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DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1

Clinical Cancer Research · 2016 · Vol. 22(20) · pp. 5097–5108

Yusuke Ogitani✉(Daiichi Sankyo (Germany))Tetsuo Aida(Daiichi Sankyo (Germany))Katsunobu Hagihara(Daiichi Sankyo (Germany))Junko Yamaguchi(Daiichi Sankyo (Germany))Chiaki Ishii(Daiichi Sankyo (Germany))Naoya Harada(Daiichi Sankyo (Germany))Masako Soma(Daiichi Sankyo (Germany))Hiromi Okamoto(Daiichi Sankyo (Germany))Masataka Oitate(Daiichi Sankyo (Germany))Shingo Arakawa(Daiichi Sankyo (Germany))Takehiro Hirai(Daiichi Sankyo (Germany))Ryo Atsumi(Daiichi Sankyo (Germany))Takashi Nakada(Daiichi Sankyo (Germany))Ichiro Hayakawa(Daiichi Sankyo (Germany))Yuki Abe(Daiichi Sankyo (Germany))Toshinori Agatsuma(Daiichi Sankyo (Germany))

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Abstract

DS-8201a exhibited a potent antitumor activity in a broad selection of HER2-positive models and favorable pharmacokinetics and safety profiles. The results demonstrate that DS-8201a will be a valuable therapy with a great potential to respond to T-DM1-insensitive HER2-positive cancers and low HER2-expressing cancers. Clin Cancer Res; 22(20); 5097-108. ©2016 AACR.

Cancer therapeutics and mechanisms HER2/EGFR in Cancer Research Synthesis and Biological EvaluationTopoisomeraseCancer researchTopoisomerase inhibitorPharmacologyDNAChemistryMedicineBiochemistry

MeSH terms

TrastuzumabCheckpoint Kinase 1Ado-Trastuzumab EmtansineAnimalsAntibody-Dependent Cell CytotoxicityAntineoplastic AgentsBreast NeoplasmsCamptothecinFemaleHistonesHumansMacaca fascicularisMaytansineMice, NudePancreatic Neoplasms

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