PARP-targeting Prodrug Development
Online Inquiry

PARP-targeting Prodrug Development

Poly(ADP-ribose) polymerase (PARP) inhibitors have emerged as a significant advancement in cancer therapy, particularly for tumors with deficiencies in homologous recombination repair, such as those involving BRCA1 and BRCA2 mutations. To address these challenges, Alfa Cytology is dedicated to provideding PARP-targeting prodrug development services for combating various diseases for our clients.

Introduction to PARP-targeting Prodrug

PARP inhibitors exploit the concept of synthetic lethality, where the inhibition of PARP leads to cell death in the presence of DNA repair deficiencies. Despite their therapeutic potential, some PARP inhibitors are limited by poor pharmacokinetic properties and significant side effects, including hematologic toxicity.

To address these challenges, the development of PARP-targeting prodrugs has gained traction. Prodrugs are pharmacologically inactive compounds that convert into active drugs through metabolic processes. This strategy aims to enhance drug solubility, improve bioavailability, and minimize toxicity, making it a promising avenue for optimizing PARP inhibitors.

Fig. 1 Chemical structures of PARP-targeting prodrugs. (Peng X., et al. 2022)Fig. 1 Chemical structures of PARP-targeting prodrugs. (Peng X., et al. 2022)

PARP-targeting Prodrug Development

Recent studies have highlighted innovative approaches in the design of PARP-targeting prodrugs. These developments underscore the versatility of prodrug strategies in optimizing PARP inhibition, enhancing the selectivity and potency of treatments while addressing the limitations of existing therapies.

Our Services

At Alfa Cytology, we specialize in the development and optimization of PARP-targeting prodrugs. Our team of experienced scientists and skilled technicians is dedicated to supporting the development of innovative PARP-targeting prodrugs and other targeted therapeutics. Our comprehensive services include:

Conceptualization and Design

  • Select PARP Enzymes
  • Define Therapeutic Objectives
  • Prodrug Design

Synthesis of Prodrug Candidates

  • Synthesize Prodrug Compounds
  • Purification and Characterization
  • High-Throughput Screening

In Vitro Evaluation

  • PARP Inhibition Assays
  • Cytotoxicity Studies
  • ADME

Optimization and Reformulation

  • Analyze In Vitro and In Vivo Data
  • Formulation Development

Regulatory Consulting

  • Regulatory Submissions
  • Engage with Regulatory Authorities

Through our dedicated services, Alfa Cytology aims to accelerate the development of innovative PARP-targeting therapies, supporting the pharmaceutical industry's quest for more effective cancer treatments. For inquiries regarding our PARP-targeting prodrug development services or to discuss potential collaborations, please don't hesitate to contact us. Our team of experts is ready to assist you in navigating the complexities of drug development and optimizing therapeutic strategies for cancer treatment.

Reference

  1. Peng X., Pan W., and et al. Selective PARP1 inhibitors, PARP1-based dual-target inhibitors, PROTAC PARP1 degraders, and prodrugs of PARP1 inhibitors for cancer therapy. Pharmacol Res. 2022, 186: 106529.

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