Mechanism of action of adagrasib

The U.S. Food and Drug Administration (FDA)approved accelerated approval of adagrasib (Adagrasib) for the treatment of adult patients with KRAS G12C-mutated, locally advanced or metastatic non-small cell lung cancer who have received at least 1 prior systemic therapy, as determined by an FDA-approved trial. This decision was based on data from KRYSTAL-1.

In normal cells, KRAS is activated by binding to guanosine triphosphate (GTP), which promotes activation of the MAP kinase pathway and intracellular signal transduction. KRAS is inactivated when GTP is hydrolyzed to guanosine diphosphate (GDP). This mechanism acts as an "on"/"off" system to regulate cell growth. Substitution of Gly12 by cysteine u200bu200bin KRAS (KRASG12C) impairs GTP hydrolysis and allows KRAS to maintain its active form. Therefore, the presence of this mutation can lead to uncontrolled cell proliferation and growth, as well as malignant transformation. Adagrasiib is a covalent inhibitor of KRASG12C that irreversibly and selectively binds and locks KRASG12C in its inactive, guanosine diphosphate-bound state. Consequently, the use of adagrasib inhibited tumor cell growth and viability in KRAS G12C mutant cancers with minimal off-target activity.

Since the original drug of adagrasib has not yet been launched in China, patients can only purchase adagrasib through overseas channels. The specifications of the original version of adagrasib in the United States The price of each box of 200mg*180 tablets is more than 100,000 yuan (the price may fluctuate due to the exchange rate), which is very expensive. Currently, there are no generic adagrasibu produced in other countries overseas. For more drug information and specific prices, please consult Yaode Medical Consultant.