) and a potent CYP3A inhibitor (ketoconazole). This review summarizes the pharmacokinetic profile of bedaquiline as well as the results of the drug-drug interaction studies.
DrugBank Data that Cites this Article
- Drug Carriers
Drug Carrier Kind Organism Pharmacological Action Actions Bedaquiline Alpha-1-acid glycoprotein 1 Protein Humans NoBinderDetails Bedaquiline Serum albumin Protein Humans NoBinderDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareBedaquilineMidostaurin The metabolism of Bedaquiline can be decreased when combined with Midostaurin. BedaquilineRitonavir The metabolism of Bedaquiline can be decreased when combined with Ritonavir. BedaquilineVoriconazole The metabolism of Bedaquiline can be decreased when combined with Voriconazole. BedaquilineEfavirenz The metabolism of Bedaquiline can be decreased when combined with Efavirenz. BedaquilineDelavirdine The metabolism of Bedaquiline can be decreased when combined with Delavirdine.