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Drug intelligence / Profile preview
BPI-460372
- Development stage
- Phase 1
- Lead developer
- Betta Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
BPI-460372 is an orally available, covalent, irreversible small molecule inhibitor of the transcriptional enhanced associate domain (TEAD) 1/3/4 transcription factors. It targets the Hippo signaling pathway and is being developed for the treatment of cancers with Hippo pathway alterations, including solid tumors with NF2 defects, YAP/TAZ fusion, LATS1/2 mutations, and other related abnormalities. Preclinical studies have demonstrated potent *in vitro* and *in vivo* antitumor activity as well as favorable pharmacokinetic properties and safety profile. The drug is currently in phase 1 clinical trials for advanced solid tumors such as malignant mesothelioma and epithelioid hemangioendothelioma[1][3][5][6].
02
Targets
TEAD1TEAD3TEAD4
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