Ratutrelvir
CAS 2929236-94-0
MF C27H32F3N5O4 MW547.6 g/mol
(1R,2S,5S)-N-[(1S)-1-cyano-2-(2-oxo-1,3-dihydroindol-3-yl)ethyl]-3-[(2S)-3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
(1R,2S,5S)-N-{(1S)-1-cyano-2-[(3RS)-2-oxo-2,3-dihydro-1H-indol-3-yl]ethyl}-3-[(2S)-3,3-dimethyl-2-(2,2,2-trifluoroacetamido)butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
protease inhibitor, antiviral, TRX01, 83-0060, TRX 01, VR2S5588W2,
Ratutrelvir is an investigational new drug that is being evaluated by Traws Pharma[1] for the treatment of COVID-19 infections.[2][3] It is a 3C-like protease inhibitor.[3][4]
Clinical trials
Ratutrelvir is currently in a phase 2 clinical trial to test the effectiveness and safety of the drug in patients with COVID-19[5] and a preliminary analysis of the results has been released.[6]
Ratutrelvir (also known as TRX01 or 83-0060) is an investigational, oral antiviral medication being developed by Traws Pharma for the treatment of mild-to-moderate COVID-19.
Key Characteristics
- Mechanism: It functions as a covalent inhibitor of the SARS-CoV-2 main protease (\(M^{pro}\) / 3CL protease), preventing the virus from replicating.
- Ritonavir-Free: Unlike Paxlovid, ratutrelvir does not require a metabolic booster like ritonavir. This prevents severe drug-drug interactions and broadens its usability.
- Dosing: It is designed as a once-daily oral regimen taken over 10 days.
Clinical Development & Trial Results
According to Phase 2 data released by Traws Pharma in early 2026:
- Efficacy: Shows a comparable or faster time to sustained symptom resolution compared to Paxlovid.
- No Viral Rebound: Patients treated with ratutrelvir experienced no viral rebound events.
- Paxlovid-Ineligible Benefit: The drug successfully treated patients who could not take Paxlovid due to medical contraindications.
- Fewer Side Effects: It reported fewer treatment-related adverse events (10% vs 23.3% for Paxlovid) and avoids taste disturbances (dysgeusia).
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2023093834&_cid=P11-MSWMDL-65476-1
Example 1: Preparation of (1R,2S,5S)-N-((2S)-1-amino-1-carbonyl-3-(2-carbonyldihydroindole-3-yl)propane-2-yl)-3-((S)-3,3-dimethyl-2-(2,2,2-trifluoroacetamido)butyryl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide (compound 1)
[0138]The synthesis route is as follows:
The structural characterization data of compound 1-P2 are as follows:
[0153]m/z(ESI):548[M+H] 。
[0154]
1H NMR:(400MHz,DMSO-d6)δ10.58-10.41(m,1H),9.42-9.00(m,2H),7.39-7.26(m,1H),7.21-7.13(m,1H),7.03-6.78(m,2H),5.30-5.16(m,1H),4.44-4.30(m,1H),4.22(s,1H),4.00-3.86(m,1H),3.75-3.64(m,1H),3.58-3.47(m,1H),2.19-2.05(m,1H),1.63-1.54(m,1H),1.35(d,J＝7.7Hz,1H),1.04(s,3H),1.01-0.96(m,2H),0.94(s,2H),0.90-0.79(m,9H)。
PAT
Synthesis of compound (I)
31.
ASB
Synthesis of compound (I)
31.
ASB
PAT
- Compounds for treatment a coronavirus infectionPublication Number:WO-2023245162-A2Priority Date:2022-06-17
- Compounds for treatment a coronavirus infectionPublication Number:EP-4540227-A2Priority Date:2022-06-17
- Pyrrolidine antiviral compoundPublication Number:WO-2023093834-A1Priority Date:2021-11-26
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References
References
- WO 2023245162, Rogovoy B, Kysil V, Berishvili V, Pauza CD, Zapata JC, Moreno SM, Li H, Orry A, Lam PC, Abagyan R, Savchuk N, “Compounds for treatment a coronavirus infection”, published 2023-12-21, assigned to Trawsfynydd Therapeutics Inc.
- “International Nonproprietary Names for Pharmaceutical Substances (INN) Recommended INN: List 94” (PDF). WHO Drug Information. 39 (3). World Health Organization: 809–1060 (976). 2025.
- “Travatrelvir – Traws Pharma”. AdisInsight. Springer Nature Switzerland AG. Retrieved 5 July 2026.
- “Ratutrelvir | Ligand page”. IUPHAR/BPS Guide to PHARMACOLOGY.
- “Early-stage Trial to Determine a Safe and Effective Dose for Ratutrelvir in Patients With Mild to Moderate COVID-19”. ClinicalTrials.gov. U.S. National Library of Medicine. 17 January 2026. Clinical trial record for NCT07157007. Retrieved 5 July 2026.
- Contagion Editorial Team (8 July 2026). “Traws Pharma Reports Differentiated COVID-19 and Influenza Antiviral Progress”. Contagion Live.
 | |
| Clinical data | |
|---|---|
| Other names | 83-0060, TRX01 |
| Identifiers | |
| IUPAC name | |
| CAS Number | 2929236-94-0 |
| PubChem CID | 169861725 |
| IUPHAR/BPS | 13737 |
| UNII | VR2S5588W2 |
| Chemical and physical data | |
| Formula | C27H32F3N5O4 |
| Molar mass | 547.579 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
///////////ratutrelvir, anax labs, protease inhibitor, antiviral, TRX01, 83-0060, TRX 01, VR2S5588W2,