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Darunavir

Darunavir is a protease inhibitor medication used to treat human immunodeficiency virus (HIV) infection.
It works by blocking the action of HIV protease, an enzyme essential for the replication of the virus.
Darunavir is often used in combination with other antiretroviral drugs to suppress viral load and slow the progression of HIV disease.
Researchers can use PubCompare.ai to optimize Daruzavir research by enhancing reproducibility and accuracy, locating relevant protocols, and utilizing AI-driven comparisons to identify the best products and methods for their studies.
This streamlined approach can help researchers achieve more reliable results in their Darunavir-related investigations.

Most cited protocols related to «Darunavir»

Substrate 1 was dissolved at a concentration of 1.0 mM in DMF containing TFA (0.1% v/v). Fluorescence of the EDANS moiety was measured on a M1000 Pro plate reader from Tecan (Maennedorf, Switzerland) by excitation at 340 nm and observation of emission at 490 nm. A fluorophore calibration was performed to enable quantitation of assay data. The product exhibits a fluorescence of 70 RFU/nM at a gain setting of 216, and all assays were performed at this gain setting unless indicated otherwise. Assays were performed in a Corning black, flat bottom, non-binding surface, 96-well plate. Assays were conducted at room temperature in 200 μL of 50 mM sodium acetate buffer, pH 5.0, containing NaCl (0.10 M), DMF (2% v/v), substrate 1 (1–40 μM), and HIV-1 protease (25 pM–6.5 nM). Assays with 30 and 40 μM of substrate 1 required 3% and 4% v/v DMF, respectively. Inhibition assays were conducted with picomolar–nanomolar inhibitor (depending on the enzyme concentration and Ki value) and 10 μM substrate 1. Inhibition assays were monitored for until ≤7% of the substrate was converted to product. Initial velocities were measured in quadruplicate.
Solution concentrations of HIV-1 protease (10.7 kDa) was determined by measuring the absorbance at 280 nm and estimating the extinction coefficient as 12,500 M−1cm−1 with software from ExPASy28 (link). The fraction of active enzyme was determined by active-site titration using darunavir as the titrant and found to be 76% with respect to the value based on the A280 nm. Fluorescence was monitored over the linear range of the detector, which corresponds to 700 nM of product formation at a gain setting of 216.
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Publication 2015
5-((2-aminoethyl)amino)naphthalene-1-sulfonic acid Biological Assay Buffers Darunavir Enzymes Extinction, Psychological Fluorescence p16 protease, Human immunodeficiency virus 1 Psychological Inhibition Sodium Acetate Sodium Chloride Titrimetry
The PubMed/MEDLINE, Embase, and Cochrane databases were systematically searched (up to August 2013) to identify randomized controlled trials (RCTs) evaluating efficacy and/or safety of ATV/r, DRV/r, DTG, EFV, EVG/c, LPV/r, RAL, or RPV in treatment-naive HIV-1 patients. PubMed and EMBASE search terms were “HIV-1 [mesh] OR HIV infections [mesh] NOT pregnancy [mesh] AND ((dolutegravir OR GSK1349572) OR (efavirenz OR Sustiva OR Stocrin OR DMP-266) OR (raltegravir OR Isentress OR MK-0518) OR (elvitegravir OR GS-9137 OR JTK-303) OR (rilpivirine OR Edurant OR TMC 278) OR (darunavir OR Prezista OR TMC-114) OR (atazanavir OR Reyataz OR BMS-232632) OR (lopinavir OR ABT-378 OR Aluviran OR Koletra OR Kaletra) OR (Atripla OR Quad OR Stribild OR Eviplera OR Complera))”. The ClinicalTrials.gov registry, US FDA summary basis of approvals, EMA EPAR scientific discussions, and references of published systematic reviews and meta-analyses were also searched for any additional data. Abstracts of the 2013 meeting of the International AIDS Society and the Interscience Conference on Antimicrobial Agents and Chemotherapy were searched to identify recent presentations. Two phase 3 studies of DTG with data available after August 2013 were also included.
Study selection was conducted by two independent researchers who performed an initial review and selection of study titles/abstracts followed by full text review and selection. Disagreements between the reviewers were resolved by consensus. Pre-specified inclusion criteria included treatment-naive patients with HIV-1 infection; studies published in English; phase 3 or 4 RCT; patients aged ≥13 years; use of at least one of the third agents of interest; and reporting at least one of the efficacy outcomes of interest after 48 weeks of treatment. Non-randomized observational studies; single-arm studies; and studies examining different dosages of the same drug, structured treatment interruptions, maintenance treatments, or treatment switching were excluded, as were publications where outcomes specific to a treatment-naive population could not be distinguished. Studies reporting outcomes such that results could not be obtained for each treatment arm individually were also excluded. The Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines were followed through all phases in the study [14] (link).
Three researchers independently abstracted data from the final selection of studies into a structured Microsoft Access database and data were reconciled for accuracy. The Effective Public Health Practice Project Quality Assessment, a quality assessment tool, was used to assess selection bias, study design, confounders, blinding, data collection methods, and withdrawals and dropouts [15] (link).
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Publication 2014
ABT 378 Acquired Immunodeficiency Syndrome Aftercare Atazanavir Atripla BMS 232632 Complera Conferences Darunavir DMP 266 efavirenz elvitegravir GS 9137 HIV-1 HIV Infections Infection Isentress JTK-303 Kaletra Lopinavir Microbicides MK 0518 Patients Pharmaceutical Preparations Pharmacotherapy Pregnancy Prezista Raltegravir Reyataz Rilpivirine Safety Stocrin Stribild Sustiva TMC 114 TMC 278

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Publication 2017
Animals Animals, Laboratory Autopsy Cells Darunavir Diet Disease Progression Females Herpesvirus 1, Cercopithecine Human respiratory syncytial virus Infection Institutional Animal Care and Use Committees isolation Macaca mulatta Maraviroc Metals Plasma Primates Proteins Raltegravir Ritonavir RNA, Viral Superinfection Tenofovir Therapeutics Treatment Protocols Tuberculosis Viremia Virus
Every six months the CPQA PT program offered prepared plasma samples containing pre-specified concentrations (unknown to CPLs) of up to 21 ARV analytes: abacavir (ABC), amprenavir (APV), atazanavir (ATV), darunavir (DRV), didanosine (DDI), efavirenz (EFV), emtricitabine (FTC), etravirine (ETR), indinavir (IDV), lamivudine (3TC), lopinavir (LPV), maraviroc (MVC), nelfinavir (NFV), nevirapine (NVP), raltegravir (RGV), ritonavir (RTV), saquinavir (SQV), stavudine (D4T), tenofovir (TFV), tipranavir (TPV), zidovudine (ZDV). In each round and for each ARV, 5 concentrations, spanning an expected therapeutic range of each ARV, as well as occasional concentrations below or above, were provided. Samples are prepared by an outside subcontractor and tested by the CPQA lab prior to distribution. PT samples were stored at −70 ± 15°C and then shipped on dry ice to participating laboratories with detailed instructions. Upon arrival, each laboratory confirmed sample integrity and indicated planned reporting of specific analytes. Results were reported either through an online Laboratory Data Management System (LDMS) or via a template which was then uploaded into the LDMS database. At the end of the submission period, a completeness evaluation was performed to confirm that all planned results were received; discrepancies were queried for resolution. To summarize the proficiency of individual labs, a pre-specified scoring algorithm was applied to the RCs (see next paragraph). The scoring algorithm reflects US Clinical Laboratory Improvement Act (CLIA) PT regulations[13 (link)]. After review and approval by the CPQA advisory board chair, a final report was sent to the participating laboratories (with laboratories de-identified) and key leadership (laboratories identified per network leader).
An individual RC is deemed Acceptable provided a concentration is present where expected, and the concentration is within 20% of the final target (FT)[14 (link)]. (If a concentration is reported as below the lower limit of quantification (BLQ), and the run lower limit was below 80%*FT, the concentration was labeled Unacceptable.) For a given prepared sample, if the number of labs reporting for that sample is large enough, the variability between CPLs is small enough (≤15%) and the percent deviation of the group mean (GM, determined after removal of outliers, if any)from the weighed-in value (WIV) is >5%, the FT is set to the GM. Otherwise, FT is set to the WIV. At the analyte level, a CPL’sperformance is deemed Satisfactory for the round provided at least 80% of RCs are Acceptable. If the CPL score is <80% for an analyte, the CPL submits a corrective action plan to reestablish accuracy; a root cause is requested. Finally, in accordance with CLIA rules, a lab is classified as successful for an analyte provided the round-specific score was Satisfactory in at least 2 of the last 3 rounds (including the current).
Publication 2013
abacavir amprenavir Atazanavir Clinical Laboratory Services Darunavir Dry Ice efavirenz etravirine Indinavir Lopinavir Maraviroc Nelfinavir Nevirapine Plant Roots Plasma Raltegravir Ritonavir Saquinavir Tenofovir Therapeutics tipranavir Zidovudine
Study A5257 was a Phase 3, randomized, open label trial. Participants were followed, regardless of meeting an endpoint, for 96 weeks after enrollment of the final volunteer. Participants were randomly assigned 1:1:1 to receive one of three regimens: 300 mg of atazanavir (Reyataz, Bristol-Myers Squibb) with 100 mg of ritonavir (Norvir, Abbott Laboratories) both once daily (ritonavir-boosted atazanavir), 800 mg of darunavir (Prezista, Janssen Therapeutics) with 100 mg of ritonavir both once daily (ritonavir-boosted darunavir), or 400 mg of raltegravir (Isentress, Merck Inc.) twice daily – each with a fixed-dose combination of 300 mg of tenofovir DF plus 200 mg of emtricitabine (Truvada, Gilead Sciences). Randomization used permuted blocks stratified according to the HIV-1 RNA level (≥100,000 vs. <100,000 copies/mL) with balancing by institution. To ensure treatment balance by cardiovascular risk for an embedded cardiovascular substudy (8 (link)), randomization was stratified by intent to participate in the substudy and Framingham 10-year risk of myocardial infarction or coronary death (<6% vs. ≥6%). Screening HIV-1 RNA levels were performed at Clinical Laboratory Improvement Amendments compliant laboratories, subsequent levels were measured using the Abbott RealTime HIV-1 assay at Johns Hopkins University. Study evaluations were completed before entry, at entry, at weeks 4, 8, 16, 24, 32 and every 16 weeks thereafter.
At the time of protocol-defined virologic failure, genotyping of the HIV-1 reverse transcriptase and protease regions was performed at both Brigham and Women’s Hospital and at the University of Alabama, Birmingham; samples obtained at study entry were also assayed concurrently. Genotyping of the HIV-1 integrase region was performed in batch at the end of the study at Brigham and Women’s Hospital for subjects with virologic failure on raltegravir and for a small number of randomly selected participants from each PI-containing arm. In the event of treatment changes for virologic or tolerability failure, within-class substitutions for protease inhibitor-regimens were recommended but not mandated. Adverse events were graded using the 2004 Division of AIDS toxicity scale. (9 )
Publication 2014
Acquired Immunodeficiency Syndrome Atazanavir atazanavir, ritonavir drug combination AT protocol Cardiac Death Cardiovascular System Clinical Laboratory Services Darunavir Emtricitabine Endopeptidases HIV-1 Isentress Myocardial Infarction Norvir p31 integrase protein, Human immunodeficiency virus 1 Prezista Protease Inhibitors Raltegravir reverse transcriptase, Human immunodeficiency virus 1 Reyataz Ritonavir Tenofovir Disoproxil Fumarate Testing, AIDS Treatment Protocols Truvada Voluntary Workers Woman

Most recents protocols related to «Darunavir»

OATP1B1, OATP1B3, NTCP and vector control cell lines were cultured and subsequent transporter assays conducted as described above using the same transporter‐specific probe substrates and incubation times. For OATP1B1, the probe substrate was [3H]‐estradiol 17β‐D‐glucuronide (0.02 μM) incubated for 2 min, with rifamycin SV (100 μM) as positive control inhibitor. For IC50 determinations, the only difference to the method performed above was that the 15‐min pre‐incubation step contained a range of six concentrations of protease inhibitor drug, and subsequent incubations were conducted with the same six concentration levels of drug rather than with a single concentration. All four protease inhibitor drugs were studied against OATP1B1 using pre‐incubation/incubation concentrations of either 0.1, 0.3, 1, 3, 10 and 30 μM for atazanavir and darunavir, or 0.03, 0.1, 0.3, 1, 3 and 10 μM for lopinavir and ritonavir. Based upon the results determined from the inhibition screen, only atazanavir and lopinavir were studied against OATP1B3 or NTCP using concentrations of 0.1, 0.3, 1, 3, 10 and 30 μM and 0.03, 0.1, 0.3, 1, 3 and 10 μM, or 0.3, 1, 3, 10, 30 and 50 μM and 0.1, 0.3, 1, 3, 10 and 20 μM, respectively.
For each drug, determined percentage (vehicle) control transport activity was plotted against nominal inhibitor concentration and fitted using SigmaPlot 12.5 (Systat Software Inc., Chicago, IL; four parameter logistic equation) to determine the concentration that produces half‐maximal inhibition of probe substrate transport (IC50; equivalent to Ki assuming competitive inhibition as probe substrate concentration in the assay is at least 10‐times lower than its Km).
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Publication 2023
Atazanavir Biological Assay Cell Lines Darunavir Estradiol Glucuronides Lopinavir Membrane Transport Proteins Pharmaceutical Preparations Protease Inhibitors Psychological Inhibition rifamycin SV Ritonavir
The mean IC50 (equating to Ki) values obtained for atazanavir, darunavir, lopinavir and ritonavir versus a range of transporters were incorporated into the adapted Rowland‐Matin mechanistic static equation (Equation 1) previously described by Elsby et al.1, 13, 19 in order to predict the change in rosuvastatin AUC based upon inhibition of an BCRP, OATP1B1, OATP1B3, NTCP, all combined hepatic transporter (OATP1B1/OATP1B3/NTCP; Equation 2), and OAT3 fraction excreted (ƒe) value of 0.5, 0.38, 0.11, 0.21, 0.7 and 0.25, respectively.13 Overall AUCR arising from multiple pathways, is simply the product (multiplication) of the AUCR determined for each separate ADME pathway, e.g., for combined inhibition of intestinal BCRP and hepatic OATP1B1, the overall AUCR is equal to the Equation 1‐derived AUCR for BCRP × the Equation 1‐derived AUCR for OATP1B1. For inhibition of BCRP and of combined hepatic uptake as one process (e.g., OATP1B1+OATP1B3+NTCP), then it would be the Equation 1‐derived AUCR for BCRP × the Equation 2‐derived AUCR (combined OATP1B1+OATP1B3+NTCP). AUCR=1ƒe1+I/Ki+1ƒe
AUCR=1ƒeTransporters1+2+31+I/KiTrspt1+I/KiTrspt2+I/KiTrspt3+1ƒeTransporters1+2+3 where Ki = absolute inhibition constant (equating to IC50 for transporters as the probe [S] <<<< Km in the transporter inhibition assay and assuming competitive inhibition, based on the Cheng‐Prusoff equation)20 and [I] = unbound maximum hepatic inlet concentration (Iin max u = fu × (Cmax + (((FaFg × ka × dose (mol))/Qh))/RB)) for hepatic transporters, or [I] = maximum enterocyte concentration (Ig = (FaFg × ka × dose (mol))/Qent) for intestinal transporters,19 or [I] = unbound maximum plasma concentration at steady state (Cmax u = fu × Cmax) for renal transporters.19 fu = unbound fraction in plasma, Cmax = maximum total plasma concentration of inhibitor at steady state, FaFg = fraction of the dose absorbed after oral administration, ka = absorption rate constant (min−1), Qh = hepatic blood flow (1617 mL/min), RB is the blood‐to‐plasma concentration ratio (default = 1.0) and Qent = enterocyte blood flow (300 mL/min).
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Publication 2023
Administration, Oral Atazanavir Biological Assay Blood Circulation Darunavir Enterocytes Intestines Kidney Lopinavir Membrane Transport Proteins Plasma Psychological Inhibition Ritonavir Rosuvastatin
Both HTE and non-HTE PLWH were identified based on their ART history and current ART regimen taken on December 31, 2016. The criteria for identifying HTE PLWH were based on preliminary work in OPERA, in which 2–11% of PLWH who were active in care were classified as HTE according to different definitions (Additional file 1: Fig. S1, Table S1) [9 ]. In the current study, HTE PLWH were defined as either (1) PLWH with exposure to at least three core agent classes prior to their baseline regimen, or (2) PLWH on a baseline regimen indicative of HTE. Core agent classes included non-nucleoside reverse transcriptase inhibitors (NNRTI), protease inhibitors (PI), integrase strand transfer inhibitors (INSTI), fusion inhibitors, and CCR5 antagonists. Regimens indicative of HTE contained either (a) dolutegravir with twice daily dosing; (b) darunavir with twice daily dosing; (c) etravirine; (d) both an INSTI and a PI; (e) maraviroc; or (f) enfuvirtide. Non-HTE PLWH were identified as PLWH who were ART-experienced, on a baseline regimen consisting of one core agent with two NRTIs, and who did not meet the definition of HTE described above; all other ART regimens were ineligible.
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Publication 2023
antagonists CCR5 protein, human Darunavir dolutegravir Enfuvirtide etravirine inhibitors Integrase Inhibitors Maraviroc Nucleosides Protease Inhibitors Reverse Transcriptase Inhibitors Treatment Protocols
Pregnant women were considered exposed to antiretroviral combination if they started antiretroviral treatment before or during pregnancy, and continued at least until delivery. Antiretroviral combination was defined by at least three drugs: namely two nucleoside reverse transcriptase inhibitors (NRTI) associated with a PI (lopinavir/ritonavir, atazanavir/ritonavir, darunavir/ritonavir, fosamprenavir, saquinavir and nelfinavir) or a NNRTI (efavirenz or nevirapine). We categorised the exposure into three different periods: pre-conception, early pregnancy (first trimester) and late pregnancy (second and third trimester).
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Publication 2023
atazanavir, ritonavir drug combination Conception Darunavir efavirenz fosamprenavir lopinavir-ritonavir drug combination Nelfinavir Nevirapine Nucleosides Obstetric Delivery Pharmaceutical Preparations Pregnancy Pregnant Women Reverse Transcriptase Inhibitors Ritonavir Saquinavir
We did a systematic review and meta-analysis according to the Preferred Reporting Items for Systematic review and Meta-Analysis (PRISMA) guidelines [19 (link)]. The protocol of this review was registered in PROSPERO, the International prospective register of systematic reviews (CRD42022306896). The bibliographic research was based on both published and unpublished studies from 01/01/2002 to 29/10/2021 relative to adverse perinatal outcomes in HIV women who received antiretroviral combination during pregnancy.
Searches were conducted on four electronic scientific literature databases: PubMed, Reprotox, Clinical Trial registry (clinicaltrials.gov) and the abstracts from HIV conferences (Conference on Retroviruses and Opportunists Infections, International AIDS Society, European AIDS Clinical Society, British HIV Association and International Workshop on HIV Pediatrics). We used the keywords and MeSH terms presented in the Table 1.

Keywords and MeSH terms used in bibliographical researches

Data sourcesKeywords and MeSH terms
Electronic scientific literature database (Pubmed)("pregnancy outcome"[MeSH Terms] OR ("pregnancy"[All Fields] AND "outcome"[All Fields]) OR "pregnancy outcome"[All Fields] OR ("pregnancy"[All Fields] AND "outcomes" [All Fields]) OR "pregnancy outcomes"[All Fields]) AND ("hiv"[MeSH Terms] OR "hiv"[All Fields]) AND (antiretroviral [All Fields] OR cART [All Fields])
Electronic scientific literature databases (Reprotox, Clinical Trial registry (clinicaltrials.gov)) and abstracts from HIV conferences“3TC, ABC, AZT, ZDV, d4T, TDF, FTC, NRTI, NNRTI, nucleoside, nucleotide, protease, DLV, EFV, ETR, NVP, APV, ATV, DRV, IDV, LPV, RTV, NFV, TPV, T-20, MVC, Atripla, lamivudine, abacavir, zidovudine, stavudine, zalcitabine, didanosine, emtricitabine, epzicom, kivexa, Trizivir, Combivir, Truvada, delavirdine, efavirenz, nevirapine, amprenavir, fosamprenavir, atazanavir darunavir, indinavir, lopinavir, ritonavir, saquinavir, tipranavir, enfurvitide, maraviroc, raltegravir, tenofovir, breast, mother, infant, baby, pregnant, pregnancy, perinatal, postnatal, feeding, breastfeeding, vertical, mtct, pmtct, “when to start” OR timing OR (“early” AND “initia*”)”
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Publication 2023
abacavir Acquired Immunodeficiency Syndrome amprenavir Atazanavir Atripla Breast CART protein, human Combivir Conferences Darunavir Delavirdine Didanosine efavirenz Emtricitabine Epzicom Europeans fosamprenavir Indinavir Infant Kivexa Lamivudine Lopinavir Maraviroc Mothers Nevirapine Nucleosides Nucleotides Opportunistic Infections Peptide Hydrolases Pregnancy Raltegravir Retroviridae Ritonavir Saquinavir Stavudine Tenofovir tipranavir Trizivir Truvada Woman Zalcitabine Zidovudine

Top products related to «Darunavir»

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Lopinavir is a laboratory product manufactured by Merck Group. It is a protease inhibitor used in research applications.
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Atazanavir is a protease inhibitor drug used in the treatment of HIV-1 infection. It is a prescription medication developed and manufactured by Bristol-Myers Squibb.
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Darunavir is a laboratory product that functions as a protease inhibitor. It is used in scientific research and development.
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Darunavir is a laboratory equipment product manufactured by Merck Group. It is a protease inhibitor used in the analysis and research of pharmaceutical compounds.
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Ritonavir is a pharmaceutical product developed by Merck Group. It is a protease inhibitor used in the treatment of HIV infection. The core function of Ritonavir is to prevent the human immunodeficiency virus (HIV) from multiplying in the body by inhibiting the activity of the HIV protease enzyme.
Darunavir is a type of laboratory equipment designed for use in chemical and pharmaceutical research. It is a protease inhibitor that functions by inhibiting the activity of the HIV-1 protease enzyme, which is essential for the replication of the HIV virus. The core function of Darunavir is to serve as a tool for researchers studying HIV and related diseases.
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Amprenavir is a protease inhibitor used in the treatment of HIV infection. It is a laboratory reagent used in research and development. The core function of Amprenavir is to inhibit the activity of the HIV protease enzyme, which is essential for the replication of the virus.
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Ritonavir is a pharmaceutical ingredient used in the production of antiviral medications. It is a protease inhibitor that can be utilized in the development of various therapeutic products. The core function of Ritonavir is to inhibit the activity of certain enzymes, which can be beneficial in the treatment of viral infections.
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Dolutegravir is a chemical compound used as a laboratory tool. It functions as an integrase inhibitor, which is a type of antiretroviral medication. Dolutegravir is utilized in research settings to study its effects and potential applications.
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Darunavir is a protease inhibitor used in the treatment of HIV-1 infection. It is a laboratory product designed for research and analytical purposes. The core function of Darunavir is to inhibit the activity of the HIV-1 protease enzyme, which is essential for the replication of the virus.

More about "Darunavir"

Darunavir is a vital antiretroviral medication used in the treatment of human immunodeficiency virus (HIV) infection.
As a protease inhibitor, it works by blocking the action of the HIV protease enzyme, which is essential for the virus's replication.
Darunavir is often used in combination with other antiretroviral drugs, such as Lopinavir, Atazanavir, Ritonavir, and Amprenavir, to effectively suppress viral load and slow the progression of HIV disease.
Researchers can optimize their Darunavir-related investigations by utilizing the powerful tools and insights offered by PubCompare.ai.
This innovative platform can enhance the reproducibility and accuracy of Darunavir research by enabling researchers to locate relevant protocols from the literature, preprints, and patents.
Additionally, the AI-driven comparisons provided by PubCompare.ai can help researchers identify the best products and methods for their studies, streamlining the research process and leading to more reliable results.
When it comes to HIV treatment, Dolutegravir is another important integrase inhibitor that may be used in combination with Darunavir and other antiretrovirals to effectively manage the disease.
By leveraging the capabilities of PubCompare.ai, researchers can ensure that their investigations into Darunavir and other HIV-related therapies are as efficient, accurate, and impactful as possible.