Apalutamide


Thông tin thuốc gốc
Chỉ định và Liều dùng
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).
Cách dùng
May be taken with or without food.
Chống chỉ định
Females. Pregnancy and lactation.
Thận trọng
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.
Tác dụng không mong muốn
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.
Chỉ số theo dõi
Monitor for signs and symptoms of seizures and dermatologic toxicity. Assess for fall and fracture risk. Monitor thyroid function (e.g. TSH) as necessary.
Tương tác
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).
Tác dụng
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.
Đặc tính

Chemical Structure Image
Apalutamide

Source: National Center for Biotechnology Information. PubChem Database. Apalutamide, CID=24872560, https://pubchem.ncbi.nlm.nih.gov/compound/Apalutamide (accessed on Jan. 20, 2020)

Bảo quản
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.
Phân loại MIMS
Liệu pháp nội tiết trong điều trị ung thư
Phân loại ATC
L02BB05 - apalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
Tài liệu tham khảo
Anon. Apalutamide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/09/2019.

Buckingham R (ed). Apalutamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/09/2019.

Erleada Tablet, Film Coated (Janssen Products, LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/09/2019.

Joint Formulary Committee. Apalutamide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/09/2019.

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