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Drug Metabolism & Pharmacokinetics

Physiological barriers exist animal models (in vivo), which reduce the amount of dosed compound that reaches systemic circulation and ultimately the target. Therefore, an ideal drug candidate should possess properties that enable good absorption, distribution, low metabolism, reasonable elimination (ADME) and low toxicity in order to reach these targets, this is true especially in the context of orally administered drugs, which form our research target drug profiles. First pass metabolism occurs here followed by metabolism in the liver. Distribution happens when the compound permeates into the tissues from the blood capillaries, with elimination occurring simultaneously by removal of the compound from the bloodstream by the liver and the kidneys. 

Our DMPK platform allows for the assessment of parameters that constitute an efficient ADME processes including:  

  1. Physicochemical Properties i.e. Solubility, permeability, lipophilicity, chemical metabolic stability. 

  1. Pharmacokinetic Properties i.e. Clearance (CLint), Half-life (t1/2), Oral bioavailability (%F), Drug-drug interactions, LD50 etc. 

  1. Biochemical - Metabolism, transport and protein/tissue binding 

Furthermore, our DMPK stream focuses on continuous development of assays as well as the investigation of the metabolism profiles in the African population. Details and capabilities of the DMPK research can be found in our publications [http://www.kellychibaleresearch.uct.ac.za/2020-0]