Sotorasib is an oral small molecule targeted inhibitor that specifically inhibits GTPase activity and blocks abnormal activation of the RAS signaling pathway by covalently binding to the switch pocket of KRAS G12C mutant protein.

1、 Indications

Sotoraxib is a KRAS GTPase family inhibitor, suitable for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) adult patients with confirmed KRAS G12C mutation detected by FDA testing, and patients must have received at least one systemic treatment.It is also used in combination with panitumumab for the treatment of adult patients with KRAS G12C mutant metastatic colorectal cancer (mCRC).

2、 Usage and dosage specifications

The recommended dosage is 960mg orally once daily (8 tablets 120mg) until disease progression or intolerable toxicity occurs. It can be taken on an empty stomach or after a meal, and should be swallowed whole without chewing or crushing. If the missed dose exceeds 6 hours, skip the dose and take the original plan the next day. After vomiting, there is no need to take additional medication, and medication should be taken normally the next day. For patients with swallowing difficulties, the tablets can be dispersed in 120mL of non carbonated water and stirred before taking within 2 hours. During medication, it is advisable to avoid using proton pump inhibitors (PPIs) or H2 receptor antagonists in combination. If antacids are needed, an interval of 4 hours (before) or 10 hours (after) should be used.

3、 Side effects and precautions

Common adverse reactions include diarrhea (42%), musculoskeletal pain (35%), nausea (26%), fatigue (26%), hepatotoxicity (25%), and cough (20%). Special attention should be paid to the following serious risks: liver toxicity is manifested by elevated transaminase levels, and liver function should be monitored every 3 weeks for the first 3 months of treatment; Interstitial lung disease (ILD) can be fatal, and new episodes of respiratory distress/cough/fever require immediate medical attention. Laboratory abnormalities include decreased lymphocytes (48%), decreased hemoglobin (43%), and increased AST/ALT (39%/38%). Pregnant and lactating women are prohibited from using the medication, and breastfeeding is prohibited during the medication period and within one week of discontinuation.

4、 Drug interactions

Avoid combination with strong CYP3A4 inducers, and adjust the dosage when combined with CYP3A4 or P-gp substrates. Combination therapy with proton pump inhibitors (PPIs) or H2 receptor antagonists can significantly reduce the blood concentration of Sotolaxib and should be avoided. If antacids must be used, the time interval requirements must be strictly followed.

Sotorasibinformation