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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.
Sotoraxib is a KRAS GTPase family inhibitor, suitable for the treatment of KRAS confirmed by FDA-approved testing Adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with G12C mutations who have received at least one systemic therapy. Also used in combination with panitumumab for the treatment of adult patients with KRAS G12C mutated metastatic colorectal cancer (mCRC).
The recommended dose is 960 mg (8 tablets of 120 mg) taken orally once a day until disease progression or intolerable toxicity occurs. It can be taken on an empty stomach or after meals. The tablet should be swallowed whole and should not be chewed or crushed. If you miss a dose for more than 6 hours, skip the dose and take the medicine as originally planned the next day. No need to take additional doses after vomiting, just take the medicine as normal the next day. For patients with dysphagia, the tablets can be dispersed in 120 mL of non-carbonated water and taken within 2 hours after stirring. During the medication period, avoid taking it in combination with proton pump inhibitors (PPIs) or H2 receptor antagonists. If you need to use antacids, there should be an interval of 4 hours (before) or 10 hours (after).
Common adverse reactions include diarrhea (42%), musculoskeletal pain (35%), nausea (26%), fatigue (26%), liver toxicity (25%) and cough (20%). Special attention should be paid to the following serious risks: hepatotoxicity manifests as elevated transaminases, and liver function needs to be monitored every 3 weeks for the first 3 months of treatment; interstitial lung disease (ILD) may be fatal, and new onset of dyspnea/cough/fever requires immediate medical attention. Laboratory abnormalities included lymphopenia (48%), decreased hemoglobin (43%), increased AST/ALT (39%/38%), etc. Pregnant and lactating women are prohibited from breastfeeding. Breastfeeding is prohibited during medication and within 1 week of discontinuation of medication.
Avoid combination with strong CYP3A4 inducers. Dosage adjustment is required when combined with CYP3A4 or P-gp substrates. Combined use with proton pump inhibitors (PPIs) or H2 receptor antagonists will significantly reduce the plasma concentration of sotoraxib and should be avoided. If antacids must be used, strict time intervals must be followed.