Drug discovery and development includes a series of processes, such as the target identification and validation, hit identification, hit-to-lead, and clinical evaluation of drug candidates. In this process, we often encounter problems such as poor medicinal properties, poor pharmacokinetic characteristics, toxicity and side effects of lead compounds. To enhance the ability of lead compounds to be used as drugs and expedite the process of developing new medications, optimization of lead compounds has become the key link of new drug research and development. Lead optimization refers to the process of designing and improving a pre-determined lead compound, involving pharmaceutical chemists using advanced organic synthesis methods or biotechnological methods to modify the structure of the lead compound to improve multiple of the properties described above, while reducing any defects found in its structure. Therefore, in this process, the optimization and evaluation of ADMET properties (absorption, distribution, metabolism, excretion and toxicity) of lead compounds as well as the activity, stability and selectivity of lead compounds become the goal and focus. With extensive capabilities in chemistry, biology, structural biology, ADME and proteomics, we provide wide and world-class services to support the most complex lead optimization projects.
Our Lead Optimization Services
Our company has highly trained and knowledgeable pharmaceutical chemists with many years of experience in drug discovery. We offer a range of services for lead optimization to accelerate your drug candidate generation process. Our complete portfolio of lead optimization service includes:
- Drug Design and Optimization: This includes structure-based drug design and optimization/molecular modeling.
- Evaluation of physical and chemical properties: This includes evaluation of water solubility, lipid solubility, stability and other chemical/physical properties.
- In Vitro and In Vivo ADME: This includes CYP induction, CYP inhibition, drug interaction, permeability, plasma protein binding, metabolic stability, metabolite identification and analysis, etc.
- In Vivo and In Vitro DMPK: This includes bioavailability, route evaluation of administration, DRF (Dose Range Finding), drug distribution, preclinical efficacy, etc.
- In Vivo Pharmacology: This includes metabolic stability, PK feasibility, maximum tolerated dose (MTD) determination, various animal models to describe dose frequency, dose-response relationship, in vivo therapeutic effect, etc.
- Toxicological Studies: This includes toxicokinetics, single dose toxicity, repeated dose toxicity, etc.
- Others: PK/PD modeling and simulation, histology services, formulation and delivery strategies, biomarker identification and evaluation, regulatory guidance are also available at our company.
Typical Advanced Equipment
State-of-the-art biophysical testing equipment underlies our lead optimization services and is a strong support for accelerating the development of potential drug candidates. Some typical equipment at our company is described below:
Bio-Layer Interferometry (BLI)
BLI is a label-free optical technique for measuring kinetics and affinity of interactions of biomolecules such as proteins, nucleic acids, and peptides. It measures macromolecular interactions by analyzing the interference pattern of white light reflected from the surface of the biosensor tip.
Surface Plasmon Resonance (SPR)
SPR is a biophysical technique for detecting molecular interactions based on the principles of physical optics. This method can detect the interaction between molecules in real time with high sensitivity. SPR and BLI became key technologies for our lead optimization.
lsothermal Titration Calorimetry (ITC)
ITC is a labeling free method for measuring the binding of any two molecules that release or absorb heat when combined. ITC can be used to measure thermodynamic parameters of biomolecular interactions, including enthalpy, affinity and stoichiometry.
Nuclear Magnetic Resonance (NMR)
NMR studies the structural characteristics, dynamic behaviors and interactions of molecules, thereby revealing the three-dimensional structure of biomolecules.
Why Choose Us?
Expertise
At our company, lead optimization services are provided by experienced professionals who have expertise in drug discovery and development.
Efficiency
We collaborate closely with our clients, establishing a streamlined workflow that accelerates the lead optimization process.
Robust Analytics
Our bioinformatics team can efficiently process and analyze the vast data often associated with discovery research projects. This facilitates the rapid progression from initial biological validation to drug discovery.
Customization
Lead optimization services can be tailored to meet the specific needs and requirements of each pharmaceutical company.
Related Services
It should be noted that our service is only used for research, not for clinical use.
