Xtandi

Adult men w/ high-risk biochemical recurrent non-metastatic hormone-sensitive prostate cancer who are unsuitable for salvage-RT as monotherapy or in combination w/ androgen deprivation therapy; metastatic hormone-sensitive prostate cancer; high-risk non-metastatic castration-resistant prostate cancer (CRPC); metastatic CRPC 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 w/ sufficient amount of water. Do not chew/dissolve/open. Take at approx the same time every day.

Hypersensitivity. Women who are or may become pregnant.

Hypersensitivity reactions eg, face, tongue, lip & pharyngeal edema, & rash. Permanently discontinue treatment in patients who develop seizure during treatment. Discontinue use if hypersensitivity symptoms occur; in patients who develop posterior reversible encephalopathy syndrome. Recent MI (in past 6 mth) or unstable angina (in past 3 mth), NYHA class III or IV heart failure except if LVEF ≥45%, bradycardia or uncontrolled HTN. Monitor INR in concomitant use w/ anticoagulants metabolised by CYP2C9 eg, warfarin or acenocoumarol. Avoid concomitant use w/ medicinal products that are sensitive substrates of many metabolising enzyme or transporters; warfarin & coumarin-like anticoagulants; strong CYP2C8 inhibitors. Concomitant use w/ cytotoxic chemotherapy eg, IV docetaxel. May affect ability to drive & use machines. 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. 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, cognitive disorder; gynaecomastia, nipple pain, breast tenderness; dry skin, pruritus.

Increased AUC_0-inf w/ gemfibrozil; itraconazole. Decreased AUC_0-inf w/ rifampin. Decreased AUC of midazolam, S-warfarin & omeprazole. Decreased AUC & C_max of 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). Increased AUC & C_max of digoxin. Possible loss of pharmacological effects of CYP2B6, CYP3A4, CYP2C9, CYP2C19 or UGT1A1 substrates. Possible induction of 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.

S