PSI-6130

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PSI-6130

PSI-6130 is a nucleoside analogue and a potent antiviral agent. It is primarily known for its activity against Hepatitis C virus (HCV). PSI-6130 is the parent nucleoside for the active metabolite R-7128, which has been developed into the prodrug Sofosbuvir, a direct-acting antiviral medication used to treat chronic Hepatitis C.

Chemistry

PSI-6130 is a cytidine analogue, where the natural ribose sugar is replaced with a 2'-fluoro-2'-C-methyl substituent. This modification enhances the compound's resistance to degradation by nucleoside and nucleotide metabolizing enzymes, thereby increasing its half-life in the body.

Mechanism of Action

PSI-6130 exerts its antiviral activity by acting as a RNA polymerase inhibitor. It is metabolized in the body to its active triphosphate form, which competes with the natural cytidine triphosphate for incorporation into the growing RNA chain. Once incorporated, it causes premature termination of the RNA chain, thereby inhibiting viral replication.

Clinical Development

The clinical development of PSI-6130 was initially focused on its potential as a standalone treatment for HCV. However, it was later developed into the prodrug Sofosbuvir, which is now a key component of several combination therapies for chronic Hepatitis C.

See Also

• Sofosbuvir
• Hepatitis C virus
• Antiviral drug
• Nucleoside analogue

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

• Fusion Inhibitors (HIV)
  • Enfuvirtide, Maraviroc

• Integrase Inhibitors (HIV)
  • Dolutegravir, Elvitegravir, Raltegravir

• Monoclonal Antibodies
  • Ibalizumab

• Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
  • Delavirdine, Efavirenz, Etravirine, Nevirapine, Rilpivirine

• Nucleoside Analogues (HIV)
  • Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine

• Protease Inhibitors (HIV)
  • Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir,Ritonavir, Saquinavir, Tipranavir

Drugs for Hepatitis B

• • Alpha Interferon, Adefovir, Emtricitabine, Entecavir, Lamivudine, Telbivudine, Tenofovir

Drugs for Hepatitis C

• Interferon Based Therapies
  • Alpha Interferon and Peginterferon, Ribavirin

HCV NS5A Inhibitors

• Daclatasvir, Elbasvir, Ledipasvir, Ombitasvir, Pibrentasvir, Velpatasvir

HCV NS5B (Polymerase) Inhibitors

• Dasabuvir, Sofosbuvir

HCV Protease Inhibitors

• Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir

Combination Therapies

• Epclusa, Harvoni, Mavyret, Technive, Viekira Pak, Vosevi, Zepatier

Drugs for Herpes Virus Infections (HSV, CMV, others)

• Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

Drugs for Influenza

• Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir