Is Pimitespib on the market?
Pimitespib (Pimitespib)is an oral small molecule inhibitor of the α and β isoforms of heat shock protein 90 (HSP90) . HSP90α and HSP90β regulate the stability and activity of many proteins critical for tumor development. Taihe Pharmaceutical is developing pimetibib for the treatment of solid tumors, including gastrointestinal stromal tumors (GIST) , and received its first approval in Japan in June 2022. It is sold under the trade name Jeselhy for gastrointestinal stromal tumors that have progressed after chemotherapy. Pimetibi is under Phase I development for the treatment of solid tumors in the EU and the United States.
Pimetibib is believed to inhibit the formation of higher-order structures of client proteins by HSP90, thereby reducing the expression levels of proteins related to tumor growth, inducing apoptosis, etc., thereby exhibiting tumor growth inhibition. In vitro, pimetibi showed a growth inhibitory effect on theGIST-T1 cell line derived from human gastrointestinal stromal tumors; in vivo, pimetibib showed a tumor growth inhibitory effect in nude mice subcutaneously transplanted with theGIST-T1 cell line.
In a phase III study, pimetibib significantly prolonged progression-free survival compared with placebo (median 2.8 months vs. 1.4 months; hazard ratio, 0.51; 95% CI 0.30-0.87; p = 0.006). Common treatment-related adverse events include diarrhea, decreased appetite, increased serum creatinine, malaise, nausea, and ocular abnormalities. The efficacy and safety of pimetibib are being studied in other tumor types and in combination with other anticancer therapies.
Pimetibi is not marketed in China, and it has been on the market overseas for a short time, and there is little information about its price and other related information.
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