PARP Inhibitor Development
Poly(ADP-ribose) polymerase (PARP) inhibitors have emerged as a transformative therapeutic approach in the management of breast cancer, particularly for patients harboring deleterious mutations in the BRCA1 and BRCA2 genes. At Alfa Cytology, we specialize in the preclinical discovery of PARP inhibitors and promotes the development of new therapies for breast cancer.
Introduction to PARP Inhibitor for Breast Cancer
The underlying principle behind PARP inhibitor therapy lies in the concept of "synthetic lethality." PARP enzymes are responsible for the base excision repair (BER) pathway, which mends single-strand breaks in DNA. In the absence of functional BRCA1 or BRCA2 proteins, cancer cells become highly dependent on the PARP-mediated BER pathway for survival. By inhibiting PARP activity, these DNA single-strand breaks accumulate and ultimately lead to the formation of lethal double-strand breaks, triggering apoptosis selectively in the BRCA-deficient tumor cells.
Fig.1 PARP inhibitors (olaparib and talazoparib) suppress PARP catalytic activity and cause cell death in tumors with BRCA1 and BRCA2 mutations. (Demir Cetinkaya B., et al. 2022)
PARP Inhibitor Development for Breast Cancer
The remarkable efficacy and favorable safety profile of PARP inhibitors have made them a transformative addition to the breast cancer treatment landscape, particularly for patients with BRCA-mutated disease. Ongoing research aims to build upon these successes and further optimize the use of these targeted therapies.
| NCT | Targets | Therapeutics | Phase |
| NCT05582499 | PARP inhibitor + CDK inhibitor |
Fluzoparib + dalpiciclib/fluzoparib + chemotherapy | |
| NCT05332561 | PARP inhibitor | Olaparib | |
| NCT05761470 | PARP inhibitor + IO | Fluzoparib + camrelizumab + chemotherapy | |
| NCT02849496 | PARP inhibitor + IO | Olaparib + atezolizumab | |
| NCT04481113 | PARP inhibitor + CDK inhibitor |
Niraparib + abemaciclib | |
| NCT05834582 | PARP inhibitor | Fluzoparib + chemotherapy | |
| NCT03911453 | PARP inhibitor | Rucaparib | |
| NCT05498155 | PARP inhibitor + IO | Olaparib ± durvalumab | |
| NCT045842555 | PARP inhibitor + IO | Olaparib ± durvalumab |
Our Services
As a leading preclinical CRO, Alfa Cytology is committed to advancing the development of innovative cancer therapies, including PARP inhibitors for breast cancer. Our state-of-the-art facilities and multidisciplinary team of experts provide comprehensive services to support the entire drug development process, from target identification and validation to preclinical studies and biomarker development.
PARP Degrader (PROTAC) Development
PARP Inhibitor Development for Breast Cancer
PARP Peptide Inhibitor Development
Dual inhibitor Development
- PARP/HDAC Dual Targeting Inhibitor Development
- PARP/PI3K Dual Targeting Inhibitor Development
- PARP/EGFR Dual Targeting Inhibitor Development
- PARP/EZH2 Dual Targeting Inhibitor Development
- PARP/PI3K Dual Targeting Inhibitor Development
Alfa Cytology provides development services for PARP inhibitors, covering drug design, screening, and efficacy research to find ideal drug candidates for you and accelerate preclinical research on your breast cancer therapeutics. To learn more about our capabilities in PARP inhibitor development for breast cancer or to discuss potential collaborative opportunities, please don't hesitate to contact us.
Reference
- Demir Cetinkaya B., Biray Avci C. Molecular perspective on targeted therapy in breast cancer: a review of current status. Med Oncol. 2022, 39(10): 149.