Enzacord-40

Adult men w/ metastatic hormone-sensitive prostate cancer (mHSPC); 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 not surgically castrated Continue medical castration w/ LH-releasing hormone analogue. 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 inhibitor Reduce dose to 80 mg once daily.

May be taken with or without food: Swallow whole w/ water. Do not chew/dissolve/open.

Hypersensitivity. Pregnancy.

Hypersensitivity reactions eg, rash, or face, tongue, lip, or pharyngeal oedema; severe cutaneous adverse reactions. Discontinue treatment in patients who develop posterior reversible encephalopathy syndrome. Risk of seizure. 2nd primary malignancies eg, bladder cancer, adenocarcinoma of colon, transitional cell carcinoma & bladder transitional cell carcinoma. Promptly seek medical attention if signs of GI bleeding, macroscopic haematuria, dysuria or urinary urgency develop during treatment. Patients w/ recent MI (in the past 6 mth) or unstable angina (in the past 3 mth), NYHA class III or IV heart failure except if left ventricular ejection fraction ≥45%, bradycardia or uncontrolled HTN. Assess benefit risk ratio including potential for Torsade de pointes prior to initiating treatment in patients w/ history of, or risk factors for QT prolongation & those receiving concomitant medicinal products that might prolong QT interval. Closely monitor for skin reactions. Conduct additional INR monitoring if co-administered w/ anticoagulant metabolised by CYP2C9 (eg, warfarin or acenocoumarol). Avoid concomitant use w/ medicinal products that are sensitive substrates of many metabolising enzymes or transporters if therapeutic effect is of large importance & if dose adjustments cannot easily be performed based on monitoring of efficacy or plasma conc; warfarin & coumarin-like anticoagulants. Concomitant use w/ cytotoxic chemotherapy. Not to be used in patients w/ rare hereditary problems of fructose intolerance. May have moderate influence on ability to drive & use machines. Severe renal impairment or ESRD. Increased t_½ in patients w/ severe hepatic impairment. Male patients must use condom during & for 3 mth after treatment if engaging in sexual activity w/ pregnant woman; & another form of birth control if patient engages in sexual intercourse w/ woman of childbearing potential. Not for use in women. Not indicated in ped.

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

Increased AUC & decreased C_max w/ strong CYP2C8 inhibitors eg, gemfibrozil. Decreased AUC of midazolam (CYP3A4 substrate), S-warfarin (CYP2C9 substrate), & omeprazole (CYP2C19 substrate). Decreased AUC & C_max of docetaxel. Possible loss pharmacological effects of CYP3A4, CYP2B6, CYP2C9, CYP2C19 or UGT1A1 substrates. Higher risk of liver injury w/ paracetamol. 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), immunosuppressants (eg, tacrolimus), PPIs (eg, omeprazole), CYP3A4-metabolised statins (eg, atorvastatin, simvastatin), thyroid agents (eg, levothyroxine); P-gp substrates w/ narrow therapeutic range (eg, colchicine, dabigatran etexilate, digoxin); medicinal products known to prolong 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. Possible induction of BCRP & MRP2 (in the intestine), organic anion transporter 3 & organic cation transporter 1 (systemically).

Cancer Hormone Therapy

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

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