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Small molecule drugs are low - molecular - weight chemical entities (generally with a molecular weight of less than 900 Da) that are either synthesized chemically or derived from the modification of natural products. These drugs interact with specific targets, such as enzymes, receptors, and ion channels, in a reversible binding mode, thereby modulating signaling pathways associated with diseases.
In comparison to macromolecular drugs, small molecule drugs exhibit several core advantages. These include remarkable tissue penetration capabilities, favorable oral bioavailability, the potential for optimizing chemical structures, and well - established large - scale manufacturing processes. As a result, they have become fundamental therapeutic agents in the treatment of oncology, cardiovascular diseases, metabolic disorders, and infectious diseases.
The research and development of small molecule drugs initiates with the discovery and validation of drug targets. This process entails the utilization of genomics, proteomics, and in - depth investigations into disease mechanisms to identify targets that are closely related to the disease progression and possess the property of "druggability". Once a target has been validated, the subsequent stage involves the discovery of lead compounds. Leveraging the structural features of the target, lead compounds capable of either activating or inhibiting the target are identified through extensive screening procedures. The screening of lead compounds represents a critical juncture in the small molecule drug development process and can be classified into two main approaches: cell-based assay and cell-free assay.
Vazyme offers a comprehensive process and multi dimensional innovative solution for the research phase of small molecule drugs, spanning all aspects from early stage R&D to process development. By leveraging cutting-edge technology platforms and providing customized services, we assists pharmaceutical enterprises in surmounting key bottlenecks.
Hit-to-Lead Discovery
Identify lead compounds (Leads) that activate or inhibit the target through large-scale screening.
(1)Hit Compound Screening:
Biophysical Screening: Techniques like SPR (Surface Plasmon Resonance) or ITC (Isothermal Titration Calorimetry) to detect binding affinity.
Biochemical Screening: Functional assays (e.g., enzyme inhibition, receptor activation) to evaluate compound activity.
(2)Lead Generation:
Secondary Screening: Validate hits in dose-response assays.
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Preclinical Study
Select a Preclinical Candidate Compound (PCC) by conducting comprehensive studies.
Test Article Selection: Optimize lead compounds based on potency, selectivity, and synthetic feasibility.
In Vivo/In Vitro Efficacy Studies: Validate therapeutic effects in disease-relevant models.
Pharmacokinetics (PK): Assess bioavailability, half-life, and tissue distribution.
Non-Clinical Safety Studies: Evaluate toxicity (acute/chronic), organ-specific effects, and potential off-target liabilities.
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