Τετάρτη 9 Δεκεμβρίου 2020

Preclinical discovery and development of abemaciclib used to treat breast cancer.

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Preclinical discovery and development of abemaciclib used to treat breast cancer.

Expert Opin Drug Discov. 2020 Dec 07;:

Authors: Wright MD, Abraham MJ

Abstract
Introduction Cyclin-dependent kinase (CDK) 4/6 inhibitors have altered the standard-of-care treatment for patients with ER-positive, HER2-negative metastatic breast cancer. One such inhibitor, abemaciclib, a reversible ATP-competitive CDK4/6 inhibitor developed by Eli Lilly and Company, was approved by the FDA for ER-positive, HER2-negative metastatic breast cancer. Areas Covered: Preclinical studies revealed abemaciclib's distinct structure, efficacy as monotherapy, and ability to penetrate the Central Nervous System. In this review, the authors have examined the literature regarding the development of CDK 4/6 inhibitors before providing a focused review on the preclinical discovery and development of abemaciclib. The authors then conclude their manuscript by providing their expert opinion and future perspectives. Expert opinion Understanding the genesis and evolution from concept to approval and beyond will allow one to analyze the impact of abemaciclib. With its unique cha racteristics, abemaciclib has provided a meaningful addition to the therapeutic arsenal for metastatic breast cancer. There is, however, a need for predictive biomarkers to identify patients who may not benefit from or may develop resistance to CDK4/6 inhibition.

PMID: 33280445 [PubMed - as supplied by publisher]

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