gamitrinib

Gamitrinib is a first-in-class small molecule inhibitor that targets mitochondrial heat shock protein 90 (Hsp90), specifically the mitochondrial chaperone TRAP1. It is a resorcinolic-based compound derived from geldanamycin and linked to the mitochondrial-targeting moiety triphenylphosphonium (TPP). By selectively accumulating in mitochondria of tumor cells and inhibiting Hsp90/TRAP1 function within this organelle, gamitrinib induces proteotoxic stress and disrupts multiple mitochondrial functions including bioenergetics. This leads to acute mitochondrial dysfunction—loss of membrane potential and rupture—resulting in apoptosis of susceptible cancer cells. Preclinical studies have demonstrated potent antitumor activity across various cancer models including glioblastoma and prostate cancer. A phase I clinical trial is ongoing for patients with advanced cancers[1][3][5][6].

Brand names

Gamitrinib TPP

Other names

17-Demethoxy-17-((6-(triphenylphosphonio)hexyl)amino)geldanamycinGeldanamycin, 17-demethoxy-17-((6-(triphenylphosphonio)hexyl)amino)-Gamitrinib-TPPUNII-M6LC47TUG3UNII-M-6LC47TUG3UNII-M 6LC47TUG3CHEMBL4802112CHEMBL-4802112CHEMBL 4802112SCHEMBL13881137SCHEMBL-13881137SCHEMBL 13881137