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Abemaciclib: The Newest CDK4/6 Inhibitor for the Treatment of Breast Cancer
Alison Palumbo1, Gary Lau1, Megan Saraceni1
11 Oregon Health and Science University, Portland, OR, USA.
Objective:
To review the pharmacology, efficacy, and safety of the cyclin-dependent kinase (CDK) inhibitor, abemaciclib, in the treatment of advanced or metastatic breast cancer (MBC).
Data Sources:
Relevant information was identified through a MEDLINE/PubMed (January 2000 to June 2018) literature search. The new drug application, prescribing information, and abstracts and posters from scientific meetings were also reviewed.
Study Selection/Data Extraction:
The literature search was limited to human studies published in the English language. Phase 1, 2, and 3 studies evaluating the pharmacology, efficacy, or safety of abemaciclib for breast cancer were included.
Data Synthesis:
Abemaciclib is an oral, potent, small molecule inhibitor of CDK4 and CDK6 activity, which blocks retinoblastoma tumor suppressor protein phosphorylation and thereby prevents progression through the cell cycle. Three major clinical trials, MONARCH 1, 2, and 3, established the efficacy and safety of abemaciclib for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or MBC. In these trials, response rates were promising, ranging from 19.7% to 59%, and median progression-free survival was significantly prolonged over the control arm in 2 of the trials. Common adverse effects included diarrhea, neutropenia, nausea, abdominal pain, infections, and fatigue. Relevance to Patient Care and Clinical Practice: Although no head-to-head studies have been completed between the CDK4/6 inhibitors, abemaciclib may be an attractive option because of its continuous dosing and ability to be used as monotherapy.
Conclusions:
Abemaciclib is an effective and well-tolerated treatment for HR-positive, HER2-negative advanced or metastatic breast cancer.
Insights
Abemaciclib effectively treats advanced or metastatic breast cancer by inhibiting CDK4/6. This cyclin-dependent kinase inhibitor shows promising response rates and prolonged progression-free survival in HR-positive, HER2-negative patients.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Advanced or metastatic breast cancer (MBC) remains a significant clinical challenge.
- Hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) subtypes constitute a large proportion of MBC cases.
- Targeted therapies are crucial for improving outcomes in MBC patients.
Purpose of the Study:
- To review the pharmacology, efficacy, and safety of abemaciclib, a cyclin-dependent kinase (CDK) inhibitor.
- To evaluate abemaciclib's role in treating advanced or metastatic breast cancer (MBC).
Main Methods:
- Literature search of MEDLINE/PubMed (January 2000 to June 2018).
- Inclusion of Phase 1, 2, and 3 human studies published in English.
- Review of new drug applications, prescribing information, and scientific meeting abstracts/posters.
Main Results:
- Abemaciclib is an oral inhibitor of CDK4 and CDK6, blocking cell cycle progression.
- MONARCH 1, 2, and 3 trials demonstrated efficacy in HR+, HER2- MBC with response rates from 19.7% to 59%.
- Common adverse effects include diarrhea, neutropenia, nausea, and fatigue; generally well-tolerated.
Conclusions:
- Abemaciclib is an effective treatment option for HR+, HER2- advanced or metastatic breast cancer.
- Continuous dosing and monotherapy potential make abemaciclib an attractive therapeutic choice.
- Abemaciclib offers a well-tolerated treatment for patients with advanced or metastatic breast cancer.
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