ganetespib

Ganetespib is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90), a molecular chaperone essential for the stability and function of numerous oncogenic client proteins. By binding to the ATP-binding domain at the N-terminus of Hsp90, ganetespib disrupts its chaperone activity, leading to proteasomal degradation of client proteins involved in signal transduction, cell cycle regulation, and apoptosis—including kinases (such as c-Kit, EGFR, Bcr-Abl), transcription factors, and hormone receptors. This results in inhibition of tumor cell proliferation and increased sensitivity to environmental stress. Ganetespib has demonstrated antitumor activity across a broad range of human cancers in preclinical models and has been investigated clinically for indications such as breast cancer, non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), myelodysplastic syndrome (MDS), among others[1][2][4][5][7]. It was developed by Synta Pharmaceuticals.

Other names

ganetespib