Amerigo Scientific is dedicated to providing drug metabolism related products and services to our global clients, aiming to support the success of your research projects.
Drug metabolism refers to the process of drug metabolic breakdown generally via specialized enzymatic systems and the chemical alterations of the molecules after entering living organisms. As a discipline, drug metabolism serves a key role in the research and development of drugs, exerting vital effects on pharmacokinetics (PK) and pharmacodynamics (PD), as well as safety. It acts as a milestone of multiple crucial parameters, including the distribution, absorption, excretion, and toxicity of interested drugs, which will be rigorously evaluated in the preclinical stage of drug R&D.
There are numerous enzymes and other modulators participating in drug metabolism, which biochemically assist in improving the efficiency of transforming substrates into products as catalysts, by lowering the threshold of required energy for reactions. Currently, there are two categories of drug metabolism widely recognized by researchers, termed as phase I and phase II reactions.
Phase I metabolism is the first step in drug metabolism, in which a variety of enzymes introduce reactive and polar groups into their substrates, performing modifications in preparation for phase II metabolism. In this phase, by uptake transporters or passive diffusion, xenobiotics and lipophilic endobiotics enter cells, and phase I enzymes trigger the enzymatic reactions that aim to clear them from the organism. In the following phase II reactions, these activated metabolites are conjugated with charged species, like glutathione (GSH), glucuronic acid, glycine, sulfate, etc. Reactions in phase II are the detoxification pathways, producing highly water-soluble metabolites. Besides, after phase II metabolism, the metabolite conjugates can be further modified and metabolized.
Fig.1 Overview of drug metabolic phases.1
Considering the key roles of drug metabolism in treatments and drug development, targeting regulators and pathways in drug metabolism has been widely recognized as promising components of precision medicine strategies, which is aimed at individualizing treatment for different patients to maximally optimize therapeutic efficacy and reduce drug toxicity. Drug metabolism is intensively mediated by a diversity of genes encoding drug-metabolizing enzymes (DMEs), especially the cytochrome P450 (CYP) enzymes, which partake in the regulation of drug responses.
It has been proven that the induction of CYP by active parent drugs leads to the stimulation of metabolism and drug clearance, thus suppressing therapeutic effects. Accordingly, repressing CYP contributes to inhibited drug metabolism and enhanced drug accumulation, thus enhancing pharmacological effects. Several official guidelines have been published, allowing the translation of preclinical experimental results into prescription decisions.
As a pioneer in the field of antibody research and development, Amerigo Scientific has gained rich knowledge and resources in targeting a diversity of mechanisms including drug metabolism, as well as the genes and pathways related. We are proud to introduce our antibody products and customized services for various applications to our esteemed clients around the world, please feel free to for more information.
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