2019年10月30日 · Our efforts have led to the discovery of AMG 510, which is, to our knowledge, the first KRAS (G12C) inhibitor in clinical development. In preclinical analyses, treatment with AMG 510 led to the...

2019年12月10日 · Biopharmaceutical optimization of the resulting leads culminated in the identification of AMG 510, a highly potent, selective, and well-tolerated KRAS G12C inhibitor currently in phase I clinical trials (NCT03600883). This publication is licensed for personal use by The American Chemical Society.

2021年6月25日 · The CodeBreaK 100 trial, funded by Amgen and NCI, is testing sotorasib (previously called AMG510) as a treatment for people with solid tumors that have KRAS G12C. The mutation, a hallmark of damage from cigarette smoke, is most common in lung cancer.

Our efforts have led to the discovery of AMG 510, which is, to our knowledge, the first KRAS (G12C) inhibitor in clinical development. In preclinical analyses, treatment with AMG 510 led to the regression of KRAS G12C tumours and improved the anti-tumour efficacy of chemotherapy and targeted agents.

2020年9月20日 · Sotorasib (AMG 510) is a small molecule that specifically and irreversibly inhibits KRAS G12C through a unique interaction with the P2 pocket (Fig. S1 in the Supplementary Appendix,...

In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer [3].

2020年1月9日 · Biopharmaceutical optimization of the resulting leads culminated in the identification of AMG 510, a highly potent, selective, and well-tolerated KRAS G12C inhibitor currently in phase I clinical trials (NCT03600883). KRAS^G12C has emerged as a promising target in the treatment of solid tumors.

THOUSAND OAKS, Calif., May 29, 2020 /PRNewswire/ -- Amgen (NASDAQ:AMGN) today announced new data from the CodeBreaK 100 clinical development program evaluating investigational AMG 510 (proposed INN sotorasib) in heavily pretreated patients with a range of KRAS G12C -mutant solid tumors.

2023年9月14日 · AMG510 is the first medication of its kind to reach clinical testing and binds to mutated KRAS protein which “turns off” the signals it sends to trigger cell division and cancer cell growth.

Titled "The Clinical KRAS G12C Inhibitor AMG 510 Drives Anti-Tumor Immunity," the paper highlights novel structural insights that led to the discovery of AMG 510, the preclinical evidence of AMG 510 activity, its potential ability to induce tumor-cell killing as both a monotherapy and in combination with other therapies, and its impact on the im...