Abemaciclib

Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins.

• VERZENIO ® is a kinase inhibitor indicated: in combination with endocrine therapy (tamoxifen or an aromatase inhibitor) for the adjuvant treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, node-positive, early breast cancer at high risk of recurrence. ( 1.1 , 14.1 ) in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.ICD-10: C50.919

• None. None.contraindicated

VERZENIO tablets are taken orally with or without food. ( 2.1 ) Recommended starting dose in combination with fulvestrant, tamoxifen, or an aromatase inhibitor: 150 mg twice daily. ( 2.1 ) Recommended starting dose as monotherapy: 200 mg twice daily. ( 2.1 ) Dosing interruption and/or dose reductions may be required based on individual safety and tolerability. ( 2.2 ) 2.1 Recommended Dose and Schedule When used in combination with fulvestrant, tamoxifen, or an aromatase inhibitor, the recommended dose of VERZENIO is 150 mg taken orally twice daily. Refer to the Full Prescribing Information for the recommended dose of the fulvestrant, tamoxifen, or aromatase inhibitor being used. Pre/perimenopausal women and men treated with the combination of VERZENIO plus an aromatase inhibitor should be treated with a gonadotropin-releasing hormone agonist (GnRH) according to current clinical practice standards. Pre/perimenopausal women treated with the combination of VERZENIO plus fulvestrant should be treated with a GnRH according to current clinical practice standards When used as monotherapy, the recommended dose of VERZENIO is 200 mg taken orally twice daily. For early breast cancer, continue VERZENIO until completion of 2 years of treatment or until disease recurrence, or unacceptable toxicity. For advanced or metastatic breast cancer, continue treatment until disease progression or unacceptable toxicity. VERZENIO may be taken with or without food [see Clinical Pharmacology ( 12.3 )] . Instruct patients to take their doses of VERZENIO at approximately the same times every day.

Diarrhea: VERZENIO can cause severe cases of diarrhea, associated with dehydration and infection. Instruct patients at the first sign of loose stools to initiate antidiarrheal therapy, increase oral fluids, and notify their healthcare provider. ( 2.2 , 5.1 ) Neutropenia: Monitor complete blood counts prior to the start of VERZENIO therapy, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated. ( 2.2 , 5.2 ) Interstitial Lung Disease (ILD)/Pneumonitis: Severe and fatal cases of ILD/pneumonitis have been reported. Monitor for clinical symptoms or radiological changes indicative of ILD/pneumonitis. Permanently discontinue VERZENIO in all patients with Grade 3 or 4 ILD or pneumonitis. ( 2.2 , 5.3 ) Hepatotoxicity: Increases in serum transaminase levels have been observed. Perform liver function tests (LFTs) before initiating treatment with VERZENIO. Monitor LFTs every two weeks for the first two months, monthly for the next 2 months, and as clinically indicated. ( 2.2 , 5.4 ) Venous Thromboembolism: Monitor patients for signs and symptoms of thrombosis and pulmonary embolism and treat as medically appropriate. ( 2.2 , 5.5 ) Embryo-Fetal Toxicity: Can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception. ( 5.6 , 8.1 , 8.3 ) 5.1 Diarrhea Severe diarrhea associated with dehydration and infection occurred in patients treated with VERZENIO. Across four clinical trials in 3691 patients, diarrhea occurred in 81% to 90% of patients who received VERZENIO.

The following adverse reactions are discussed in greater detail in other sections of the labeling: Diarrhea [see Warnings and Precautions ( 5.1 )] . Neutropenia [see Warnings and Precautions ( 5.2 )] . Interstitial Lung Disease (ILD) or Pneumonitis [see Warnings and Precautions ( 5.3 )] . Hepatotoxicity [see Warnings and Precautions ( 5.4 )] . Venous Thromboembolism [see Warnings and Precautions ( 5.5 )] . Most common adverse reactions (incidence ≥20%) were diarrhea, neutropenia, nausea, abdominal pain, infections, fatigue, anemia, leukopenia, decreased appetite, vomiting, headache, alopecia, and thrombocytopenia. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Eli Lilly and Company at 1-800-LillyRx (1-800-545-5979) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety population described in the Warnings and Precautions reflect exposure to VERZENIO in 3691 patients from four clinical trials: monarchE, MONARCH 1, MONARCH 2, and MONARCH 3. The safety population includes exposure to VERZENIO as a single agent at 200 mg twice daily in 132 patients in MONARCH 1 and to VERZENIO at 150 mg twice daily in 3559 patients administered in combination with fulvestrant, tamoxifen, or an aromatase inhibitor in monarchE, MONARCH 2, and MONARCH 3.

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, VERZENIO can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data informing the drug-associated risk. Advise pregnant women of the potential risk to a fetus. In animal reproduction studies, 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 ( see Data). Advise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4% and of miscarriage is 15 to 20% of clinically recognized pregnancies. Data Animal Data In an embryo-fetal development study, pregnant rats received oral doses of abemaciclib up to 15 mg/kg/day during the period of organogenesis. Doses ≥4 mg/kg/day caused decreased fetal body weights and increased incidence of cardiovascular and skeletal malformations and variations.

Metabolism

The pharmacokinetics of abemaciclib were characterized in patients with solid tumors, including breast cancer, and in healthy subjects. Following single and repeated twice daily dosing of 50 mg (0.3 times the approved recommended 150 mg dosage) to 200 mg of abemaciclib, the increase in plasma exposure (AUC) and C max was approximately dose proportional.

• Sep 28, 2017NDANDA208716Eli Lilly And Co

1. 1Diarrhoea5,68030%
2. 2Fatigue2,31112%
3. 3Nausea1,96711%
4. 4Vomiting1,0555.6%
5. 5Malignant Neoplasm Progression1,0405.6%
6. 6Decreased Appetite8754.7%
7. 7Asthenia7834.2%
8. 8Death7534.0%
9. 9Drug Ineffective7143.8%
10. 10White Blood Cell Count Decreased6553.5%
11. 11Anaemia6513.5%
12. 12Constipation6353.4%
13. 13Abdominal Pain Upper6113.3%
14. 14Neutropenia5963.2%
15. 15Alopecia5422.9%

The 10 most recently updated of 284 ClinicalTrials.gov registrations naming Abemaciclib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• LY3214996 and Cetuximab Alone or in Combination With Abemaciclib for the Treatment of Unresectable or Metastatic Colorectal Cancer
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 46 enrolled · M.D. Anderson Cancer Center
  NCT04616183updated 2026-06-12
• Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 435 enrolled · Stemline Therapeutics, Inc.
  NCT05563220updated 2026-06-12
• Testing the Safety and Efficacy of the Combination of Two Anti-cancer Drugs, ZEN003694 and Abemaciclib, for Adult and Pediatric Patients (12-17 Years) With Metastatic or Unresectable NUT Carcinoma, Breast Cancer and Other Solid Tumors
  Recruiting · Phase 1 · Interventional · 45 enrolled · National Cancer Institute (NCI)
  NCT05372640updated 2026-06-11
• A Phase 1 Study of Neoadjuvant Abemaciclib in Combination With Radiation Therapy for Liposarcomas
  Recruiting · Phase 1 · Interventional · 18 enrolled · University of Washington
  NCT06025747updated 2026-06-11
• A Study of Elacestrant Alone or in Combination With Abemaciclib in People With Endometrial Cancer
  Recruiting · Phase 2 · Interventional · 75 enrolled · Memorial Sloan Kettering Cancer Center
  NCT07209449updated 2026-06-10
• A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer
  Recruiting · Phase 1 · Phase 2 · Interventional · 316 enrolled · Hoffmann-La Roche
  NCT04802759updated 2026-06-09
• A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors
  Active not recruiting · Phase 2 · Interventional · 176 enrolled · Hoffmann-La Roche
  NCT04931342updated 2026-06-08
• Study of Abemaciclib in Dedifferentiated Liposarcoma
  Active not recruiting · Phase 2 · Interventional · 33 enrolled · Memorial Sloan Kettering Cancer Center
  NCT02846987updated 2026-06-08
• Cyclin-Dependent Kinase (CDK)4/6 Inhibitor Abemaciclib for Neurofibromatosis Type I (NF1) Related Atypical Neurofibromas
  Recruiting · Phase 1 · Phase 2 · Interventional · 55 enrolled · National Cancer Institute (NCI)
  NCT04750928updated 2026-06-05
• ONO-4578-06:Phase I Study of ONO-4578 and Letrozole Plus CDK4 /6 Inhibitors in Breast Cancer
  Completed · Phase 1 · Interventional · 46 enrolled · Ono Pharmaceutical Co., Ltd.
  NCT06570031updated 2026-06-05

Frequently asked questions

How does Abemaciclib work?

Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins.

What is Abemaciclib used for?

According to FDA labeling, Abemaciclib carries indications including: VERZENIO ® is a kinase inhibitor indicated: in combination with endocrine therapy (tamoxifen or an aromatase inhibitor) for the adjuvant treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, node-positive, early breast cancer at high risk of recurrence. ( 1.1 , 14.1 ) in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Abemaciclib?

Abemaciclib is classified as Cyclin-dependent kinase (CDK) inhibitors, Kinase Inhibitor, Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Abemaciclib?

Abemaciclib is marketed under brand names including Verzenio.

What are the contraindications for Abemaciclib?

Abemaciclib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.