Sotolacib

manual

Sotolacib instructions

Product Name: Sotokras

Manufacturer: Alliance Pharmaceuticals

Chinese name: Sotolacib

English name: Sotorasib

Drug approval number: 06 L 0981/23

【Summary】

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

【Indications】

For the treatment of adult patients with KRAS G12C mutant locally advanced or metastatic non-small cell lung cancer who have received at least one prior systemic therapy.

【Specification】

120mg/tablet, 56 tablets/box.

【Storage】

Store at 20°C to 25°C (68°C to 77°F); short-distance transport is permitted at a temperature range of 15 to 30°C (59–86°F).

【Usage and Dosage】

Recommended dose: 960 mg orally once daily.

Take 1 dose daily, around the same time.

Can be taken with or without food.

Swallow the tablet whole; do not chew, crush, or break the tablet.

【Adverse Reactions】

The most common adverse reactions (≥ 20%) were diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, and cough. The most common laboratory abnormalities (≥ 25%) were lymphocytopenia, hemoglobin decrease, aspartate aminotransferase increase, alanine aminotransferase increase, calcium decrease, alkaline phosphatase increase, urine protein increase, and sodium decrease.

【Taboo】

none

【Notes】

Hepatotoxicity: Monitor liver function tests every 3 weeks during the first 3 months of treatment, then monthly as clinically indicated. Based on severity, withhold, reduce dose, or permanently discontinue LuciSot.

Interstitial Lung Disease (ILD)/Pneumonitis: Monitor for new or worsening pulmonary symptoms. For suspected ILD/pneumonitis, immediately discontinue LuciSot and permanently discontinue if no other underlying cause of ILD/pneumonitis is found.

Safety and efficacy

Sotorasib is the first KRAS G12C inhibitor to enter clinical development and now has the potential to become the first targeted therapy approved for the treatment of patients with advanced NSCLC carrying the KRAS G12C mutation.

The marketing application for sotorasib is based on the positive results of the Phase II CodeBreaK 100 study in the cohort of advanced NSCLC patients who had previously progressed after chemotherapy and/or immunotherapy. The full results of the study were announced at the 21st World Lung Cancer Conference (WCLC) online meeting in 2020. The data showed that in patients with advanced NSCLC with KRAS G12C mutations who had previously progressed after chemotherapy and/or PD-1/PD-L1 immunotherapy, sotorasib showed durable anti-tumor activity and a positive benefit-risk profile: the confirmed objective response rate (ORR) was 37.1%, the disease control rate (DCR) was 80.6%, the median duration of response (DOR) was 10 months, and the median progression-free survival (PFS) was 6.8 months.