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Verzenio (abemaciclib)
Abemaciclib inhibits CDK4 and CDK6, blocking Rb phosphorylation and G1/S cell cycle progression.
Abemaciclib is a CDK4/6 inhibitor indicated for HR+/HER2- breast cancer in combination with endocrine therapy or as monotherapy. It demonstrates strong protein binding (>93%) and hepatic metabolism via CYP3A4 with an 18.3-hour half-life, requiring dose adjustments with CYP3A inhibitors. The drug carries significant drug interaction risks, particularly with ketoconazole and other CYP3A inhibitors, necessitating careful monitoring and dose management. Clinical efficacy is established across early, advanced, and metastatic HR+/HER2- breast cancer settings.
At a glance
| Generic name | abemaciclib |
|---|---|
| Sponsor | Eli Lilly |
| Drug class | Kinase inhibitor |
| Target | Cyclin-dependent kinases 4 and 6 (CDK4/CDK6) |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2017 |
| Annual revenue | 3700 |
Mechanism of action
Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6), which 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.
Approved indications
- Hormone receptor positive malignant neoplasm of breast
- Human epidermal growth factor 2 negative carcinoma of breast
Common side effects
- Nausea
- Diarrhoea
- Fatigue
- Asthenia
- Alopecia
- Vomiting
- Decreased appetite
- Constipation
- Abdominal pain
- Neutrophil count decreased
- Headache
- Neutropenia
Drug interactions
- Ketoconazole
- Other strong CYP3A inhibitors
- Moderate CYP3A inhibitors
- Strong and moderate CYP3A inducers
- Grapefruit products
Key clinical trials
- A Study of Abemaciclib (LY2835219) In Participants With Previously Treated Breast Cancer That Has Spread (PHASE2)
- A Study of Abemaciclib (LY2835219) Combined With Fulvestrant in Women With Hormone Receptor Positive HER2 Negative Breast Cancer (PHASE3)
- Endocrine Therapy With or Without Abemaciclib (LY2835219) Following Surgery in Participants With Breast Cancer (PHASE3)
- 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 (PHASE1)
- Testing the Addition of an Anti-cancer Drug, Abemaciclib, to the Usual Chemotherapy Treatment (Gemcitabine) for Soft Tissue Sarcoma (PHASE1,PHASE2)
- Testing the Addition of an Anti-Cancer Drug, Abemaciclib, to the Usual Chemotherapy Treatment (5-Fluorouracil) for Metastatic, Refractory Colorectal Cancer (PHASE1)
- A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors (PHASE1)
- A Master Protocol (LY900023) That Includes Several Clinical Trials of Drugs for Children and Young Adults With Cancer (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
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- Eli Lilly portfolio CI