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Addressing delivery and resistance issues of CDK4/6 inhibitors as cancer therapeutics

Kshitiz Luthra1, Nalla Usha Kumari1, Sri Pada Datta Chigurupati1

  • 1Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, India.

Drug Discovery Today
|April 8, 2026
PubMed

Insights

Novel nanoformulations enhance cyclin-dependent kinases-4 and -6 (CDK4/6) inhibitors for breast cancer treatment. These advanced strategies aim to improve efficacy and overcome resistance, offering a promising future for targeted cancer therapy.

Area of Science:

  • Oncology
  • Nanomedicine
  • Pharmacology

Background:

  • Conventional cancer therapies face limitations in specificity, efficacy, and resistance.
  • Cyclin-dependent kinases-4 and -6 (CDK4/6) inhibitors have improved hormone receptor-positive breast cancer treatment.
  • Challenges remain with CDK4/6 inhibitors, including high dosage, frequent administration, and acquired resistance.

Purpose of the Study:

  • To review advanced formulation strategies for CDK4/6 inhibitors.
  • To explore nanoformulations for enhancing CDK4/6 inhibitor efficacy.
  • To address resistance mechanisms associated with CDK4/6 inhibitor therapy.

Main Methods:

  • Review of current literature on nanoformulations and advanced drug delivery systems.
  • Analysis of lipid and polymeric-based systems, salt forms, and inclusion complexes.
  • Investigation of strategies to circumvent resistance to CDK4/6 inhibitors.

Main Results:

  • Nanoformulations and advanced strategies show potential for improving CDK4/6 inhibitor delivery.
  • These approaches can enhance anti-cancer efficacy and overcome resistance mechanisms.
  • Novel formulations offer a promising route to optimize therapeutic applications.

Conclusions:

  • Advanced formulation strategies, particularly nanoformulations, are crucial for maximizing the potential of CDK4/6 inhibitors.
  • These innovations represent a significant step forward in overcoming limitations of current targeted cancer therapies.
  • Further development of these strategies could lead to improved clinical outcomes for breast cancer patients.

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