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Olgotrelvir sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells[1]. | [in vivo]
Olgotrelvir (400-1000 mg/kg; p.o.; twice a day immediately after viral inoculation) sodium 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.
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| [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.
[2] Mao L, et al. Olgotrelvir, a dual inhibitor of SARS-CoV-2 Mpro and cathepsin L, as a standalone antiviral oral intervention candidate for COVID-19. Med. 2024 Feb 9;5(2):169-171. DOI:10.1016/j.medj.2024.01.013 |
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