Drug intelligence / Profile preview

dabrafenib + rifampin

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of dabrafenib**, a selective inhibitor of BRAF V600-mutant kinases, with **rifampin**, a potent inducer of cytochrome P450 enzymes. **Dabrafenib** selectively inhibits mutant BRAF serine-threonine kinases involved in cell signaling and proliferation, particularly in cancers with BRAF V600 mutations. **Rifampin** is an antibiotic that acts by inhibiting bacterial DNA-dependent RNA polymerase but is also a strong inducer of several CYP450 isoenzymes, most notably CYP2C8 and CYP3A4. The combination is not used therapeutically as a fixed combination product; rather, the interaction is clinically significant: co-administration results in a **marked reduction of dabrafenib exposure** due to rifampin’s induction of CYP3A4 and CYP2C8 metabolism, potentially leading to loss of antineoplastic efficacy[1][2][4].

Brand names
Rifadin
Other names
dabrafenibrifampicin
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)RNAP (Bacterial dna-dependent RNA polymerase)CYP2C8 (Cytochrome P450 2C8)CYP3A4 (Cytochrome P450 3A4)

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