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<p>Palbociclib is a selective cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor that emerged as a significant therapeutic agent in the treatment of hormone receptor-positive, HER2-negative breast cancer. This review comprehensively highlights the pharmacological significance of palbociclib and its recently developed derivatives, focusing on mechanisms of action, chemical synthesis strategies, pharmacological profile and potential benefits in cancer treatment. We explored the rationale behind structural modifications and chemical derivatization of palbociclib that have been developed to enhance its therapeutic efficacy and mitigate side effects. This review offers an update on the latest advancement in palbociclib derivatives and explores their potential to improve therapeutic efficacy with minimal side effects. The detailed analysis of recent developments and ongoing research will support the designing of more efficient CDK4/6 inhibitors and provide direction in development of future cancer treatment. We anticipate that the information provided in this review will be beneficial to readers and scientist working towards development of effective cancer treatment specifically towards next-generation CDK4/6 inhibitors with improved therapeutic and safety profiles.</p><p></p>

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Pharmacological significance of palbociclib and its derivatives in cancer treatment and prevention: an update

  • 期刊论文

  • 发表日期：

    2025年4月25日

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  • Shagufta,
  • Irshad Ahmad,
  • Laila Zeyad Bazbouz,
  • Noora Ali Nasar,
  • Fatme Ghassan Ibrahim,
  • Dana Mahmoud Alkheder

摘要

Palbociclib is a selective cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor that emerged as a significant therapeutic agent in the treatment of hormone receptor-positive, HER2-negative breast cancer. This review comprehensively highlights the pharmacological significance of palbociclib and its recently developed derivatives, focusing on mechanisms of action, chemical synthesis strategies, pharmacological profile and potential benefits in cancer treatment. We explored the rationale behind structural modifications and chemical derivatization of palbociclib that have been developed to enhance its therapeutic efficacy and mitigate side effects. This review offers an update on the latest advancement in palbociclib derivatives and explores their potential to improve therapeutic efficacy with minimal side effects. The detailed analysis of recent developments and ongoing research will support the designing of more efficient CDK4/6 inhibitors and provide direction in development of future cancer treatment. We anticipate that the information provided in this review will be beneficial to readers and scientist working towards development of effective cancer treatment specifically towards next-generation CDK4/6 inhibitors with improved therapeutic and safety profiles.