Beyond darunavir: recent development of next generation HIV-1 protease inhibitors to combat drug resistance
We report our recent development of a conceptually new generation of exceptionally potent non-peptidic HIV-1 protease inhibitors that displayed excellent pharmacological and drug-resistance profiles. Our X-ray structural studies of darunavir and other designed inhibitors from our laboratories led us to create a variety of inhibitors incorporating fused ring polycyclic ethers and aromatic heterocycles to promote hydrogen bonding interactions with the backbone atoms of HIV-1 protease as well as van der Waals interactions with residues in the S2 and S2' subsites. We have also incorporated specific functionalities to enhance v...
Source: Chemical Communications - October 6, 2022 Category: Chemistry Authors: Arun K Ghosh Irene T Weber Hiroaki Mitsuya Source Type: research
Beyond darunavir: recent development of next generation HIV-1 protease inhibitors to combat drug resistance
We report our recent development of a conceptually new generation of exceptionally potent non-peptidic HIV-1 protease inhibitors that displayed excellent pharmacological and drug-resistance profiles. Our X-ray structural studies of darunavir and other designed inhibitors from our laboratories led us to create a variety of inhibitors incorporating fused ring polycyclic ethers and aromatic heterocycles to promote hydrogen bonding interactions with the backbone atoms of HIV-1 protease as well as van der Waals interactions with residues in the S2 and S2' subsites. We have also incorporated specific functionalities to enhance v...
Source: Chemical Communications - October 6, 2022 Category: Chemistry Authors: Arun K Ghosh Irene T Weber Hiroaki Mitsuya Source Type: research
Third-line antiretroviral therapy, including raltegravir (RAL), darunavir (DRV/r) and/or etravirine (ETR), is well tolerated and achieves durable virologic suppression over 144 weeks in resource-limited settings: ACTG A5288 strategy trial
CONCLUSIONS: Third-line regimens comprising of RAL, DRV/r and/or ETR were very well tolerated and had high rates of durable virologic suppression among PLWH in LMICs who were failing on second-line PI-based ART prior to the availability of dolutegravir.PMID:36039892 | DOI:10.1002/jia2.25905 (Source: Journal of the International AIDS Society)
Source: Journal of the International AIDS Society - August 30, 2022 Category: Infectious Diseases Authors: Anchalee Avihingsanon Michael D Hughes Robert Salata Catherine Godfrey Caitlyn McCarthy Peter Mugyenyi Evelyn Hogg Robert Gross Sandra W Cardoso Aggrey Bukuru Mumbi Makanga Sharlaa Badal-Aesen Vidya Mave Beatrice Wangari Ndege Sandy Nerette Fontain Wadzan Source Type: research
Third-line antiretroviral therapy, including raltegravir (RAL), darunavir (DRV/r) and/or etravirine (ETR), is well tolerated and achieves durable virologic suppression over 144 weeks in resource-limited settings: ACTG A5288 strategy trial
CONCLUSIONS: Third-line regimens comprising of RAL, DRV/r and/or ETR were very well tolerated and had high rates of durable virologic suppression among PLWH in LMICs who were failing on second-line PI-based ART prior to the availability of dolutegravir.PMID:36039892 | PMC:PMC9332128 | DOI:10.1002/jia2.25905 (Source: Journal of the International AIDS Society)
Source: Journal of the International AIDS Society - August 30, 2022 Category: Infectious Diseases Authors: Anchalee Avihingsanon Michael D Hughes Robert Salata Catherine Godfrey Caitlyn McCarthy Peter Mugyenyi Evelyn Hogg Robert Gross Sandra W Cardoso Aggrey Bukuru Mumbi Makanga Sharlaa Badal-Aesen Vidya Mave Beatrice Wangari Ndege Sandy Nerette Fontain Wadzan Source Type: research
Impact of age and gender disparity on CD4+ cell counts to control disease progression using specific HAART in HIV-1 positive patients: A case-control study
CONCLUSION: The administration of specific HAART (NRTIs and novel protease inhibitors) in HIV patients had a notable improvement in the CD4+ cell count and viral load with significant age and gender disparity.PMID:35980078 | DOI:10.2174/1574887117666220817123002 (Source: Reviews on Recent Clinical Trials)
Source: Reviews on Recent Clinical Trials - August 18, 2022 Category: Cancer & Oncology Authors: Aakansha Singh Manoj Kumar Ashok K Singh Neeraj Verma Source Type: research
Impact of age and gender disparity on CD4+ cell counts to control disease progression using specific HAART in HIV-1 positive patients: A case-control study
CONCLUSION: The administration of specific HAART (NRTIs and novel protease inhibitors) in HIV patients had a notable improvement in the CD4+ cell count and viral load with significant age and gender disparity.PMID:35980078 | DOI:10.2174/1574887117666220817123002 (Source: Reviews on Recent Clinical Trials)
Source: Reviews on Recent Clinical Trials - August 18, 2022 Category: Cancer & Oncology Authors: Aakansha Singh Manoj Kumar Ashok K Singh Neeraj Verma Source Type: research
A 28-Year-Old Man With Diffuse Bilateral Pulmonary Nodules
Chest. 2022 Jul;162(1):e9-e13. doi: 10.1016/j.chest.2022.02.022.ABSTRACTA 28-year-old man with a history of congenital HIV sought treatment at the ED with a chief symptom of generalized malaise and confusion of 3 days' duration. He had mild dyspnea, but no respiratory distress, and he reported no fever, chest pain, or headache. We were unable to obtain past medical, family, or social history because of encephalopathy and we had no available contact person. Review of the patient's medical record revealed he made an initial clinic visit to the Department of Pediatric Infectious Disease 5 years previously. At the time of that...
Source: Chest - July 9, 2022 Category: Respiratory Medicine Authors: Kiran Pokhrel Suzanne Barry Ammoura Ibrahim Thomas Smith Amit Chopra Source Type: research
A 28-Year-Old Man With Diffuse Bilateral Pulmonary Nodules
Chest. 2022 Jul;162(1):e9-e13. doi: 10.1016/j.chest.2022.02.022.ABSTRACTA 28-year-old man with a history of congenital HIV sought treatment at the ED with a chief symptom of generalized malaise and confusion of 3 days' duration. He had mild dyspnea, but no respiratory distress, and he reported no fever, chest pain, or headache. We were unable to obtain past medical, family, or social history because of encephalopathy and we had no available contact person. Review of the patient's medical record revealed he made an initial clinic visit to the Department of Pediatric Infectious Disease 5 years previously. At the time of that...
Source: Chest - July 9, 2022 Category: Respiratory Medicine Authors: Kiran Pokhrel Suzanne Barry Ammoura Ibrahim Thomas Smith Amit Chopra Source Type: research
A 28-Year-Old Man With Diffuse Bilateral Pulmonary Nodules
Chest. 2022 Jul;162(1):e9-e13. doi: 10.1016/j.chest.2022.02.022.ABSTRACTA 28-year-old man with a history of congenital HIV sought treatment at the ED with a chief symptom of generalized malaise and confusion of 3 days' duration. He had mild dyspnea, but no respiratory distress, and he reported no fever, chest pain, or headache. We were unable to obtain past medical, family, or social history because of encephalopathy and we had no available contact person. Review of the patient's medical record revealed he made an initial clinic visit to the Department of Pediatric Infectious Disease 5 years previously. At the time of that...
Source: Chest - July 9, 2022 Category: Respiratory Medicine Authors: Kiran Pokhrel Suzanne Barry Ammoura Ibrahim Thomas Smith Amit Chopra Source Type: research
A 28-Year-Old Man With Diffuse Bilateral Pulmonary Nodules
Chest. 2022 Jul;162(1):e9-e13. doi: 10.1016/j.chest.2022.02.022.ABSTRACTA 28-year-old man with a history of congenital HIV sought treatment at the ED with a chief symptom of generalized malaise and confusion of 3 days' duration. He had mild dyspnea, but no respiratory distress, and he reported no fever, chest pain, or headache. We were unable to obtain past medical, family, or social history because of encephalopathy and we had no available contact person. Review of the patient's medical record revealed he made an initial clinic visit to the Department of Pediatric Infectious Disease 5 years previously. At the time of that...
Source: Chest - July 9, 2022 Category: Respiratory Medicine Authors: Kiran Pokhrel Suzanne Barry Ammoura Ibrahim Thomas Smith Amit Chopra Source Type: research
A 28-Year-Old Man With Diffuse Bilateral Pulmonary Nodules
Chest. 2022 Jul;162(1):e9-e13. doi: 10.1016/j.chest.2022.02.022.ABSTRACTA 28-year-old man with a history of congenital HIV sought treatment at the ED with a chief symptom of generalized malaise and confusion of 3 days' duration. He had mild dyspnea, but no respiratory distress, and he reported no fever, chest pain, or headache. We were unable to obtain past medical, family, or social history because of encephalopathy and we had no available contact person. Review of the patient's medical record revealed he made an initial clinic visit to the Department of Pediatric Infectious Disease 5 years previously. At the time of that...
Source: Chest - July 9, 2022 Category: Respiratory Medicine Authors: Kiran Pokhrel Suzanne Barry Ammoura Ibrahim Thomas Smith Amit Chopra Source Type: research
A 28-Year-Old Man With Diffuse Bilateral Pulmonary Nodules
Chest. 2022 Jul;162(1):e9-e13. doi: 10.1016/j.chest.2022.02.022.ABSTRACTA 28-year-old man with a history of congenital HIV sought treatment at the ED with a chief symptom of generalized malaise and confusion of 3 days' duration. He had mild dyspnea, but no respiratory distress, and he reported no fever, chest pain, or headache. We were unable to obtain past medical, family, or social history because of encephalopathy and we had no available contact person. Review of the patient's medical record revealed he made an initial clinic visit to the Department of Pediatric Infectious Disease 5 years previously. At the time of that...
Source: Chest - July 9, 2022 Category: Respiratory Medicine Authors: Kiran Pokhrel Suzanne Barry Ammoura Ibrahim Thomas Smith Amit Chopra Source Type: research
A randomized controlled trial of combined ivermectin and zinc sulfate versus combined hydroxychloroquine, darunavir/ritonavir, and zinc sulfate among adult patients with asymptomatic or mild coronavirus-19 infection
Conclusion: We demonstrated that both treatment regimens were safe, but both treatment regimens had no virological or clinical benefit. Based on this result and current data, there is no supporting evidence for the clinical benefit of ivermectin for coronavirus-19. (Source: Journal of Global Infectious Diseases)
Source: Journal of Global Infectious Diseases - June 29, 2022 Category: Infectious Diseases Authors: Sireethorn Nimitvilai Yupin Suputtamongkol Ussanee Poolvivatchaikarn Dechatorn Rassamekulthana Nuttawut Rongkiettechakorn Anek Mungaomklang Susan Assanasaen Ekkarat Wongsawat Chompunuch Boonarkart Waritta Sawaengdee Source Type: research
Analysis of virological response to therapy and resistance profile in treatment-experienced and naive HIV-1 infected Romanian patients receiving regimens containing darunavir boosted with ritonavir or cobicistat
Biomed Pharmacother. 2022 Jun;150:113077. doi: 10.1016/j.biopha.2022.113077. Epub 2022 May 6.ABSTRACT77% of Romanians infected with HIV receive antiretroviral therapy, with the challenge of maintaining long-term therapeutic success (the viral load becoming/remaining undetectable). The main purpose of this study was to provide comparative analysis of the long-term virological response to therapeutic regimens containing pharmacokinetically enhanced darunavir (DRV) with ritonavir (RTV) or cobicistat (COBI). The second aim was to evaluate the viral resistance profile to therapy, by number/type/frequency of viral mutations. Thi...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - June 5, 2022 Category: Drugs & Pharmacology Authors: Ruxandra-Cristina Marin Adrian Streinu-Cercel Lavinia Cristina Moleriu Simona Gabriela Bungau Source Type: research
