Safety, Oral Absorption, and Half-Life Confirmed

Binding structure of 3CL protease and JNC-11139.

Binding structure of 3CL protease and JNC-11139.

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[Asia Economy Reporter Lee Gwanju] CrystalGenomics and JNC Science announced on the 26th that they have discovered a 3CL protease inhibitor candidate substance with the same mechanism of action as Pfizer's COVID-19 treatment 'Paxlovid.'


The COVID-19 treatment candidate substance 'JNC-11139,' jointly developed by the two companies, confirmed safety at a high concentration of 2000 mg/kg per day in acute toxicity studies in small animals (mice), and showed an oral absorption rate of over 68% and an in vivo half-life (the time it takes for the drug concentration or amount to decrease by 50%) of more than 4 hours in large animals (beagle dogs).


Regarding this, the companies explained that JNC-11139 is expected to be stable in human liver metabolism and therefore would not require co-administration with the CYP3A4 enzyme inhibitor 'ritonavir.' In the case of Paxlovid, ritonavir is added to the main ingredient nirmatrelvir to prolong its efficacy, which limits its use in patients taking other disease treatments.


Previously, in the bioavailability study of JNC-11139, when administered to large animals at doses of 10 mg/kg and 30 mg/kg respectively, it showed 68.3% and 87%, confirming sufficient development potential as an oral drug.


CrystalGenomics and JNC Science discovered the new drug candidate JNC-11139, which inhibits the 3CL protease, an essential protein for viral replication, through research using three-dimensional structural analysis technology of target proteins and medicinal chemistry technology in November last year. The two companies plan to apply for a national project titled ‘Development of SARS-CoV-2 Therapeutics Using Novel Low Molecular Synthetic Compound 3CLpro Inhibitors.’



Choi Jongryu, CEO of JNC Science, said, "It took seven months from the discovery of the candidate in November last year through role-sharing with the CrystalGenomics team to confirm the development candidate," adding, "We plan to enter preclinical and clinical stages by the end of this year or early next year to promote rapid development."


This content was produced with the assistance of AI translation services.

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