Sotoxen

Generic name: sotorasib

Trade name: Lumakras

Full names: sotorasib, Lumakras, AMG510, sotorasib

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 systemic therapy.

Usage and dosage:

Recommended dosage: 960 mg orally once a day.

Take once a day, around the same time.

It 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%) are diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity and cough. The most common laboratory test abnormalities (≥ 25%) were lymphopenia, decreased hemoglobin, increased aspartate aminotransferase, increased alanine aminotransferase, decreased calcium, increased alkaline phosphatase, increased urinary protein, and decreased sodium.

Taboos:

None.

Precautions:

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

Interstitial Lung Disease (ILD)/Pneumonia: Monitor for new or worsening pulmonary symptoms. For suspected ILD/pneumonitis, discontinue LUMAKRAS immediately or permanently if no other potential cause of ILD/pneumonitis is identified.

Storage:

Store at a temperature of 20℃ to 25℃ (68℉ to 77℉). Allows a shift from 15℃ to 30℃ (59℉ to 86℉)

Mechanism of action:

Sotorasib (AMG 510) is one of the first small molecule inhibitors to successfully target KRAS and enter human clinical development. It can target and inhibit the KRAS protein carrying 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.

Safety and efficacy:

Sotorasib is the first KRAS G12C inhibitor to enter clinical development. Now, the drug has the potential to become the first targeted therapy approved for the treatment of patients with advanced NSCLC carrying KRAS G12C mutations.

The marketing application for sotorasib is based on positive results from the phase II CodeBreaK 100 study in a cohort of patients with advanced NSCLC whose disease progressed after prior chemotherapy and/or immunotherapy. The full results of the study were announced at the 21st World Conference on Lung Cancer (WCLC) Online Meeting in 2020. The data showed that: KRAS patients whose disease progressed after previously receiving chemotherapy and/or PD-1/PD-L1 immunotherapy In patients with G12C mutated advanced NSCLC, sotorasib showed durable anti-tumor activity and a positive 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.