General Information

Nirmatrelvir Impurities and Nirmatrelvir 

Daicel Pharma is a reliable source for synthesizing high-quality Nirmatrelvir impurities, specifically Nirmatrelvir Acid impurity, Nirmatrelvir chloro impurity, Nirmatrelvir Impurity-1 Hydrochloride, Nirmatrelvir INT Diastereomer -1, Nirmatrelvir INT Diastereomer -2, etc. These impurities help assess the quality, stability, and safety of the active pharmaceutical ingredient, Nirmatrelvir. Daicel Pharma also offers custom synthesis of Nirmatrelvir impurities, which can be shipped worldwide.

Nirmatrelvir [CAS: 2628280-40-8] is an oral medication and functions as a peptidomimetic inhibitor of the main protease (Mpro) of the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), also known as the 3C-like protease or 3CL protease or nsp5 protease. Its potential antiviral activity is directed against SARS-CoV-2 and other types of coronaviruses.

Nirmatrelvir: Use and Commercial Availability  

Nirmatrelvir, in combination with ritonavir, has been granted emergency use authorization by the FDA for the treatment of mild-to-moderate COVID-19 in patients who have tested positive for SARS-CoV-2 and are at high risk for severe disease. The same combination is also approved for use in Canada and Europe under conditional marketing authorization. Paxlovid is a co-packaged combination of Nirmatrelvir and Ritonavir used to treat COVID-19 in adults at increased risk for progressing to severe disease and do not require supplemental oxygen.

Nirmatrelvir Structure and Mechanism of Action

The chemical name of Nirmatrelvir is (1R,2S,5S)-N-{(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-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. Its chemical formula is C₂₃H₃₂F₃N₅O₄, and its molecular weight is approximately 499.5 g/mol.

Nirmatrelvir inhibits cysteine residue in the 3CL^PRO of SARS-CoV-2. It restricts the activity of 3CL^PRO_, thus preventing virus replication.

Nirmatrelvir Impurities and Synthesis

There is limited information available on the impurities of Nirmatrelvir. However, as with any drug substance, impurities may form during the manufacturing process¹, storage, or stability testing. They can affect the drug quality, safety, and efficacy. Therefore, it is essential to identify and control them within acceptable limits throughout the drug development process.

Daicel Pharma provides a Certificate of Analysis (CoA) for Nirmatrelvir impurity standards, which include Nirmatrelvir Acid impurity, Nirmatrelvir chloro impurity, Nirmatrelvir Impurity-1 Hydrochloride, Nirmatrelvir INT Diastereomer -1, Nirmatrelvir INT Diastereomer -2, etc. The CoA is from an analytical facility that adheres to current Good Manufacturing Practices (cGMP) and includes complete characterization data, such as 1H NMR, 13C NMR, IR, MASS, and HPLC purity². We give additional characterization data such as 13C-DEPT and CHN on request. Daicel Pharma can also generate unknown Nirmatrelvir impurities or degradation products and provide labeled compounds to assess the effectiveness of Nirmatrelvir. Further, Daicel Pharma offers Nirmatrelvir-D9, a deuterium-labeled Nirmatrelvir standard used in bio-analytical research, such as BA/BE studies. A complete characterization report is a part of each delivery.