Cell cycle protein-dependent kinases 4 and 6 (CDK4/6) are key proteins in the human cell division and proliferation cycle, and they play an important role in controlling the G1/S phase transition of the cell cycle. To date, the development of CDK4/6 inhibitors has now become a focus of prostate cancer therapy. At Alfa Cytology, we are committed to providing comprehensive one-stop CDK4/6 inhibitor development services for prostate cancer.
The cell cycle contains key regulators that control cell growth. These factors include enzymes such as cyclin-dependent kinase (CDK). In cancer, this pathway is commonly disrupted, leading to tumorigenesis. The development of CDK4/6 inhibitors (CDK4/6i) has now become a focus of cancer therapy.
Fig. 1 Androgen
regulation of cell cycle and CDK4/6 pathway. (Kase, A. M., et al. 2020)
Estrogen receptors, as well as androgen receptors, are key regulators of the cell cycle and tools to regulate transcribed genes, allowing for the G1 to S transition. In prostate cancer (PCa), this hormonal pathway can be targeted with ADT. However, PCa eventually becomes androgen resistant, which provides an opportunity to disrupt AR signaling using CDK4/6i.
In exploring the potential and use of CDK4/6 inhibitors in the treatment of prostate cancer, we have paid particular attention to their effects in combination with other agents. The following table summarizes data from clinical trials of CDK4/6 inhibitors in combination with androgen signaling inhibitors.
Table 1. CDK4/6 Inhibitor with Androgen Signaling Inhibitor Combination Trials. (Kase, A. M., et al. 2020)
Name | Phase | Patient population | Status | Identifier |
ADT+/- Palbociclib | Phase II | mHSPC, RB-positive | Completed | NCT02059213 |
Palbociclib | Phase II | mCRPC | Recruiting | NCT02905318 |
Enzalutamide +/- Ribociclib | Phase IB/II | mCRPC chemo-naïve that retain RB expression | Recruiting | NCT02555189 |
Ribociclib + Docetaxel | Phase Ib/II | mCRPC | Recruiting | NCT02494921 |
Abiraterone +/- Abemaciclib | Phase II | mCRPC | Recruiting | NCT03706365 |
The development of CDK4/6 inhibitors has become a focal point for prostate cancer therapy. This is because they are able to selectively inhibit CDK4/6, restoring the normal regulation of the cell cycle and thus inhibiting the proliferation of tumor cells. At Alfa Cytology, our team of scientists boasts profound expertise in the development of CDK4/6 inhibitors, and we are dedicated to offering a full range of integrated services for the development of CDK4/6 inhibitors tailored to prostate cancer.
As with most cancer therapies, drug resistance develops over time. Therefore, further understanding of potential combination therapies that explore CDK4/6 to slow or overcome drug resistance is critical.
Small Molecule Drug Development
Offer complete development of small molecule inhibitors, from discovering lead compounds to enhancing their chemistry, screening, and adjusting them for better performance.
Provide solutions to meet customers' needs for genetically engineered mouse models, including Large-fragment gene editing model, knock-out/knock-in model, and transgenic model.
Preclinical Testing and Evaluation
Offer comprehensive preclinical services tailored to unique needs of prostate cancer research. Our expertise spans a wide range of areas, including efficacy evaluation, DMPK/ADME and safety assessment.
Alfa Cytology aims to provide customized one-stop CDK4/6 inhibitors development services in the field of prostate cancer therapy. If you are interested in our services, please don't hesitate to contact us for further information and pricing details.
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