4yr
A Novel CDK4/6 and PARP Dual Inhibitor ZC-22 Effectively Suppresses Tumor Growth and Improves the Response to Cisplatin Treatment in Breast and Ovarian Cancer - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/35270034/
In recent years, three PARP inhibitors and three CDK4/6 inhibitors have been approved by the FDA for the treatment of recurrent ovarian cancer and advanced ER-positive breast cancer, respectively. However, the clinical benefits of the PARPi or CDK4/6i monotherapy are not as satisfied as expected and ...
Conclusion/Relevance: Altogether, our study has demonstrated the potency of a novel CDK4/6 and PARP dual inhibitor, which can potentially be developed into a monotherapy or combinatorial therapy with cisplatin for breast and ovarian cancer patients with HR proficiency.
• Source: International Journal of Molecular Sciences
• Conclusion: “We developed a novel compound, ZC-22, as a CDK4/6 and PARP dual inhibitor, which displays high therapeutic potential for advanced breast and ovarian cancer patients regardless their HR status, either alone or in combination with platinum-based agent.”
• Therapeutic synergy between PARPi and CDK4/6i has been shown in breast and ovarian cancer patients with HR proficiency in recent studies, thus the investigators developed a new compound, ZC-22, which could inhibit both PARP and CDK4/6. This novel agent exhibited more anti-tumor efficacy than either PARPi or CDK4/6i alone or in combination. This new agent also enhanced the response of breast and ovarian cancer cells to cisplatin treatment.
• In this preclinical study, ZC-22 inhibited breast and ovarian cancer cells by triggering cell cycle arrest and severe DNA damage both in vitro and in vivo.