Generic
Sunitinib
3 brands available in the market
At a glance
Sunitinib is a multi-tyrosine kinase inhibitor used for gastrointestinal stromal tumor (GIST), advanced renal cell carcinoma (RCC), and pancreatic neuroendocrine tumors (pNET).
Description
Sunitinib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs), including PDGFRα/β, VEGFR1/2/3, KIT, FLT3, CSF-1R, and RET. It exhibits antitumor activity by blocking signaling pathways involved in tumor growth, pathologic angiogenesis, and metastasis.
Indications
- Gastrointestinal stromal tumor (GIST) – after progression on or intolerance to imatinib
- Advanced renal cell carcinoma (RCC)
- Adjuvant treatment of RCC (high risk after nephrectomy)
- Advanced pancreatic neuroendocrine tumors (pNET)
Therapeutic class
Targeted Cancer Therapy
Pharmacological class
Multi-Tyrosine Kinase Inhibitor (TKI)
Pharmacology
Sunitinib inhibits multiple receptor tyrosine kinases including PDGFR, VEGFR, KIT, FLT3, CSF-1R, and RET. It blocks signaling pathways involved in tumor cell proliferation, angiogenesis, and metastasis, reducing tumor growth and promoting apoptosis.
Mechanism of action
Inhibits tumor growth, angiogenesis, and metastasis by blocking tyrosine kinase signaling.
Dosage
Adult Dose (Oral):
- GIST/Advanced RCC: 50 mg once daily (4 weeks on, 2 weeks off – 4/2 schedule)
- Adjuvant RCC: 50 mg once daily (4/2 schedule) – nine 6-week cycles
- pNET: 37.5 mg once daily continuously (no scheduled off period)
Administration
- Can be taken with or without food
- Take at the same time each day
- Do not chew, crush, or break tablets
- Follow the 4/2 schedule as prescribed
Missed dose
If you miss a dose, skip it and continue with your normal schedule; do not double the dose.
Side effects
Common Side Effects:
- Nausea, vomiting, weakness
- Diarrhea, constipation
- Hypertension
- Skin discoloration, hair discoloration
- Painful blisters on hands and feet
- Fatigue, fever, loss of appetite, weight loss
Precautions & warnings
- Hepatotoxicity: Monitor liver enzymes
- Cardiovascular events, QT prolongation
- Hypertension: Regular monitoring
- Hemorrhage, thrombotic microangiopathy
- Thyroid dysfunction: Regular monitoring
- Hypoglycemia: Caution in diabetic patients
- Wound healing delay: Discontinue before surgery
Contraindications
- Hypersensitivity to any component
Drug interactions
- Strong CYP3A4 inhibitors (ketoconazole, ritonavir, itraconazole): Increase sunitinib plasma concentrations; consider dose reduction
- Strong CYP3A4 inducers (rifampin, phenytoin, carbamazepine, St. John's wort): Decrease plasma concentrations; consider dose increase
- Grapefruit juice: Increases sunitinib levels (avoid)
Food interactions
It is not known whether alcohol is safe with Sunitinib; consult your doctor.
Use in pregnancy
Use in Pregnancy: Unsafe; evidence of fetal risk; use only in life-threatening situations; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unsafe; drug may cause toxicity to the baby; do not breastfeed during treatment and for 4 weeks after the last dose; consult your doctor.
Pediatric use
Pharmacokinetics not evaluated in pediatric patients
Geriatric use
No significant differences between older and younger patients
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; no dose adjustment needed; ESRD on hemodialysis has 47% lower exposure; consult your doctor.
Hepatic Impairment: Mild-moderate (Child-Pugh A/B): no dose adjustment; severe: not studied; consult your doctor.
Overdose effects
No specific antidote for overdose; provide supportive care; if indicated, eliminate unabsorbed drug by emesis or gastric lavage; overdose up to 1500 mg has been reported without adverse reactions.
Storage conditions
Store at 25°C in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Sunitinib