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pyrotinib + efavirenz
- Development stage
- Phase 1
- Lead developer
- Jiangsu HengRui Medicine Co., Ltd.
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
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
02
Targets
EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)Human immunodeficiency virus type 1 reverse transcriptase
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