Sunitinib

BRAND NAME:

Sutent – It is available in capsules with sunitinib maleate as an active ingredient which works as an anti-cancer drug.

MECHANISM OF ACTION:

Sunitinib is a small medication that inhibits many RTKs, including those implicated in tumor growth, pathologic angiogenesis, and cancer spread. Sunitinib inhibited platelet-derived growth factor receptors, vascular endothelial growth factor receptors, stem cell factor receptor Fms-like tyrosine kinase-3, colony stimulating factor receptor Type 1, and glial cell-line derived neurotrophic factor receptors.

PHARMACOKINETICS:

Absorption: The oral absorption of sunitinib takes 6 to 12 hours to reach its maximum plasma peak concentration.

Distribution: The apparent volume of distribution for sunitinib is 2230L.

Metabolism: It is primarily metabolized by CYP3A4 to its primary activity metabolite, which is metabolized by CYP3A4.

Excretion: 61% of the dose is excreted through feces and 16% through urine.

DOSAGE AND ADMINISTRATION:

Sunitinib is available as oral capsules in different strengths 12.5 mg, 25 mg, 37.5 mg and 50 mg. The dosage of the medicine will differ between patients. The amount of medicine prescribed varies depending on the strength of the medication, the patient's condition, and the number of doses taken per day.

• For pancreatic cancer or pancreatic neuroendocrine tumors, the recommended oral dose in adults is 37.5mg once a day. Based on the patient's tolerance the dose may be increased. The dose should not exceed more than 50mg per day.

• For kidney cancer treatment the recommended dose in adults is 50mg once a day for 4 weeks.

• For treatment of kidney cancer after surgical kidney removal in adults, the recommended dose is 50mg once a day for 4 weeks.

DRUG INTERACTIONS:

While taking sunitinib, have to check if the drug is interacting with any other drugs that were already been used in the other treatments. When the drug interacts with other drugs the working of the drug may change and lead to serious side effects. Below are the drugs with which sunitinib interacts.

• Blood thinners – Anticoagulants like Warfarin, heparin

• Antifungals – Itraconazole, ketoconazole.

• Antibiotics – Erythromycin, clarithromycin, rifampicin

• Seizures drugs – Phenytoin, phenobarbital, carbamazepine

• Steroid medicine – Dexamethasone

• Herbal antidepressant – Hypericum perform

FOOD INTERACTIONS:

Avoid grapefruits and grapefruit juices while taking sunitinib.

ADVERSE EFFECTS:

• Hyperammonemia

• Liver problems 

• Heart failure

• Breathlessness

• Bleeding problems

• Cough

• Loss of appetite

• Bruising and bleeding

• Change of thyroid hormones 

• Difficulty in sleeping

• Headache

• Dizziness

• Hair loss

• Irregular menstrual cycle

• Blurred vision

• Diarrhea

• Constipation

• Mouth ulcers

• Blisters

• Fatigue

• Soreness, and redness on palm

• Muscle pains

• Joint pains

• High levels of uric acid and creatine

• Oedema

TOXICITY:

Overdose consumption of sunitinib causes toxic effects

• Impaired muscle coordination

• Gastrointestinal distress

• Ocular discharge

• Hypoactivity

• Head shakes

• Piloerection