Oral Hormone receptor positive, HER2-negative locally advanced carcinoma of breast, Hormone receptor positive, HER2-negative metastatic carcinoma of breast
Adult: In patient with disease progression following endocrine therapy in combination with fulvestrant, [and a gonadotropin releasing hormone agonist if pre- or perimenopausal]: 150 mg bid. As monotherapy in patient with disease progression following endocrine therapy or chemotherapy: 200 mg bid, continue dose until disease progression or unacceptable toxicity. In combination with aromatase inhibitor in postmenopausal women: 150 mg bid, continue dose until disease progression or unacceptable toxicity. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline).
Special Patient Group
Patients taking strong CYP3A4 inhibitors: Reduce dose to 100 mg bid, further reduce to 50 mg bid according to individual safety or tolerability.
Severe (Child-Pugh class C): Reduce dosing frequency to once daily.
Tab: May be taken with or without food. Take at the same time each day. Swallow whole, do not chew/crush/split.
Pregnancy and lactation.
Severe hepatic and renal impairment. Patients taking concomitant strong CYP3A4 inhibitors.
Significant: Bone marrow suppression (e.g. anaemia, leukopenia, thrombocytopenia), diarrhoea, increased in ALT and AST, infections. Blood and lymphatic system disorders: Lymphopaenia. Eye disorders: Increased lacrimation. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, constipation, stomatitis. General disorders and administration site conditions: Fatigue, pyrexia. Metabolism and nutrition disorders: Decreased appetite, dehydration. Musculoskeletal and connective tissue disorders: Arthralgia, muscular weakness. Nervous system disorders: Dysgeusia, headache, dizziness. Respiratory, thoracic and mediastinal disorders: Cough. Skin and subcutaneous tissue disorders: Alopecia, pruritus, rash, dry skin. Potentially Fatal: Interstitial lung disease, pneumonitis, neutropenia, venous thromboembolic events.
Patient Counseling Information
This drug may cause dizziness or fatigue, if affected, do not drive or operate machinery.
Evaluate pregnancy status and hepatitis B virus screening prior to initiation of therapy. Monitor CBC with differential and platelets at baseline, every 2 weeks for the 1st 2 months, monthly for the next 2 months, then as clinically indicated; ALT, AST, and serum bilirubin at baseline, every 2 weeks for the 1st 2 months, monthly for the next 2 months, then as clinically indicated. Monitor for signs and symptoms of diarrhoea, dehydration, interstitial lung disease, pneumonitis, venous thrombosis and pulmonary embolism.
Increased plasma concentrations with strong CYP3A4 inhibitors (e.g. clarithromycin, itraconazole, ketoconazole, lopinavir/ritonavir, posaconazole, voriconazole). Decreased plasma concentrations with the strong CYP3A4 inducer (e.g. carbamazepine, phenytoin, rifampicin).
Decreased plasma concentrations with St. John’s wort. Increased plasma concentrations with grapefruit.
Description: Abemaciclib is a potent and selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK 4 and CDK 6). It blocks retinoblastoma tumour suppressor protein phosphorylation and prevents progression through the cell cycle, resulting in arrest at the G1 phase. Pharmacokinetics: Absorption: Bioavailability: 45% (following 200 mg single oral dose). Time to peak plasma concentration: 8 hours (range: 4.1-24 hours). Distribution: Volume of distribution: Approx 690.3 L. Plasma protein binding: Approx 96%. Metabolism: Metabolised in the liver primarily by CYP3A4 and forms primary metabolite N-desethylabemaciclib (M2); hydroxyabemaciclib (M20), and hydroxy-N-desethylabemaciclib (M18) active metabolites; and oxidative metabolite (M1). Excretion: Via faeces (approx 81%, as metabolites); urine (approx 3%). Elimination half-life: 18.3 hours.
Store below 30°C. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
L01EF03 - abemaciclib ; Belongs to the class of cyclin-dependent kinase (CDK) inhibitors. Used in the treatment of cancer.
Anon. Abemaciclib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/07/2021.Anon. Abemaciclib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/07/2021.Buckingham R (ed). Abemaciclib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/07/2021.Joint Formulary Committee. Abemaciclib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/07/2021.Verzenio Tablet (Eli Lilly and Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/07/2021.Verzenios 50 mg Film-coated Tablets (Eli Lilly Nederland B.V.). MHRA. https://products.mhra.gov.uk. Accessed 06/07/2021.