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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Clinical Development of the CDK4/6 Inhibitors Ribociclib and Abemaciclib in Breast Cancer

Romualdo Barroso-Sousa1, Geoffrey I Shapiro2, Sara M Tolaney3

  • 1Breast Oncology Program, Department of Medical Oncology, Dana-Farber Cancer Institute and Harvard Medical School, Boston, MA, USA, MA, USA.

Breast Care (Basel, Switzerland)
|August 6, 2016
PubMed

Insights

Cyclin-dependent kinase (CDK) 4/6 inhibitors show promise for breast cancer treatment. This review focuses on abemaciclib and ribociclib, comparing their clinical data, CNS penetration, and side effects to palbociclib.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Cyclin-dependent kinases (CDKs) 4 and 6 are crucial for cell cycle progression.
  • CDK4/6 inhibitors have emerged as a significant therapeutic strategy for breast cancer.
  • Palbociclib, a CDK4/6 inhibitor, is approved for hormone receptor-positive advanced breast cancer when combined with endocrine therapy.

Purpose of the Study:

  • To review and compare the clinical data of abemaciclib and ribociclib, two emerging CDK4/6 inhibitors.
  • To highlight key differences between abemaciclib, ribociclib, and palbociclib.
  • To discuss ongoing clinical trials and future directions for CDK4/6 inhibitors in breast cancer treatment.

Main Methods:

  • Review of clinical trial data for abemaciclib and ribociclib.
  • Comparative analysis of efficacy, safety, and pharmacokinetic profiles.
  • Examination of central nervous system penetration and adverse events.

Main Results:

  • Abemaciclib and ribociclib are in late-stage clinical development for breast cancer.
  • These agents show distinct profiles in terms of single-agent activity, CNS penetration, and adverse event profiles compared to palbociclib.
  • Ongoing trials are evaluating their efficacy in various breast cancer settings.

Conclusions:

  • Abemaciclib and ribociclib represent important advancements in CDK4/6 inhibition for breast cancer.
  • Understanding their unique characteristics is crucial for optimizing patient selection and treatment strategies.
  • Further research will define their role in combination therapies and potential for overcoming resistance.
Keywords:
AbemaciclibBreast cancerCyclin-dependent kinasePalbociclibRibociclib

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