Venetoclax


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Chronic lymphocytic leukaemia, Small lymphocytic lymphoma
Adult: In patient with or without 17p chromosome deletion abnormality or TP53 mutation: As monotherapy: Dose titration schedule: Week 1: Initially, 20 mg once daily; week 2: 50 mg; week 3: 100 mg; week 4: 200 mg; week 5 and thereafter: 400 mg. Continued until disease progression or unacceptable toxicity. In combination with rituximab after 5-week dose titration: 400 mg once daily, continued for 24 months starting cycle 1 day 1 of rituximab. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline).

Oral
Acute myeloid leukaemia
Elderly: ≥75 years In newly-diagnosed patient with comorbidities: Initially, 100 mg on day 1, then 200 mg on day 2, then 400 mg on day 3. Then on day 4 and thereafter, 400 mg combined with azacitidine or decitabine or 600 mg combined with cytarabine. Continue until disease progression or unacceptable toxicity. Do not initiate in patient with WBC >25,000/mm3.
Cách dùng
Should be taken with food. Take approx at the same time each day. Swallow whole, do not chew/crush/break.
Chống chỉ định
Concomitant use with strong CYP3A4 inhibitors at initiation and during dose titration phase. Administration of live vaccines.
Thận trọng
Patient with high tumour burden (e.g. lymph node with diameter ≥5 cm or lymphocyte count of ≥25 x 109/L). Renal and hepatic impairment. Elderly.
Phản ứng phụ
Significant: Anaemia, neutropenia, thrombocytopenia.
Gastrointestinal disorders: Diarrhoea, vomiting, nausea, constipation.
General disorders and administration site conditions: Fatigue, pyrexia.
Hepatobiliary disorders: Increased AST.
Metabolism and nutrition disorders: Hyperkalaemia, hyperphosphataemia, hypocalcaemia, hyperuricaemia, peripheral oedema.
Musculoskeletal and connective tissue disorders: Back pain, musculoskeletal pain, arthralgia.
Nervous system disorders: Headache.
Respiratory, thoracic and mediastinal disorders: Pneumonia, upper respiratory tract infection.
Potentially Fatal: Tumour lysis syndrome (TLS), serious infection including sepsis.
MonitoringParameters
Assess potassium, uric acid, phosphorus, calcium, and creatine level and correct abnormalities prior to initiation of treatment. Monitor TLS at pre-dose, then at 6-8 hours after each titration and 24 hours after reaching final dose. Monitor CBC with differential throughout the therapy. Perform tumour burden assessment including radiographic evaluation (e.g. CT scan) prior to therapy.
Tương tác
Decreased serum concentration and efficacy with moderate to strong CYP3A4 inducers (e.g. carbamazepine, phenytoin, rifampicin).
Potentially Fatal: Increased serum concentration and risk of TLS with strong CYP3A4 inhibitors (e.g. itraconazole, clarithromycin, ritonavir). May diminish therapeutic effect of live vaccines.
Food Interaction
Reduced efficacy with St. John’s wort. Increased plasma concentration with grapefruit products, Seville oranges and/or star fruit.
Tác dụng
Description: Venetoclax selectively inhibits B-cell lymphoma-2 (BCL-2), an anti-apoptic protein, resulting to displacement of pro-apoptotic proteins like BIM, initiation of mitochondrial outer membrane permeabilisation, restoration of the apoptotic process or programmed cell death.
Pharmacokinetics:
Absorption: Increased absorption with food. Time to peak plasma concentration: 5-8 hours.
Distribution: Highly bound to plasma proteins. Volume of distribution: 256-321 L.
Metabolism: Metabolised in the liver by CYP3A4 to major metabolite M27.
Excretion: Via faeces (>99.9%; 20.8% as unchanged drug); urine (<0.1%). Elimination half-life: Approx 26 hours.
Đặc tính

Chemical Structure Image
Venetoclax

Source: National Center for Biotechnology Information. PubChem Database. Venetoclax, CID=49846579, https://pubchem.ncbi.nlm.nih.gov/compound/Venetoclax (accessed on Jan. 23, 2020)

Bảo quản
Store below 30°C.
Phân loại MIMS
Phân loại ATC
L01XX52 - venetoclax ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
References
Anon. Venetoclax. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 13/03/2019.

Anon. Venetoclax. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/03/2019.

Buckingham R (ed). Venetoclax. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/03/2019.

Venclexta (AbbVie Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/03/2019.

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