索托拉西布片Sotorasib 120mg

Sotorasib (AMG 510) is one of the first small-molecule inhibitors that successfully targets KRAS and enters human clinical development. It can selectively inhibit the KRAS protein harboring the G12C mutation. Sotorasib specifically and irreversibly inhibits the pro-proliferative activity of G12C-mutant KRAS protein by locking it in an inactive GDP-bound state.

Indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring KRAS G12C mutation, who have received at least one prior systemic therapy.

120 mg per tablet; 56 tablets per box.

Store at 20°C to 25°C (68°F to 77°F). Short-term excursions between 15°C and 30°C (59°F and 86°F) are permitted for transportation.

Recommended Dose: 960 mg orally once daily, which is equivalent to 8 tablets of 120 mg each. Administration Instructions: Take at approximately the same time each day. May be taken with or without food. Swallow the tablets whole. Do not chew, crush or split the tablets.

Most Common Adverse Reactions (≥20%): Diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, cough. Most Common Laboratory Abnormalities (≥25%): Lymphopenia, decreased hemoglobin, increased aspartate aminotransferase (AST), increased alanine aminotransferase (ALT), decreased calcium, increased alkaline phosphatase, increased urine protein.

Hepatotoxicity Monitor liver function tests every 3 weeks during the first 3 months of treatment, then monthly as clinically indicated. Withhold, reduce the dose, or permanently discontinue sotorasib based on the severity of hepatotoxicity. Interstitial Lung Disease (ILD)/Pneumonitis Monitor for new or worsening pulmonary symptoms. Immediately discontinue sotorasib in patients with suspected ILD/pneumonitis. Permanently discontinue the drug if no other potential causes of ILD/pneumonitis are identified.

Sotorasib is the first KRAS G12C inhibitor to enter clinical development, with the potential to become the first approved targeted therapy for patients with advanced NSCLC harboring KRAS G12C mutation. The marketing application of sotorasib is based on the positive results from the advanced NSCLC cohort in the phase II CodeBreaK 100 study. The study enrolled patients with disease progression after prior chemotherapy and/or immunotherapy, and the full results were presented at the 2020 21st World Conference on Lung Cancer (WCLC) virtual meeting. The data demonstrated durable anti-tumor activity and a favorable benefit-risk profile of sotorasib: Confirmed objective response rate (ORR): 37.1% Disease control rate (DCR): 80.6% Median duration of response (DOR): 10 months Median progression-free survival (PFS): 6.8 months