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Amgen Announces First Clinical Data Evaluating Novel Investigational KRASG12C Inhibitor AMG 510 At ASCO 2019
AMG 510 is the First KRASG12C Inhibitor to Reach Clinical Stage After Three Decades of RAS Research First-In-Human Results Show Preliminary Safety,
About this update from Amgen Inc.
[{"type":"text","content":"AMG 510 is the First KRASG12C Inhibitor to Reach Clinical Stage After Three Decades of RAS Research\nFirst-In-Human Results Show Preliminary Safety, Tolerability Data and Anti-Tumor Activity in KRAS Mutant Solid Tumors\nFDA Grants AMG 510 Orphan Drug Designation for KRASG12C-Positive Non-Small Cell Lung and Colorectal Cancers\n THOUSAND OAKS, Calif., June 3, 2019 /PRNewswire/ -- Amgen (NASDAQ: AMGN) today announced the first clinical results from a Phase 1 study evaluating investigational AMG 510, the first KRASG12C inhibitor to reach the clinical stage. In the trial, there were no dose-limiting toxicities at tested dose levels. AMG 510 showed anti-tumor activity when administered as a monotherapy in patients with locally-advanced or metastatic KRASG12C mutant solid tumors. These data are being presented during an oral session at the 55th Annual Meeting of the American Society of Clinical Oncology (ASCO) in Chicago.\n\"KRAS has been a target of active exploration in cancer research since it was identified as one of the first oncogenes more than 30 years ago, but it remained undruggable due to a lack of traditional small molecule binding pockets on the protein. AMG 510 seeks to crack the KRAS code by exploiting a previously hidden groove on the protein surface,\" said David M. Reese, M.D., executive vice president of Research and Development at Amgen. \"By irreversibly binding to cysteine 12 on the mutated KRAS protein, AMG 510 is designed to lock it into an inactive state. With high selectivity for KRASG12C, we believe investigational AMG 510 has high potential as both a monotherapy and in combination with other targeted and immune therapies.\"\nThe Phase 1, first-in-human, open-label multicenter study enrolled 35 patients with various tumor types (14 non-small cell lung cancer [NSCLC], 19 colorectal cancer [CRC] and two other). Eligible patients were heavily pretreated with at least two or more prior lines of treatment, consistent with their tumor type and stage of disease. The primary endpoint is safety, and key secondary endpoints include pharmacokinetics, objective response rate (assessed every six weeks), duration of response and progression-free survival. Patients were enrolled in four dose cohorts - 180 mg, 360 mg, 720 mg and 960 mg, taken orally once a day. \nFive out of 10 evaluable patients with NSCLC experienced a par...