Verzenio Tablets / Film-coated
Abemaciclib
100 mg
ELI LILLY & COMPANY
| Pack size | 14’s Blister |
|---|---|
| Dispensing mode | POM |
| Source | USA |
| Agent | PHARMATRADE |
| Retail Price | 7050.00 AED |
Available as:
Indications
Verzenio Tablets / Film-coated is used for:
Breast Cancer
Adult Dose
Breast Cancer
Indicated for HR+/HER2- advanced or metastatic breast cancer with disease progression following endocrine therapy as either monotherapy or in combination with fulvestrant
Also, indicated in combination with an aromatase inhibitor as initial endocrine-based therapy for postmenopausal women with HR+/HER2- advanced or metastatic breast cancer
Monotherapy
200 mg PO BID
Continue until disease progression or unacceptable toxicity
Combination therapy
With aromatase inhibitor
Abemaciclib: 150 mg PO BID PLUS
Aromatase inhibitor: See Prescribing Information
Continue until disease progression or unacceptable toxicity
With fulvestrant
Abemaciclib: 150 mg PO BID PLUS
Fulvestrant: 500 mg IM on Days 1, 15, and 29, and then once monthly thereafter
Continue until disease progression or unacceptable toxicity
Hepatic impairment
Mild or moderate (Child-Pugh A or B): No dose adjustment required
Severe (Child-Pugh C): Reduce dosing frequency to once daily
Child Dose
Renal Dose
Renal impairment
Mild or moderate (CrCl 30-89 mL/min): No dose adjustment required
Severe, ESRD, or dialysis: Not studied
Administration
May take with or without food
Instruct patient to take dose at approximately the same time each day
Contra Indications
Precautions
Venous thromboembolism
In clinical trials, venous thromboembolic events (VTE) reported in patients treated with abemaciclib plus an aromatase inhibitor (5%) and in patients treated with abemaciclib plus fulvestrant (5%)
VTE (eg, deep vein thrombosis, pulmonary embolism, cerebral venous sinus thrombosis, pelvic venous thrombosis, subclavian and axillary vein thrombosis, inferior vena cava thrombosis) reported in patients receiving abemaciclib and fulvestrant
Monitor for signs and symptoms of venous thrombosis and pulmonary embolism and appropriately treat
Hepatotoxicity
Increased transaminases were observed in clinical trials
In patients who had grade ≥3 ALT elevation, median time-to-onset was 57 days; whereas, grade <3 was 14 days
In patients who had grade ≥3 AST elevation, median time-to-onset was 185 days; whereas, grade <3 was 13 days
Neutropenia
Neutropenia observed in clinical trials; in patients with grade >3 neutropenia, median time time-to-onset was 29 days and median duration was 15 days
Febrile neutropenia reported in <1% of patients exposed to abemaciclib in the MONARCH studies; 2 deaths due to neutropenic sepsis were observed in MONARCH 2
Diarrhea
Diarrhea occurred in 81% of patients receiving abemaciclib plus an aromatase inhibitor in MONARCH 3, 86% of patients receiving abemaciclib plus fulvestrant in MONARCH 2, and 90% of patients receiving abemaciclib alone in MONARCH 1
Episodes of diarrhea have been associated with dehydration and infection; diarrhea incidence was greatest during the first month of dosing
Pregnancy-Lactation
Pregnancy
There are no available human data informing the drug-associated risk
Based on findings from animal studies and the mechanism of action, can cause fetal harm when administered to a pregnant woman
In animal data, administration of abemaciclib during organogenesis was teratogenic and caused decreased fetal weight at maternal exposures that were similar to human clinical exposure based on AUC at the maximum recommended human dose
Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment
Advise females of reproductive potential to use effective contraception during treatment and for at least 3 weeks after the last dose
Based on findings in animals, abemaciclib may impair fertility in males of reproductive potential
Lactation
Unknown if distributed in human breast milk
Because of the potential for serious adverse reactions in breastfed infants, advise lactating women not to breastfeed while taking abemaciclib and for at least 3 weeks after the last dose
Interactions
Ketoconazole: Avoid coadministration
Other strong CYP3A inhibitors: Decrease recommended starting dose (see Dosage Modifications)
Strong CYP3A inducers: Avoid coadministration
Adverse Effects
Side effects of Abemaciclib :
>10% (Monotherapy)
Creatinine increased (98%)
Diarrhea (90%)
Decreased WBCs (91%)
Decreased neutrophil count (88%)
Anemia (68%)
Fatigue (65%)
Nausea (64%)
Decreased appetite (45%)
Decreased lymphocyte count (42%)
Decreased platelet count (41%)
Abdominal pain (39%)
Neutropenia (37%)
Vomiting (35%)
Infection (31%)
ALT increased (31%)
AST increased (30%)
Decreased WBC, grade 3 (28%)
Anemia (25%)
Decreased neutrophil count, grade 3 (22%)
Thrombocytopenia (20%)
Diarrhea, grade 3 (20%)
Headache (20%)
Cough (19%)
Neutropenia, grade 3 (19%)
Constipation (17%)
Leukopenia (17%)
Arthralgia (15%)
Dry mouth (14%)
Stomatitis (14%)
Weight decreased (14%)
Decreased lymphocyte count, grade 3 (13%)
Dysgeusia (12%)
Alopecia (12%)
Dizziness (11%)
Pyrexia (11%)
>10% (Combination Therapy)
Creatinine increased (98%)
Decreased WBCs (90%)
Decreased neutrophil count (80-87%)
Diarrhea (86%)
Anemia (29-82%)
Decreased lymphocyte count (53-63%)
Decreased platelet count (36-53%)
Neutropenia (46%)
Fatigue (46%)
Nausea (45%)
Infections (43%)
ALT increased (13-41%)
AST increased (12-37%)
Abdominal pain (35%)
Decreased neutrophil count, grade 3 (29%)
Leukopenia (28%)
Decreased appetite (27%)
Vomiting (26%)
Neutropenia, grade 3 (24%)
Decreased WBC, grade 3 (23%)
Headache (20%)
Dysgeusia (18%)
Thrombocytopenia (16%)
Alopecia (16%)
Stomatitis (15%)
Pruritus (13%)
Diarrhea, grade 3 (13%)
Cough (13%)
Dizziness (12%)
Decreased lymphocyte count, grade 3 (7-12%)
Peripheral edema (12%)
Rash (11%)
Pyrexia (11%)
Mechanism of Action
Inhibits cyclin-dependent kinases (CDKs) 4 and 6
These kinases are activated upon binding to D cyclins and play a crucial role in signaling pathways, which lead to cell cycle progression and cellular proliferation
In ER-positive breast cancer cells, cyclin D1 and CDK4/6 promote phosphorylation of the retinoblastoma protein (Rb), cell cycle progression, and cell proliferation
Note
Verzenio 100 mg Tablets / Film-coated manufactured by ELI LILLY & COMPANY. Its generic name is Abemaciclib. Verzenio is availble in United Arab Emirates.
Farmaco UAE drug index information on Verzenio Tablets / Film-coated is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.