Sunitinib

Concomitant use with strong CYP3A4 inducers (e.g. rifampicin):
Gastrointestinal stromal tumour; Advanced renal cell carcinoma:
Avoid concomitant use with strong CYP3A4 inducers. If concomitant use cannot be avoided, may increase dose in increments of 12.5 mg up to a Max of 87.5 mg daily based on safety or tolerability.

Pancreatic neuroendocrine tumour:
Avoid concomitant use with strong CYP3A4 inducers. If concomitant use cannot be avoided, may increase dose in increments of 12.5 mg up to a Max of 62.5 mg daily based on safety or tolerability.

Concomitant use with strong CYP3A4 inhibitors (e.g. ketoconazole):
Gastrointestinal stromal tumour; Advanced renal cell carcinoma:
Avoid concomitant use with strong CYP3A4 inhibitors. If concomitant use cannot be avoided, may decrease dose to a minimum dose of 37.5 mg daily based on safety or tolerability.

Pancreatic neuroendocrine tumour:
Avoid concomitant use with strong CYP3A4 inhibitors. If concomitant use cannot be avoided, may decrease dose to a minimum dose of 25 mg daily based on safety or tolerability.

Recommendations on dose adjustment may vary between countries (refer to country-specific product guidelines).

Sunitinib May be taken with or without food.

Patient with risk for or history of CV events (e.g. heart failure, cardiomyopathy, myocardial ischaemia, MI); history of QT interval prolongation; bradycardia, electrolyte disturbances, thyroid dysfunction, hypertension, history of aneurysm; diabetes mellitus, prior thromboembolic disease; dental disease, high tumour burden. Patients undergoing surgery (including invasive dental procedures). Renal impairment. Elderly. Pregnancy. Breastfeeding is not recommended. Concomitant use with strong CYP3A4 inducers or strong CYP3A4 inhibitors.

Significant: QT interval prolongation, torsades de pointes, hypertension, palmar-plantar erythrodysaesthesia syndrome, hand-foot skin reactions, hyperthyroidism, hypothyroidism, thyroiditis, symptomatic hypoglycaemia, medication-related osteonecrosis of the jaw; hyperammonemic encephalopathy, seizures; gastrointestinal disorders (e.g. diarrhoea, nausea, vomiting, abdominal pain, dyspepsia, stomatitis, oral pain, oesophagitis); increased serum lipase and amylase; DVT, skin and/or hair depigmentation or discolouration, pyoderma gangrenosum, decreased absolute neutrophil counts, decreased platelet counts, anaemia, impaired wound healing; hypersensitivity reactions (including angioedema).
Blood and lymphatic system disorders: Leucopenia, lymphopenia.
Eye disorders: Periorbital oedema, eyelid oedema, increased lacrimation.
Gastrointestinal disorders: Taste disturbance, constipation, GERD, dysphagia, abdominal distention or discomfort, gingival bleeding, mouth ulceration, proctalgia, cheilitis, haemorrhoids, glossodynia, dry mouth, flatulence, eructation, oral discomfort.
General disorders and administration site conditions: Mucosal inflammation, fatigue, oedema, pyrexia, chest pain, influenza-like illness, chills.
Infections and infestations: Viral infections, abscess, fungal infections, sepsis.
Investigations: Increased TSH, uric acid and creatinine; decreased ejection fraction, weight, Hb.
Metabolism and nutrition disorders: Decreased appetite, dehydration.
Musculoskeletal and connective tissue disorders: Pain in extremity, arthralgia, back pain, musculoskeletal pain, muscle spasms, myalgia, muscular weakness.
Nervous system disorders: Dizziness, headache, peripheral neuropathy, paraesthesia, hypoaesthesia, hyperaesthesia.
Psychiatric disorders: Insomnia, depression.
Renal and urinary disorders: Chromaturia, UTI.
Respiratory, thoracic and mediastinal disorders: Dyspnoea, respiratory infections, cough, pleural effusion, haemoptysis, oropharyngeal pain, nasal congestion or dryness.
Skin and subcutaneous tissue disorders: Alopecia, dry skin, rash, skin exfoliation, eczema, blister, erythema, acne, pruritus, skin hyperpigmentation, skin lesion, hyperkeratosis, dermatitis, nail disorder, skin infections.
Vascular disorders: Hot flush, flushing.
Potentially Fatal: Hepatotoxicity, liver failure (e.g. jaundice, elevated transaminases, hyperbilirubinaemia); CV events (e.g. heart failure, cardiomyopathy, myocardial ischaemia, MI, myocarditis, LVEF decline to below the lower limit of normal); haemorrhagic events (e.g. pulmonary haemorrhage, epistaxis, haemorrhage involving the brain, tumour sites, gastrointestinal, respiratory, or urinary tract); pulmonary embolism, tumour lysis syndrome; thrombotic microangiopathy, including thrombotic thrombocytopenic purpura (TTP) and haemolytic uraemic syndrome (HUS); serious infection with or without neutropenia; increased risk of aneurysm and artery dissection; reversible posterior leucoencephalopathy syndrome, gastrointestinal perforation; serious pancreatic events; arterial thromboembolic events, including cerebral infarction, CVA and TIA; renal impairment, renal failure and/or acute renal failure; proteinuria, nephrotic syndrome; severe cutaneous reactions (e.g. erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), necrotising fasciitis (e.g. perinium necrotising fasciitis, fasciitis secondary to fistula formation); thrombocytopenia, neutropenic infections.

PO: Z (Not recommended by some manufacturers unless benefits outweigh risks.)

This drug may cause dizziness, if affected, do not drive or operate machinery. Women of childbearing potential must use effective birth control methods during treatment.

Evaluate pregnancy status before treatment initiation. Monitor LFTs at baseline, during each cycle and as clinically indicated; ECG, blood pressure, blood glucose levels, and serum chemistries (e.g. magnesium, phosphate, calcium, potassium) before each treatment cycle. Perform urinalysis, serial CBC and physical examination. Evaluate LVEF and thyroid function at baseline and clinically as indicated. Assess for signs and symptoms of bleeding, thyroid disorders, CV disorders, gastrointestinal complications, and hand-foot skin reactions.

Increased plasma concentration with strong CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, erythromycin, itraconazole, ritonavir). Decreased plasma concentration with strong CYP3A4 inducers (e.g. rifampicin, dexamethasone, phenytoin, carbamazepine, phenobarbital). Increased risk of QT prolongation and arrhythmias with antiarrhythmics or QT prolonging drugs. Increased risk of osteonecrosis of the jaw with IV bisphosphonates.

Increased plasma concentration with grapefruit juice. Decreased plasma concentration with St. John's wort.

Description:
Overview: Sunitinib has antitumour and antiangiogenic properties.
Mechanism of Action: Sunitinib inhibits multiple receptor tyrosine kinases (RTK), including platelet-derived growth factors (PDGFRα and PDGFRβ), vascular endothelial growth factors (VEGFR1, VEGFR2, and VEGFR3), stem cell factor receptor (KIT), FMS-like tyrosine kinase-3 (FLT3), colony-stimulating factor type 1 (CSF-1R), and glial cell-line-derived neurotrophic factor receptor (RET).This results in the inhibition of tumour growth, pathologic angiogenesis and metastatic progression of cancer.
Pharmacodynamics: In vivo studies have shown that sunitinib effectively suppressed the phosphorylation of various RTKs (e.g. PDGFRβ, VEGFR2, KIT) in tumour xenografts expressing these RTK targets, where this inhibition was associated with tumour growth reduction, tumour regression, or inhibition of metastases in certain experimental cancer models. Additionally, sunitinib exhibits the capability to directly prevent the growth of tumour cells expressing dysregulated RTK targets (e.g. PDGFR, RET, FLT3 or KIT) and hindered tumour angiogenesis.

In a dose-dependent manner, sunitinib may cause QT interval prolongation, which may increase the risk of ventricular arrhythmias (e.g. torsades de pointes).
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 6-12 hours.
Distribution: Apparent volume of distribution: 2,230 L. Plasma protein binding: 95% (sunitinib); 90% (active metabolite).
Metabolism: Metabolised in the liver mainly by CYP3A4 isoenzyme to SU12662 (primary active metabolite).
Excretion: Mainly via faeces (approx 61%); urine (16%). Terminal elimination half-life: 40-60 hours (sunitinib); 80-110 hours (active metabolite).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5329102, Sunitinib. https://pubchem.ncbi.nlm.nih.gov/compound/Sunitinib. Accessed Oct. 29, 2025.

Store below 30°C. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.

Targeted Cancer Therapy

L01EX01 - sunitinib ; Belongs to the class of other protein kinase inhibitors. Used in the treatment of cancer.

Alsuni Capsules 12.5 mg, 25 mg and 50 mg (Lotus Healthcare Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 10/09/2025.

Brayfield A, Cadart C (eds). Sunitinib Malate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/09/2025.

Joint Formulary Committee. Sunitinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/09/2025.

REX Medical Ltd. Sunitinib 12.5 mg, 25 mg and 50 mg Capsules data sheet 23 June 2025. Medsafe. http://www.medsafe.govt.nz. Accessed 10/09/2025.

Sunitinib 25 mg Hard Capsules (Eugia [UK] Ltd). MHRA. https://products.mhra.gov.uk. Accessed 10/09/2025.

Sunitinib Malate Capsule (NorthStar RxLLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 10/09/2025.

Sunitinib Malate. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/09/2025.

Sunitinib. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/09/2025.