LuciSot Sotorasib LUMAKRAS

Product Name: LuciSot

Chinese Name: Suotuolaxibu

English Name: Sotorasib

[Overview]

Sotorasib (AMG 510) is one of the first small-molecule inhibitors to successfully target KRAS and enter human clinical development; it specifically targets and inhibits KRAS proteins harboring the G12C mutation. Sotorasib specifically and irreversibly inhibits the proliferative activity of KRAS G12C mutant proteins by locking them into an inactive, GDP-bound state.

[Indications]

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

[Specification] 120 mg/tablet; 56 tablets/box.

[Dosage and Administration]

Recommended Dosage: 960 mg orally once daily.

Take once daily, at approximately the same time each day.

May be taken with or without food.

Swallow tablets whole; do not chew, crush, or split the tablets.

[Adverse Reactions]

The most common adverse reactions (≥ 20%) are diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, and cough. The most common laboratory abnormalities (≥ 25%) are lymphopenia, decreased hemoglobin, increased aspartate aminotransferase (AST), increased alanine aminotransferase (ALT), hypocalcemia, increased alkaline phosphatase, increased urine protein, and hyponatremia.

[Contraindications] None.

[Precautions]

Hepatotoxicity: Monitor liver function tests every 3 weeks during the first 3 months of treatment, and monthly thereafter as clinically indicated. Withhold, reduce the dose, or permanently discontinue LuciSot based on the severity of the reaction.

Interstitial Lung Disease (ILD)/Pneumonitis: Monitor for new or worsening pulmonary symptoms. For suspected ILD/pneumonitis, immediately withhold LuciSot; if no other potential causes of ILD/pneumonitis are identified, permanently discontinue the drug. [Safety and Efficacy]

Sotorasib was the first KRAS G12C inhibitor to enter clinical development; it now holds the potential to become the first targeted therapy approved for the treatment of patients with advanced non-small cell lung cancer (NSCLC) harboring the KRAS G12C mutation.

The marketing application for Sotorasib is based on positive results from the advanced NSCLC patient cohort in the Phase II CodeBreaK 100 study, which enrolled patients whose disease had progressed following prior chemotherapy and/or immunotherapy. The full results of this study were presented at the virtual meeting of the 21st World Conference on Lung Cancer (WCLC) in 2020. The data demonstrated that, in patients with advanced NSCLC harboring the KRAS G12C mutation—whose disease had progressed after receiving prior chemotherapy and/or PD-1/PD-L1 immunotherapy—Sotorasib exhibited durable anti-tumor activity and a favorable benefit-risk profile: a confirmed objective response rate (ORR) of 37.1%, a disease control rate (DCR) of 80.6%, a median duration of response (DOR) of 10 months, and a median progression-free survival (PFS) of 6.8 months.

[Storage]

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).