|AHFS/Drugs.com||International Drug Names|
|Elimination half-life||5 to 6 hours|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||628.814 g·mol−1|
|3D model (JSmol)|
It was patented in 1995 and approved for medical use in 2000.
Side effects, interactions, and contraindications have only been evaluated in the drug combination lopinavir/ritonavir.
Lopinavir is highly bound to plasma proteins (98–99%).
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.
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. Lopinavir has been shown to impair protein synthesis via AMP-activated protein kinase (AMPK) and eEF2 kinase (eEF2K) activation, a mechanism that is similar to the antiviral effect of protein phosphatase 1 inhibitors.
Lopinavir was found to inhibit MERS-CoV replication in the low-micromolar range in cell cultures. 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.
- "FDA Approved Drug Products: Kaletra". Retrieved 30 April 2004.
- Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 510. ISBN 9783527607495.
- Kaletra (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
- Capparelli EV, Holland D, Okamoto C, Gragg B, Durelle J, Marquie-Beck J, et al. (June 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.
- HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.
- Stecher C, Marinkov S, Mayr-Harting L, Katic A, Kastner MT, Rieder-Rommer FJ, et al. (2021). "Protein phosphatase 1 regulates Human Cytomegalovirus protein translation by restraining AMPK signaling". Frontiers in Microbiology. 12: 698603. doi:10.3389/fmicb.2021.698603. ISSN 1664-302X. PMC 8320725. PMID 34335531.
- Ammosova T, Platonov M, Ivanov A, Kont YS, Kumari N, Kehn-Hall K, et al. (November 2014). "1E7-03, a low MW compound targeting host protein phosphatase-1, inhibits HIV-1 transcription". British Journal of Pharmacology. 171 (22): 5059–75. doi:10.1111/bph.12863. PMC 4253456. PMID 25073485.
- de Wilde AH, Jochmans D, Posthuma CC, Zevenhoven-Dobbe JC, van Nieuwkoop S, Bestebroer TM, 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): 4875–84. doi:10.1128/AAC.03011-14. PMC 4136071. PMID 24841269.
- Cao B, Wang Y, Wen D, Liu W, Wang J, Fan G, et al. (May 2020). "A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19". The New England Journal of Medicine. 382 (19): 1787–1799. doi:10.1056/NEJMoa2001282. PMC 7121492. PMID 32187464.
- "Lopinavir". Drug Information Portal. U.S. National Library of Medicine.