Lopinavir
Other / unclassified targets CYP17A1, CYP21A2 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 2 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | EU (EMA) | Kaletra | — | 2001-03-19 | europa.eu ↗ |
| Approved | US (FDA) | KALETRA | — | 2000-09-15 | fda.gov ↗ |
Trials 136 · started per year
News releases announcing trial results or a regulatory action · 15
| Date | Issuer | Release |
|---|---|---|
| 2022-06-14 | Drugs for Neglected Diseases | Regulatory Cipla and DNDi launch child-friendly 4-in-1 antiretroviral treatment for young children living with HIV in South Africa dndi.org ↗
The South African Health Products Regulatory Authority (SAHPRA) has approved a sweet-tasting, heat-stable, ‘4-in-1’ fixed-dose combination of four antiretroviral (ARV) treatments composed of abacavir, lamivudine, lopinavir, and ritonavir that is specifically designed for infants and young children with HIV. |
| 2017-12-21 | GlaxoSmithKline | Regulatory FDA approves US label update on ICS/LABA combinations in asthma, based on review of safety data gsk.com ↗
These labelling updates were approved on December 20th 2017, after a review of safety data from 4 randomized controlled safety trials submitted by three companies, including GSK. |
| 2017-07-25 | GlaxoSmithKline | Results ViiV Healthcare announces superior efficacy of dolutegravir versus lopinavir/ritonavir in second-line HIV treatment in resource-limited settings gsk.com ↗
The 24-week interim data showed an 82% response rate in the dolutegravir arm versus 69% for lopinavir/ritonavir (p<0.001). |
| 2017-06-05 | Drugs for Neglected Diseases | Regulatory Child-friendly formulation of WHO-recommended HIV treatment now approved by the CDSCO | DNDi dndi.org ↗
On 25 May, an expert committee of the Central Drugs Standard Control Organization (CDSCO), the Indian drug regulatory authority, finally permitted the child-friendly and heat-stable pellet formulation of the HIV drug lopinavir/ritonavir (LPV/r) to be registered. |
| 2017-02-13 | Drugs for Neglected Diseases | Results Study confirms key therapeutic advance for children living with HIV and tuberculosis | DNDi dndi.org ↗
The study, presented as a late-breaker this week at the Conference on Retroviruses and Opportunistic Infections (CROI) in Seattle, provides essential evidence and data to counter the negative interactions between two critical HIV and TB treatments. |
| 2015-06-02 | Drugs for Neglected Diseases | Regulatory Child-friendly formulation of WHO-recommended treatment now approved by the US FDA for children living with HIV | DNDi dndi.org ↗
Infants and young children living with HIV will finally have access to an improved formulation of an antiretroviral (ARV) treatment, following the U.S. Food and Drug Administration’s (FDA) tentative approval last week of lopinavir/ritonavir (LPV/r) oral pellets developed by the Indian generic company Cipla. |
| 2012-03-06 | Merck Sharp & Dohme LLC | Results Results from Investigational Studies with VICTRELIS™ (boceprevir) Presented at the Conference on Retroviruses and Opportunistic Infections to Understand Potential Use in Patients Coinfected with Chronic Hepatitis C and HIV-1 merck.com ↗
In this study, concomitant administration of VICTRELIS with ritonavir (Norvir ® ) in combination with atazanavir (Reyataz ® ) or darunavir (Prezista ® ), or with lopinavir/ritonavir (Kaletra ® ) resulted in reduced exposures of the HIV medicines and VICTRELIS. |
| 2012-02-08 | Merck Sharp & Dohme LLC | Results Merck Informs U.S. Physicians of Results of Drug Interaction Study of Co-Administration of VICTRELIS™ with Ritonavir-Boosted HIV Protease Inhibitors merck.com ↗
In this study, concomitant administration of VICTRELIS with ritonavir (Norvir®) in combination with atazanavir (Reyataz®) or darunavir (Prezista®),or with lopinavir/ritonavir (Kaletra®) resulted in reduced exposures of the HIV medicines and VICTRELIS. |
| 2008-10-26 | Bristol-Myers Squibb | Results 96-Week Data From CASTLE Study Continue to Show Similar Efficacy Between Once-Daily REYATAZ(R) (atazanavir sulfate)/Ritonavir and Twice-Daily Lopinavir/Ritonavir In Previously Untreated HIV-1 Infected Adult Patients bms.com ↗
The CASTLE results demonstrated the non-inferiority of REYATAZ/r once daily versus lopinavir/r twice daily, each as part of HIV combination therapy in previously untreated HIV-1 infected adult patients. |
| 2008-08-05 | Bristol-Myers Squibb | Results CORRECTING and REPLACING CASTLE Data Showed Boosted REYATAZ(R) (atazanavir sulfate) and Lopinavir/r Achieved Similar Results for Undetectable Viral Load in Treatment-Naive HIV-1 Infected Patients, Regardless of Gender bms.com ↗
CASTLE DATA SHOWED BOOSTED REYATAZ ® (ATAZANAVIR SULFATE) AND LOPINAVIR/R ACHIEVED SIMILAR RESULTS FOR UNDETECTABLE VIRAL LOAD IN TREATMENT-NAIVE HIV-1 INFECTED PATIENTS, REGARDLESS OF GENDER |
| 2008-08-05 | Bristol-Myers Squibb | Results CASTLE Data Showed Boosted REYATAZ® (atazanavir sulfate) and Lopinavir/r Achieved Similar Results for Undetectable Viral Load in Treatment-Naive HIV-1 Infected Patients, Regardless of Gender bms.com ↗ |
| 2008-02-06 | Bristol-Myers Squibb | Results CASTLE Study Showed Similar Efficacy Between Once-Daily REYATAZ® (atazanavir sulfate)/ritonavir and Twice-Daily lopinavir/ritonavir at 48 Weeks in Previously Untreated HIV-Infected Adult Patients bms.com ↗ |
| 2006-09-28 | Vertex Pharmaceuticals Incorporated | Results Vertex Pharmaceuticals and GlaxoSmithKline Announce Virologic and Drug Resistance Results from Protease Inhibitor Study vrtx.com ↗
Although four PI mutations emerged during treatment, they did not confer reduced susceptibility to fosamprenavir or lopinavir. |
| 2006-08-17 | Vertex Pharmaceuticals Incorporated | Results Head-to-Head Study Comparing LEXIVA(R) (fosamprenavir calcium) to Kaletra Presented at IAC 2006 and Published in The Lancet vrtx.com ↗
This month, The Lancet published results of a study showing that HIV regimens using LEXIVA (Telzir) Tablets+ritonavir and Kaletra (lopinavir/ritonavir) Capsules both given twice-daily had comparable (non-inferior) efficacy and tolerability in adults who had no previous exposure to HIV medicines. |
| 2006-05-16 | Vertex Pharmaceuticals Incorporated | Results GlaxoSmithKline and Vertex Pharmaceuticals Announce Preliminary 48-Week Results from Head-to-Head Clinical Study of HIV Protease Inhibitors Lexiva (Telzir) and Kaletra in Treatment-naive Patients with HIV vrtx.com ↗
Based on these results from this study, researchers have concluded that Lexiva appears to be comparable to Kaletra and has met the primary endpoints of this non-inferiority trial. |
All press releases naming this drug 16 releases
Evidence & citations 18 cited values
Every value below carries the sentence it was read from. 254 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | lopinavir | “Generic names: Efavirenz/Emtricitabine/Tenofovir, Lamivudine/Zidovudine, Emtricitabine, Lamivudine, Abacavir/Lamivudine, Zidovudine, Abacavir/Lamivudine/Zidovudine,...” NCT00624195 ↗239“Patients with HIV who are virologically suppressed on a lopinavir/ritonavir combination highly active antiretroviral therapy (HAART) regimen but with elevated non-HDL...” NCT00120393 ↗ “This study will compare the ability of fosamprenavir 700 mg with ritonavir 100 mg twice a day or lopinavir 400 mg with ritonavir 100 mg twice a day both combined with a fixed...” NCT00085943 ↗ “Six hundred and eighty-eight antiretroviral-naive, HIV-1-infected patients were randomized in this double-blind, placebo-matched, multicenter, noninferiority study to receive a...” PMID 19542866 ↗ Jul 2009 “ART that concurrently contains combinations of non-nucleoside reverse transcriptase inhibitors (NNRTIs), such as efavirenz, and protease-inhibitors (PIs), such as...” NCT05044962 ↗ “one tablet of Truvada a day at standard dose of Tenofovir 300mg and Emtricitabine 200mg and four tablets of Kaletra once a day for a total dose of lopinavir 800mg and ritonavir...” NCT01614405 ↗ “The first-line combination provided to pregnant women will be standardized following consultation with the Ministry of Health, but will likely include ZDV, lamivudine (3TC) and...” NCT00753324 ↗ “Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised...” PMID 17617272 ↗ Jul 2007 “Evaluation of the Pharmacokinetics and Tolerability of Increased Dosage of Lopinavir/Ritonavir(LPV/r) in Individuals Experiencing Viremia on Standard Dose LPV/r Using LPV/r...” NCT00414284 ↗ “Tenofovir / emtricitabine + lopinavir / ritonavir for all HIV-1+2-infected patients and all women who do not use effective contraception or who have a history of nevirapine use...” NCT00495651 ↗ “Baseline regimen of antiretroviral therapy with a ritonavir- or cobicistat-boosted protease inhibitor (atazanavir, darunavir, or lopinavir) administered according to the...” NCT02397096 ↗ |
| Known as | A-157378-0 | ChEMBL registry synonym — accepted as the source's own label CHEMBL729 ↗ |
| Known as | ABT-378 | ChEMBL registry synonym — accepted as the source's own label CHEMBL729 ↗ |
| Known as | Aluviran | ChEMBL registry synonym — accepted as the source's own label CHEMBL729 ↗ |
| Known as | Kaletra | “Background regimen may consist of the following ritonavir (RTV)-boosted PIs (PI/r): lopinavir/r (Kaletra), atazanavir/r, darunavir/r, tipranavir/r, or fosamprenavir/r.” NCT01923311 ↗2“400 mg lopinavir and 100 mg ritonavir (Kaletra capsules, Abbott Laboratories)” NCT00966160 ↗ “Kaletra (lopinavir [LPVr])” NCT00192621 ↗ |
| Known as | Koletra | ChEMBL registry synonym — accepted as the source's own label CHEMBL729 ↗ |
| Known as | Lopinavir component of kaletra | ChEMBL registry synonym — accepted as the source's own label CHEMBL729 ↗ |
| Known as | Lopinavir, (s-(2s,4s,5s))- | ChEMBL registry synonym — accepted as the source's own label CHEMBL729 ↗ |
| Known as | lopinavir/r | “The study-treatment were lopinavir/r 100/400mg bid or indinavir/r 100/400mg bid for PI-class, for NNRTI-class, efavirenz or nevirapine and all NRTIs except D4T and DDC at usual dosage.” NCT00122668 ↗6“Background regimen may consist of the following ritonavir (RTV)-boosted PIs (PI/r): lopinavir/r (Kaletra), atazanavir/r, darunavir/r, tipranavir/r, or fosamprenavir/r.” NCT01923311 ↗ “protease inhibitors : lopinavir/r, darunavir/r ou atazanavir/r” NCT03256422 ↗ “Azidothimidine + lamivudine + lopinavir/r Or” NCT01174914 ↗ “lopinavir/r,” NCT02157311 ↗ |
| Known as | Lopinavirum | ChEMBL registry synonym — accepted as the source's own label CHEMBL729 ↗ |
| Known as | LPV | “DESIGN: ICE-001 is a phase IV, randomized, two-arm unblinded study, comparing the effect on immune reconstitution of open-label ritonavir (RTV)-enhanced lopinavir (LPV) to...” NCT00775606 ↗18“The ANRS 12174 trial assessed the efficacy and tolerance of lopinavir (LPV)-ritonavir (LPV/r) prophylaxis versus those of lamivudine (3TC) prophylaxis administered to breastfed...” PMID 27895016 ↗ Jan 2017 “Lopinavir (LPV) plasma AUC(0,τ), C(max) and Cτ decreased by 23%, 14% and 40%, respectively, following administration of lopinavir/ritonavir with GSK2248761.” PMID 22288567 ↗ Aug 2012 “Population PK models were developed for lopinavir (LPV) and ritonavir (RTV) to evaluate the impact of RTV on the oral clearance (CL/F) of LPV.” PMID 38247190 ↗ Jan 2024 “The two combinations are abacavir/lamivudine/zidovudine (ABC/3TC/ZDV) and zidovudine/lamivudine (ZDV/3TC) plus lopinavir/ritonavir (LPV/RTV).” NCT00086359 ↗ “The preferred study-supplied HAART regimen was lopinavir/ritonavir (LPV/RTV) plus fixed dose combination tenofovir/emtricitabine (TDF/FTC).” NCT00955968 ↗ “allowed PIs include atazanavir (ATV), darunavir (DRV), fosamprenavir (FPV), lopinavir (LPV), or saquinavir (SQV)” NCT01475838 ↗ “boosted lopinavir (LPV/rtv 200/50 mg 2 tbs BID) or boosted darunavir (DRV 400 mg 2 tbs plus RTV 100 mg QD)” NCT01905059 ↗ “allowed boosted 3rd ARV agents: lopinavir (LPV), atazanavir (ATV), darunavir (DRV)” NCT02285114 ↗ “Lopinavir (LPV) exposure is reduced during the third trimester of pregnancy.” PMID 19237646 ↗ Feb 2009 “Tenofovir (TDF) + emtricitabine (FTC) + lopinavir/ritonavir (LPV/RTV)” NCT00759070 ↗ |
| Known as | LPV/r | “ritonavir boosted lopinavir (LPV/r)” NCT02469246 ↗1“Kaletra (lopinavir [LPVr])” NCT00192621 ↗ |
| Known as | NANO-Lopinavir | “a new pharmaceutical formulation of lopinavir (NANO-lopinavir) in HIV negative healthy volunteers” NCT02631473 ↗ |
| Action | Inhibit | “BACKGROUND: With increasing recognition of the benefits of early antiretroviral therapy initiation in perinatally HIV-infected infants, data are needed regarding the...” PMID 19209098 ↗ Mar 2009 |
| Modality | Other / unclassified | “lopinavir-ritonavir plus zidovudine-lamivudine (the protease-inhibitor group)” PMID 20554983 ↗ Jun 2010 |
| Route | Oral | “when administered orally in antiretroviral-HIV-1 infected subjects” NCT00004578 ↗ |
| Target | CYP17A1 | “Lopinavir, but not ritonavir, inhibited CYP17A1 and CYP21A2 activity in H295R cells.” PMID 31633158 ↗ Aug 2020 |
| Target | CYP21A2 | “Lopinavir, but not ritonavir, inhibited CYP17A1 and CYP21A2 activity in H295R cells.” PMID 31633158 ↗ Aug 2020 |