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tuxobertinib
- Development stage
- Discontinued
- Lead developer
- Black Diamond Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tuxobertinib (formerly known as BDTX-189) is an orally available, irreversible small molecule inhibitor designed to selectively target oncogenic allosteric mutations in the ErbB family of receptor tyrosine kinases, specifically epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It acts as an ATP-competitive antagonist that irreversibly binds to and inhibits a broad spectrum of allosteric EGFR and HER2 mutant variants while sparing wild-type EGFR. This selectivity aims to minimize toxicity associated with wild-type EGFR inhibition. Tuxobertinib was developed by Black Diamond Therapeutics for the treatment of advanced solid tumors harboring these specific mutations, but its clinical development has been discontinued.
- Other names
- BDTX-189BDTX189BDTX 189tuxobertinib
02
Targets
EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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