Xtandi

Enzalutamide

In combination w/ androgen deprivation therapy for metastatic hormone-sensitive prostate cancer (mHSPC) in adult men. High-risk non-metastatic castration-resistant prostate cancer (CRPC) in adult men. Metastatic CRPC in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated. Metastatic CRPC in adult men whose disease has progressed on or after docetaxel therapy.

160 mg (4 cap) as a single oral daily dose. Reduce dose to 80 mg once daily if co-administered w/ a strong CYP2C8 inhibitor.

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

Hypersensitivity. Women who are or may become pregnant.

Risk of hypersensitivity reactions; seizure; QT interval prolongation. Reports of severe cutaneous adverse reactions; posterior reversible encephalopathy syndrome; 2nd primary malignancies. Avoid co-administration w/ medicinal products that are sensitive substrates of many metabolising enzymes or transporters; warfarin & coumarin-like anticoagulants; strong CYP2C8 inhibitors. Safety & efficacy of concomitant use w/ cytotoxic chemotherapy has not been established. Possible increase in occurrence of docetaxel-induced neutropenia. Contains sorbitol. Moderate influence on the ability to drive & use machines. 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; severe renal impairment or ESRD. Increased t_½ observed in patients w/ severe hepatic impairment. Use contraception during & for 3 mth after treatment if engaging in sexual activity w/ pregnant woman or woman of childbearing potential. Not for use in women. No relevant use in paed population.

Hot flush, HTN; fractures; asthenia, fatigue; fall. Anxiety; headache, memory impairment, amnesia, disturbance in attention, dysgeusia, restless legs syndrome; ischemic heart disease; dry skin, pruritus; gynaecomastia.

Increased AUC w/ strong CYP2C8 inhibitors (eg, gemfibrozil). Increased risk for liver injury w/ paracetamol. Reduced plasma conc (or increased risk of active metabolite formation) of substrates of CYP3A4, CYP2B6, CYP2C9, CYP2C19, or UGT1A1 eg, 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); immunosuppressants (eg, tacrolimus); PPIs (eg, omeprazole); CYP3A4-metabolised statins (eg, atorvastatin, simvastatin); thyroid agents (eg, levothyroxine). Possible inhibition or induction of MRP2 (in the intestine), OAT3 & OCT1 (systemically). Caution w/ concomitant use of P-gp substrates w/ narrow therapeutic range (eg, colchicine, dabigatran etexilate, digoxin); medicinal products known to prolong the QT interval or those able to induce torsade de pointes eg, class IA (eg, quinidine, disopyramide) or class III (eg, amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmics, methadone, moxifloxacin, antipsychotics.

Cancer Hormone Therapy

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

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