expect [3:<30 mL/min, C-G), end stage renal disease, or in patients on dialysis is unknown. 1 Hepatic Impairment No dosage adjustments are necessary in patients with mild or moderate hepatic impairment (Child-Pugh A or B). 1 Reduce the dosing frequency when administering abemaciclib to patients with severe hepatic impairment (Child-Pugh C). 1 Common Adverse Effects Most common adverse reactions (incidence 20%) were diarrhea, neutropenia, nausea, abdominal pain, infections, fatigue, anemia, leukopenia, decreased appetite, vomiting, headache, and thrombocytopenia. 1 Drug Interactions Specific Drugs It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights: CYP3A Inhibitors: Avoid concomitant use of ketoconazole. Reduce the abemaciclib dose with concomitant use of other strong CYP3A inhibitors. 1 CYP3A Inducers: Avoid concomitant use of strong CYP3A inducers. 1 Actions Mechanism of Action Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins. In estrogen receptor-positive (ER+) breast cancer cell lines, cyclin D1 and CDK4/6 promote phosphorylation of the retinoblastoma protein (Rb), cell cycle progression, and cell proliferation. In vitro, continuous exposure to abemaciclib inhibited Rb phosphorylation and blocked progression from G1 into S phase of the cell cycle, resulting in senescence and apoptosis. In breast cancer xenograft models, abemaciclib dosed daily without interruption as a single agent or in combination with antiestrogens resulted in reduction of tumor size. 1 Advice to Patients Advise patients to read the FDA-approved Patient Information. 1 Diarrhea Abemaciclib may cause diarrhea, which may be severe in some cases. 1 Early identification and intervention is critical for the optimal management of diarrhea. Instruct patients that at the first sign of loose stools, they should start antidiarrheal therapy (for example, loperamide) and notify their healthcare provider for further instructions and appropriate follow up. 1 Encourage patients to increase oral fluids. 1 If diarrhea does not resolve with antidiarrheal therapy within 24 hours to Grade 1, suspend abemaciclib dosing. 1 Neutropenia Advise patients of the possibility of developing neutropenia and to immediately contact their healthcare provider should they develop a fever, particularly in association with any signs of infection. 1 Hepatotoxicity Inform patients of the signs and symptoms of hepatotoxicity. Advise patients to contact their healthcare provider immediately for signs or symptoms of hepatotoxicity. 1 Venous Thromboembolism Advise patients to immediately report any signs or symptoms of thromboembolism such as pain or swelling in an extremity, shortness of breath, chest pain, tachypnea, and tachycardia. 1 Embryo-Fetal Toxicity Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception during abemaciclib therapy and for at least 3 weeks after the last dose. Advise patients to inform their healthcare provider of a known or suspected pregnancy. 1 Lactation Advise lactating women not to breastfeed during abemaciclib treatment and for at least 3 weeks after the last dose. 1 Drug Interactions Inform patients to avoid concomitant use of ketoconazole. Dose reduction may be required for other strong CYP3A inhibitors. 1 Grapefruit may interact with abemaciclib. Advise patients not to consume grapefruit products while on treatment with abemaciclib. 1 Advise patients to avoid concomitant use of CYP3A inducers and to consider alternative agents. 1 Advise patients to inform their healthcare providers of all concomitant medications, including prescription medicines, over-the-counter drugs, vitamins, and herbal products. 1 Dosing Instruct patients to take the doses of abemaciclib at approximately the same times every day and to swallow whole (do not chew, crush, or split them prior to swallowing). 1 If patient vomits or misses a dose, advise the patient to take the next prescribed dose at the usual time. 1 Advise the patient that abemaciclib may be taken with or without food. 1 Additional Information AHFS First Release . For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity. Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Abemaciclib Routes Dosage Forms Strengths Brand Names Manufacturer Oral Tablet 50 mg Verzenio Eli Lilly and Company 100 mg Verzenio Eli Lilly and Company 150 mg Verzenio Eli Lilly and Company 200 mg Verzenio Eli Lilly and Company AHFS Drug Information. Copyright 2017, Selected Revisions October 16, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. Eli Lilly and Company. Verzenio (abemaciclib) ORAL prescribing information. 2017 Sep. Next Interactions Print this page Add to My Med List More about abemaciclib Drug Interactions Support Group 0 Reviews Add your own review/rating Drug class: CDK 4/6 inhibitors Consumer resources Abemaciclib Professional resources Other brands: Verzenio Related treatment guides Breast Cancer> ] FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only Approval History Drug history at FDA Drug Class CDK 4 / 6 inhibitors Related Drugs Breast Cancer methotrexate , anastrozole , tamoxifen , letrozole , Arimidex , Femara , exemestane , fluorouracil , Xeloda , Taxol , capecitabine , Aromasin , Ibrance , Herceptin , Faslodex , Taxotere , cyclophosphamide , paclitaxel , gemcitabine , Gemzar , Abraxane , Cytoxan , docetaxel , Afinitor , Adriamycin , More... 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