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Page 1
TAS-116 (Pimitespib), an Oral HSP90 Inhibitor, in Combination with Nivolumab in Patients with Colorectal Cancer and Other Solid Tumors: An Open-Label, Dose-Finding, and Expansion Phase Ib Trial (EPOC1704).
Kawazoe A, Itahashi K, Yamamoto N, Kotani D, Kuboki Y, Taniguchi H, Harano K, Naito Y, Suzuki M, Fukutani M, Higuchi T, Ikeno T, Wakabayashi M, Sato A, Koyama S, Nishikawa H, Shitara K. Kawazoe A, et al. Clin Cancer Res. 2021 Dec 15;27(24):6709-6715. doi: 10.1158/1078-0432.CCR-21-1929. Epub 2021 Sep 30. Clin Cancer Res. 2021. PMID: 34593531 Clinical Trial.
PURPOSE: This is a phase Ib trial of TAS-116, an oral HSP90 inhibitor, plus nivolumab for colorectal cancer and other solid tumors. PATIENTS AND METHODS: Enrolled patients received TAS-116 plus nivolumab in a dose-finding part to estimate the recommend …
PURPOSE: This is a phase Ib trial of TAS-116, an oral HSP90 inhibitor, plus nivolumab for colorectal cancer and other solid tu …
TAS-116 inhibits oncogenic KIT signalling on the Golgi in both imatinib-naive and imatinib-resistant gastrointestinal stromal tumours.
Saito Y, Takahashi T, Obata Y, Nishida T, Ohkubo S, Nakagawa F, Serada S, Fujimoto M, Ohkawara T, Nishigaki T, Sugase T, Koh M, Ishida T, Tanaka K, Miyazaki Y, Makino T, Kurokawa Y, Nakajima K, Yamasaki M, Hirota S, Naka T, Mori M, Doki Y. Saito Y, et al. Br J Cancer. 2020 Mar;122(5):658-667. doi: 10.1038/s41416-019-0688-y. Epub 2019 Dec 20. Br J Cancer. 2020. PMID: 31857719 Free PMC article.
We also evaluated the effects of TAS-116 on the other HSP90 client protein, EGFR, by using lung cell lines. ...We found KIT was activated mainly in intracellular compartments, such as trans-Golgi cisternae, and TAS-116 reduced autophosphorylated KIT in …
We also evaluated the effects of TAS-116 on the other HSP90 client protein, EGFR, by using lung cell lines. ...We found KIT wa …
TAS-116 (pimitespib), a heat shock protein 90 inhibitor, shows efficacy in preclinical models of adult T-cell leukemia.
Ikebe E, Shimosaki S, Hasegawa H, Iha H, Tsukamoto Y, Wang Y, Sasaki D, Imaizumi Y, Miyazaki Y, Yanagihara K, Hamaguchi I, Morishita K. Ikebe E, et al. Cancer Sci. 2022 Feb;113(2):684-696. doi: 10.1111/cas.15204. Epub 2021 Nov 27. Cancer Sci. 2022. PMID: 34794206 Free PMC article.
Given orally, TAS-116 also showed significant inhibitory effects against tumor cell growth in ATL cell-xenografted mice. ...TAS-116 suppressed the activator protein-1 and tumor necrosis factor pathways in all examined cells. ...
Given orally, TAS-116 also showed significant inhibitory effects against tumor cell growth in ATL cell-xenografted mice. ... …
Combination of pimitespib (TAS-116) with sunitinib is an effective therapy for imatinib-resistant gastrointestinal stromal tumors.
Teranishi R, Takahashi T, Obata Y, Nishida T, Ohkubo S, Kazuno H, Saito Y, Serada S, Fujimoto M, Kurokawa Y, Saito T, Yamamoto K, Yamashita K, Tanaka K, Makino T, Nakajima K, Hirota S, Naka T, Eguchi H, Doki Y. Teranishi R, et al. Int J Cancer. 2023 Jun 15;152(12):2580-2593. doi: 10.1002/ijc.34461. Epub 2023 Feb 21. Int J Cancer. 2023. PMID: 36752576
The recently-developed heat shock protein 90 (HSP90) inhibitor pimitespib (PIM; TAS-116) demonstrated clinical benefits in some clinical trials; however, the effects were limited. ...
The recently-developed heat shock protein 90 (HSP90) inhibitor pimitespib (PIM; TAS-116) demonstrated clinical benefits in som …
TAS-116, a Well-Tolerated Hsp90 Inhibitor, Prevents the Activation of the NLRP3 Inflammasome in Human Retinal Pigment Epithelial Cells.
Ranta-Aho S, Piippo N, Korhonen E, Kaarniranta K, Hytti M, Kauppinen A. Ranta-Aho S, et al. Int J Mol Sci. 2021 May 5;22(9):4875. doi: 10.3390/ijms22094875. Int J Mol Sci. 2021. PMID: 34062977 Free PMC article.
TAS-116 has a better in vitro therapeutic index than geldanamycin. In summary, TAS-116 appears to be a well-tolerated Hsp90 inhibitor, with the capability to prevent the activation of the NLRP3 inflammasome in human RPE cells....
TAS-116 has a better in vitro therapeutic index than geldanamycin. In summary, TAS-116 appears to be a well-tole …
TAS-116, a Novel Hsp90 Inhibitor, Selectively Enhances Radiosensitivity of Human Cancer Cells to X-rays and Carbon Ion Radiation.
Lee Y, Sunada S, Hirakawa H, Fujimori A, Nickoloff JA, Okayasu R. Lee Y, et al. Mol Cancer Ther. 2017 Jan;16(1):16-24. doi: 10.1158/1535-7163.MCT-16-0573. Epub 2016 Nov 9. Mol Cancer Ther. 2017. PMID: 28062703 Free PMC article.
TAS-116 also decreased expression of the cdc25 cell-cycle progression marker, markedly increasing G(2)-M arrest. ...The promising results of combination TAS-116 + carbon ion radiotherapy of tumor xenografts justify further exploration of TAS- …
TAS-116 also decreased expression of the cdc25 cell-cycle progression marker, markedly increasing G(2)-M arrest. ...The promis …
TAS-116, a highly selective inhibitor of heat shock protein 90alpha and beta, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models.
Ohkubo S, Kodama Y, Muraoka H, Hitotsumachi H, Yoshimura C, Kitade M, Hashimoto A, Ito K, Gomori A, Takahashi K, Shibata Y, Kanoh A, Yonekura K. Ohkubo S, et al. Mol Cancer Ther. 2015 Jan;14(1):14-22. doi: 10.1158/1535-7163.MCT-14-0219. Epub 2014 Nov 21. Mol Cancer Ther. 2015. PMID: 25416789
Moreover, TAS-116 showed activity against orthotopically transplanted NCI-H1975 lung tumors. Together, these data suggest that TAS-116 has a potential to maximize antitumor activity while minimizing adverse effects such as visual disturbances that are …
Moreover, TAS-116 showed activity against orthotopically transplanted NCI-H1975 lung tumors. Together, these data suggest that …
Combining the HSP90 inhibitor TAS-116 with metformin effectively degrades the NLRP3 and attenuates inflammasome activation in rats: A new management paradigm for ulcerative colitis.
Shaaban AA, Abdelhamid AM, Shaker ME, Cavalu S, Maghiar AM, Alsayegh AA, Babalghith AO, El-Ahwany E, Amin NA, Mohammed OA, Eissa H, Gaafar AGA, Batiha GE, Saber S. Shaaban AA, et al. Biomed Pharmacother. 2022 Sep;153:113247. doi: 10.1016/j.biopha.2022.113247. Epub 2022 Jun 17. Biomed Pharmacother. 2022. PMID: 35724510 Free article.
Herein, we evaluated the effect of autophagy induction using metformin in the context of HSP90 inhibition by TAS-116 in the dextran sodium sulfate (DSS)-induced UC in rats. We revealed that TAS-116-induced interruption of the protein complex containing …
Herein, we evaluated the effect of autophagy induction using metformin in the context of HSP90 inhibition by TAS-116 in the de …
Optimizing antidotal treatment with the oral HSP90 inhibitor TAS-116 against hydrochloric acid-induced pulmonary fibrosis in mice.
Solopov PA, Colunga Biancatelli RML, Dimitropolou C, Day T, Catravas JD. Solopov PA, et al. Front Pharmacol. 2022 Nov 7;13:1034464. doi: 10.3389/fphar.2022.1034464. eCollection 2022. Front Pharmacol. 2022. PMID: 36419627 Free PMC article.
Furthermore, TAS-116 normalized lung mechanics and decreased the deposition of extracellular matrix proteins in the lungs of mice exposed to HCl. Delayed and shortened treatment with TAS-116, successfully blocked the adverse chronic effects associated …
Furthermore, TAS-116 normalized lung mechanics and decreased the deposition of extracellular matrix proteins in the lungs of m …
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.
Doi T, Kurokawa Y, Sawaki A, Komatsu Y, Ozaka M, Takahashi T, Naito Y, Ohkubo S, Nishida T. Doi T, et al. Eur J Cancer. 2019 Nov;121:29-39. doi: 10.1016/j.ejca.2019.08.009. Epub 2019 Sep 16. Eur J Cancer. 2019. PMID: 31536852 Free article. Clinical Trial.
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. CONCLUSION: TAS-116 showed significant ac …
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 modi …
22 results