Phase 2 Study of the Focal Adhesion Kinase Inhibitor Defactinib (VS-6063) in Previously Treated Advanced KRAS Mutant Non-small Cell Lung Cancer

Despite years of research, KRAS mutant non-small cell lung cancer (NSCLC) remains a major unmet clinical need. KRAS mutations, the second most common genomic alteration in human cancer after TP53 mutations, occur in 25-30 percent of lung adenocarcinomas [1,2]. High affinity binding of KRAS to its GTP substrate has hindered the development of therapeutic agents that directly inhibit KRAS. Only recently have KRAS-specific inhibitors have been developed [3,4]. Among them, direct, covalent KRASG12C inhibitors have demonstrated encouraging efficacy and appear well tolerated [5,6].

Source: Lung Cancer - November 5, 2019 Category: Cancer & Oncology Authors: David E. Gerber, D. Ross Camidge, Daniel Morgensztern, Jeremey Cetnar, Ronan J. Kelly, Suresh S. Ramalingam, David R. Spigel, Woondong Jeong, Pier P. Scaglioni, Song Zhang, Marilyn Li, David T. Weaver, Louis Vaikus, Mitchell Keegan, Joanna C. Horobin, Tim Source Type: research