Lopinavir Ritonavir, supplied by Gilead Sciences, used in various techniques. Bioz Stars score: 99/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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1) Product Images from "Impact of combination antiretroviral therapy in the NOD.c3c4 mouse model of autoimmune biliary disease"
Article Title: Impact of combination antiretroviral therapy in the NOD.c3c4 mouse model of autoimmune biliary disease
Journal: Liver International
Figure Legend Snippet: Antiretroviral regimens associated with reduction in serum liver enzyme levels from baseline. (A) After 4 weeks of treatment, only mice receiving Truvada and Kaletra experienced a significant mean reduction in alkaline phosphatase levels as compared to placebo, whereas by the end of 12 weeks therapy mice treated with regimens containing Truvada with or without Kaletra experienced significant reduction. (B) A significant reduction in serum alanine transaminase levels was observed in mice receiving Truvada and Kaletra but not Combivir and Kaletra [Combivir (zidovudine and lamivudine), Truvada (tenofovir and emtricitabine), Kaletra (lopinavir and ritonavir); data shown as means ± SEM; * P
Techniques Used: Mouse Assay
2) Product Images from "Current COVID-19 treatments: Rapid review of the literature"
Article Title: Current COVID-19 treatments: Rapid review of the literature
Journal: Journal of Global Health
Figure Legend Snippet: SARS-CoV-2 gene targets. Proteins are translated from the SARS-CoV-2 genome. Lopinavir targets 3CL protease produced by the ORF1a gene. Remdesivir and ribavirin targets RNA-dependent RNA polymerase (RdRp) translated from ORF1b. Chloroquine/ hydroxychloroquine, convalescent plasma and monoclonal antibodies have effects against the spike protein.
Techniques Used: Produced
Figure Legend Snippet: Progression to cytokine storm. Peak viral replication occurs in the initial 7-10 days and primary immune response usually occurs by day 10-14 which is followed by virus clearance [ 1 ]. Therefore, therapies appear to be most beneficial when given before 14 days of infection. Days 0-5: incubation period. SARS-CoV-2 enter cell via ACE2 receptors on human type 1/2 pneumocytes and start replicating. Hydroxychloroquine (HCQ) targets glycosylation of viral surface. Lopinavir, remdesivir targets the viral replication. Until day 10: moderate symptoms. The initial immune response produces IL-18, IP-10, MCP-1 and MIP-1α which starts to recruit specific immune cells. Interferon (IFN), HCQ and convalescent plasma (CP) is most effective. Day 10: severe infection leading to risk of mortality. Macrophages via BTK, T-cells via JAK, neutrophils and B-cells produce cytokines, resulting in a cytokine storm by day 14. Ruxolitinib, baricitinib, tocilizumab, anakinra, acalabrutinib and corticosteroids can be used [ 1 ].
Techniques Used: Infection, Incubation
3) Product Images from "Effect of COVID‐19 medications on corrected QT interval and induction of torsade de pointes: Results of a multicenter national survey, et al. Effect of COVID‐19 medications on corrected QT interval and induction of torsade de pointes: Results of a multicenter national survey"
Article Title: Effect of COVID‐19 medications on corrected QT interval and induction of torsade de pointes: Results of a multicenter national survey, et al. Effect of COVID‐19 medications on corrected QT interval and induction of torsade de pointes: Results of a multicenter national survey
Journal: International Journal of Clinical Practice
Figure Legend Snippet: Survival function estimated by the Kaplan‐Meier analysis among the eight different drug regimens used to treat COVID‐19. Log‐rank P‐value was significant among the patients who received hydroxychloroquine or lopinavir‐ritonavir with and without azithromycin combination therapy
4) Product Images from "Lopinavir-ritonavir and hydroxychloroquine for critically ill patients with COVID-19: REMAP-CAP randomized controlled trial"
Article Title: Lopinavir-ritonavir and hydroxychloroquine for critically ill patients with COVID-19: REMAP-CAP randomized controlled trial
Journal: Intensive Care Medicine
Figure Legend Snippet: Organ support-free days and mortality. A Organ support-free days in patients allocated to lopinavir-ritonavir, hydroxychloroquine, combination therapy and control among critically ill patients in the COVID-19 Antiviral Therapy Domain of the REMAP-CAP trial. Distributions of organ support-free days are displayed as the cumulative proportion ( y axis) for each study group by day ( x axis). Curves that rise more slowly are more favorable. The height of each curve at “ − 1” indicates the in‐hospital mortality for each intervention. The height of each curve at any time point indicates the proportion of patients who had that number of organ support-free days or fewer. The difference in the height of the curves at any point represents the difference in the percentile in the distribution of organ support-free days associated with that number of days alive and free of organ support. B Organ support-free days are displayed as horizontally stacked proportions by study group. Red represents worse values and blue represents better values. On primary analysis of organ support-free days, the three interventions decreased organ support-free days compared to control, with corresponding median adjusted ORs and 95% credible intervals of 0.73 (0.55–0.99), 0.57 (0.35–0.83) and 0.41 (0.24–0.72), respectively, yielding high posterior probabilities of futility (99% or greater) and high posterior probabilities of harm compared to control (98%, 99.9% and > 99.9%, respectively). C Empirical distribution of survival for lopinavir–ritonavir, hydroxychloroquine, combination therapy and control. Lopinavir-ritonavir, hydroxychloroquine and combination therapy resulted in reduced survival over 90 days compared to control, with adjusted median hazard ratios (95% CrI) of 0.83 (0.65, 1.07), 0.71 (0.45, 0.97), 0.58 (0.36, 0.92), yielding high probabilities of harm compared with control of 92% and 98.4% and 98.7%, respectively
Figure Legend Snippet: Screening, randomization, and follow-up of patients in the REMAP-CAP COVID-19 Antiviral Therapy Domain randomized controlled trial. a Patients could meet more than one ineligibility criterion (Table S2, Supplementary Appendix). b Details of platform exclusions are provided in the Supplementary Results (Supplementary Appendix). c The primary analysis of organ support-free days (OSFD) and hospital survival were conducted on the REMAP-CAP intention-to-treat cohort which included all patients enrolled in the trial who met COVID-19 severe state criteria and were randomized within at least one domain, adjusting for patient factors and for assignment to interventions in other domains (Table S3, Supplementary Appendix). ^Contraindications include hypersensitivity, receiving the study drug as usual medication prior to hospitalization, human immune deficiency (HIV) infection (contraindication of lopinavir-ritonavir), severe liver failure (contraindication of lopinavir-ritonavir), receiving amiodarone as a usual medication prior to this hospitalization or any administration of amiodarone within the 72 h prior to assessment (contraindication of lopinavir-ritonavir) and high clinical risk of sustained ventricular dysrhythmia (contraindication of hydroxychloroquine) (Table S2, Supplementary Appendix)
Techniques Used: Infection
5) Product Images from "Perspective on the Role of Antibodies and Potential Therapeutic Drugs to Combat COVID-19"
Article Title: Perspective on the Role of Antibodies and Potential Therapeutic Drugs to Combat COVID-19
Journal: The Protein Journal
Figure Legend Snippet: Inhibitory functions and roles of different antibodies and re-purposed drugs for battling COVID-19. The COVID-19 (coronavirus disease of 2019) infection begins with the attachment of the spike protein of the SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) to the ACE2 (angiotensin converting enzyme 2) human receptor. Various monoclonal (mAb) and polyclonal antibodies are being designed and convalescent plasma collected from the donor patients are being used to inhibit the attachment of the novel virus. This is followed by the virus and host membrane fusion and entry of the virus which is inhibited by drugs like Hydroxychloroquine (HCQ) and Chloroquine (CQ). Once the uncoating occurs and the viral RNA is released, it starts replicating with the help of the enzyme RNA dependent RNA polymerase (RdRp). Drugs like Remdesivir, Favipiravir and Ribavirin, interfere with the activity of this enzyme. In order to further generate viral proteins, the processing (capping) of the viral RNA is required for maintaining its stability. This processing is inhibited by drugs like Ribavirin. On the other hand, combination of Lopinavir and Ritonavir is used for inhibiting the proteases like 3CL pro (chymotrypsin like cysteine protease) which are mainly responsible for the proteolytic cleavage and generation of non-structural proteins involved in viral replication. Once the viral assembly is complete and the new virions are ready, the exocytosis of these virions occur. This is inhibited by drugs like CQ and HCQ. The infection by the novel virus and release of the new virions which infect the neighbouring cells of the body lead to an exaggerated cytokine release which can be managed using drugs like corticosteroids, various mAbs targeting different cytokines and cytokine receptors, etc.
Techniques Used: Infection, Activity Assay
Article Title: Urine tenofovir and emtricitabine concentrations provide biomarker for exposure to HIV preexposure prophylaxis
Article Snippet: In this study of persons prescribed daily oral Truvada, we observed complete concordance in detection of drugs between urine and plasma, indicating detection of TFV and FTC in urine predicts detection in plasma.
Article Title: Antiviral Efficacies of FDA-Approved Drugs against SARS-CoV-2 Infection in Ferrets
Article Snippet: ..
Article Title: Highly synergistic drug combination prevents vaginal HIV infection in humanized mice
Article Snippet: .. Discussion An oral regimen of TDF and
Article Title: Prevention of Vaginal SHIV Transmission in Macaques by a Coitally-Dependent Truvada Regimen
Article Snippet: Simian/human immunodeficiency virus (SHIV) infection of macaques is a well-established model of HIV transmission that can be used to investigate the efficacy of oral and topical PrEP in preventing rectal and vaginal transmission , . .. We have previously modeled the efficacy of daily oral FTC, TDF, and
Article Title: Oral Administration of the Nucleoside EFdA (4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine) Provides Rapid Suppression of HIV Viremia in Humanized Mice and Favorable Pharmacokinetic Properties in Mice and the Rhesus Macaque
Article Snippet: EFdA was dissolved in sterile phosphate-buffered saline (PBS) and administered to 7 mice per group twice daily by subcutaneous injection in 200 μl at a range of dosage levels (0.3, 1, 3, and 10 mg/kg of body weight/day) beginning the day before HIV inoculation. ..