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Paxlovid

Paxlovid structure

CAS No:
2628280-40-8
Formula:
C23H32F3N5O4
Chemical Name:
Paxlovid
Synonyms:
PF-07321332;3-Azabicyclo[3.1.0]hexane-2-carboxamide,N- [(1S)-1-cyano-2-[(3S)-2-oxo-3-pyrrolidinyl]ethyl]- 3-[(2S)-3,3-dimethyl-1-oxo-2-[(2,2,2- trifluoroacetyl)amino]butyl]-6,6-dimethyl-, (1R,2S,5S)-;PF07321332(Paxlovid);nirmatrelvir;Nirmatrelvir (PF-07321332);PF-07321332-005;(1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-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;3-Azabicyclo[3.1.0]hexane-2-carboxamide,N- [(1S)-1-cyano-2-[...
Categories:
Active Pharmaceutical Ingredients > Veterinary Raw Materials

Description

PF-07321332 is an azabicyclohexane that is (1R,5S)-3-azabicyclo[3.1.0]hexane substituted by {(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl}aminoacyl, 3-methyl-N-(trifluoroacetyl)-L-valinamide, methyl and methyl groups at positions 2S, 3, 6 and 6, respectively. It is an inhibitor of SARS-CoV-2 main protease which is currently under clinical development for the treatment of COVID-19. It has a role as an EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor and an anticoronaviral agent. It is a nitrile, a member of pyrrolidin-2-ones, a secondary carboxamide, a pyrrolidinecarboxamide, a tertiary carboxamide, an organofluorine compound and an azabicyclohexane.

PF-07321332 is an oral COVID-19 antiviral clinical candidate. By inhibiting the main protease, PF-07321332 prevents the virus from cleaving long protein chains into the parts it needs to reproduce itself.

Paxlovid is a new potential drug discovered by Pfizer. Paxlovid is composed of two active ingredients, Nirmatrelvir and Ritonavir. Similarly, a mixture of Lopinavir and Ritonavir drugs is already used against HIV. Ritonavir is a drug approved in 1996 which is widely used, not exclusively, to treat HIV/AIDS. Another component of Paxlovid, Nirmatrelvir (PF-07321332) is a new potential drug developed by Pfizer. It inhibits the SARS-CoV-1 virus protease (Mpro), which fragments long protein chains into the parts the virus needs to reproduce. Nirmatrelvir acts as a substrate for the virus protease in the cell, thereby deceiving the virus and blocking its replication.

Paxlovid Basic Attributes

Molecular Weight：

499.53

Exact Mass：

499.24063901

EC Number：

605-001-5

UNII：

7R9A5P7H32

Color/Form：

White to off-white

Characteristics

Density：

1.267±0.06 g/cm3(Predicted)

Boiling Point：

742.4±60.0 °C(Predicted)

PKA：

10.26±0.46(Predicted)

Critical Temperature & Pressure：

Store at -20°C

Safety Information

wgk germany：

WGK 3

Drug Information

MeSH Entry Terms：

(1R,2S,5S)-N-((1S)-1-cyano-2-((3S)-2-oxopyrrolidin-3-yl)ethyl)-6,6-dimethyl-3-(3-methyl-N-(trifluoroacetyl)-l-valyl)-3-azabicyclo(3.1.0)hexane-2-carboxamide

Paxlovid Use and Manufacturing

PF-07321332 (nirmatrelvir) is an oral antiviral clinical lead. It is a covalent inhibitor of SARS-CoV-2 Mpro (main protease, 3CLpro) that binds to cysteine145 within the enzyme's catalytic domain. Mpro is essential for coronavirus replication. Inhibiting Mpro actvity blocks replication at an early stage in the virus' life cycle. Due to structural similarities between the Mpro's of other coronavirusus, PF-07321332 offers the potential of pan-coronavirus activity. In vitro it is suggested to inhibit replication of CoV-2 variants including delta and omicron.

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