Pimitespib (Jeselhy)

Mechanism of action

From the NCI Drug Dictionary: A specific inhibitor of heat shock protein 90 (Hsp90) subtypes alpha and beta, with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, Hsp90alpha/beta inhibitor TAS-116 specifically binds to and inhibits the activity of Hsp90 alpha and beta; this results in the proteasomal degradation of oncogenic client proteins, which inhibits client protein dependent-signaling, induces apoptosis, and inhibits the proliferation of cells overexpressing HSP90alpha/beta.

Diseases for which it is used

• Gastrointestinal stromal tumor

History of changes in PMDA indication

• 2022-06-20: A drug with a new active ingredient indicated for the treatment of gastrointestinal stromal tumor that has progressed after cancer chemotherapy.

Also known as

• Code name: TAS-116
• Brand name: Jeselhy