Lead Optimization

Lead Optimization

A lead is a compound that exhibits pharmacological or biological activity but may possess certain undesirable properties such as high toxicity, low bioavailability, or poor metabolic stability. These compounds require further optimization of their structure to improve their activity, selectivity, solubility, pharmacokinetic properties, and drug interactions. Alta Stomatology is a drug R&D company for oral diseases, our team consists of professionals with rich experience in drug development, chemical modification, and biological testing, who can provide our clients with high-quality lead compound optimization services, whether small molecule or biologic. If you have any needs, please feel free to contact us.

Lead Optimization

Our Services

Structure-Activity Relationship (SAR) Analysis

SAR analysis is a cornerstone of lead optimization, focusing on understanding the relationship between a compound's chemical structure and its biological activity. At Alta Stomatology, our expert medicinal chemists leverage advanced computational modeling and high-throughput screening techniques to systematically explore and optimize lead compounds. Through SAR analysis, we identify key molecular features responsible for desired pharmacological effects and iteratively design analogs with enhanced potency and specificity.

Pharmacokinetics and ADME Assessment

We conduct comprehensive pharmacokinetic and ADME (absorption, distribution, metabolism, and excretion) studies to evaluate the bioavailability, stability, and distribution of lead compounds. This information helps us optimize the pharmacokinetic properties of lead compounds to ensure that they reach the target site in the appropriate concentration and are efficiently metabolized in the body.

Early Assessment of DMPK Properties Efficacy Drug Distribution
Metabolic Stability Metabolite Identification Bioavailability
Solubility and Stability Permeability Assays Others

In vitro and In vivo Testing

In vitro and in vivo testing are essential components of lead optimization, providing valuable insights into a compound's pharmacological activity, toxicity, and pharmacokinetic properties. At Alta Stomatology, we offer a comprehensive suite of in vitro and in vivo assays tailored to assess various aspects of lead compound efficacy and safety. Our integrated approach enables thorough characterization of lead compounds under physiologically relevant conditions, guiding informed decision-making throughout the optimization process.

Hepatotoxicity Mitochondrial Toxicity Genotoxicity
Cytotoxicity Drug-Drug Interaction Cardiac Toxicity

Biophysical Assays

In addition to traditional pharmacological assays, Alta Stomatology offers advanced biophysical techniques to characterize the molecular interactions between lead compounds and their targets. These techniques provide valuable insights into binding kinetics, affinity, and mechanism of action, guiding rational drug design and optimization.

Surface Plasmon Resonance Services (SPR) Bio-Layer Interferometry Services (BLI)
Isothermal Titration Calorimetry (ITC) Nuclear Magnetic Resonance Services (NMR)

Why Choose Alta Stomatology?

  • Rich Experience in Lead Compound Optimization

Our team possesses extensive experience in various lead compound optimization methods. We are adept at employing a range of advanced techniques to enhance drug-binding activity, reduce toxicity, and improve pharmacokinetic properties. With our deep expertise, we can effectively navigate the complexities of lead optimization to achieve superior outcomes.

  • Integrated Platform

Alta Stomatology has established an integrated platform combining computational-assisted drug design, medicinal chemistry, and biological testing. This integrated platform ensures seamless coordination between molecular design, synthesis, and testing, significantly enhancing the efficiency of lead optimization. By streamlining the optimization process, we accelerate project timelines and deliver results more rapidly.

  • Cost Optimization

Leveraging our integrated platform and extensive R&D experience, we prioritize cost optimization without compromising on quality. Our streamlined processes and efficient workflows enable us to complete lead optimization in shorter timeframes and at lower costs.

For research use only. Not intended for any clinical use.
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