PROTAC In Vivo Evaluation


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In the process of drug development, the evaluation of drug effectiveness is one of the keys to determine whether the drug can be put on the market eventually. Drug efficacy studies include pharmacodynamic studies in animal trials and effectiveness studies in human clinical trials. Because in vivo studies have the potential to provide conclusive insights into the safety assessment of PROTAC, they are of vital significance in exploring the most potential PROTAC that can be used in clinical trials. BOC Sciences specializes in in vivo evaluation research to facilitate PROTAC discovery and development projects prior to the clinical phase.

Introduction

PROTAC is a small molecule composed of target protein ligand, E3 ligase ligand and connector. Because the degradation function targets the pathogenic protein, it may be a potential drug. According to the classification of drugs and the characteristics of pharmacological effects, the main efficacy and mechanism of drugs are reflected through appropriate models in vitro and in vivo, so as to provide a basis for new drug development and provide effective support for clinical research. The purpose of preclinical pharmacokinetic studies related to pharmacodynamics is to reveal the dynamic changes of new drugs in animals and to clarify the processes and characteristics of drug absorption, distribution, metabolism and excretion. Preclinical pharmacokinetic study is also an important content to support the research. the absorption, distribution, metabolism and excretion of drugs in vivo are closely related to the actual efficacy and safety of drugs. therefore, preclinical pharmacokinetic studies should not be isolated from pharmacodynamic and toxicological studies, but should be closely combined with it from trial design to result evaluation to give full play to its bridging effect.

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References:

  1. Guo, J., Liu, J., & Wei, W. (2019). Degrading proteins in animals:“PROTAC” tion goes in vivo. Cell research, 29(3), 179-180.
  2. Kounde, C., Shchepinova, M. M., & Tate, E. (2019). A Caged E3 Ligase Ligand for PROTAC-Mediated Protein Degradation with Light. ChemRxiv. Preprint.

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