Sotorasib (AMG510) is a KRASG12C mutation inhibitor, indicated for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with KRASG12C mutation in patients who have received at least one prior systemic therapy.

Precautions for Administration of Sotorasib (AMG510)

Dosage and Administration Methods

Standard Dosage: 960 mg (8 tablets of 120 mg each) orally, once daily. It can be taken with or without food. The tablets must be swallowed whole and should not be chewed, split, or crushed.

Missed Dose Management: If a dose is missed by more than 6 hours, skip the missed dose and take the next dose as scheduled the following day. If vomiting occurs after taking a dose, no additional dose should be taken to make up for it.

For Patients with Dysphagia: Tablets can be dispersed in 120 mL of non-carbonated water. Stir the mixture and drink it immediately, and complete the entire dose within 2 hours.

Contraindications and Precautions

Contraindications:

Contraindicated in patients with hypersensitivity to any component of the drug.

Contraindicated in pregnant women (may cause fetal malformation).

Precautions:

Patients of childbearing age should use contraception during treatment.

Lactating women should avoid breastfeeding during treatment and for 1 week after discontinuing the drug.

Drug Interactions

Acid-Suppressing Drugs: Concomitant use of proton pump inhibitors (PPIs) and H2-receptor antagonists should be avoided. If co-administration is necessary, an interval between doses is required (LUMAKRAS should be taken either 4 hours before or 10 hours after the acid-suppressing drug).

Strong CYP3A4 Inducers: Drugs such as rifampicin may reduce the plasma concentration of sotorasib, so concomitant use should be avoided.

CYP3A4/P-gp Substrates: For drugs like midazolam and digoxin, the dosage of the co-administered drug should be adjusted.

Medication Monitoring for Sotorasib (AMG510)

Liver Function Monitoring

Monitoring Frequency: Before treatment, once every 3 weeks for the first 3 months of treatment, and then once a month thereafter. More frequent monitoring is required if abnormalities are detected.

Management of Abnormalities:

If ALT/AST > 3 × upper limit of normal (ULN) accompanied by symptoms, or ALT/AST > 5 × ULN: Suspend the drug, and resume treatment at a reduced dose after liver function recovers to ≤ Grade 1.

If ALT/AST > 3 × ULN accompanied by bilirubin > 2 × ULN: Discontinue the drug permanently.

Pulmonary Toxicity Monitoring

Symptom Recognition: New or worsening dyspnea, cough, and fever (may indicate interstitial lung disease [ILD]/pneumonitis).

Management: If ILD is suspected, suspend the drug immediately; discontinue the drug permanently if ILD is confirmed.

Gastrointestinal and Cutaneous Reactions

Diarrhea: If diarrhea is Grade ≥ 3, suspend the drug and resume at a reduced dose after symptoms resolve. Antidiarrheal drugs should be initiated at the first occurrence of loose stools.

Rash: If rash is Grade ≥ 3, suspend the drug and resume at a reduced dose after symptoms resolve.

Laboratory Index Monitoring

Routine Items: Complete blood count (lymphocytes, hemoglobin), electrolytes (calcium, sodium), liver and kidney function (AST/ALT, alkaline phosphatase), and urine protein.

Creatine Kinase (CPK): When muscle pain or darkening of urine occurs, check for rhabdomyolysis.