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Nirmatrelvir
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 3CLPRO of SARS-CoV-2. It restricts the activity of 3CLPRO, 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.
References
FAQ's
References
- Owen, Dafydd Rhys; Pettersson, Martin Youngjin; Reese, Matthew Richard; Sammons, Matthew Forrest; Tuttle, Jamison Bryce; Verhoest, Patrick Robert; Wei, Liuqing; Yang, Qingyi; Yang, Xiaojing, Nitrile-containing antiviral compounds, Pfizer Inc., United States, US11351149B2, June 7, 2022
- Zheng, Lewei; Wang, Lingqiao; Li, Dan; Xie, Chongjun; Gao, Zhiyuan; Lin, Jinsheng; Ye, Jian; Chen, Wenbin; Li, Min, Investigation of nirmatrelvir epimerization occurred in analytical sample solution by using high resolution LC-MSn, NMR, and hydrogen/deuterium exchange study, Journal of Pharmaceutical and Biomedical Analysis, Volume: 227, Pages: 115284, 2023
Frequently Asked Questions
What is the acceptable limit for Nirmatrelvir impurities?
The acceptable limit for impurities in Nirmatrelvir is determined by regulatory agencies such as the FDA, EMA, and ICH. The limit varies depending on the impurity and its potential impact on the drug’s quality, safety, and efficacy.
How are Nirmatrelvir impurities controlled during the manufacturing process of the drug?
Impurities in Nirmatrelvir are controlled during the manufacturing process by implementing good manufacturing practices (GMP) and using appropriate analytical methods for impurity identification and quantification. Purification techniques such as crystallization, distillation, and chromatography to remove impurities.
What is the genotoxic impurity in Nirmatrelvir?
A genotoxic impurity in Nirmatrelvir is an impurity that has the potential to cause genetic mutations or other genetic damage. Regulatory agencies have strict limits for the presence of genotoxic impurities in pharmaceuticals due to their potential carcinogenicity.
What are the temperature conditions required to store Nirmatrelvir impurities?
Nirmatrelvir impurities are stored at a controlled room temperature between 2-8 ⁰C or as indicated on the Certificate of Analysis (CoA).
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