pimitespib

Pimitespib (TAS-116) is an orally bioavailable small molecule inhibitor of heat shock protein 90 (HSP90), specifically targeting the HSP90α and HSP90β isoforms. By inhibiting HSP90, pimitespib destabilizes and reduces levels of multiple client proteins involved in cancer cell growth and survival, including KIT, PDGFRA, HER2, and EGFR. This mechanism leads to anti-tumor effects through downregulation of oncogenic signaling pathways such as NF-κB in certain cancer cells and induction of cell cycle arrest or apoptosis in others. Pimitespib has demonstrated efficacy in preclinical models for adult T-cell leukemia/lymphoma (ATL) as well as clinical activity in patients with advanced gastrointestinal stromal tumor (GIST) refractory to standard treatments. It also acts as a radiosensitizer by inhibiting DNA double-strand break repair via suppression of RAD51-mediated homologous recombination[1][2][4][5][6][7].

Other names

pimitespibTAS-116TAS116TAS 116PIM