Drug reference

Sunitinib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplasticATC L01XE04

CDSCO approvedSchedule HATC L01XE04

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AnagrelideSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter

Mechanism

Sunitinib is an oral multitarget receptor tyrosine kinase inhibitor that simultaneously blocks VEGFR-1, -2, and -3 (anti-angiogenic), PDGFR-α and -β (tumor stroma disruption), c-KIT (gastrointestinal stromal tumors), FLT-3 (acute myeloid leukemia), and RET (thyroid cancer). This broad kinase inhibition profile provides both direct anti-tumor and anti-angiogenic effects. Its active metabolite SU12662 has similar potency and a half-life of 80-110 hours, contributing to sustained target inhibition with a 4-weeks-on/2-weeks-off dosing schedule.

Indications

metastatic renal cell cancerpancreatic NETsGIST in patients who have developed resistance to imatinib (due to c-KIT mutations)Metastatic renal cell carcinomaResistant g.i. stromal tumour (GIST)Advanced, progressive pancreatic neuroendocrine tumors (NETs)

Dosing

Adult: 16 Guidance on intravenous infusions

Pharmacokinetics

Half-life

80 to 110 h (active metabolite SU12662)

Metabolism

CYP3A4 (to active metabolite SU12662)

Side effects

Common

fatigue (50%–70%)hypothyroidism (40%–60%)bone marrow suppressiondiarrheaPPESHypertensionRashesDiarrhoeaWeaknessBleedingProteinureaHypothyroidismNeutropeniaProteinuriaFatigue

Serious