What is the Role of Drug Metabolism and Pharmacokinetics (DMPK) in Drug Discovery

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What is the Role of Drug Metabolism
andPharmacokinetics (DMPK) in Drug Discovery
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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. 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

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• 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.

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• 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.

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• The excretion of the drug compound is the removal
  of the drug from the body. If the substances
  arent 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.

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• 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.

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• Thanks