Jun12682

Last updated

Jun12682
Jun12682.svg
Clinical data
Other namesHY-157403, CS-0915641, XB5
Routes of
administration 		By mouth
Identifiers
  • 5-[2-(dimethylamino)ethoxy]-N-[(1R)-1-[3-(1-ethylpyrazol-3-yl)-5-(1-methylpyrazol-4-yl)phenyl]ethyl]-2-methylbenzamide
CAS Number
PubChem CID
Chemical and physical data
Formula C29H36N6O2
Molar mass 500.647 g·mol−1
3D model (JSmol)
  • CCN1C=CC(=N1)C2=CC(=CC(=C2)[C@@H](C)NC(=O)C3=C(C=CC(=C3)OCCN(C)C)C)C4=CN(N=C4)C
  • InChI=1S/C29H36N6O2/c1-7-35-11-10-28(32-35)24-15-22(14-23(16-24)25-18-30-34(6)19-25)21(3)31-29(36)27-17-26(9-8-20(27)2)37-13-12-33(4)5/h8-11,14-19,21H,7,12-13H2,1-6H3,(H,31,36)/t21-/m1/s1
  • Key:ZOMNORZQANASQP-OAQYLSRUSA-N

Jun12682 is an experimental antiviral medication being studied as a potential treatment for COVID-19. It is believed to work by inhibiting SARS-CoV-2 papain-like protease (PLpro), a crucial enzyme for viral replication. [1] [2] [3] [4]

Mechanism of action

The SARS-CoV-2 virus utilizes several proteases to assist in creating proteins that are essential for viral replication. Among these, the papain-like protease (PLpro) is responsible for cleaving specific sites in the viral polyproteins, facilitating the production of functional viral proteins. By binding to both the BL2 groove and Val70Ub site of PLpro protease, Jun12682 is believed to interfere with the virus's ability to produce new viral proteins, thereby inhibiting the viral replication process. In a study involving mice infected with SARS-CoV-2, mice orally administered Jun12682 experienced reduced viral loads in their lungs, decreased lung lesions, reduced weight loss, and improved survival when compared to those in the control group. [1] [2] [3]

The protease targeted by Jun12682 (PLpro) is distinct from the protease targeted by some other antiviral medications, such as nirmatrelvir/ritonavir, which specifically inhibit the SARS-CoV-2 main protease (Mpro). Laboratory studies have indicated that Jun12682 may retain efficacy against certain strains of SARS-CoV-2 that have developed resistance to other antiviral agents, including nirmatrelvir. This characteristic may position Jun12682 as an option in the treatment of COVID-19 in cases where viral resistance to existing therapies is a concern. [1] [2] [3] [4]

References

  1. 1 2 3 Tan B, Zhang X, Ansari A, Jadhav P, Tan H, Li K, Chopra A, Ford A, Chi X, Ruiz FX, Arnold E, Deng X, Wang J (March 2024). "Design of a SARS-CoV-2 papain-like protease inhibitor with antiviral efficacy in a mouse model". Science. 383 (6690): 1434–1440. Bibcode:2024Sci...383.1434T. doi:10.1126/science.adm9724. PMC   10705561 . PMID   38547259.
  2. 1 2 3 Bolinger AA, Li J, Xie X, Li H, Zhou J (July 2024). "Lessons learnt from broad-spectrum coronavirus antiviral drug discovery". Expert Opinion on Drug Discovery: 1–19. doi:10.1080/17460441.2024.2385598. PMID   39078037.
  3. 1 2 3 Nazir F, John Kombe Kombe A, Khalid Z, Bibi S, Zhang H, Wu S, Jin T (July 2024). "SARS-CoV-2 replication and drug discovery". Molecular and Cellular Probes. 77 101973. doi: 10.1016/j.mcp.2024.101973 . PMID   39025272.
  4. 1 2 Smith, Andrew (28 March 2024). "Rutgers Racing to Develop Paxlovid Replacement". Rutgers University. Retrieved 4 August 2024.
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