ADMET (drug absorption, distribution, metabolism, excretion and toxicity) pharmacokinetic method is a very important method in contemporary drug design and drug screening.

ADMET (acyclic diene metathesis) is a special type of olefin metathesis reaction that can form new cis or trans double bonds, and the cis-trans ratio depends on the structure of the monomer and the catalyst.



Early studies of ADMET properties of drugs mainly focused on human-derived or humanized tissue functional proteins as "drug targets". In vitro research techniques were combined with computer simulation and other methods to study the interaction between drugs and in vivo biophysical and biochemical barrier factors. . The early ADME/T properties evaluation method of drugs can effectively solve the problem of species differences, significantly improve the success rate of drug development, reduce drug development costs, reduce drug toxicity and side effects, and can guide the clinical rational use of drugs.

A: Absorption: The process by which the drug enters the systemic circulation from the site of action

D: Distribution: The process of transporting the drug to various tissues, organs or body fluids through the cell membrane barrier after absorption

M: Metabolism (Biotransformation): The process of structural transformation of drugs in the body by the action of the enzyme system or the intestinal flora

E: Excretion: The process by which drugs are excreted from the body in the form of prototypes or metabolites

T: Toxicity: Toxicity of the drug to the body

ADMET is a comprehensive study of drug absorption, distribution, metabolism, excretion and toxicity. Among them, ADME is the research content of Pharmacokinetics (PK)

Function: Drug screening, Drug design, Drug synthesis, Drug formulation, Biopharmaceutics, and TCM herbs research

Features: 1. Analysis methods based on cells or biological macromolecules: small samples, high content and high throughput analysis capabilities; able to clarify the molecular mechanism of drug properties; establish a structure-drug property quantitative structure-activity relationship; 2. Application of human-derived materials

ADMET (acyclic diene metathesis) is a special type of olefin metathesis reaction that can form new cis or trans double bonds, and the cis-trans ratio depends on the structure of the monomer and the catalyst. It is a gradual polymerization and polycondensation reaction; while other metathesis polymerization reactions and ring-opening metathesis polymerization are addition polymerization reactions of chain growth.

ADMET is driven by the release of volatile ethylene gas (while the ring-opening metathesis polymerization is driven by the release of ring-strain).

The concept of ADMET has been discussed in the scientific literature since the 1970s. The first ADMET polymerization was successful in 1991. In the report, the group of Wagener, KB combined 1,5-hexadiene and 1,9-decene The dienes are polymerized into 1,4-polybutadiene and poly(octylene), respectively. Polybutadiene has an average molecular weight of 28,000 (Mw) and contains more than 70% of trans double bonds. Poly(octylene) has an average molecular weight of 108,000 (Mw) and contains more than 90% trans double bonds

ADMET has been used in the synthesis of many interesting polymers. Because ADMET is more controllable than traditional free radical polymerization, it has been used to synthesize model polymers that are difficult to prepare. Examples include pure linear polyethylene, alternating copolymers and block copolymers of ethylene with various other vinyl monomers, chiral polymers, and polymers with embedded amino acids.



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