pyrotinib + efavirenz

The combination of pyrotinib and efavirenz is primarily utilized in clinical pharmacology studies to evaluate drug-drug interactions (DDI). Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor (TKI) developed by Jiangsu Hengrui Pharmaceuticals, targeting HER2, EGFR, and HER4 for the treatment of HER2-positive breast cancer. Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the management of HIV-1 infection and is recognized as a potent inducer of the cytochrome P450 3A4 (CYP3A4) enzyme. Because pyrotinib is a substrate of CYP3A4, co-administration with efavirenz leads to a significant reduction in pyrotinib plasma exposure (Cmax and AUC), which is critical for determining clinical dosing guidelines and potential contraindications.

Brand names

IreenaStocrin

Other names

SHR1258 + efavirenzpyrotinib and efavirenz