Tasigna

Nilotinib

Newly diagnosed Philadelphia chromosome +ve chronic myelogenous leukaemia (CML) in chronic phase in adult & paed patients. Philadelphia chromosome +ve CML in chronic phase in paed patients w/ resistance or intolerance to prior therapy including imatinib. 200-mg cap: Chronic & accelerated phase Philadelphia chromosome +ve CML in adult patients w/ resistance or intolerance to prior therapy including imatinib; efficacy data in patients w/ CML in blast crisis are not available.

Adult Newly diagnosed Philadelphia chromosome +ve CML in chronic phase 300 mg bd. Philadelphia chromosome +ve CML in chronic or accelerated phase resistant or intolerant to prior therapy 400 mg bd. Paed patient Philadelphia chromosome +ve CML 230 mg/m² bd, rounded to the nearest 50 mg dose. Max single dose: 400 mg.

Should be taken on an empty stomach: Swallow whole w/ water. Take at least 2 hr before meals & refrain from eating for at least 1 hr after intake. Avoid grapefruit products.

Hypersensitivity.

Risk of myelosuppression; QT prolongation; fluid retention & oedema; CV events; hepatitis B reactivation; atherosclerosis-related diseases; elevation in serum lipase; tumour lysis syndrome. Reports of uncommon cases of sudden deaths in patients w/ imatinib-resistant or intolerant CML in chronic or accelerated phase w/ past medical history of cardiac disease or significant cardiac risk factors. Perform CBCs every 2 wk for the 1st 2 mth, then mthly thereafter, or as clinically indicated. Closely monitor QTc interval & perform baseline ECG prior to treatment initiation & as clinically indicated. Correct hypokalaemia or hypomagnesaemia before Tasigna administration & monitor periodically during therapy. Evaluate, monitor & actively manage CV status & risk factors during therapy. Monitor Ph+ CML patients in chronic phase who achieved a sustained deep molecular response. Determine lipid profiles & assess glucose levels prior to & during treatment. Higher risk of hepatotoxicity in paed population. Bioavailability might be reduced in patients w/ total gastrectomy. Avoid concomitant use w/ strong CYP3A4 inhibitors. Co-administration of alternative therapeutic agents w/ less potential for CYP3A4 induction should be selected. Patients w/ rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product. Caution in patients w/ hepatic impairment. Women of childbearing potential must use highly effective contraception during & for up to 2 wk after ending treatment. Should not be used during pregnancy unless clinical condition requires. Women should not breast-feed during treatment & for 2 wk after the last dose.

Rash, pruritus, headache, nausea, fatigue, thrombocytopenia, hyperbilirubinaemia. 150-mg cap: Alopecia, myalgia, upper abdominal pain, neutropenia, anaemia, increased ALT/AST, lipase, blood bilirubin. 200-mg cap: URTI, arthralgia.

Increased exposure w/ CYP3A4 inhibitors (ketoconazole, itraconazole, voriconazole, ritonavir, clarithromycin, & telithromycin; grapefruit juice). Reduced exposure w/ CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, phenobarb & St. John's Wort). Modest decrease in absorption w/ esomeprazole. Increased systemic exposure (AUC & C_max) of oral midazolam; CYP3A4 substrates (eg, certain HMG-CoA reductase inhibitors; CYP3A4 substrates w/ narrow therapeutic index: alfentanil, cyclosporine, dihydroergotamine, ergotamine, fentanyl, sirolimus & tacrolimus). Increased risk of QT interval prolongation w/ anti-arrhythmic medicinal products (eg, amiodarone, disopyramide, procainamide, quinidine & sotalol); chloroquine, halofantrine, clarithromycin, haloperidol, methadone & moxifloxacin. Increased absorption & bioavailability w/ food.

Targeted Cancer Therapy

L01EA03 - nilotinib ; Belongs to the class of BCR-ABL tyrosine kinase inhibitors. Used in the treatment of cancer.

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