Inlyta

Axitinib

Advanced renal cell carcinoma (RCC) after failure of 1 prior systemic therapy w/ sunitinib, cytokine or sorafenib.

Recommended starting dose: 5 mg twice daily approx 12 hr apart. May be increased to 7 mg twice daily if no AR >grade 2 occur, patient is normotensive & not receiving antihypertensive medication. May be further increased to a max of 10 mg twice daily using the same criteria. Reduce dose to 3 mg & further to 2 mg twice daily when necessary for management of adverse drug reactions. Co-administration w/ strong CYP3A4/5 inhibitors Reduce dose by ½. Patient w/ moderate hepatic impairment (Child-Pugh class B) Starting dose: 2 mg twice daily.

May be taken with or without food: Swallow whole.

Hypersensitivity.

Monitor for signs & symptoms of cardiac failure; GI perforation or fistula; proteinuria; liver function tests periodically throughout treatment. BP should be well-controlled prior to initiation of therapy, carefully consider initiation in patients w/ risk factors eg, HTN or history of aneurysm. Monitor patients for HTN & treat as needed. Temporarily interrupt treatment in patients who develop severe HTN & restart at lower dose. Consider MRI in case of severe or persistent arterial HTN & symptoms suggestive of posterior reversible encephalopathy syndrome. Monitor thyroid function, hemoglobin & hematocrit prior to initiation of & periodically throughout treatment & treat accordingly. Patients who are at risk for or who have a history of arterial & venous thromboembolic events. Hemorrhage. Not to be used in patients who have evidence of untreated brain metastasis or recent active GI bleeding. Discontinue treatment at least 24 hr prior to surgery. Temporarily interrupt or permanently discontinue treatment in patients w/ signs & symptoms of reversible posterior leukoencephalopathy syndrome. May impair ability to drive & use machines. Moderate & severe hepatic impairment. Pregnancy & lactation. Childn <18 yr.

Hypothyroidism; decreased appetite; headache, dysgeusia; HTN, haemorrhage; dyspnoea, cough, dysphonia; diarrhea, vomiting, nausea, abdominal pain, stomatitis, constipation, dyspepsia; palmar-plantar erythrodysaesthesia (hand-foot syndrome), rash, dry skin; arthralgia, pain in extremity; proteinuria; fatigue, asthenia, mucosal inflammation; decreased wt. Anaemia, thrombocytopenia, polycythaemia; hyperthyroidism; dehydration, hyperkalaemia, hypercalcaemia; dizziness; tinnitus; cardiac failure events; venous thromboembolic events, arterial thrombotic events; oropharyngeal pain; upper abdominal pain, haemorrhoids, glossodynia, GI perforation & fistula, flatulence; hyperbilirubinaemia; erythema, pruritus, alopecia; myalgia; renal failure; increased TSH, lipase, blood creatinine, ALT, alkaline phosphatase, AST, amylase.

Increased AUC & C_max w/ CYP3A4/5 inhibitors eg, ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin. Reduced AUC & C_max w/ CYP3A4/5 inducers eg, rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentin, phenobarb, St. John's wort, bosentan, efavirenz, etravirine, modafinil, nafcillin. Increased plasma conc of CYP1A2 substrates eg, theophylline. Grapefruit, CYP1A2 & CYP2C19 may also increase axitinib plasma conc.

Targeted Cancer Therapy

L01EK01 - axitinib ; Belongs to the class of vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors. Used in the treatment of cancer.

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