sunitinibi

Sunitinib, marketed as Sutent, is a small-molecule tyrosine kinase inhibitor used to treat certain cancers. It inhibits several tyrosine kinases, notably VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-α, PDGFR-β, c-KIT, FLT3, CSF-1R, and RET, producing anti-angiogenic and anti-proliferative effects.

It is approved for gastrointestinal stromal tumor (GIST) and advanced renal cell carcinoma (RCC); it was later approved for pancreatic neuroendocrine tumors and has been studied in other cancers and combination regimens.

Sunitinib is taken by mouth, typically as an oral capsule. A common dosing schedule is 50 mg once daily for 4 weeks on treatment followed by 2 weeks off to allow a rest period in a 6-week cycle; dosing may be adjusted based on tolerance and toxicity. It has a relatively long terminal half-life (about 40–60 hours) and an active metabolite, SU12662, which contribute to activity. The drug is metabolized primarily by hepatic CYP3A4 and excreted mainly in bile.

Common adverse effects include fatigue, diarrhea, nausea, mucositis, rash, hypertension, hand–foot syndrome, and elevated liver enzymes. Serious risks include hepatotoxicity, cytopenias, hypertension, thromboembolic or cardiac events, and thyroid dysfunction. Monitoring typically includes liver function tests, blood pressure, and thyroid function.

Drug interactions are important: strong CYP3A4 inhibitors or inducers can alter exposure, necessitating dose adjustments or avoidance of certain combinations. Sunitinib is generally contraindicated in pregnancy and may require dose modification in hepatic impairment. It remains a widely used multi-target anticancer therapy with benefits in selected indications balanced against toxicity and interaction risks.