An open-label, crossover study to compare different formulations and evaluate effect of food on pharmacokinetics of pimitespib in patients with advanced solid tumors

Randomized, double-blind, placebo (PL)-controlled, phase III trial of pimitespib (TAS-116), an oral inhibitor of heat shock protein 90 (HSP90), in patients (pts) with advanced gastrointestinal stromal tumor (GIST) refractory to imatinib (IM), sunitinib (SU) and regorafenib (REG).

(2021) Yoshitaka Honma et al.   JOURNAL OF CLINICAL ONCOLOGY

Randomized, Open-Label, Crossover Studies Evaluating the Effect of Food and Liquid Formulation on the Pharmacokinetics of the Novel Focal Adhesion Kinase (FAK) Inhibitor BI 853520

(2019) Remy B. Verheijen et al.   Targeted Oncology

First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors

(2019) Akihiko Shimomura et al.   MOLECULAR CANCER THERAPEUTICS

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

(2019) Toshihiko Doi et al.   EUROPEAN JOURNAL OF CANCER

High expression of HSP90 is associated with poor prognosis in patients with colorectal cancer

(2019) Shuming Zhang et al.   PeerJ

Targeted cancer therapy through 17-DMAG as an Hsp90 inhibitor: Overview and current state of the art

(2018) Hassan Mellatyar et al.   BIOMEDICINE & PHARMACOTHERAPY

Food, gastrointestinal pH, and models of oral drug absorption

(2017) Ahmad Y. Abuhelwa et al.   EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS

HSP90 promotes cell glycolysis, proliferation and inhibits apoptosis by regulating PKM2 abundance via Thr-328 phosphorylation in hepatocellular carcinoma

(2017) Qiuran Xu et al.   Molecular Cancer

Acquired resistance to 5-fluorouracil via HSP90/Src-mediated increase in thymidylate synthase expression in colon cancer

(2015) Ji-Young Ahn et al.   Oncotarget

A Phase 1, Dose-Escalation, Pharmacokinetic and Pharmacodynamic Study of BIIB021 Administered Orally in Patients with Advanced Solid Tumors

(2013) M. W. Saif et al.   CLINICAL CANCER RESEARCH

High Expression of Heat Shock Protein 90 Is Associated with Tumor Aggressiveness and Poor Prognosis in Patients with Advanced Gastric Cancer

(2013) Jiahong Wang et al.   PLoS One

A Heat-Shock Protein Axis Regulates VEGFR2 Proteolysis, Blood Vessel Development and Repair

(2012) Alexander F. Bruns et al.   PLoS One

Genetics and clinical characteristics of hereditary pheochromocytomas and paragangliomas

(2011) Jenny Welander et al.   ENDOCRINE-RELATED CANCER

Multicenter Phase II Trial of the Heat Shock Protein 90 Inhibitor, Retaspimycin Hydrochloride (IPI-504), in Patients With Castration-resistant Prostate Cancer

(2011) William K. Oh et al.   UROLOGY

Reactive oxygen species mediate hepatotoxicity induced by the Hsp90 inhibitor geldanamycin and its analogs

(2010) Yuval Samuni et al.   FREE RADICAL BIOLOGY AND MEDICINE