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New targeted drug for non-small cell lung cancer -- KRAS G12C inhibitor

Amgen announced yesterday (December 16) that it had submitted its new drug application (NDA) to the US FDA for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) patients with KRAS G12C mutation. These patients had received at least one systemic treatment before. FDA will review NDA under the real-time Oncology Review (RTOR) pilot program as scheduled.

On December 10, a week ago, Amgen announced that FDA had granted breakthrough drug qualification (BTD) and real-time Oncology Review (RTOR) for targeted anticancer drug sotorasib (AMG 510). The drug is a krasg 12C inhibitor for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) patients with a KRAS G12C mutation confirmed by an FDA approved test method.

KRAS is one of the first cancer genes discovered, belonging to the ras gene family. It encodes a small GTPase membrane binding protein, which plays a major role in the signal transduction of cell growth regulation. KRAS gene has the greatest impact on human cancer. When activated, KRAS transmits upstream signals from cell surface receptors to downstream pathways to control normal cell function and proliferation.

KRAS gene mutation exists in about 1 / 4 of human tumors, and it is one of the most clear targets in the field of oncology drug research and development. However, it is a pity that KRAS is a non characteristic, nearly spherical structure, without obvious binding sites, so it is difficult to synthesize a compound that can target binding and inhibit phase activity, which has been almost impossible to overcome for a long time. At present, KRAS has become the synonym of "non drug" target in the field of tumor drug research and development.

KRAS is one of the most common mutational carcinogenic genes in NSCLC, and it is also a "magic spell" existence. Since it was discovered for more than half a century, the research and development of small molecule targeted drugs, antibody drugs and vaccines have failed. KRAS mutation can cause KRAS protein to maintain the activation state of GTP binding, initiate downstream signal transduction and lead to uncontrolled cell growth and proliferation. Among them, the second-line treatment of patients with NSCLC driven by KRAS G12C has a high degree of unsatisfied demand and poor prognosis. At present, there is no drug approved for KRAS G12C targeted therapy, and there is no drug available for KRAS mutation patients.

KRAS G12C inhibitor sotorasib has unlimited potential


Sotorasib is the first KRAS G12C inhibitor developed in clinical practice. It can specifically and irreversibly inhibit its proliferative activity by locking the G12C mutant KRAS protein in a non activated GDP binding state. It is expected to be the first target drug approved for the treatment of advanced NSCLC patients with KRAS G12C mutation.

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