Sortorasirb (AMG510) is a highly selective targeted drug against KRASG12C mutations, developed by Amgen. It received accelerated approval from the US FDA in 2021 for the treatment of non-small cell lung cancer (NSCLC).
What is Sotorasirb (AMG510)?
Sortorasirb (AMG510) is a highly selective targeted drug against KRASG12C mutations. It covalently binds to the mutated cysteine residues of the KRASG12C protein, locking it in an inactive state, inhibiting the downstream MAPK signaling pathway, thereby blocking tumor cell proliferation and inducing apoptosis.
Sortorasirb (AMG510) Specifications and Characteristics
Drug Composition and Dosage Form
(1) Active Ingredient: Each tablet contains 120 mg of sotorasirb (equivalent to free base form), present in sulfate form.
(2) Excipients: Microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, etc. Film coating contains polyvinyl alcohol, titanium dioxide, polyethylene glycol, etc.
Appearance and Specifications
(1) Dosage Form: Yellow oval film-coated tablets, one side engraved with "AMG" and the other side engraved with "120".
(2) 120 tablets per bottle (NDC55513-488-02)
(3) 240 tablets per bottle (NDC55513-488-24)
Storage Conditions
Store at room temperature of 20°C~25°C (68°F~77°F). Short-term storage at 15°C~30°C (59°F~86°F) is permissible.
Sotorasirb (AMG510) Dosage and Administration
Recommended Dosage
Standard Dosage: 960 mg (8 tablets, 120 mg each) orally once daily until disease progression or intolerable toxicity.
Directions for Use
(1) Swallow whole; do not chew, break, or crush.
(2) Can be taken with food or on an empty stomach (food can increase AUC by 25%).
(3) If dispersible administration: Add the tablet to 120 mL of non-carbonated water, stir to form small granules, and drink immediately. Consume within 2 hours, and rinse the container with 120 mL of water.
Dosage Adjustments
(1) Hepatotoxicity: Discontinue use if AST/ALT ≥ grade 3 or accompanied by elevated bilirubin. After recovery, reduce the dose to 480 mg or 240 mg once daily.
(2) ILD/Pneumonia: Discontinue use immediately for suspected cases; permanently discontinue use after diagnosis.
(3) Other grade 3-4 adverse reactions: such as diarrhea, nausea, and vomiting. Discontinue use until grade ≤1, then reduce the dose and resume.
Drug Interactions
(1) Avoid concurrent use with PPIs/H2 receptor antagonists. If necessary, stagger the dose by 4 hours (antacids) or 10 hours (H2 antagonists).
(2) Avoid strong CYP3A4 inducers (e.g., rifampin) and sensitive CYP3A4/P-gp substrates (e.g., midazolam, digoxin).
(3) Missed dose management: If more than 6 hours have passed, skip this dose and take it as scheduled the next day.
