sotorasib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
sotorasib: clinical details
Prescribing considerations
- Confirm KRAS G12C using a validated test before initiation.
- Initiation and supervision require a clinician experienced with anticancer treatments.
- Review prior immunotherapy and radiotherapy because recent immunotherapy may increase hepatotoxicity and pneumonitis risk.
- Review acid suppression, enzyme inducers, narrow-therapeutic-index CYP3A4 or P-glycoprotein substrates, and BCRP substrates.
- Use caution in severe hepatic impairment; moderate and severe renal impairment have not been adequately studied.
Contraindications and cautions
- Hypersensitivity to sotorasib or an excipient.
- The tablets contain lactose and should not be used in people with galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.
Monitoring
- Check ALT, AST, alkaline phosphatase and total bilirubin before treatment, every three weeks during the first three months, then monthly or when clinically indicated.
- Monitor liver tests more frequently after recent immunotherapy or following serious hepatotoxicity.
- Monitor for new or worsening dyspnoea, cough or fever and withhold treatment while suspected interstitial lung disease or pneumonitis is investigated.
- Assess gastrointestinal toxicity, hydration, blood counts and clinically relevant electrolyte abnormalities.
Clinical pharmacology
A selective, covalent and irreversible KRAS G12C inhibitor that locks mutant KRAS in its inactive state. It is also a moderate CYP3A4 inducer, a P-glycoprotein inhibitor and a weak BCRP inhibitor; elimination is predominantly faecal.
Formulation and product differences
- The selected product is an immediate-release, film-coated tablet containing lactose and is essentially sodium-free.
- Tablets may be swallowed whole or dispersed in non-carbonated water without crushing.
- The dispersion can be administered through a nasogastric or gastrostomy tube using the product-specific procedure.
sotorasib preparations and strengths
Tablet
Route: Oral
Strengths: 240 mg
sotorasib interactions
Sotorasib has clinically important interactions. Check prescription, non-prescription and herbal products before treatment and whenever medicines change.
Proton-pump inhibitors and H2-receptor antagonists
Medicines such as omeprazole or famotidine reduce sotorasib exposure and may reduce its effect; specialist administration instructions are needed if concurrent use is unavoidable.
Local antacids
Antacids containing substances such as calcium carbonate or magnesium hydroxide must be separated from sotorasib according to the product instructions.
Strong CYP3A4 inducers
Rifampicin, carbamazepine, phenytoin, phenobarbital and St John's wort may lower sotorasib exposure, so concurrent use is not recommended.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.