pimitespib + imatinib

**Pimitespib + imatinib** is a combination drug regimen under investigation for the treatment of gastrointestinal stromal tumors (GIST), especially in patients who have failed or are refractory to imatinib monotherapy. - **Pimitespib** is an oral heat shock protein 90 (HSP90) inhibitor that destabilizes and reduces levels of multiple oncoproteins, including KIT, PDGFRA, HER2, and EGFR. It shows activity in imatinib-sensitive and -resistant GIST and is approved in Japan as a fourth-line option for GIST. - **Imatinib** is a tyrosine kinase inhibitor targeting BCR-ABL, KIT, and PDGFRA kinases, and is standard first-line therapy for advanced GIST. Combined, the regimen aims to synergistically inhibit KIT-driven signaling in GIST, including those with resistance to imatinib, by both direct kinase inhibition (imatinib) and chaperone protein inhibition leading to client protein degradation (pimitespib). The combination is currently being evaluated in clinical trials for safety, pharmacokinetics, and efficacy, mainly in solid tumors and GIST patients refractory to imatinib[1][5][7].

Brand names

Jeselhy