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Sotorasib is an oral small molecule targeted inhibitor that covalently binds to KRAS The switch pocket of the G12C mutant protein specifically inhibits GTPase activity and blocks abnormal activation of the RAS signaling pathway.
1. Generic name: Sotorasib (Sotorasib)
2. Trade name: LUMAKRAS™
For the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have a KRASG12C mutation confirmed by an FDA-approved test and who have received at least one prior systemic therapy. This indication received accelerated approval based on overall response rate (ORR) and duration of response (DOR).
1. Specifications: 120mg per tablet
2. Properties: tablets.
Active ingredient: sotoraxibu (molecular formula C30H30F2N6O3). Excipients include microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, etc.
1. Recommended dose : 960 mg (8 tablets) orally once a day until disease progression or intolerable toxicity occurs.
2. How to take : Swallow the whole tablet, with food or on an empty stomach. If you need to disperse the tablets, add the tablets to 120 mL of non-carbonated room temperature water and stir until dispersed. Drink immediately and finish within 2 hours.
3. Treatment of missed doses : If you miss a dose for more than 6 hours, skip the dose and take the medicine as originally planned the next day. No make-up dose is allowed.
4. Vomiting treatment : If you vomit after taking the medicine, there is no need to take a supplement. You can continue taking the original dose the next day.
1. Hepatotoxicity or adverse reactions : suspend, reduce the dose (first reduction to 480mg/day, second reduction to 240mg/day) or permanent discontinuation according to severity.
2. Interstitial lung disease (ILD) : Suspected ILD requires immediate discontinuation of medication, and permanent discontinuation after diagnosis.
1. Effect of diet : A high-fat diet may increase drug exposure by 25%, but no deliberate adjustment is required.
2. Gastric acid regulator : Avoid combined use with proton pump inhibitors (PPI) or H2 receptor antagonists. When combined use is necessary, an interval of 4 hours (antacids) or 10 hours (H2 antagonists) is required.
3. Drug interactions : Avoid combined use with strong CYP3A4 inducers, CYP3A4 substrates or P-gp substrates, which may affect efficacy or increase toxicity.
1. Pregnant women : There is no human data and animal tests have not shown teratogenicity, but the risks need to be weighed.
2. Lactation : Avoid breastfeeding during treatment and within 1 week after the last dose.
3. U200c for the elderly: No dose adjustment is required.
1. Common (≥20%) include diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity and cough. Laboratory abnormalities include lymphopenia, decreased hemoglobin, and elevated transaminases.
2. Serious adverse reactions include pneumonia (8%), liver toxicity (3.4%), etc.
There are no clear contraindications.
1. Strong CYP3A4 inducer : Reduce the concentration of sotoraxib and avoid combined use.
2. CYP3A4/P-gp substrate : The dosage of combined drugs may need to be adjusted (such as digoxin).
Store at room temperature 20°C to 25°C (68°F to 77°F), allowing short-term fluctuations of 15°C to 30°C (59°F to 86°F).