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In drug discovery and development, we utilize Drug Metabolism and Pharmacokinetic (DMPK) studies for the assessment of bioavailability, half-life, metabolic properties, and clearance profile of a given drug compound.
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What is the Role of Drug Metabolism andPharmacokinetics (DMPK) in Drug Discovery
In drug discovery and development, we utilize Drug Metabolism and Pharmacokinetic (DMPK) studies for the assessment of bioavailability, half-life, metabolic properties, and clearance profile of a given drug compound. One primary goal of conducting DMPK pharmacokinetics is to analyze several drug compounds present in the drug product, understand the underlying properties, and assess the metabolic activities of these compounds. Hence, if the DMPK studies are not effectively concluded, it can cause discontinuation of the drug due to the unwanted toxicity and side-effects. DMPK and ADMET Studies
Earlier, the DMPK studies were only a medium for assessing the safety profile of the drug compound. However, the DMPK studies have recently started exhibiting a major role in the development of pharmaceutical medicine for an intended illness or disease. Various modifications in the use of DMPK in early stages of the drug development such as discovery and nonclinical studies have proved significant in the assessment of the safety profile of the drug product.The DMPK and ADME studies allow the finding of new drug compounds or molecular entities with efficiency. The process is conducted such that the end outcome is a suitable drug compound safe for administration by human volunteers. The ADME studies, a part of pharmacokinetic properties, contribute a lot to the DMPK studies due to the ability to find metabolism carried out by the drug in the human body.
These properties impart knowledge of various aspects such as drug-drug interactions, the concentration of drug at the site of action, and overall design efficiency of the drug compound. The life-cycle of ADMET studies is given below: ➢ After the administration, the drug is absorbed in the body through various methods. This aspect provides the bioavailability of the drug compound. ➢ The drug is distributed in the body which gives the distribution rate and related properties. ➢ During metabolism , the drug copound is converted to metabolites. Understanding this conversation gives a clear knowledge of the toxic or therapeutic impact of the drug compound.
The excretion of the drug compound is the removal of the drug from the body. If the substances aren’t eliminated properly, various health issues can occur. Role of Drug Metabolism and Pharmacokinetics in Drug Discovery The DMPK studies have recently gained extreme importance in the early drug discovery phase. This is because during drug discovery and nonclinical studies knowing the affinity, bioavailability, metabolic properties, and clearance helps in maintain safe administration of the drug.
The safety profile, target protein potency, drug-drug interactions, PK parameters, and bioavailability of the drug compound can be maintained for the successful release of the drug in the market. Currently, the drug attrition rates are alarmingly high, which bring forth the need for sustainable, effective measures or studies. DMPK studies form a path for drug discovery and development to improve the effectiveness of the drug compound in the early stages. Hence, the assessment of these properties has a significant role in the release of a pharmaceutical drug.
