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Ref Type Journal Article
PMID (31536852)
Authors Doi T, Kurokawa Y, Sawaki A, Komatsu Y, Ozaka M, Takahashi T, Naito Y, Ohkubo S, Nishida T
Title Efficacy and safety of TAS-116, an oral inhibitor of heat shock protein 90, in patients with metastatic or unresectable gastrointestinal stromal tumour refractory to imatinib, sunitinib and regorafenib: a phase II, single-arm trial.
Journal European journal of cancer (Oxford, England : 1990)
Vol 121
Issue
Date 2019 11
URL
Abstract Text We evaluated the efficacy and safety of TAS-116, a novel class of an orally active selective inhibitor of heat shock protein 90, in patients with advanced gastrointestinal stromal tumour (GIST) after failure of three or more lines of standard treatment with imatinib, sunitinib and regorafenib.In this single-arm phase II study, patients received 160 mg/day oral TAS-116 for five consecutive days, followed by a 2-day rest. The primary end-point was centrally assessed progression-free survival (PFS). The secondary end-points were objective response rate, disease control rate, overall survival (OS), metabolic response rate, safety, pharmacokinetics and pharmacogenomics.Forty-one patients were enrolled in Japan, and 40 patients underwent efficacy and safety evaluation. At the cut-off date, the median PFS was 4.4 months (95% confidence interval [CI], 2.8-6.0) and 12-week progression-free rate was 73.4% (95% CI, 58.1-88.7). Thirty-four patients (85.0%) had stable disease for ≥ 6 weeks. The median OS was 11.5 months (95% CI, 7.0-not reached). All patients experienced at least one treatment-related adverse event (AE), including diarrhoea (80.0%), decreased appetite (45.0%) and increase in blood creatinine level (42.5%). Grade ≥3 AEs and treatment-related grade ≥3 AEs occurred in 23 (57.5%) and 21 (52.5%) patients, respectively. All AEs resolved after dose modification, and no TAS-116-related AEs led to treatment discontinuation.TAS-116 showed significant activity in advanced GIST refractory to standard treatment. Further development of TAS-116 is warranted.JapicCTI-163182.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Pimitespib TAS-116|TAS116 HSP90 Inhibitor 36 Pimitespib (TAS-116) is a selective inhibitor of HSP90-alpha and HSP90-beta, which may lead to decreased tumor growth (PMID: 25416789, PMID: 31857719, PMID: 31536852, PMID: 30679388).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown gastrointestinal stromal tumor not applicable Pimitespib Phase II Actionable In a Phase II trial, treatment with Pimitespib (TAS-116) in patients with a gastrointestinal stromal tumor who failed previous therapy (n=40) resulted in a progression-free survival of 4.4 months, a median overall survival of 11.5 months, a 0% objective response rate, and a disease control rate of 85%, with 34 patients achieving stable disease, and one patient experienced a 37.2% decrease in tumor size after the analysis cut-off date (PMID: 31536852). 31536852