The drug discovery process is the foundation of an entire drug development project. It begins with discovering and identifying potential molecules, right to the validation of lead compounds. Initial discovery and identification of potential therapeutic compounds come from several sources. Basic and applied research can provide new insights into the working and mechanism of disease pathways. Which can be exploited and intervened with drug products.
On the other hand, pharmaceutical companies perform large-scale screening studies to identify prospective molecular compounds. This approach is generally utilized early during the discovery phase to calculate the likeability of a drug candidate to proceed through the preclinical and clinical stages of drug development. The current article covers the basics of drug discovery. It also discusses pharmacological approaches to drug discovery.
Introduction to drug discovery
The drug discovery phase may have thousands of potential leads as a therapeutic for diseases and medical conditions. However, only a few robust candidates reach the preclinical phase of drug development. The drug discovery process can be divided into five stages, each demanding its own requirements. Let us understand how bioanalytical labs perform these stages of drug discovery.
Target identification and validation
This step is the beginning of a drug discovery process. Naturally occurring structures or cellular components that play a vital role in disease progression or pathogenicity are usually the targets for drug compounds. A good target needs to be safe and efficacious and should be easily targeted by a drug molecule.
Once a target is identified, bioanalytical laboratory services validate the approach of the lead candidate to assess efficacy. Generally, the process must include assessing disease association, preclinical evidence in healthy systems, preclinical evidence in primary cells, and a literature survey.
Hit identification and validation
The next step bioanalytical lab services employ is to determine the efficacy of lead molecules for their desired effects. Some approaches for assessing hits are knowledge-based, high-throughput screening, and virtual screening. Once the initial screening is done, sponsors validate the selected hits.
Lead generation
After the initial hit series, the next goal is to refine each series to identify and choose more selective compounds. Generally, multiple hits are assessed in tandem, as some are likely to fail. However, failure is usually due to individual characteristics of the hit series.
Lead optimization
At this stage of drug discovery, sponsors aim to maintain the desired characteristics of the lead compound while trying to shape it as a potential preclinical drug candidate. Besides, lead optimization aims to discover any concerning side effects or understand drug metabolism in the intended body area. Generally, a combination of medicinal chemistry, computational chemistry, and drug metabolism approach can help provide insights into the safety and efficacy of the potential lead candidate.
Late lead optimization
The late lead optimization step further assesses the safety of the lead compound before it progresses to the preclinical stage of drug development. Inadequate efforts in the late lead optimization step may miss potential issues related to the safety, efficacy, and pharmacokinetics of a potential lead candidate. Besides, characterizing safety issues is the primary goal where sponsors aim to remove toxic leads, profile safety assessments, and establish a relationship between hazard and translational risk of the drug candidate.
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