Effect of adagrasib on brain metastasis of lung cancer

Patients with KRAS mutant non-small cell lung cancer ((NSCLC)) with brain metastasis have a poor prognosis. Adagrasib is an effective oral small molecule KRAS G12C inhibitor that irreversibly and selectively binds to KRAS G12C, locking it is established in the inactive state. Adagrasiib has been optimized to have favorable pharmacokinetic properties, including long half-life (24 hours), broad tissue distribution, dose-dependent pharmacokinetics, and central nervous system penetration; however, the brain metastasis (BM)-specific antitumor activity of KRASG12C inhibitors remains to be fully characterized.

Preliminary clinical data from 2 patients enrolled in the KRYSTAL-1 untreated BM cohort indicate that adagrasib concentrations in the cerebrospinal fluid (CSF) are higher than the target cellIC50. Furthermore, the mean Kp, uu value determined for these patients (0.47) is consistent with observations of exposure and antitumor activity in nonclinical models and also exceeds previously demonstrated values for CNS penetration and antitumor activity of TKIs in bone marrow (16-18). Furthermore, a decrease in BM was observed in both patients. Most of the treatment-related adverse events reported by these patients were grade 1 or 2 in severity, and no new safety signals were observed. Although preliminary, in a very small number of patients, these data support further development of clinical use of adagrasib in patients with active and treatment-naïve bone marrow patients with KRAS G12C-mutant non-small cell lung cancer.

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.