TAS-116. Second-generation HSP90-alpha/beta inhibitor, Cancer therapy
Heat shock protein 90 (HSP90) is a molecular chaperone required for the stability and function of proteins, including oncoproteins. Therefore, HSP90 inhibition is thought to be an attractive therapeutic option for cancer treatment. Although a number of HSP90 inhibitors have been developed and show significant antitumor effects in preclinical studies, first-generation HSP90 inhibitors have shown various unfavorable toxicities. Therefore, HSP90 inhibitors with more favorable side effect profiles are required in the clinical setting. TAS-116 is a second-generation orally bioavailable HSP90-alpha/beta inhibitor with minimal side effects. TAS-116 induces downregulation of key oncoproteins and shows antiproliferative activity against various cancers, including multiple myeloma. Moreover, TAS-116 overcomes the antiapoptotic effect conferred by the bone marrow microenvironment. In addition, TAS-116 can be an attractive chemosensitizer or radiosensitizer for cancer treatment. Importantly, a first-in-human phase I clinical trial of TAS-116 in advanced solid tumors is now ongoing (TAS-116-101 study) and shows acceptable pharmacokinetic and safety profiles. Taken together, these data suggest that TAS-116 may improve patient outcomes in various cancers..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2018 |
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| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:043 |
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| Enthalten in: |
Drugs of the future - 043(2018), 1, Seite 0013 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Suzuki,US!aR. [VerfasserIn] |
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| 520 | |a Heat shock protein 90 (HSP90) is a molecular chaperone required for the stability and function of proteins, including oncoproteins. Therefore, HSP90 inhibition is thought to be an attractive therapeutic option for cancer treatment. Although a number of HSP90 inhibitors have been developed and show significant antitumor effects in preclinical studies, first-generation HSP90 inhibitors have shown various unfavorable toxicities. Therefore, HSP90 inhibitors with more favorable side effect profiles are required in the clinical setting. TAS-116 is a second-generation orally bioavailable HSP90-alpha/beta inhibitor with minimal side effects. TAS-116 induces downregulation of key oncoproteins and shows antiproliferative activity against various cancers, including multiple myeloma. Moreover, TAS-116 overcomes the antiapoptotic effect conferred by the bone marrow microenvironment. In addition, TAS-116 can be an attractive chemosensitizer or radiosensitizer for cancer treatment. Importantly, a first-in-human phase I clinical trial of TAS-116 in advanced solid tumors is now ongoing (TAS-116-101 study) and shows acceptable pharmacokinetic and safety profiles. Taken together, these data suggest that TAS-116 may improve patient outcomes in various cancers. | ||
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