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| Verfasst von: | Wick, Antje [VerfasserIn]  |
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| | Bähr, Oliver [VerfasserIn] |
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| | Schuler, Martin [VerfasserIn] |
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| | Rohrberg, Kristoffer [VerfasserIn] |
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| | Chawla, Sant P. [VerfasserIn] |
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| | Janku, Filip [VerfasserIn] |
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| | Schiff, David [VerfasserIn] |
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| | Heinemann, Volker [VerfasserIn] |
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| | Narita, Yoshitaka [VerfasserIn] |
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| | Lenz, Heinz-Josef [VerfasserIn] |
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| | Ikeda, Masafumi [VerfasserIn] |
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| | Ando, Yuichi [VerfasserIn] |
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| | Wick, Wolfgang [VerfasserIn] |
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| | Steinbach, Joachim P. [VerfasserIn] |
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| | Burger, Michael C. [VerfasserIn] |
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| | Wenger, Katharina [VerfasserIn] |
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| | Lassen, Ulrik [VerfasserIn] |
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| | Sankhala, Kamalesh K. [VerfasserIn] |
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| | Roggia, Cristiana [VerfasserIn] |
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| | Genvresse, Isabelle [VerfasserIn] |
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| | Munhoz, Catya [VerfasserIn] |
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| | Rentzsch, Christine [VerfasserIn] |
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| | Reschke, Susanne [VerfasserIn] |
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| | Langer, Simon [VerfasserIn] |
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| | Wagner, Markus [VerfasserIn] |
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| | Kaulfuss, Stefan [VerfasserIn] |
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| | Cai, Charles [VerfasserIn] |
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| | Lagkadinou, Eleni [VerfasserIn] |
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| | Jeffers, Michael [VerfasserIn] |
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| | Peña, Carol [VerfasserIn] |
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| | Tabatabai, Ghazaleh [VerfasserIn] |
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| Titel: | Phase I assessment of safety and therapeutic activity of BAY1436032 in patients with IDH1-mutant solid tumors |
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| Verf.angabe: | Antje Wick, Oliver Bähr, Martin Schuler, Kristoffer Rohrberg, Sant P. Chawla, Filip Janku, David Schiff, Volker Heinemann, Yoshitaka Narita, Heinz-Josef Lenz, Masafumi Ikeda, Yuichi Ando, Wolfgang Wick, Joachim P. Steinbach, Michael C. Burger, Katharina Wenger, Ulrik Lassen, Kamalesh K. Sankhala, Cristiana Roggia, Isabelle Genvresse, Catya Munhoz, Christine Rentzsch, Susanne Reschke, Simon Langer, Markus Wagner, Stefan Kaulfuss, Charles Cai, Eleni Lagkadinou, Michael Jeffers, Carol Peña, and Ghazaleh Tabatabai |
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| E-Jahr: | 2021 |
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| Jahr: | February 23, 2021 |
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| Umfang: | 11 S. |
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| Fussnoten: | Gesehen am 21.02.2022 |
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| Titel Quelle: | Enthalten in: Clinical cancer research |
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| Ort Quelle: | Philadelphia, Pa. [u.a.] : AACR, 1995 |
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| Jahr Quelle: | 2021 |
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| Band/Heft Quelle: | 27(2021), 10 vom: 15. Mai, Seite 2723-2733 |
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| ISSN Quelle: | 1557-3265 |
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| Abstract: | BAY1436032, an inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1), was active against multiple IDH1-R132X solid tumors in preclinical models. This first-in-human study was designed to determine the safety and pharmacokinetics of BAY1436032, and to evaluate its potential pharmacodynamics and antitumor effects.The study comprised of dose escalation and dose expansion cohorts. BAY1436032 tablets were orally administered twice daily on a continuous basis in subjects with mIDH1 solid tumors.In dose escalation, 29 subjects with various tumor types were administered BAY1436032 across five doses (150-1,500 mg twice daily). BAY1432032 exhibited a relatively short half-life. Most evaluable subjects experienced target inhibition as indicated by a median maximal reduction of plasma R-2-hydroxyglutarate levels of 76%. BAY1436032 was well tolerated and an MTD was not identified. A dose of 1,500 mg twice daily was selected for dose expansion, where 52 subjects were treated in cohorts representing four different tumor types [lower grade glioma (LGG), glioblastoma, intrahepatic cholangiocarcinoma, and a basket cohort of other tumor types]. The best clinical outcomes were in subjects with LGG (n = 35), with an objective response rate of 11% (one complete response and three partial responses) and stable disease in 43%. As of August 2020, four of these subjects were in treatment for >2 years and still ongoing. Objective responses were observed only in LGG.BAY1436032 was well tolerated and showed evidence of target inhibition and durable objective responses in a small subset of subjects with LGG. |
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| DOI: | doi:10.1158/1078-0432.CCR-20-4256 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1158/1078-0432.CCR-20-4256 |
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| | DOI: https://doi.org/10.1158/1078-0432.CCR-20-4256 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| K10plus-PPN: | 1793372039 |
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| Verknüpfungen: | → Zeitschrift |
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Phase I assessment of safety and therapeutic activity of BAY1436032 in patients with IDH1-mutant solid tumors / Wick, Antje [VerfasserIn]; February 23, 2021 (Online-Ressource)
