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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.
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)
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.
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:
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 |
|
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
SAR Studies
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
For research use only. Not intended for any clinical use.