Lopinavir/ritonavir in the treatment of HIV-1 infection: a review

Abstract

Lopinavir/ritonavir is the fi rst and only coformulated HIV-1 protease inhibitor (PI). Large clinical trials have demonstrated lopinavir/ritonavir's clinical effi cacy in both antiretroviral-naïve and -experienced patients. The immunologic and virologic benefi ts of treatment with this agent have been proven in HIV-infected adults, adolescents, and children. Smaller studies support the use of lopinavir/ritonavir monotherapy as a therapeutic option in certain patients. The drug is characterized by a high genetic barrier to resistance, and appears to be more forgiving of non-adherence than earlier, unboosted PIs. The most frequent side effects observed are diarrhea, nausea, and vomiting. These gastrointestinal adverse effects are generally mild to moderate. Metabolic derangements, including hyperlipidemia and glucose intolerance, have also been observed in lopinavir/ritonavir recipients. As the menu of available antiretroviral agents continues to expand, lopinavir/ritonavir remains a proven and effective drug for the treatment of HIV infection.

Nucleophilic Cyclization/Electrophilic Substitution of (2,2-Dialkoxyethyl)ureas: Highly Regioselective Access to Novel 4-(Het)arylimidazolidinones and Benzo[d][1,3]diazepinones

“…Some of them inhibit various ferments, such as leucyl-tRNA synthetase, 6 -secretase, 7 HIV-1 protease, 8,9 and biotin biosynthesis, 10 and exhibit antimicrobial and antihepatitis С activity 11 (Figure 1). The six-membered cyclic urea moiety is also found in a number of drugs, such as well-known barbiturates, the anti-HIV drug lopinavir, 12 the antibiotic sparsomycin, 13 and the actively studied anticancer agent troxacitabine. 14 Other examples of cyclic ureas of biological importance include 1,3-diazepinone derivatives, which possess anti-HIV [15][16][17][18][19][20][21][22] and anticancer [23][24][25][26] activity and were proposed for the treatment of Alzheimer's and Parkinson's disease.…”

Clinico-Immunological Status and Neurocognitive Function of Perinatally Acquired HIV-Positive Children on cART: A Cross-Sectional Correlational Study in South Africa

“…All participants received the first-line cART consisting of lopinavir/ritonavir (LPV/r)-based regimen in combination with two nucleoside/nucleoside reverse transcriptase inhibitors, including zidovudine, lamivudine/emtricitabine, abacavir, and efavirenz. Studies have shown LPV/r-based regimens to have a better safety profile and to be more effective in HIV-infected children (17,18).…”

Potential Therapeutic Agents for COVID-19 Based on the Analysis of Protease and RNA Polymerase Docking

“…At the Rajavithi Hospital in Thailand, the infectious disease team used a combination of oseltamivir (antiinfluenza agent) and lopinavir/ritonavir (anti-HIV agent) to successfully improve patients with severe conditions. Lopinavir and ritonavir are both HIV protease inhibitors that suppress the cleaving of a polyprotein into multiple functional proteins 1 . Likewise, various clinical trials are also now being undergone on nucleotide analogue drugs such as Remdesivir, an antiviral drug proven to be effective against a wide range of RNA viruses in vitro 2 .…”