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32 Diseases |  |
11 Trials |
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11 Trials |  |
1696 News |  |
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- || Prezista (darunavir) / J&J, Actemra IV (tocilizumab) / Roche, JW Pharma
Clinical, Journal: Tocilizumab and steroid treatment in patients with COVID-19 pneumonia. (Pubmed Central) - Sep 2, 2020
Early adjunctive treatment with tocilizumab, methylprednisolone or both may improve outcomes in non-intubated patients with COVID-19 pneumonia.
- || Prezista (darunavir) / J&J, Actemra IV (tocilizumab) / Roche, JW Pharma
Clinical, Review, Journal: Coronavirus Disease 2019 (COVID-19) in Children: Prevalence, Diagnosis, Clinical Symptoms, and Treatment. (Pubmed Central) - Aug 28, 2020
Antiviral medication (lopinavir, darunavir, favipiravir, remdesivir, ribavirin, oseltamivir, tocilizumab, and umifenovir), ACE inhibitors, interferon-α2b, co-therapy with azithromycin, inhaling iNO, and oxygen therapy can be used for treatment. For the treatment of children without any clinical and infection symptoms, home isolation protocol has been recommended.
- | Prezista (darunavir) / J&J, Genvoya (elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide) / Gilead
Trial completion, Enrollment change: PEP2: Body Compartment Pharmacokinetics of Anti- Retroviral Agents That May be Used for Future HIV Post- Exposure Prophylaxis. (clinicaltrials.gov) - Aug 27, 2020
P1, N=35, Completed, Sponsor: Emory University
For the treatment of children without any clinical and infection symptoms, home isolation protocol has been recommended. Recruiting --> Completed | N=58 --> 35
- | Prezista (darunavir) / J&J
Journal: An apparent paradox: resistance mutations in HIV-1 DNA predict improved virological responses to antiretroviral therapy. (Pubmed Central) - Aug 23, 2020
P3
Recruiting --> Completed | N=58 --> 35 Pre-existing NRTI and NNRTI RAMs are associated with improved virological responses to NRTI-sparing ART in sub-Saharan Africa, indicating a predictive effect that is independent of residual NRTI activity.
- | Prezista (darunavir) / J&J
Journal, Monotherapy: Evaluation of HIV-1 reservoir levels as possible markers for virological failure during boosted darunavir monotherapy. (Pubmed Central) - Aug 23, 2020
P3
HIV-1 reservoir markers correlate with therapy failure in ritonavir-boosted darunavir monotherapy. However, their role as a predictive marker combined with other markers in a routine clinical setting should be further explored.
- | Preclinical, Journal: Assessing the lymphoid tissue bioavailability of antiretrovirals in human primary lymphoid endothelial cells and in mice. (Pubmed Central) - Aug 23, 2020
PK studies of representative ARVs in LT of mice were concordant with HLEC bioavailability. These findings support further development of this approach and its translational predictability in humans.
- || Prezista (darunavir) / J&J
Clinical, Journal: Description of COVID-19 in HIV-infected individuals: a single-centre, prospective cohort. (Pubmed Central) - Aug 22, 2020
HIV-infected individuals should not be considered to be protected from SARS-CoV-2 infection or to have lower risk of severe disease. Generally, they should receive the same treatment approach applied to the general population.
- | Prezista (darunavir) / J&J
Retrospective data, Journal: Morning vs. evening administration of antiviral therapy in COVID-19 patients. A preliminary retrospective study in Ferrara, Italy. (Pubmed Central) - Aug 22, 2020
The morning regimen was associated with a significant reduction in CRP values. Further confirmations with larger and multicenter samples of patients could reveal novel potentially useful insights.
- Prezista (darunavir) / J&J
[VIRTUAL] Development of the generic pregnancy physiologically based pharmacokinetic (PBPK) model to support regulatory evaluations of the safety and efficacy of therapeutic agents (On Demand Oral) - Aug 20, 2020 - Abstract #ACSFall2020ACS-Fall_7374;
A user-friendly interface is under development to facilitate the usage of the adaptable PBPK model by reviewers or non-modelers. Furthermore, by incorporating the population analysis, the current model can be expanded to simulate drug pharmacokinetics based on population variability.
- || Clinical, PK/PD data, Journal: Population pharmacokinetics of dolutegravir: influence of drug-drug interactions in a real-life setting. (Pubmed Central) - Aug 20, 2020
Furthermore, by incorporating the population analysis, the current model can be expanded to simulate drug pharmacokinetics based on population variability. Patients co-treated with dolutegravir and rifampicin might benefit from therapeutic drug monitoring and individualized dosage increase, up to 100 mg/12 h in some cases.
- || Clinical, Journal: Antiretroviral drug reduction in highly experienced HIV-infected patients receiving a multidrug regimen: the ECOVIR study. (Pubmed Central) - Aug 20, 2020
Patients co-treated with dolutegravir and rifampicin might benefit from therapeutic drug monitoring and individualized dosage increase, up to 100 mg/12 h in some cases. In experienced patients with high-level resistance, individualized strategies based on expert advice can offer DR regimen options with fewer drug-drug interactions and a significant economic impact while ensuring virological success.
- Pifeltro (doravirine) / Merck (MSD)
[VIRTUAL] Efficacy and Safety of Doravirine in Treatment-Naïve Adults ≥50 Years Old With HIV-1 () - Aug 14, 2020 - Abstract #IDWeek2020IDWEEK_1262;
DOR is a beneficial option for adults ≥50 years old, given its similar efficacy and favorable safety profile compared to younger adults. Doravirine Phase 2 and Phase 3 Trials in Treatment-Naïve Adults
- | Prezista (darunavir) / J&J
Journal: New mechanisms of resistance in virological failure to protease inhibitors: selection of non-described protease, Gag and Gp41 mutations. (Pubmed Central) - Aug 12, 2020
In some cases of VF to PIs, we observed the emergence of protease, Gag or Gp41 mutations that had not previously been associated with VF or PI resistance. These mutations should be further studied, in particular the 15V/64M/70R pattern in the protease gene identified among CRF02_AG viruses.
- | Journal: SARS CoV-2: Recent Reports on Antiviral Therapies Based on Lopinavir/Ritonavir, Darunavir/Umifenovir, Hydroxychloroquine, Remdesivir, Favipiravir and Other Drugs for the Treatment of the New Coronavirus. (Pubmed Central) - Aug 12, 2020
Since the recoveries/deaths ratio in the last weeks significantly increased, especially in China, it is clear that the experimental antiviral therapy, together with the availability of intensive care unit beds in hospitals and rigorous government control measures, all play an important role in dealing with this virus. This also stresses the urgent need for the scientific community to devote its efforts to find other more specific antiviral strategies.
- | Prezista (darunavir) / J&J
Journal: Periconceptional exposure to lopinavir, but not darunavir, impairs decidualization: a potential mechanism leading to poor birth outcomes in HIV-positive pregnancies. (Pubmed Central) - Aug 11, 2020
L.S. reports personal fees from ViiV Healthcare for participation in a Women and Transgender Think Tank.
- | Review, Journal: Anti-Inflammatory Properties of Drugs Used to Control COVID-19 and their Effects on the Renin-Angiotensin System and Angiotensin-Converting Enzyme-2. (Pubmed Central) - Aug 11, 2020
Herein, we present a review of the current drugs, which are being used in the management of the disease and their anti-inflammatory properties. We also investigated if these drugs directly interact with Angiotensin-Converting Enzyme (ACE 2), which is a crucial component of the virus entry to the cells.
- | Prezista (darunavir) / J&J
Trial completion, Enrollment change: Drug-drug Interactions Between Antiretroviral Drugs and Cardiovascular Drugs in Elderly Patients (clinicaltrials.gov) - Aug 8, 2020
P=N/A, N=21, Completed, Sponsor: Centre Hospitalier Universitaire Vaudois
We also investigated if these drugs directly interact with Angiotensin-Converting Enzyme (ACE 2), which is a crucial component of the virus entry to the cells. Recruiting --> Completed | N=60 --> 21
- | Prezista (darunavir) / J&J, Prezcobix (darunavir/cobicistat) / Gilead, J&J
Journal: Lack of Antiviral Activity of Darunavir against SARS-CoV-2. (Pubmed Central) - Aug 4, 2020
Recruiting --> Completed | N=60 --> 21 Overall, the data do not support the use of DRV for the treatment of COVID-19.
- || Prezista (darunavir) / J&J, ritonavir / Generic mfg., emtricitabine/tenofovir disoproxil fumarate / Generic mfg.
Clinical, PK/PD data, Journal: Pharmacokinetics of Tenofovir Alafenamide, Tenofovir, and Emtricitabine Following Administration of Coformulated Emtricitabine/Tenofovir Alafenamide in Healthy Japanese Subjects. (Pubmed Central) - Jul 31, 2020
Boosting effects of RTV and COBI on TAF bioavailability were slightly lower than we expected, less than a 2.5-fold increase, but it was within the range of exposures associated with efficacy and safety in phase 3 studies. Therefore, it was not considered clinically relevant.
- || Prezista (darunavir) / J&J
Clinical, PK/PD data, Journal: Evaluating darunavir/ritonavir dosing regimens for HIV-positive pregnant women using semi-mechanistic pharmacokinetic modelling. (Pubmed Central) - Jul 31, 2020
Darunavir/ritonavir 600/100 mg q12h should therefore be the preferred regimen during pregnancy unless (adherence) issues dictate q24h dosing. The value of alternative dosing regimens seems limited.
- || Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
Clinical, Journal, Real-World Evidence: Real-World Experience with Dolutegravir-Based Two-Drug Regimens. (Pubmed Central) - Jul 30, 2020
Prior to commercial availability of the single-tablet 2DRs, DTG 2DR components were primarily used in treatment-experienced patients for treatment simplification and avoidance of long-term toxicities. Many of these patients achieved and maintained virologic suppression, with low discontinuation rates.
- ||| Clinical, P3 data, Journal, Head-to-Head: Doravirine versus ritonavir-boosted darunavir in antiretroviral-naive adults with HIV-1 (DRIVE-FORWARD): 96-week results of a randomised, double-blind, non-inferiority, phase 3 trial. (Pubmed Central) - Jul 25, 2020
P3
Many of these patients achieved and maintained virologic suppression, with low discontinuation rates. These results through 96 weeks support the efficacy and safety results reported previously for doravirine at 48 weeks, supporting the use of doravirine for the long-term treatment of adults with previously untreated HIV-1 infection.
- || Prezista (darunavir) / J&J, lamivudine / Generic mfg.
Clinical, Journal: Association of maternal antiretroviral use with microcephaly in children who are HIV-exposed but uninfected (SMARTT): a prospective cohort study. (Pubmed Central) - Jul 25, 2020
These results through 96 weeks support the efficacy and safety results reported previously for doravirine at 48 weeks, supporting the use of doravirine for the long-term treatment of adults with previously untreated HIV-1 infection. These findings support consideration of alternatives to efavirenz as part of first-line antiretroviral therapy for pregnant women.
- | Prezista (darunavir) / J&J
Journal: Exploring the energetic basis of binding of currently used drugs against HIV-1 subtype CRF01_AE protease via molecular dynamics simulations. (Pubmed Central) - Jul 24, 2020
Overall, the data presented in this study can guide the computer-aided rational design of more potent drugs targetting HIV-1 PR. Communicated by Ramaswamy H. Sarma.
- | Prezista (darunavir) / J&J
Journal: An in silico pharmacological approach toward the discovery of potent inhibitors to combat drug resistance HIV-1 protease variants. (Pubmed Central) - Jul 21, 2020
Lopinavir (LPV) and darunavir (DRV), two second-generation drugs are the most potent among PIs, hustling the drug resistance when mutations occur in the active and nonactive site of the protease (PR)...Interestingly, NCI-524545 and ZINC12866729 exhibit direct interactions with I50/50' by replacing the conserved water molecule as evidenced by MDS, which indicates the credible potency of these compounds. Hence, we concluded that NCI-524545 and ZINC12866729 have great puissant to restrain the role of drug resistance HIV-1 PR variants, which can also show better activity through in vivo and in vitro conditions.
- | Prezista (darunavir) / J&J
Journal: HIV-1 protease, Gag and gp41 baseline substitutions associated with virological response to a PI-based regimen. (Pubmed Central) - Jul 21, 2020
In this study, new baseline substitutions in Gag, protease and g41, potentially impacting PI-based regimen outcome, were evidenced. Phenotypic analyses are required to confirm their role in the PI-resistance mechanism.
- || Clinical, Journal: Covid-19: A systemic disease treated with a wide-ranging approach: A case report. (Pubmed Central) - Jul 21, 2020
His condition improved, and in the ensuing days, the treatment gradually switched to a high-flow nasal cannula (HFNC); after 18 days, the patient's clinical condition was good.The successful results we have been able to obtain are closely associated with avoidance of invasive ventilation that may lead to intensive care unit (ICU)-related superinfections. In our opinion, it is fundamental to understand that COVID-19 is a systemic disease that is a consequence of an overwhelming inflammatory response, which can cause severe medical conditions, even in young patients.
- || Prezista (darunavir) / J&J
Clinical, Journal: Polymorphisms and drug resistance analysis of HIV-1 isolates from patients on first line antiretroviral therapy (ART) in South-eastern Nigeria. (Pubmed Central) - Jul 10, 2020
Interpretation based on Stanford algorithm showed that Darunavir/ritonavir is the only regimen whose potency was not compromised by the circulating mutations. Identification of major and minor PI resistance mutations in this study underscores the need for drug resistance testing prior to initiation of second line antiretroviral therapy in Nigeria.
- | Prezista (darunavir) / J&J, ritonavir / Generic mfg.
Journal: Data and Text Mining Help Identify Key Proteins Involved in the Molecular Mechanisms Shared by SARS-CoV-2 and HIV-1. (Pubmed Central) - Jul 10, 2020
We applied a text and data mining workflow and identified a list of 46 targets, which can be essential for the development of infections caused by SARS-CoV-2 and HIV-1. We show that SARS-CoV-2 and HIV-1 share some molecular pathways involved in inflammation, immune response, cell cycle regulation.
- | Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
Journal: Trends in HIV-1 Drug Resistance Mutations from a U.S. Reference Laboratory from 2006 to 2017. (Pubmed Central) - Jul 9, 2020
Sequences with ≥1 darunavir DRM declined from 18.1% to 4.8% by 2017...Prevalence of elvitegravir-associated DRMs T66A/I/K, E92Q, S147G, and the dolutegravir-associated DRM R263K increased...These trends may inform the need for baseline genotypic resistance testing. The detection of treatment-emergent DRMs in serially-tested patients confirms the value of genotypic testing following virologic failure.
- || Prezista (darunavir) / J&J, ritonavir / Generic mfg., Tivicay (dolutegravir) / ViiV Healthcare
Clinical, Journal: Efficacy and safety of dolutegravir plus boosted-darunavir dual therapy among highly treatment-experienced patients. (Pubmed Central) - Jul 9, 2020
P=N/A
The detection of treatment-emergent DRMs in serially-tested patients confirms the value of genotypic testing following virologic failure. In highly treatment-experienced who were virologically suppressed, switching to the combination of dolutegravir plus boosted-darunavir dual therapy was effective and well tolerated, improving lipid and renal parameters.
- | Prezista (darunavir) / J&J
Trial completion date: A Study of Darunavir in Combination With Cobicistat or Ritonavir, and Dabigatran Etexilate in Healthy Participants (clinicaltrials.gov) - Jul 7, 2020
P1, N=28, Recruiting, Sponsor: Janssen Research & Development, LLC
In highly treatment-experienced who were virologically suppressed, switching to the combination of dolutegravir plus boosted-darunavir dual therapy was effective and well tolerated, improving lipid and renal parameters. Trial completion date: Nov 2020 --> Mar 2021
- | Prezista (darunavir) / J&J
Journal: Low frequency of protease inhibitor resistance mutations and insertions in HIV-1 subtype C protease inhibitor naïve sequences. (Pubmed Central) - Jul 7, 2020
Occurrence of insertions in subtype C viruses is rare and viruses remain sensitive to currently used PIs (Lopinavir/r, Atazanavir/r and Darunavir/r). However, ongoing characterization of isolates is required to identify changes that may impact PI treatment since PIs are part of standard SA regimens.
- | Prezista (darunavir) / J&J
Journal: Drug susceptibility and replication capacity of a rare HIV-1 subtype C protease hinge region variant. (Pubmed Central) - Jul 7, 2020
These variations are classified as secondary mutations, and indirectly impact inhibitor binding, enzyme fitness and enzyme stability. Additionally, polymorphisms arising in Gag can modify the impact of protease with regards to viral replication and susceptibility to protease inhibitors.
- || Prezista (darunavir) / J&J, lamivudine / Generic mfg., Tivicay (dolutegravir) / ViiV Healthcare
Clinical, Observational data, Journal, HEOR: The comparative effectiveness of NRTI-sparing dual regimens in emulated trials using observational data from the Swiss HIV Cohort Study. (Pubmed Central) - Jul 7, 2020
Estimates of relative effectiveness suggest that both dolutegravir regimens are not inferior to these alternative regimens. All four regimens seem suitable for patients needing an NRTI-sparing regimen: there were few virologic failures and few treatment changes due to toxicity.
- | Prezista (darunavir) / J&J, fluconazole / Generic mfg.
Journal: Darunavir inhibits Cryptococcus neoformans/Cryptococcus gattii species complex growth and increases the susceptibility of biofilms to antifungal drugs. (Pubmed Central) - Jul 7, 2020
Darunavir presents antifungal activity against planktonic cells of Cryptococcus species and synergism with amphotericin B. In addition, darunavir led to reduced biofilm formation and showed activity against mature biofilms of Cryptococcus species. Activity of the antifungals against mature biofilms was enhanced in the presence of darunavir.
- | Journal: Doravirine: a new non-nucleoside reverse transcriptase inhibitor for the treatment of HIV infection. (Pubmed Central) - Jul 1, 2020
Doravirine has a more favorable drug interaction profile compared with earlier NNRTIs as it neither inhibits nor induces the cytochrome P450 3A4 (CYP3A4) enzyme. Doravirine has been added to the category of Recommended Initial Regimens in Certain Clinical Situations in the United States Department of Health and Human Services Antiretroviral Guidelines for Adults and Adolescents.
- | Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
Retrospective data, Journal: Two treatment strategies for management of Neurosymptomatic cerebrospinal fluid HIV escape in Pune, India. (Pubmed Central) - Jul 1, 2020
Four deaths were noted, 2 of which were in individuals who interrupted ART.This is a unique sCVE cohort that was managed with 1 of 2 approaches based on treatment history and the availability of GRT. At least 75% of participants responded to either approach with virologic suppression and improvement in symptoms.
- | Prezista (darunavir) / J&J, emtricitabine/tenofovir disoproxil fumarate / Generic mfg.
Journal: Lower pretreatment gut integrity is independently associated with fat gain on antiretroviral therapy. (Pubmed Central) - Jun 29, 2020
While ART induces changes in soluble markers of gut barrier dysfunction (with subtle differences between regimens), the extent to which they improve or worsen gut barrier function remains unclear. Nevertheless, markers of gut barrier dysfunction in ART-naïve individuals predict increases in total and visceral abdominal fat with treatment initiation.
- | Prezista (darunavir) / J&J
Journal: Novel protease inhibitors containing C-5-modified bis-THF and aminobenzothiazole as P2 and P2' ligands that exert potent antiviral activity against highly multidrug-resistant HIV-1 with high genetic barrier against the emergence of drug resistance. (Pubmed Central) - Jun 26, 2020
Darunavir (DRV) represents a most efficacious and well-tolerated protease inhibitor (PI) with a high genetic barrier to the emergence of drug-resistant HIV-1...Moreover, GRL-057-14's P1-bis-fluoro-methylbenzene form strong hydrogen bonding and effective van der Waals interactions. The present data suggest that the combination of C-5-aminoalkyl-bis-THF, P1-bis-fluoro-methylbenzene, and P2'-Cp-Abt confers highly potent activity against wild-type and multi-PI-resistant HIV strains and warrant further development of the three PIs, in particular, GRL-057-14, as potential therapeutic for HIV-1 infection and AIDS.
- Prezista (darunavir) / J&J
[VIRTUAL] Darunavir is cost-effective compared to lopinavir for second-line treatment in sub-Saharan Africa: A modeling analysis (Poster Channel - Track E) - Jun 22, 2020 - Abstract #AIDS2020AIDS_3716;
- Prezista (darunavir) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
[VIRTUAL] Sufficient plasma levels within 24 weeks of antiretroviral HIV therapy of dolutegravir combined with boosted darunavir: A pharmacologic subgroup analysis of the DUALIS study (Poster Channel - Track B) - Jun 22, 2020 - Abstract #AIDS2020AIDS_2442;
- [VIRTUAL] Cost-based estimated prices for key HIV, HCV, and MDRTB medicines (Abstract Sessions On-Demand Channel) - Jun 22, 2020 - Abstract #AIDS2020AIDS_1930;
Current prices for medicines are up to 1000 times more than cost-based estimated generic prices. Originator prices are often incongruous with country income level, with implications for access and scale-up of treatment programmes.
- [VIRTUAL] Surveillance of transmitted HIV drug resistance among treatment-na€ıve children under 18 months in Brazil (2009 to 2018) (Abstract Sessions On-Demand Channel) - Jun 22, 2020 - Abstract #AIDS2020AIDS_1813;
The high prevalence of transmitted HIV-DR to NNTRI in CLWHIV is a matter of concern because there is a limited number of treatment options for this population. The incorporation of new drugs, such as integrase inhibitors, as prophylaxis and treatment, is essential to tackle resistance to NNTRI and improve treatment outcomes in this age group.
- [VIRTUAL] HIV-infected treatment-experienced children and adolescents from Sub-Saharan Africa: Clinical outcomes on thirdline antiretroviral treatment in the New Horizons drug donation programme (Abstract Sessions On-Demand Channel) - Jun 22, 2020 - Abstract #AIDS2020AIDS_1809;
Treatment-experienced paediatric and adolescent patients failing a second-line PI-based ART had high level HIV viraemia and high levels of NRTI thymidine analogue and PI mutations. Among those patients with VL results available at 6 and 12 months on thirdline ART containing DRV and/or ETR, the majority achieved virologic suppression.
- Prezista (darunavir) / J&J, ritonavir / Generic mfg., lamivudine / Generic mfg.
[VIRTUAL] Comparative efficacy and safety of a combination therapy of dolutegravir and lamivudine versus 3-drug antiretroviral regimens in treatment-na€ıve HIV-1 infected patients at 96 weeks: A systematic review and network meta-analysis (Abstract Sessions On-Demand Channel) - Jun 22, 2020 - Abstract #AIDS2020AIDS_1786;
Background: Dolutegravir+lamivudine (DTG + 3TC) has been shown to be comparable to guideline recommended 3-drug antiretroviral treatments (ARTs) in HIV up to week 48...The treatment difference for viral suppression at WK96 for DTG + 3TC compared to the other 10 ARTs ranged from -3% (-7%, 0%) versus DTG+TDF (or) TAF/FTC to 13% (4%, 23%) versus ritonavir-boosted darunavir (DRV/r) + TDF/FTC. DTG + 3TC offers comparable and durable efficacy and safety to guideline recommended 3-drug regimen with reduced exposure to ARTs for na€ıve patients starting treatment.
- Prezista (darunavir) / J&J, Intelence (etravirine) / J&J, Isentress (raltegravir) / Merck (MSD)
[VIRTUAL] Third-line antiretroviral therapy including raltegravir, darunavir/ritonavir and/or etravirine is well tolerated and achieves durable virologic suppression over 144 + weeks in resource-limited settings ACTG: A5288 strategy trial (Abstract Sessions On-Demand Channel) - Jun 22, 2020 - Abstract #AIDS2020AIDS_1503;
DTG + 3TC offers comparable and durable efficacy and safety to guideline recommended 3-drug regimen with reduced exposure to ARTs for na€ıve patients starting treatment. Third-line regimens containing RAL, DRV/r and/or ETR were very well tolerated and provided a high rate of durable virologic suppression among people living with HIV in RLS.
- | Prezista (darunavir) / J&J
Journal: Structural studies of antiviral inhibitor with HIV-1 protease bearing drug resistant substitutions of V32I, I47V and V82I. (Pubmed Central) - Jun 18, 2020
These inhibitors contain diverse chemical modifications on the darunavir scaffold and form new interactions with wild type protease, however, the measured inhibition constants for PR mutant range from 17 to 40 nM or significantly worse than picomolar values reported for wild type enzyme...Instead, the basic amine at P2 of inhibitor together with mutation V82I induces two alternate conformations for the side chain of Arg8 with new interactions with inhibitor and Leu10. Hence, inhibition is influenced by small coordinated changes in hydrophobic interactions.
- || Prezista (darunavir) / J&J
Clinical, Journal: Darunavir does not prevent SARS-CoV-2 infection in HIV patients. (Pubmed Central) - Jun 14, 2020
Hence, inhibition is influenced by small coordinated changes in hydrophobic interactions. No abstract available
- |||| Prezista (darunavir) / J&J, ritonavir / Generic mfg., lopinavir/ritonavir / Generic mfg.
Clinical: Case series (N=32): Pts w/ #COVID19 on direct oral anticoagulants who started antivirals (lopinavir, ritonavir, darunavir) had alarming ⬆️ in DOAC trough levels (>6-fold ⬆️ comp to pre‐hospitalization). @US_FDA @FDA_Drug_Info @DrAbernethyFDA HT @mtmdphd https://t.co/clhYJAYF74 (Twitter) - Jun 12, 2020