Lopinavir/Ritonavir - A Promising Co-Formulated Drug

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 Lopinavir/Ritonavir- A Promising Co-Formulated
Drug

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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.

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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.
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Originally, Lopinavir/ritonavir combination is
the first and only coformulated HIV-1 protease
inhibitor. Clinical trials have demonstrated
lopinavir/ritonavirs immunologic and virologic
benefits of treatment of HIV-infected adults,
adolescents, and children.
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Recently a random, controlled, open-label trial
for lopinavirritonavir (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.
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Some of the possible known and unknown impurities
of Lopinavir required in clinical trials are
tabulated below
S.No. Product Name Chemical Name CAS No.
1. Lopinavir - API Lopinavir 192725-17-0
2. Lopinavir - Impurity T 2-(2,6-Dimethylphenoxy)-N-(2S,3S,5S)-5-((2S,4S,5S)-5-(2,6-dimethylphenoxy)acetylamino-4-hydroxy-1,6-diphenylhexan-2-ylcarbamoylamino)-3-hydroxy-1,6-diphenylhexan-2-ylacetamide 1797024-56-6
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S.No. Product Name Chemical Name CAS No.
3. Lopinavir - Impurity S (2,6-Xylyloxy)acetyl Lopinavir 943250-65-5
4. Lopinavir - Impurity M (2S)-N-(1R,3R,4S)-1-Benzyl-4-2-(2,6-dimethylphenoxy)acetylamino-3-hydroxy-5-phenylpentyl-3-methyl-2-2-oxotetrahydropyrimidin-1(2H)-ylbutanamide NA
5. Lopinavir - Impurity L N,N'-(Z)-Ethene-1,2-diylbis2-(2,6-dimethylphenoxy)acetamide NA
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S.No. Product Name Chemical Name CAS No.
6. Lopinavir - Impurity I (2S)-N-(1S,2S,4S)-1-Benzyl-4-2-(2,6-dimethylphenoxy)acetylamino-2-hydroxy-5-phenylpentyl-3-methyl-2-2-oxotetrahydropyrimidin-1(2H)-ylbutanamide NA
7. Lopinavir - Impurity A (2S)-N-(1S,3S,4S)-1-Benzyl-4-amino-3-hydroxy-5-phenylpentyl-3-methyl-2-2-oxotetrahydropyrimidin-1(2H)-ylbutanamide 192726-05-9
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S.No. Product Name Chemical Name CAS No.
8. 4,5-Dehydro(pyrimidin-2(1H)-one) Lopinavir 4,5-Dehydro(pyrimidin-2(1H)-one) Lopinavir NA
9. 3-Methyl-2-(2-oxo-tetrahydro-pyrimidin-1-yl)-pentanoic Acid1-benzyl-4-2-(2-6,-dimethyl-phenoxy)-acetylamino-3-hydroxy-5-phenyl-pentyl-amide 3-Methyl-2-(2-oxo-tetrahydro-pyrimidin-1-yl)-pentanoic Acid1-benzyl-4-2-(2-6,-dimethyl-phenoxy)-acetylamino-3-hydroxy-5-phenyl-pentyl-amide NA
10. (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
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S.No. Product Name Chemical Name CAS No.
11. (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
12. (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
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S.No. Product Name Chemical Name CAS No.
13. (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
14. (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
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