zelavespib

Zelavespib is a purine-based small molecule inhibitor of heat shock protein 90 (Hsp90), specifically targeting the epichaperome complexes found in cancer cells. By binding to the altered ATP-binding site of disease-associated Hsp90, zelavespib inhibits its chaperone function, leading to proteasomal degradation of oncogenic signaling proteins that are essential for tumor cell proliferation and survival. This mechanism disrupts protein-protein interactions critical for cancer cell growth and maintenance, particularly by destabilizing proteins such as JAK2 in myeloproliferative neoplasms. Zelavespib has demonstrated antineoplastic activity in preclinical models and early-phase clinical trials for various cancers, including myelofibrosis, lymphoma, solid tumors, metastatic solid tumors, and myeloproliferative neoplasms. The drug was originally developed at Memorial Sloan-Kettering Cancer Center and is being further developed by Samus Therapeutics[1][2][3][4][6][7][8].

Other names

zelavespib