Apalutamide


Concise Prescribing Info
Indications/Uses
Non-metastatic castration-resistant prostate cancer.
Dosage/Direction for Use
Adult : PO 240 mg once daily. If ≥ Grade 3 toxicity or intolerable side effects occur, withhold treatment until symptoms improve to ≤ Grade 1 or original grade, then resume to normal dosing or reduce to 180 or 120 mg once daily if needed. Continue medical castration with gonadotropin releasing hormone analogue (GnRHa) during the treatment in patients not surgically castrated. Dose reduction or discontinuation of treatment may be required according to individual safety or tolerability (refer to detailed product guideline).
Dosage Details
Oral
Non-metastatic castration-resistant prostate cancer
Adult: 240 mg once daily. If ≥ Grade 3 toxicity or intolerable side effects occur, withhold treatment until symptoms improve to ≤ Grade 1 or original grade, then resume to normal dosing or reduce to 180 or 120 mg once daily if needed. Continue medical castration with gonadotropin-releasing hormone analogue (GnRHa) during the treatment in patients not surgically castrated. Dose reduction or discontinuation of treatment may be required according to individual safety or tolerability (refer to detailed product guideline).
Administration
May be taken with or without food.
Contraindications
Females. Pregnancy and lactation.
Special Precautions
Patient with history of seizures or predisposing factors for seizure; risk of falls or fractures; recent CV disease and QT prolongation. Severe renal and hepatic impairment.
Adverse Reactions
Significant: Falls, fractures, seizures, skin rash, hypothyroidism and elevated TSH, QT prolongation.
General disorders and administration site conditions: Fatigue.
Investigations: Decreased weight.
Metabolism and nutrition disorders: Hypercholesterolaemia, hypertriglyceridaemia.
Musculoskeletal and connective tissue disorders: Arthralgia.
Skin and subcutaneous tissue disorders: Pruritus.
MonitoringParameters
Monitor for signs and symptoms of seizures and dermatologic toxicity. Assess for fall and fracture risk. Monitor thyroid function (e.g. TSH) as necessary.
Drug Interactions
Increased serum concentration with strong CYP2C8 inhibitors (e.g. gemfibrozil) and CYP3A4 inhibitors (e.g. ketoconazole). May decrease serum concentration of P-glycoprotein substrate (P-gp) (e.g. fexofenadine, colchicine, dabigatran, etexilate, digoxin) and breast cancer resistant protein (BCRP)/organic anion transporting polypeptide 1B1 (OATP1B1) (e.g. rosuvastatin, lapatinib, methotrexate, repaglinide). Increased risk of QT prolongation and may induce Torsade de pointes with class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic agents, methadone, moxifloxacin, antipsychotics (e.g. haloperidol).
Action
Description: Apalutamide is a nonsteroidal androgen receptor inhibitor that binds directly to the androgen receptor ligand-binding domain to block androgen receptor nuclear translocation, DNA binding and androgen receptor-mediated transcription resulting to decreased tumour cell proliferation and increased apoptosis, leading to decrease in tumour volume.
Pharmacokinetics:
Absorption: Bioavailability: Approx 100%. Time to peak plasma concentration: 2 hours (range: 1-5 hours).
Distribution: Volume of distribution: Approx 276 L. Plasma protein binding: 96% (apalutamide); 95% (N-desmethyl apalutamide).
Metabolism: Metabolised in the liver by CYP2C8 and CYP3A4 enzymes to form the active metabolite N-desmethyl apalutamide.
Excretion: Via urine (65%; 1.2% as apalutamide, 2.7% as N-desmethyl apalutamide); faeces (24%; 1.5% as apalutamide, 2% as N-desmethyl apalutamide). Elimination half-life: Approx 3 days.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store below 30°C. Protect from light and moisture. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal. Wear gloves during receiving, unpacking, and placing in storage.
ATC Classification
L02BB05 - apalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
Disclaimer: This information is independently developed by MIMS based on Apalutamide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in