Xtandi

Enzalutamide

Adult men w/ metastatic hormone-sensitive prostate cancer; high-risk non-metastatic castration-resistant prostate cancer; metastatic castration-resistant prostate cancer who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated & whose disease has progressed on or after docetaxel therapy.

160 mg (four 40-mg cap) as single daily dose. Patient w/ ≥Grade 3 toxicity or intolerable adverse reaction Withhold dosing for 1 wk or until symptoms improve to ≤Grade 2, then resume at the same or reduced dose (120 mg or 80 mg) if warranted. Concomitant use w/ strong CYP2C8 inhibitors Reduce dose to 80 mg once daily.

May be taken with or without food: Swallow whole, do not chew/dissolve/open. Take at approx the same time every day.

Hypersensitivity. Pregnancy.

Permanently discontinue in patients who develop seizure during treatment. Discontinue use if hypersensitivity symptoms occur; in patients who develop posterior reversible encephalopathy syndrome. Monitor INR in concomitant use w/ CYP2C9 metabolised anticoagulants eg, warfarin or acenocoumarol. Recent MI (in past 6 mth) or unstable angina (in past 3 mth), NYHA III or IV heart failure except if LVEF ≥45%, bradycardia or uncontrolled HTN. Not to be taken by patients w/ rare hereditary problems of fructose intolerance. Avoid concomitant use w/ medicinal products that are sensitive substrates of many metabolising enzyme or transporters; warfarin & coumarin-like anticoagulants. Concomitant use w/ cytotoxic chemotherapy eg, IV docetaxel. May affect ability to drive or operate machinery. Severe renal impairment or ESRD. Males should wear condom during & for 3 mth after treatment if engaging in sexual activity w/ pregnant or childbearing potential woman. Not for use in females. Lactation. Not indicated in ped.

Asthenia, fatigue; hot flush, HTN; fracture; fall. Ischemic heart disease; anxiety; headache, memory impairment, amnesia, attention disturbance, dysgeusia, restless legs syndrome; gynaecomastia; dry skin, pruritus.

Increased AUC_0-inf w/ gemfibrozil, itraconazole. Decreased AUC_0-inf w/ rifampin. Decrease AUC of midazolam, S-warfarin, omeprazole & docetaxel. Concomitant use w/ analgesics (eg, fentanyl, tramadol), antibiotics (eg, clarithromycin, doxycycline), anticancer agents (eg, cabazitaxel), antiepileptics (eg, carbamazepine, clonazepam, phenytoin, primidone, valproic acid), antipsychotics (eg, haloperidol), antithrombotics (eg, acenocoumarol, warfarin, clopidogrel), β-blockers (eg, bisoprolol, propranolol), Ca channel blockers (eg, diltiazem, felodipine, nicardipine, nifedipine, verapamil), cardiac glycosides (eg, digoxin), corticosteroids (eg, dexamethasone, prednisolone), HIV antivirals (eg, indinavir, ritonavir), hypnotics (eg, diazepam, midazolam, zolpidem), immunosuppressives (eg, tacrolimus), PPIs (eg, omeprazole), statins metabolized by CYP3A4 (eg, atorvastatin, simvastatin), thyroid agents (eg, levothyroxine); medicinal products w/ narrow therapeutic range that are P-gp substrates (eg, colchicine, dabigatran etexilate, digoxin). Possible loss of pharmacological effects of CYP2B6, CYP3A4, CYP2C9, CYP2C19 or UGT1A1 substrates. Possible induction of BCRP, MRP2, organic anion transporter 3 & organic cation transporter 1.

Cancer Hormone Therapy

L02BB04 - enzalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.

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