The initial goal of any pharma company during drug development is to minimize the attrition rate of potential drugs under testing and development. To evaluate new drugs their DMPK profiles must be checked for properties such as half-life, bioavailability, clearance, and metabolic profile in order to get approval.

Drug metabolism and pharmacokinetic profiles are critical when it comes to drug development and drug testing. A sub-optimal DMPK profile is a strong reason to discontinue the process of drug development then and there.

The Goal of DMPK in Drug Discovery

The purpose of DMPK profile in any drug discovery procedure is to screen the compounds, conduct an elaborate evaluation of their intrinsic DMPK properties and then proceed to conduct further metabolic tests on the group of compounds likely to be the perfect prospects as new drugs. Therefore, a proper understanding of potential drug metabolic profiles is important for selecting compounds with desirable DMPK properties in early drug discovery.

Importance of DMPK

Now, Drug Metabolism and Pharmacokinetics is an old scientific discipline earlier associated with the evaluation of safety in drug development. But in the last two decades, DMPK has become a core discipline within drug discovery, development, and even post-marketing.

In addition to adequate potency against the target protein and an acceptable safety profile, a balance of optimized PK parameters and minimized drug-drug interaction (DDI) potential maximizes the chance of a candidate drug becoming a successful therapy.

In the drug discovery history of recent times, there has been much emphasis on assessing all the DMPK-related parameters at the very beginning of the drug discovery process. R&D labs have shifted their focus on formulating molecules with low clearance, high drug-target affinity, high oral bioavailability, and optimal metabolic properties.

DMPK studies are conducted in earlier stages of drug discovery, and hence, the importance of pharmacokinetics and in vitro metabolism assays have increased drastically.

Liquid chromatography-tandem mass spectrometry allows high throughput assurance and sensitivity analysis of samples for vast numbers of compounds, thereby increasing the number of drug candidates progressing through the drug discovery and development pipeline. Liquid Chromatography-Mass Spectrometry is the technique of choice for researchers conducting DMPK studies, and mass spectrometry imaging (MSI), initially developed for protein and peptide analysis, has recently been extended to DMPK using MALDI-MS. MALDI Imaging enables research labs to visualize drugs and metabolites in tissue, allowing differentiation between drug compounds and their metabolites.

Although DMPK is not the panacea for all drug development processes, the technique is one of the most helpful when it comes to the assessment of drug potential.

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