SOTOKRAS Sotorasib

[Product Name] Sotorasib Tablets

[English Name] Sotorasib Tablets

[R&D Code] AMG510

[Genetic Target] KRAS G12C

[Specification] 120 mg × 56 tablets/box

[Manufacturer] Lao United Pharmaceutical Group Co., Ltd.

[Approval Number (Lao National Drug Administration)] 06 L 0981/23

[Overview]

Sotorasib (AMG 510) is one of the first small-molecule inhibitors to successfully target KRAS and enter clinical development in humans; it specifically targets and inhibits KRAS proteins harboring the G12C mutation. Sotorasib specifically and irreversibly inhibits the pro-proliferative activity of the G12C-mutated KRAS protein by locking it 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.

[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 decreased lymphocytes, decreased hemoglobin, increased aspartate aminotransferase (AST), increased alanine transaminase (ALT), decreased calcium, increased alkaline phosphatase, increased urine protein, and decreased sodium.

[Contraindications] None

[Precautions]

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

Interstitial Lung Disease (ILD)/Pneumonitis: Monitor for new or worsening pulmonary symptoms. In cases of suspected ILD/pneumonia, immediately discontinue LuciSot; if no other potential causes for the ILD/pneumonia are identified, permanently discontinue the drug.

【Safety and Efficacy】

Sotorasib was the first KRAS G12C inhibitor to enter clinical development. Now, the drug holds the potential to become the first targeted therapy approved for the treatment of patients with advanced 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; these patients had experienced disease progression following prior treatment with chemotherapy and/or immunotherapy. The full results of this study were presented at the virtual 21st World Conference on Lung Cancer (WCLC) in 2020. The data demonstrated that, in patients with advanced NSCLC harboring the KRAS G12C mutation—who had progressed after 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).

How to Choose: Sotorasib, Fuzerece Tablets, Gesorece Tablets, or Adagrasib?

Sotorasib, Adagrasib, Fuzerece Tablets, and Gesorece Tablets are all KRAS G12C-targeted therapies, primarily indicated for the treatment of non-small cell lung cancer (NSCLC) harboring the KRAS G12C mutation. However, they differ in various aspects, including whether they are original/innovator drugs or domestically produced generics, their respective development companies, their market approval status, and their clinical data profiles. Key Distinctions Among the Three

Sotorasib: Developed by Amgen (USA); the world's first KRAS G12C inhibitor; supported by mature clinical data; carries a high price point.

Adagrasib: Developed by Mirati Therapeutics (USA); the preferred choice for patients with brain metastases; carries a relatively high price point.

Fuzeresib Tablets: Developed by Innovent Biologics (China); positioned as a domestic alternative; supported by moderately mature clinical data; eligible for medical insurance reimbursement.

Gesoresib Tablets: Jointly developed by Chia Tai Tianqing and InventisBio (China); supported by relatively early-stage clinical data.