The Discovery of a New DrugLink to LifeSciences-Montreal.comLink to MontrealInternational.comVersion française
 
 
   

Lead identification

 
Lead Identification
Photo : MDS Pharma Services
Once the therapeutic target has been identified, scientists must then find one or more leads (e.g., chemical compounds or molecules) that interact with the therapeutic target so as to induce the desired therapeutic effect, e.g., through antiviral or antibacterial activity.

In order to discover the compounds whose pharmacological properties are likely to have the required therapeutic effects, researchers must test a large variety of them on one or more targets. The pharmaceutical companies possess veritable libraries of synthetic or natural compounds, ready to be tested.

To test the chosen compounds in large numbers, scientists use an entirely automated process known as high density screening. In general, of the thousands of compounds tested, barely 1% will qualify for further and more probing analysis.

Duration: from 4 to 6 months

Between 5 and 50 000 compounds are examined in the laboratory, of which only 100 to 200 are perfected in order to be tested on systems in vitro and in vivo.

To allow biologists to complete an exhaustive evaluation of the selected compounds or molecules, specialists in process chemistry synthesize them in order to produce quantities sufficient to meet R&D needs. First of all, biologists ensure that the chosen compounds have the desired therapeutic or antiviral effect on the target. Then, they test the compounds’ relative toxicity, or, in the case of a vaccine, their viral activity, using in vitro cellular and/or tissue systems. Finally, they check their bio-availability in vivo on animals.

The compounds that demonstrate an ability to act specifically and selectively on the therapeutic target, are well absorbed and show minimum toxic effects, are patented. They become candidates for subsequent transformation into drugs.

The documentation required for patent application is prepared by the researchers (chemists and biologists) in collaboration with the patent agent. A Canadian patent protects the discovery for the next 20 years. Nonetheless, the stages remaining to be covered are critical and require an average of ten years before the drug reaches the sales counter.

 

   
 
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Lead optimization | Preclinical trials |
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