Ribociclib for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer

@article{Burris2018RibociclibFT,
  title={Ribociclib for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer},
  author={Howard A. Burris},
  journal={Expert Review of Anticancer Therapy},
  year={2018},
  volume={18},
  pages={201 - 213}
}
  • H. Burris
  • Published 19 February 2018
  • Medicine, Biology
  • Expert Review of Anticancer Therapy
ABSTRACT Introduction: The emergence of cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitors marked a significant advancement in the treatment of advanced breast cancer. Ribociclib is an orally bioavailable, highly selective inhibitor of CDK4/6. In combination with various endocrine therapies, ribociclib has demonstrated clinical activity as a first-line therapy for patients with HR+, HER2− advanced breast cancer, without compromising the favorable toxicity profile associated with endocrine… 

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References

SHOWING 1-10 OF 114 REFERENCES

Pharmacokinetic drug evaluation of ribociclib for the treatment of metastatic, hormone-positive breast cancer

The preclinical and clinical development of ribociclib are reviewed, as well as the role for novel applications of these agents outside the arena of HR-positive, HER2-negative advanced breast cancer are discussed.

Ribociclib as First-Line Therapy for HR-Positive, Advanced Breast Cancer.

Among patients receiving initial systemic treatment for HR-positive, HER2-negative advanced breast cancer, the duration of progression-free survival was significantly longer among those receiving ribociclib plus letrozole than among those received placebo plus let rozole, with a higher rate of myelosuppression in the ribocIClib group.

Abstract CT045: Ribociclib + letrozole for first-line treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer (ABC): efficacy by baseline tumor markers

An improved PFS was observed by the addition of ribociclib to letrozole in all the above patient subgroups, with hazard ratios ranging from 0.40 to 0.64, and hormone receptor positivity remains the only established biomarker of response to CDK4/6 inhibitors.

Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor-Positive Breast Cancer.

It is reported that ER-positive breast cancer cells can adapt quickly to CDK4/6 inhibition and evade cytostasis, in part, via noncanonical cyclin D1-CDK2-mediated S-phase entry, highlighting strategies to prevent the acquisition of therapeutic resistance to these agents.

Abstract P4-22-18: Phase Ib safety, efficacy, and molecular analysis of ribociclib (LEE011) plus letrozole for the treatment of ER+, HER2– advanced breast cancer

The combination of ribociclib plus letrozole demonstrated encouraging clinical activity, particularly in pts treatment-naive for aBC, with an acceptable safety profile that is in line with CDK4/6 inhibition.

MONARCH 3: Abemaciclib As Initial Therapy for Advanced Breast Cancer.

  • M. GoetzM. Toi A. Di Leo
  • Medicine
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology
  • 2017
Abemaciclib plus a nonsteroidal aromatase inhibitor was effective as initial therapy, significantly improving progression-free survival and objective response rate and demonstrating a tolerable safety profile in women with HR-positive, HER2-negative advanced breast cancer.

Targeting the cyclin-dependent kinases (CDK) 4/6 in estrogen receptor-positive breast cancers

Recent preclinical and phase I/II clinical studies using a novel, oral, reversible CDK4/6 inhibitor, palbociclib (PD-0332991), have validated the role of CDK 4/6 as a potential target in estrogen receptor-positive (ER+) breast cancers.

Clinical potential of novel therapeutic targets in breast cancer: CDK4/6, Src, JAK/STAT, PARP, HDAC, and PI3K/AKT/mTOR pathways

The clinical potential and status of new therapeutic targets in breast cancer are discussed and promising targets including cyclin-dependent kinase 4/6, phosphoinositide 3-kinase, poly adenosine diphosphate–ribose polymerase, Src, and histone deacetylase are identified.
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