Thông tin thuốc gốc
Chỉ định và Liều dùng
Metastatic non-small cell lung carcinoma
Adult: Patients with Anaplastic lymphoma kinase (ALK)-positive, previously treated with crizotinib: Initially, 90 mg once daily for 7 days, if tolerated, may increase to 180 mg once daily. Continue until disease progression or unacceptable toxicity occurs. If treatment is interrupted for 14 days or longer for reasons other than adverse effects, resume treatment at 90 mg once daily for 7 days before increasing to the previously tolerated dose. Dose reduction, interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline).
Nhóm bệnh nhân đặc biệt
Patients taking strong CYP3A4 inhibitors: Reduce dose by approx 50%, resume to usual dose upon discontinuation of treatment.
Suy thận
Severe (eGFR <30 mL/min): 60 mg once daily for 7 days, then increased to 90 mg once daily.
Suy gan
Severe (Child-Pugh class C): 60 mg once daily for 7 days, then increased to 120 mg once daily.
Cách dùng
film-coated tab: May be taken with or without food. Swallow whole, do not chew/crush.
Chống chỉ định
Pregnancy and lactation. Concomitant use with moderate and strong CYP3A4 inducers e.g. rifampicin, St. John’s wort, grapefruit or grapefruit juice.
Thận trọng
Concomitant use with strong CYP3A4 inhibitors. Renal and hepatic impairment.
Tác dụng không mong muốn
Significant: Cardiac effects (e.g. hypertension), visual disturbances (e.g. blurred vision, diplopia, reduced visual acuity, macular oedema, cataract), hyperglycaemia; elevations of CPK, pancreatic enzymes (e.g. lipase and amylase), hepatic enzymes (e.g. AST/ALT) and bilirubin.
Blood and lymphatic system disorders: Anaemia.
Cardiac disorders: Palpitations, tachycardia, chest discomfort.
Gastrointestinal disorders: Nausea, diarrhoea, vomiting, constipation, abdominal pain, dry mouth, dyspepsia, stomatitis, flatulence.
General disorders and admin site conditions: Fatigue, oedema, pyrexia, pain.
Infections and infestations: Pneumonia.
Investigations: ECG QT prolonged, weight decreased, increased alkaline phosphatase and blood lactate dehydrogenase, elevated blood creatinine, increased APTT, decreased neutrophil, lymphocyte, platelet, and WBC counts.
Metabolism and nutrition disorders: Decreased appetite, hypokalaemia, hyponatraemia, hypophosphataemia, hypomagnesaemia, hypercalcaemia, hyperinsulinaemia.
Musculoskeletal and connective tissue disorders: Myalgia, arthralgia, pain in extremity.
Nervous system disorders: Headache, dizziness, dysgeusia, peripheral neuropathy, memory impairment.
Psychiatric disorders: Insomnia.
Respiratory, thoracic and mediastinal disorders: Cough, dyspnoea, non-cardiac chest pain, upper respiratory tract infection.
Skin and subcutaneous tissue disorders: Rash, pruritus, dry skin, photosensitivity.
Potentially Fatal: Pulmonary toxicity (e.g. interstitial lung disease or pneumonitis), bradycardia.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, visual disturbances or fatigue, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Establish ALK positivity. Monitor blood pressure and heart rate after 2 weeks and at least monthly thereafter; creatine phosphokinase (CPK) and amylase/lipase levels periodically during treatment; fasting serum glucose at baseline and periodically thereafter. Assess for signs/symptoms of interstitial lung disease (ILD) or pneumonitis, muscular symptoms of CPK elevations, and visual disturbances.
Tương tác
Decreased plasma concentration and efficacy with strong CYP3A4 inducers (e.g. rifampicin, rifabutin, carbamazepine, phenytoin, phenobarbital), and moderate CYP3A4 inducers (e.g. efavirenz, modafinil, bosentan, etravine, nafcillin). Increased plasma concentration with strong CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, voriconazole, indinavir, nelfinavir, ritonavir, clarithromycin, telithromycin, troleandomycin, mibefradil, nefazodone). Increased risk of bradycardia with antihypertensive agents. May reduce plasma levels and efficacy of CYP3A substrates (e.g. alfentanil, fentanyl, quinidine, ciclosporin, tacrolimus, hormonal contraceptives). May increase plasma concentrations of transporter substrates (e.g. digoxin, dabigatran, colchicine, pravastatin, methotrexate, rosuvastatin, sulfasalazine).
Tương tác với thức ăn
Avoid grapefruit or grapefruit juice as it may increase brigatinib plasma concentrations. Avoid St. John’s wort as it may decrease brigatinib plasma concentrations.
Tác dụng
Description: Brigatinib is a multiple tyrosine kinases inhibitor with activity against anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), insulin-like growth factor-1 receptor (IGF-1R), fms-like tyrosine kinase-3 (FLT-3), and epidermal growth factor receptor (EGFR) deletion and point mutations. It inhibits the autophosphorylation of ALK and ALK-mediated phosphorylation of the downstream signalling proteins STAT3, AKT, ERK1/2, and S6 in in vitro and in vivo assays.
Absorption: Time to peak plasma concentration: Approx 1-4 hours.
Distribution: Volume of distribution: 153 L. Plasma protein binding: 91%.
Metabolism: Metabolised in the liver mainly via N-demethylation and cysteine conjugation by CYP2C8 and CYP3A4 isoenzymes to form its primary N-desmethyl brigatinib (AP26123) metabolite.
Excretion: Mainly via faeces (65%; 41% as unchanged drug); urine (25%; 86% as unchanged drug). Elimination half-life: 25 hours.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Brigatinib, CID=68165256, (accessed on Jan. 21, 2020)

Bảo quản
Store between 20-25°C. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
Phân loại MIMS
Liệu pháp nhắm trúng đích
Phân loại ATC
L01ED04 - brigatinib ; Belongs to the class of anaplastic lymphoma kinase (ALK) inhibitors. Used in the treatment of cancer.
Tài liệu tham khảo
Alunbrig Tablet, Coated (Ariad Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. Accessed 09/09/2019.

Anon. Brigatinib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. Accessed 09/09/2019.

Anon. Brigatinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 09/09/2019.

Buckingham R (ed). Brigatinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 09/09/2019.

Joint Formulary Committee. Brigatinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. Accessed 09/09/2019.

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