Lopinavir

Lopinavir is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir (lopinavir/ritonavir).[1]

Lopinavir
Clinical data
Other namesABT-378
AHFS/Drugs.comInternational Drug Names
MedlinePlusa602015
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityUnknown
Protein binding98-99%
MetabolismLiver
Elimination half-life5 to 6 hours
ExcretionMostly fecal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC37H48N4O5
Molar mass628.814 g·mol−1
3D model (JSmol)
  (verify)

It was patented in 1995 and approved for medical use in 2000.[2]

Side effects

Side effects, interactions, and contraindications have only been evaluated in the drug combination lopinavir/ritonavir.

Pharmacology

Lopinavir is highly bound to plasma proteins (98–99%).[3]

Reports are contradictory regarding lopinavir penetration into the cerebrospinal fluid (CSF). Anecdotal reports state that lopinavir cannot be detected in the CSF; however, a study of paired CSF-plasma samples from 26 patients receiving lopinavir/ritonavir found lopinavir CSF levels above the IC50 in 77% of samples.[4]

Research

A 2014 study indicates that lopinavir is effective against the human papilloma virus (HPV). The study used the equivalent of one tablet twice a day applied topically to the cervices of women with high-grade and low-grade precancerous conditions. After three months of treatment, 82.6% of the women who had high-grade disease had normal cervical conditions, confirmed by smears and biopsies.[5] In 2020 lopinavir/ritonavir was found not to work in severe COVID-19. In this trial the medication was started typically around 13 days after the start of symptoms.[6]

Lopinavir is found to inhibit MERS-CoV replication in the low-micromolar range in cell cultures.[7]

References
  1. "FDA Approved Drug Products: Kaletra". Retrieved 30 April 2004.
  2. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 510. ISBN 9783527607495.
  3. Kaletra (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
  4. Capparelli E, Holland D, Okamoto C, et al. (2005). "Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV". AIDS. 19 (9): 949–52. doi:10.1097/01.aids.0000171409.38490.48. PMID 15905676. S2CID 3162858.
  5. HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.
  6. Cao, Bin; Wang, Yeming; Wen, Danning; Liu, Wen; Wang, Jingli; Fan, Guohui; et al. (18 March 2020). "A Trial of Lopinavir–Ritonavir in Adults Hospitalized with Severe Covid-19". New England Journal of Medicine. 382 (19): 1787–1799. doi:10.1056/NEJMoa2001282. PMC 7121492. PMID 32187464.
  7. de Wilde, Adriaan H.; Jochmans, Dirk; Posthuma, Clara C.; Zevenhoven-Dobbe, Jessika C.; van Nieuwkoop, Stefan; Bestebroer, Theo M.; et al. (August 2014). "Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture". Antimicrobial Agents and Chemotherapy. 58 (8): 4875–4884. doi:10.1128/AAC.03011-14. PMC 4136071. PMID 24841269.
  • "Lopinavir". Drug Information Portal. U.S. National Library of Medicine.
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