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A Novel HER3-Targeting Antibody-Drug Conjugate, U3-1402, Exhibits Potent Therapeutic Efficacy through the Delivery of Cytotoxic Payload by Efficient Internalization.
Yuuri Hashimoto
1 ,
Kumiko Koyama
1 ,
Yasuki Kamai
2 ,
Kenji Hirotani
1 ,
Yusuke Ogitani
1 ,
Akiko Zembutsu
1 ,
Manabu Abe
1 ,
Yuki Kaneda
1 ,
Naoyuki Maeda
1 ,
Yoshinobu Shiose
1 ,
Takuma Iguchi
1 ,
Tomomichi Ishizaka
1 ,
Tsuyoshi Karibe
1 ,
Ichiro Hayakawa
1 ,
Koji Morita
1 ,
Takashi Nakada
1 ,
Taisei Nomura
3 ,
Kenichi Wakita
1 ,
Takashi Kagari
1 ,
Yuki Abe
1 ,
Masato Murakami
1 ,
Suguru Ueno
1 ,
Toshinori Agatsuma
1
December 01 2019
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Abstract
HER3 is a compelling target for cancer treatment; however, no HER3-targeted therapy is currently clinically available. Here, we produced U3-1402, an anti-HER3 antibody-drug conjugate with a topoisomerase I inhibitor exatecan derivative (DXd), and systematically investigated its targeted drug delivery potential and antitumor activity in preclinical models.