Nature Communications (Aug 2019)

The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models

  • Ryohei Katayama,
  • Bo Gong,
  • Noriko Togashi,
  • Masaya Miyamoto,
  • Masaki Kiga,
  • Shiho Iwasaki,
  • Yasuki Kamai,
  • Yuichi Tominaga,
  • Yasuyuki Takeda,
  • Yoshiko Kagoshima,
  • Yuki Shimizu,
  • Yosuke Seto,
  • Tomoko Oh-hara,
  • Sumie Koike,
  • Naoki Nakao,
  • Hiroyuki Hanzawa,
  • Kengo Watanabe,
  • Satoshi Yoda,
  • Noriko Yanagitani,
  • Aaron N. Hata,
  • Alice T. Shaw,
  • Makoto Nishio,
  • Naoya Fujita,
  • Takeshi Isoyama

DOI
https://doi.org/10.1038/s41467-019-11496-z
Journal volume & issue
Vol. 10, no. 1
pp. 1 – 12

Abstract

Read online

The treatment of ROS1-rearranged non-small cell lung cancer with the TKI crizotinib is limited due to the emergence of resistance. Here, the authors develop a new ROS1/NTRK inhibitor, DS-6051b, which overcomes crizotinib resistance in preclinical models.