Drug intelligence / Profile preview

afatinib + rifampicin

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

**afatinib + rifampicin** is a combination of two small molecule drugs: afatinib, an irreversible inhibitor of the ErbB family of tyrosine kinases used primarily as antineoplastic therapy for non-small cell lung cancer (NSCLC), and rifampicin, a potent inducer of P-glycoprotein (P-gp) and a first-line antibiotic for tuberculosis and other bacterial infections. The coadministration is not a recognized combination therapy but is clinically relevant due to known drug-drug interactions in patients who require both drugs. When the two drugs are coadministered, rifampicin significantly reduces plasma exposure of afatinib by inducing P-glycoprotein, which limits afatinib absorption. Thus, concurrent use may result in diminished antineoplastic efficacy of afatinib.

Other names
afatinibrifampin
02

Targets

RNAP (Bacterial dna-dependent RNA polymerase)ABCB1 (P-glycoprotein)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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