Lead Optimization and Preclinical Development in Drug Discovery, Slides of Biology

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Lead Preclinical Development

Once the most promising hit compounds have been identified as leads

through the efforts of hit to lead, it will enter the stage of lead

optimization and preclinical development of early drug development,

which are the key processes for finalizing drug candidates entering

clinical trials. Lead optimization aims to improve the properties of

lead compounds including stability, potency, efficacy, exposure,

safety, etc. Lead optimization involves a sophisticated iterative stage

in which the bioactivity and drug activity of the lead series are

extensively optimized through various screening filters, and

development candidates are ultimately determined for preclinical

development. Preclinical development, also known as IND-enabling

studies, involves testing development candidates in various in vitro

and in vivo assays to examine their safety pharmacology and

toxicology profile.

In Vitro ADME-Tox Profiling

Drug development is a high-risk investment, especially when entering the

clinical development stage, developers are faced with high costs and

increasing attrition rates. Therefore, early determination of the absorption,

distribution, metabolism, excretion (ADME), and toxicological (Tox)

properties of the lead series is an effective strategy to balance the risk-

reward ratio and improve project productivity. Creative Biostructure agrees

with this view of “fail early and fail cheap”, and we provide in vitro ADME-

Tox profiling solutions for global customers with drug development needs to

evaluate the ADME-Tox properties of drug candidates and prioritize them.

We have a well-trained and knowledgeable drug discovery team, and we

have gained extensive in vitro ADME-Tox expertise and experience through

cooperation with academic institutions, biotech, and pharmaceutical

companies.

Reference

Everett J R. NMR-based pharmacometabonomics: A new paradigm for

personalised or precision medicine. Progress in Nuclear Magnetic

Resonance Spectroscopy. 2017, 102: 1-14.

Excerpt from:

https://drug-discovery.creative-biostructure.com/lead-

optimization-and-preclinical-development-p