The Effect of Rifampicin on Darunavir, Ritonavir, and Dolutegravir Exposure within Peripheral Blood Mononuclear Cells: a Dose Escalation Study
This study showed a differential impact of enzyme and/or transporter induction on DRV/r concentrations in plasma and PBMCs, highlighting the usefulness of studying intra-PBMC pharmacokinetics with drug-drug interactions. (This study has been registered at ClinicalTrials.gov under registration no. NCT03892161.).PMID:35583344 | DOI:10.1128/aac.00136-22 (Source: Antimicrobial Agents and Chemotherapy)
Source: Antimicrobial Agents and Chemotherapy - May 18, 2022 Category: Microbiology Authors: Amedeo De Nicol ò Andrea Calcagno Ilaria Motta Elisa De Vivo Antonio D'Avolio Giovanni Di Perri Lubbe Wiesner Isma-Eel Ebrahim Gary Maartens Catherine Orrell Helen McIlleron Source Type: research
The Effect of Rifampicin on Darunavir, Ritonavir, and Dolutegravir Exposure within Peripheral Blood Mononuclear Cells: a Dose Escalation Study
This study showed a differential impact of enzyme and/or transporter induction on DRV/r concentrations in plasma and PBMCs, highlighting the usefulness of studying intra-PBMC pharmacokinetics with drug-drug interactions. (This study has been registered at ClinicalTrials.gov under registration no. NCT03892161.).PMID:35583344 | DOI:10.1128/aac.00136-22 (Source: Antimicrobial Agents and Chemotherapy)
Source: Antimicrobial Agents and Chemotherapy - May 18, 2022 Category: Microbiology Authors: Amedeo De Nicol ò Andrea Calcagno Ilaria Motta Elisa De Vivo Antonio D'Avolio Giovanni Di Perri Lubbe Wiesner Isma-Eel Ebrahim Gary Maartens Catherine Orrell Helen McIlleron Source Type: research
The Effect of Rifampicin on Darunavir, Ritonavir, and Dolutegravir Exposure within Peripheral Blood Mononuclear Cells: a Dose Escalation Study
This study showed a differential impact of enzyme and/or transporter induction on DRV/r concentrations in plasma and PBMCs, highlighting the usefulness of studying intra-PBMC pharmacokinetics with drug-drug interactions. (This study has been registered at ClinicalTrials.gov under registration no. NCT03892161.).PMID:35583344 | DOI:10.1128/aac.00136-22 (Source: Antimicrobial Agents and Chemotherapy)
Source: Antimicrobial Agents and Chemotherapy - May 18, 2022 Category: Microbiology Authors: Amedeo De Nicol ò Andrea Calcagno Ilaria Motta Elisa De Vivo Antonio D'Avolio Giovanni Di Perri Lubbe Wiesner Isma-Eel Ebrahim Gary Maartens Catherine Orrell Helen McIlleron Source Type: research
The Effect of Rifampicin on Darunavir, Ritonavir, and Dolutegravir Exposure within Peripheral Blood Mononuclear Cells: a Dose Escalation Study
This study showed a differential impact of enzyme and/or transporter induction on DRV/r concentrations in plasma and PBMCs, highlighting the usefulness of studying intra-PBMC pharmacokinetics with drug-drug interactions. (This study has been registered at ClinicalTrials.gov under registration no. NCT03892161.).PMID:35583344 | DOI:10.1128/aac.00136-22 (Source: Antimicrobial Agents and Chemotherapy)
Source: Antimicrobial Agents and Chemotherapy - May 18, 2022 Category: Microbiology Authors: Amedeo De Nicol ò Andrea Calcagno Ilaria Motta Elisa De Vivo Antonio D'Avolio Giovanni Di Perri Lubbe Wiesner Isma-Eel Ebrahim Gary Maartens Catherine Orrell Helen McIlleron Source Type: research
Increased viral load in a hospitalized patient on treatment with crushed bictegravir/emtricitabine/tenofovir alafenamide: A case report and review of the literature
CONCLUSION: Controlled studies are needed to verify acceptable pharmacokinetic and pharmacodynamic metrics for crushed B/FTC/TAF given via tube, with and without tube feeds, before use in this manner.PMID:35511892 | DOI:10.1093/ajhp/zxac120 (Source: American Journal of Health-System Pharmacy : AJHP)
Source: American Journal of Health-System Pharmacy : AJHP - May 5, 2022 Category: Drugs & Pharmacology Authors: Sarah M Rowe Jackson C Clary Malashia Drummond Caroline Derrick Kamla Sanasi P Brandon Bookstaver Source Type: research
Increased viral load in a hospitalized patient on treatment with crushed bictegravir/emtricitabine/tenofovir alafenamide: A case report and review of the literature
CONCLUSION: Controlled studies are needed to verify acceptable pharmacokinetic and pharmacodynamic metrics for crushed B/FTC/TAF given via tube, with and without tube feeds, before use in this manner.PMID:35511892 | DOI:10.1093/ajhp/zxac120 (Source: American Journal of Health-System Pharmacy : AJHP)
Source: American Journal of Health-System Pharmacy : AJHP - May 5, 2022 Category: Drugs & Pharmacology Authors: Sarah M Rowe Jackson C Clary Malashia Drummond Caroline Derrick Kamla Sanasi P Brandon Bookstaver Source Type: research
Darunavir-cobicistat versus lopinavir-ritonavir in the treatment of COVID-19 infection (DOLCI): A multicenter observational study
ConclusionIn patients with COVID-19 pneumonia, early treatment with lopinavir-ritonavir was associated with faster time to clinical improvement and/or virological clearance than darunavir-cobicistat. Future trials are warranted to confirm these findings. Trial registrationClinicalTrials.gov number, NCT04425382. (Source: PLoS One)
Source: PLoS One - May 4, 2022 Category: Biomedical Science Authors: Eman Zeyad I. Elmekaty Source Type: research
Pharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants
Antimicrob Agents Chemother. 2022 Mar 22:e0225121. doi: 10.1128/aac.02251-21. Online ahead of print.ABSTRACTFostemsavir is a prodrug of temsavir, a first-in-class attachment inhibitor that binds directly to HIV-1 gp120, preventing initial viral attachment and entry into host CD4+ T cells with demonstrated efficacy in phase 2 and 3. Temsavir is a P-glycoprotein and breast cancer resistance protein (BCRP) substrate; its metabolism is mediated by esterase and CYP3A4 enzymes. Drugs that induce or inhibit CYP3A, P-glycoprotein, and BCRP may affect temsavir concentrations. Understanding potential drug-drug interactions (DDIs) fo...
Source: Antimicrobial Agents and Chemotherapy - March 22, 2022 Category: Microbiology Authors: Katy Moore Nilay Thakkar Mindy Magee Heather Sevinsky Blisse Vakkalagadda Susan Lubin Cyril Llamoso Peter Ackerman Source Type: research
Pharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants
Antimicrob Agents Chemother. 2022 Mar 22:e0225121. doi: 10.1128/aac.02251-21. Online ahead of print.ABSTRACTFostemsavir is a prodrug of temsavir, a first-in-class attachment inhibitor that binds directly to HIV-1 gp120, preventing initial viral attachment and entry into host CD4+ T cells with demonstrated efficacy in phase 2 and 3. Temsavir is a P-glycoprotein and breast cancer resistance protein (BCRP) substrate; its metabolism is mediated by esterase and CYP3A4 enzymes. Drugs that induce or inhibit CYP3A, P-glycoprotein, and BCRP may affect temsavir concentrations. Understanding potential drug-drug interactions (DDIs) fo...
Source: Antimicrobial Agents and Chemotherapy - March 22, 2022 Category: Microbiology Authors: Katy Moore Nilay Thakkar Mindy Magee Heather Sevinsky Blisse Vakkalagadda Susan Lubin Cyril Llamoso Peter Ackerman Source Type: research
Pharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants
Antimicrob Agents Chemother. 2022 Mar 22:e0225121. doi: 10.1128/aac.02251-21. Online ahead of print.ABSTRACTFostemsavir is a prodrug of temsavir, a first-in-class attachment inhibitor that binds directly to HIV-1 gp120, preventing initial viral attachment and entry into host CD4+ T cells with demonstrated efficacy in phase 2 and 3. Temsavir is a P-glycoprotein and breast cancer resistance protein (BCRP) substrate; its metabolism is mediated by esterase and CYP3A4 enzymes. Drugs that induce or inhibit CYP3A, P-glycoprotein, and BCRP may affect temsavir concentrations. Understanding potential drug-drug interactions (DDIs) fo...
Source: Antimicrobial Agents and Chemotherapy - March 22, 2022 Category: Microbiology Authors: Katy Moore Nilay Thakkar Mindy Magee Heather Sevinsky Blisse Vakkalagadda Susan Lubin Cyril Llamoso Peter Ackerman Source Type: research
Mechanism of darunavir binding to monomeric HIV-1 protease: a step forward in the rational design of dimerization inhibitors
Phys. Chem. Chem. Phys., 2022, Advance Article DOI: 10.1039/D2CP00024E, PaperMohd Ahsan, Chinmai Pindi, Sanjib Senapati Binding of Darunavir (DRV) to HIV protease (HIVPR) monomer. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - Phys. Chem. Chem. Phys. latest articles)
Source: RSC - Phys. Chem. Chem. Phys. latest articles - March 8, 2022 Category: Chemistry Authors: Mohd Ahsan Source Type: research
Mechanism of darunavir binding to monomeric HIV-1 protease: A step forward in rational design of dimerization inhibitors
Phys. Chem. Chem. Phys., 2022, Accepted Manuscript DOI: 10.1039/D2CP00024E, PaperMohd Ahsan, Chinmai Pindi, Sanjib Senapati HIV protease (HIVPR) is a key target in AIDS therapeutics. All ten FDA-approved drugs that compete with the substrates in binding to this dimeric enzyme ’s active site become ineffective due... The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - Phys. Chem. Chem. Phys. latest articles)
Source: RSC - Phys. Chem. Chem. Phys. latest articles - February 28, 2022 Category: Chemistry Authors: Mohd Ahsan Source Type: research
[ASAP] An Efficient Synthesis of the Bicyclic Darunavir Side Chain Using Chemoenzymatic Catalysis
Organic Process Research& DevelopmentDOI: 10.1021/acs.oprd.2c00017 (Source: Organic Process Research and Development)
Source: Organic Process Research and Development - February 18, 2022 Category: Chemistry Authors: Paul S. Riehl, Jesmine Lim, James D. Finnigan, Simon J. Charnock, and Todd K. Hyster Source Type: research
Current status of therapeutic alternatives for COVID-19: A narrative review
Infez Med. 2021 Sep 10;29(3):312-327. doi: 10.53854/liim-2903-2. eCollection 2021.ABSTRACTSince December 2019, severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection has exploded and led to a global crisis. Currently, the global case numbers topped 200 million, and toll of dead exceeded 4 million around the world. The pathogenesis of coronavirus disease 2019 (COVID-19) is driven by two processes. During the first stage of the infection that lasts around 5-7 days, replication of SARS-CoV-2 occurs. In the second stage, the disease may progress due to an exaggerated inflammatory response leading to tissue dama...
Source: Infezioni in Medicina - February 11, 2022 Category: Infectious Diseases Authors: Abdullah Tar ık Aslan Murat Akova Source Type: research
