Xtandi

Enzalutamide

Adult men w/ metastatic hormone-sensitive prostate cancer (mHSPC); w/ non-metastatic castration-resistant prostate cancer (CRPC); w/ 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 a single oral daily dose.

May be taken with or without food: Swallow whole, do not dissolve/chew/open.

Hypersensitivity. Women who are or may become pregnant.

Permanently discontinue in patients who develop seizure during therapy. Discontinue in patients who develop posterior reversible encephalopathy syndrome (PRES). Avoid concomitant use of drugs that are sensitive substrates of many metabolising enzymes or transporters; warfarin & coumarin-like anticoagulants; cytotoxic chemotherapy. Patients w/ recent MI (in the past 6 mth) or unstable angina (in the past 3 mth), NYHA III or IV heart failure except if left ventricular ejection fraction ≥45%, bradycardia or uncontrolled HTN. Hypersensitivity reactions. Severe renal impairment or ESRD. Severe hepatic impairment. May impair ability to drive or operate machinery. Not for use in women & childn.

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

Increased AUC & decreased C_max w/ strong CYP2C8 inhibitor eg, gemfibrozil. May decrease AUC of midazolam, S-warfarin & omeprazole. Risk of liver injury w/ paracetamol. 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), immunosuppressant (eg, tacrolimus), PPI (eg, omeprazole), statins metabolized by CYP3A4 (eg, atorvastatin, simvastatin), thyroid agents (eg, levothyroxine). Mild inhibitory effect on P-gp w/ digoxin. Increased AUC & C_max of digoxin. Caution in concomitant w/ drugs w/ narrow therapeutic range that are substrates for P-gp (eg, colchicine, dabigatran etexilate, digoxin). May inhibit BCRP & MRP2, organic anion transporter 3 (OAT3) & organic cation transporter (OCT1). Decreased AUC & increased C_max of rosuvastatin.

Cancer Hormone Therapy

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

Rx