Lopinavir/Ritonavir- A promising co-Formulated drug

Published Jun 17, 2020 by pharmaffiliates
 Lopinavir/Ritonavir - A Promising Co-Formulated Drug

End of December 2019 and beginning of the year 2020 marked the emergence of, a novel coronavirus, designated SARS-CoV-2, and has caused an international outbreak of respiratory illness termed Covid-19.

The full spectrum of Covid-19 ranges from mild, self-limiting respiratory tract illness to severe progressive pneumonia, multi-organ failure, and finally death.

Although there is no therapeutic treatment for coronavirus agents till date but in a hopeful finding, studies revealed that a combination of LopinavirRitonavir were proven effective against SARS-CoV and MERS-CoV, the previous two coronaviruses that hit the globe.

Originally, Lopinavir/ritonavir combination is the first and only coformulated HIV-1 protease inhibitor. Clinical trials have demonstrated lopinavir/ritonavir’s immunologic and virologic benefits of treatment of HIV-infected adults, adolescents, and children.

Remdesivir

Recently a random, controlled, open-label trial for lopinavir–ritonavir (ritonavir helps to stabilize lopinavir) in 199 hospitalized patients with severe COVID-19 was conducted and the drug showed benefit for some secondary endpoints.

Pharmaceutical parlance, medicinal fraternity and researchers are trying ways to find a promising treatment for the deadly virus. A lot of research is going on throughout the world and a lot of hard work, knowledge, infrastructure, technology and research material is required to find a cure for COVID -19.

Some of the possible known and unknown impurities of Lopinavir required in clinical trials are tabulated below:

Product Name Chemical Name Cas No.
Lopinavir - API Lopinavir 192725-17-0
Lopinavir - Impurity T 2-(2,6-Dimethylphenoxy)-N-[(2S,3S,5S)-5-([[(2S,4S,5S)-5-[[(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenylhexan-2-yl]carbamoyl]amino)-3-hydroxy-1,6-diphenylhexan-2-yl]acetamide 1797024-56-6
Lopinavir - Impurity S (2,6-Xylyloxy)acetyl Lopinavir 943250-65-5
Lopinavir - Impurity M (2S)-N-[(1R,3R,4S)-1-Benzyl-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenylpentyl]-3-methyl-2-[2-oxotetrahydropyrimidin-1(2H)-yl]butanamide NA
Lopinavir - Impurity L N,N′-(Z)-Ethene-1,2-diylbis[2-(2,6-dimethylphenoxy)acetamide] NA
Lopinavir - Impurity I (2S)-N-[(1S,2S,4S)-1-Benzyl-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-5-phenylpentyl]-3-methyl-2-[2-oxotetrahydropyrimidin-1(2H)-yl]butanamide NA
Lopinavir - Impurity A (2S)-N-[(1S,3S,4S)-1-Benzyl-4-amino-3-hydroxy-5-phenylpentyl]-3-methyl-2-[2-oxotetrahydropyrimidin-1(2H)-yl]butanamide 192726-05-9
4,5-Dehydro(pyrimidin-2(1H)-one) Lopinavir 4,5-Dehydro(pyrimidin-2(1H)-one) Lopinavir NA
3-Methyl-2-(2-oxo-tetrahydro-pyrimidin-1-yl)-pentanoic Acid{1-benzyl-4-[2-(2-6,-dimethyl-phenoxy)-acetylamino]-3-hydroxy-5-phenyl-pentyl}-amide 3-Methyl-2-(2-oxo-tetrahydro-pyrimidin-1-yl)-pentanoic Acid{1-benzyl-4-[2-(2-6,-dimethyl-phenoxy)-acetylamino]-3-hydroxy-5-phenyl-pentyl}-amide NA
(S)-N-[(2S,4S,5S)-5-Amino-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl)butanamide (S)-N-[(2S,4S,5S)-5-Amino-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl)butanamide 192726-05-9
(S)-N-((2S,4S,5S)-5-(2-(2,6-Dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-3-methylbutanamide (S)-N-((2S,4S,5S)-5-(2-(2,6-Dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-3-methylbutanamide 192725-39-6
(S)-N-((2S,4S,5S)-4-(((6-(Cyclopropylamino)-9-((1S,4S)-4-(hydroxymethyl)cyclopent-2-en-1-yl)-9H-purin-2-yl)amino)methoxy)-5-(2-(2,6-dimethylphenoxy)acetamido)-1,6-diphenylhexan-2-yl)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl)butanamide (S)-N-((2S,4S,5S)-4-(((6-(Cyclopropylamino)-9-((1S,4S)-4-(hydroxymethyl)cyclopent-2-en-1-yl)-9H-purin-2-yl)amino)methoxy)-5-(2-(2,6-dimethylphenoxy)acetamido)-1,6-diphenylhexan-2-yl)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl)butanamide NA
(2S,3S,5S)-2-Amino-3-hydroxy-5-(tert-butyloxycarbonylamino)-1,6-diphenylhexane (2S,3S,5S)-2-Amino-3-hydroxy-5-(tert-butyloxycarbonylamino)-1,6-diphenylhexane 144163-85-9
(2S,3S,5S)-2-(2,6-Dimethylphenoxyacetyl)amino-3-hydroxy-5-trifluromethylcarbonylamino-1,6-diphenylhexane (2S,3S,5S)-2-(2,6-Dimethylphenoxyacetyl)amino-3-hydroxy-5-trifluromethylcarbonylamino-1,6-diphenylhexane NA

Pharmaffiliates provides all the above-mentioned products for research and quality control purpose. In the critical time of pandemic, Pharmaffiliates assures to deliver on time and in a cost effective manner.

We deliver all the research products with a Certificate of Analysis along with necessary data required to fulfill your regulatory needs.

Leave a Reply