Drug Metabolism and pharmacokinetics

Drug metabolism and pharmacokinetics seeks to answer three key questions:  1) does the drug reach the target in sufficiently high concentrations; this is essentially pharmacokinetics, 2) how will the drug be handled by the body’s systems in terms of chemical modification and distribution; this is broadly metabolism and, 3) what effect will the drug have when it interacts with the target; pharmacodynamics.  

At the drug design stage drug metabolism and pharmacokinetics expertise helps in identifying agents with appropriate DMPK features to ensure that the candidate drug has the best chance to become a successful medicine. 

Some of the studies that contribute to this work are as follows:

1. Safety testing

• In vitro metabolism profiles across species to help select relevant species for toxicity studies.
• Cross species metabolic profiles in vivo to support species selection and metabolite contributions to safety assessment.
• Toxicokinetics to understand the relationship between dose and drug exposure and to allow comparison across species.
• Cross species plasma protein binding to ensure that comparisons are made with systemic free drug exposure.

2. Translational science

• Comparative pharmacokinetics in animal models of human diseases and humans
• Comparative drug potency and plasma protein binding

3. Preparation for human trials and clinical development

• Estimation of human pharmacokinetics based on animal PK and in vitro metabolic clearance
• Conduct of quantitative whole body autoradiography to prepare human dosimetry estimations to enable conduct of studies in humans with radiolabelled drugs
• Study of routes, rates and systems involved in metabolism and active transport to facilitate design of human drug-drug interactions.
• Gather necessary data and information to build physiologically-based pharmacokinetic models to simulate human clinical studies of drug-drug interactions and other extrinsic factors such as age and ethnicity.

GS Drug Development Services have over 30 years’ experience in designing studies, overseeing studies as well as interpreting and integrating these concepts in drug development programmes.