The first KRAS inhibitor to receive accelerated approval from the US FDA for the treatment of non-small cell lung cancer

Lung cancer is the most common type of cancer with the highest mortality rate.

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NSCLC patients contain proto-oncogene mutations, of which KRAS is the most common mutation gene, and half of KRAS mutations are KRAS G12C mutations, accounting for about 13% of NSCLC patients, that is, one of the 8 NSCLC patients is KRAS G12C mutation.

KRAS mutations occur in about 25% of cancer cases, mainly in lung cancer, pancreatic cancer and colorectal cancer , and are associated with a very poor prognosis of the disease.

Lumakras (Sotorasib), formerly known as AMG 510, is a small molecule designed to bind to KRAS G12C to lock the protein in an inactive state and prevent it from sending signals that drive uncontrolled cell growth.

This is the first approved targeted therapy for any tumor with KRAS mutations.

"Richard Pazdur, MD, director of the U.

Researchers evaluated the efficacy of Lumakras in a study of 124 patients with locally advanced or metastatic KRAS G12C mutations in non-small cell lung cancer.

The main results of the measurement are the objective response rate (the proportion of patients whose tumors are destroyed or reduced) and the duration of the response.

The approved 960 mg dose is based on existing clinical data and the pharmacokinetic and pharmacodynamic models that support the approved dose.

The most common side effects of Lumakras include diarrhea, musculoskeletal pain, nausea, fatigue, liver damage, and cough.

Lumakras was approved through an accelerated approval route, according to which the US Food and Drug Administration can approve drugs for the treatment of serious diseases because the medical needs of these diseases have not been met, and a certain drug has been proven to have certain effects.

The US Food and Drug Administration awarded the application the title of fast track, priority review, and breakthrough therapy.

Lumakras also received the title of "orphan" drug, which provides a reward for assisting and encouraging the development of drugs for rare diseases.

In addition to Lumakras, there are currently a number of KRAS inhibitors in the clinical development stage.

Nearly 40 years ago, scientists discovered the relationship between KRAS gene mutations and cancer for the first time.
With the unremitting efforts of scientists and drug developers, we finally witnessed a milestone in breaking KRAS's "non-drugability".