| Hazard Information | Back Directory | [Uses]
Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells[1][2]. | [in vivo]
Olgotrelvir (400-1000 mg/kg; p.o.; twice a day immediately after viral inoculation) has antiviral activity and reduces lung pathology in K18-hACE2 transgenic mice[2].
| Animal Model: | K18-hACE2 transgenic mice (express human ACE2 in the lung epithelia, including airway epithelia, under the control of the human keratin 18 promoter)[2] | | Dosage: | 400, 500, 1000 mg/kg | | Administration: | Oral gavage (p.o.); twice a day immediately after SARS-CoV-2 WA-1 strain inoculation | | Result: | Prevented weight loss.
On day 5 post infection, virus was below the detectable level in the lungs.
Pathological changes caused by SARS-CoV-2 infection were relieved.
At a dose of 1000 mg/kg at the 12th hour post-infection resulted in significant reduction of viral RNA shedding and prevention of the body weight loss.
Blocked pro-inflammatory cytokine (IL-6, TNF-α, GM-CSF) release at 400 mg/kg dosage.
|
| [References]
[1] Sorrento Announces the Full Enrollment of the Pivotal Phase 3 Trial with Olgotrelvir (OVYDSOTM) (STI-1558), a Second Generation Oral Mpro Inhibitor, as a Standalone Treatment for COVID-19. |
|
|