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The importance of lead optimization and preclinical development in drug discovery. Lead optimization aims to improve the properties of lead compounds, while preclinical development involves testing development candidates for safety and toxicology. Creative Biostructure offers lead optimization and preclinical development solutions, including in vitro ADME-Tox profiling, to help improve the success rate of clinical development. The document also references a research article on NMR-based pharmacometabonomics.
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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