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afatinib + dacomitinib + pyrotinib
- Development stage
- Unknown
- Lead developer
- Boehringer Ingelheim
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This is a combination of three second-generation tyrosine kinase inhibitors (TKIs) that target the ErbB family of receptors, including EGFR (HER1), HER2, and HER4. All three drugs are irreversible inhibitors with slightly different properties. Afatinib and dacomitinib have been studied for NSCLC with uncommon EGFR mutations, while pyrotinib has shown promising activity against HER2-mutated NSCLC. Pyrotinib has a higher log P (oil-water partition coefficient) than afatinib and dacomitinib, suggesting better lipophilicity and potentially better passive absorption with fewer gastrointestinal adverse effects.
02
Targets
ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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