CDK4/6 Inhibition as a therapeutic strategy in breast cancer: palbociclib, ribociclib, and abemaciclib
Abstract
With 40,920 American women expected to die from breast cancer in 2018 and global health estimates that more than 508,000 women died in 2011 from this disease, the identification of novel therapeutic strategies for the treatment of breast cancer cannot be ignored. A breakthrough class of cancer drugs that has emerged in recent years and has had an impact in the treatment of breast cancer are the cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors, with palbociclib the first in class to have received regulatory approval for breast cancer. In this article we will compare and contrast three CDK4/6 inhibitors - palbociclib, ribociclib and abemaciclib - that have received regulatory approval for the treatment of metastatic breast cancer. Ribociclib and abemaciclib developed after the success of palbociclib represent examples of "me-too" therapies increasingly being deployed in oncology.
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The dual CDK4/6 inhibitors palbociclib, ribociclib, and abemaciclib are FDA-approved for treating patients with advanced or metastatic breast cancer and lead to prolonged progression-free survival.
“As such, CDK4/6 are attractive targets for cancer therapy, and the dual CDK4/6 inhibitors palbociclib, ribociclib, and abemaciclib have been FDA approved for treating patients with advanced or metastatic breast cancer, leading to prolonged progression-free-survival[2].”
From Development of dual and selective degraders of cyclin-dependent kinases 4 and 6 (2019) · cites this paper as [2]
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Computational insights into Croton species as sources of CDK4/6 inhibitors for cancer therapy
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BindingDB Entry 50017954: PROTACs to address the challenges facing small molecule inhibitors.
BindingDB (2023) · UC San Diego · doi:10.7270/q2p55sm1
BindingDB Entry 50007709: Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.
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BindingDB (2025) · UC San Diego · doi:10.7270/q2pr81q8
BindingDB (2021) · UC San Diego · doi:10.7270/q2c53qdz
BindingDB Entry 50007904: Synthetic Approaches to the New Drugs Approved During 2017.
BindingDB (2021) · UC San Diego · doi:10.7270/q2sx6hk5
BindingDB (2021) · UC San Diego · doi:10.7270/q23f4t3t
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- Authors
- Laderian, B., & Fojo, T.
- Affiliations
- Columbia University Irving Medical Center (US)
- Corresponding author
- Fojo, Tito
- Venue
- Seminars in Oncology
- Publisher
- Elsevier BV
- Published
- 2017-12
- Volume
- 44
- Issue
- 6
- Pages
- 395-403
- ISSN
- 0093-7754 (ISSN-L)
- OpenAlex
- W2793671087
- Cited by
- 77
- References
- 17
- Citations by year
- 2026: 8 · 2025: 6 · 2024: 5 · 2023: 12 · 2022: 11 · 2021: 10 · 2020: 14 · 2019: 9 · 2018: 2
- FWCI
- 5.65
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Seminars in Oncology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Advanced Breast Cancer Therapies
- Health Sciences › Medicine › Oncology › PARP inhibition in cancer therapy
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
- Keywords
- CDK4/6 inhibitors, breast cancer, palbociclib, ribociclib, abemaciclib, metastatic breast cancer, me-too drugs, targeted cancer therapy
- MeSH terms
- Aminopyridines, Benzimidazoles, Breast Neoplasms, Humans, Piperazines, Purines, Pyridines, Protein Kinase Inhibitors, Cyclin-Dependent Kinase 4, Cyclin-Dependent Kinase 6, Molecular Targeted Therapy
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