Pimitespib for the Treatment of Advanced Gastrointestinal Stromal tumors and Other Tumors
Creators: name: Doi, Toshihiko
name: Yamamoto, Noboru
name: Ohkubo, Shuichi
Publisher: name: Taylor & Francis
Year: 2024
Subjects: subject: Genetics
subject: FOS: Biological sciences
subject: Pharmacology
subject: Environmental Sciences not elsewhere classified
subject: Biological Sciences not elsewhere classified
subject: Cancer
subject: Science Policy

description: Pimitespib (TAS-116) is the first heat shock protein 90 (HSP90) inhibitor approved in Japan, and it is indicated for the treatment of gastrointestinal stromal tumors (GIST) that have progressed after treatment with imatinib, sunitinib and regorafenib. This review describes the preclinical and clinical research with pimitespib, including its mechanism of action, pharmacokinetics, clinical antitumour activity and safety. In a phase III study, pimitespib significantly prolonged progression-free survival compared with placebo (median 2.8 vs 1.4 months; hazard ratio 0.51; 95% CI 0.30–0.87; p = 0.006). Common treatment-related adverse events were diarrhoea, decreased appetite, increase in serum creatinine, malaise, nausea and eye disorders. The efficacy and safety of pimitespib are being investigated in other tumour types and in combination with other anticancer therapies. A summary of the new anticancer drug, pimitespib, for treating gastrointestinal stromal tumors that are unresponsive to initial treatments &amp; have spread to other parts of the body This article provides information about pimitespib, a drug that recently became available in Japan for the treatment of advanced gastrointestinal stromal tumors, or ‘GISTs’. GISTs are a type of cancer found in the gastrointestinal tract, and those that are considered ‘advanced’ have stopped responding to other treatments and have spread to other parts of the body. Pimitespib works in a way unlike other drug treatments for cancer – it inhibits a protein called heat shock protein 90, and this stops cancer cells from developing and growing. Pimitespib is taken by mouth. Studies in Japanese patients with advanced GISTs showed an increase in the time taken for the cancer to progress further and in the length of time that patients survived among those treated with pimitespib, compared with patients who did not receive the drug. These studies also found that pimitespib was not associated with serious side effects, although diarrhoea occurred frequently. Eye disorders developed in some patients, but they could be managed by interrupting or stopping treatment with pimitespib. Pimitespib is also being studied for the treatment of other cancers, alone and in combination with other anticancer drugs. There are very few treatments available for patients with advanced GISTs and, therefore, pimitespib is an important new option for such patients in Japan. If the results of ongoing studies are positive, pimitespib may become a treatment option for a wider range of cancer patients in the future. Check out our latest review examining the therapeutic potential and safety of the HSP90 inhibitor #pimitespib for advanced #gastrointestinalstromaltumors and other forms of cancer. A PDF version of this infographic is available as supplemental material.