Dual-target PARP Inhibitor Development
Online Inquiry

Dual-target PARP Inhibitor Development

At Alfa Cytology, our team of world-class scientists is dedicated to advancing the frontiers of cancer research and treatment. One area that has garnered significant attention in recent years is the development of dual-target PARP inhibitors - a novel class of therapeutics that hold immense promise in the fight against cancer.

Introduction to Dual-target PARP Inhibitor

Poly(ADP-ribose) polymerase (PARP) enzymes play a crucial role in DNA damage repair, a process that is often dysregulated in cancer cells. Traditional PARP inhibitors have demonstrated their utility in targeting this vulnerability, leading to the development of several FDA-approved drugs. However, as with any therapeutic approach, there is a constant drive to improve upon existing strategies and explore new avenues for enhancing efficacy and overcoming drug resistance.

Fig. 1 Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy. (Hu X., et al. 2022)Fig. 1 Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy. (Hu X., et al. 2022)

Enter the dual-target PARP inhibitors - molecules designed to simultaneously inhibit PARP and another key cancer-associated target. By combining the DNA repair-targeting capabilities of PARP inhibition with the disruption of a complementary cellular pathway, these innovative compounds offer the potential for superior antitumor activity, improved patient outcomes, and the ability to address drug resistance mechanisms.

Dual-target inhibitor Development

The development of dual-targeting inhibitors that combine PARP with various other key targets, such as HDAC, PI3K, Topoisomerase, EZH2, BRD4, HSP90, EGFR, and DNA-damaging agents, offers several advantages for cancer treatment:

  • Enhanced Anti-tumor Efficacy
    Improved anti-tumor efficacy through synergistic inhibition of PARP and complementary targets.
  • Synthetic Lethality
    Inducing selective and potent cytotoxicity in cancer cells through synthetic lethality.
  • Broader Applicability
    Expanding the range of cancer types that can benefit from PARP-based therapies.
  • Overcoming Resistance
    Dual-targeting strategies can help overcomresistance by sensitizing cancer cells and preventing resistant clones.
  • Personalized Treatment
    Enabling personalized and targeted treatment approaches.
  • Improved Safety
    Potentially better safety profile due to lower individual component doses.
Compound Structure Target Cancer Clinical Trials Phase
AMXI-5001

PARP1 and Microtubule TNBC; Lung Cancer NCT04503265
E7449

PARP1 and TNKS1/2 Breast Cancer NCTO3878849
BRCA-deficient Tumors NCT03562832

Our Services

At Alfa Cytology, we pride ourselves on our comprehensive suite of drug discovery and development services. Our state-of-the-art facilities and multidisciplinary team of experts are dedicated to supporting your research endeavors, from target identification and validation to lead optimization and preclinical evaluation.

PARP/HDAC Dual Targeting Inhibitor Development

PARP/PI3K Dual Targeting Inhibitor Development

PARP/Topoisomerase Dual Targeting Inhibitor Development

PARP/EZH2 Dual Targeting Inhibitor Development

PARP/PI3K Dual Targeting Inhibitor Development

PARP/BRD4 Dual Targeting Inhibitor Development

PARP/HSP90 Dual Targeting Inhibitor Development

PARP/EGFR Dual Targeting Inhibitor Development

PARP/DNA Damaging Agents Dual Targeting Inhibitor Development

Our Services Workflow

By leveraging our expertise and cutting-edge capabilities, Alfa Cytology is poised to accelerate the development of your dual-target PARP inhibitor candidates, paving the way for the next generation of targeted therapies. To learn more about our dual-target PARP inhibitor development services or to discuss your specific research needs, please don't hesitate to contact us.

References

  1. Hu X., Zhang J., and et al. Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities. European Journal of Medicinal Chemistry. 2022, 230: 114094.
  2. Zhang J, Zhang J, and et al. Dual-target inhibitors of PARP1 in cancer therapy: A drug discovery perspective. Drug Discovery Today. 2023, 28(7): 103607.

For research use only. Not intended for any clinical use.