CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.

By H. Sakamoto, T. Tsukaguchi, Sayuri Hiroshima, Tatsushi Kodama, Takamitsu Kobayashi, T. Fukami, N. Oikawa, Takuo Tsukuda, Nobuya Ishii, Y. Aoki. Cancer Cell, 2011

626 citations recorded by the source corpus.

Subfields: Molecular Biology, Oncology, Pulmonary and Respiratory Medicine

View Paper: https://www.semanticscholar.org/paper/e4a0824bf15a4286928bf052f2855e5d1cef1442

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Molecular Biology

1. Gad Getz
2. J. Engelman
3. Carlos L. Arteaga

In Oncology

1. Gad Getz
2. J. Engelman

In Pulmonary and Respiratory Medicine

1. L. Sequist
2. J. Engelman
3. Carlos L. Arteaga

Citations in the corpus

• Alectinib in Crizotinib-Refractory ALK-Rearranged Non-Small-Cell Lung Cancer: A Phase II Global Study. (2016, neutral): “Any cause, in $ 10% Patients Constipation 39 (28) 6 (4) 0 0 45 (33) Fatigue 26 (19) 8 (6) 2 (1) 0 36 (26) Peripheral edema 27 (20) 6 (4) 1 (1) 0 34 (25) Myalgia 25 (18) 5 (4) 1 (1) 0 31 (23) Asthenia 16 (12) 8 (6) 1 (1) 0 25 (18) Headache 16 (12) 4 (3) 2 (1) 0 22 (16) Cough 15 (11) 4 (3) 0 0 19 (14)”
• Mechanisms of Acquired Crizotinib Resistance in ALK-Rearranged Lung Cancers (2012, background): “CH5424802 was recently shown to be a potent inhibitor of wild-type as well as L1196Mmutant ALK (24).”
• Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer (2016, positive): “Interestingly, alectinib has demonstrated significant activity against the ALK gatekeeper mutation L1196M in preclinical models (18), yet this was observed in one (6%) post-alectinib biopsy.”