Synthesis and Clinical Development of Palbociclib: An overview

(E-pub Ahead of Print)

Author(s): Debabrata Konar, Saurabh Maru, Subhabrata Kar, Kapil Kumar*

Journal Name: Medicinal Chemistry


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Abstract:

Breast cancer is the second most commonly identified cancer in women in the United States after skin cancer. The past few years have seen a substantial increase in breast cancer awareness campaigns and active research in fields of diagnosis and targeted therapy. These factors have led to a better mechanistic understanding of the disease, detection at earlier stages and more personalized approach to treatment, ultimately causing a crucial increase in the survival rates after detection. However, with the advances in treatment, cases of patients developing primary resistance and acquired resistance are increasing. Most of the breast cancers which develop resistance to therapy are ER+ and are typically treated with tamoxifen and fulvestrant. These drugs either lower the levels of estrogen or inhibit the receptors for estrogen and prevent the tumor from spreading. Around one third of women treated with these drugs develop resistance to them, lowering their chances of survival. This has directed to the search of newer drug therapies to target advanced breast cancer and resistance. One of these efforts has resulted in the development of Palbociclib, a first in class inhibitor of cyclin dependent kinases 4 and 6 (CDK4 and CDK6), which was granted accelerated approval from FDA for combination therapy in postmenopausal women with ER+, HER2- metastatic breast cancer. This review is focused on the various aspects of “Palbociclib” including its synthesis, molecular modeling studies and efficacy and safety profile with clinical trials data.

Keywords: Palbociclib, Breast cancer, CDK4, CDK6, Clinical trial

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Article Details

Published on: 04 December, 2020
(E-pub Ahead of Print)
DOI: 10.2174/1573406417666201204161243
Price: $95

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