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Tenofovir and Doravirine Are Potential Reverse-Transcriptase Analogs in Combination with the New Reverse-Transcriptase Translocation Inhibitor (Islatravir) Among Treatment-Experienced Patients in Cameroon: Designing Future Treatment Strategies for Low- and Middle-Income Countries.
Viruses
January 2025
Chantal BIYA International Reference Centre for Research on HIV/AIDS Prevention and Management, Yaoundé P.O. Box 3077, Cameroon.
Islatravir (ISL) is a novel antiretroviral that inhibits HIV-1 reverse transcriptase translocation. The M184V mutation, known to reduce ISL's viral susceptibility in vitro, could arise from prolonged exposure to nucleoside reverse transcriptase inhibitors (NRTI) (3TC). This study evaluated the predictive efficacy of ISL and identified potentially active antiretrovirals in combination among treatment-experienced patients in Cameroon, where NRTIs (3TC) have been the backbone of ART for decades now.
View Article and Find Full Text PDFBRAF-Mutated Melanoma Cell Lines Develop Distinct Molecular Signatures After Prolonged Exposure to AZ628 or Dabrafenib: Potential Benefits of the Antiretroviral Treatments Cabotegravir or Doravirine on BRAF-Inhibitor-Resistant Cells.
Int J Mol Sci
November 2024
Section of Biochemistry, Department of Neuroscience, Biomedicine and Movement Sciences, University of Verona, Strada Le Grazie 8, 37134 Verona, Italy.
Melanoma is an aggressive cancer characterized by rapid growth, early metastasis, and poor prognosis, with resistance to current therapies being a significant issue. BRAF mutations drive uncontrolled cell division by activating the MAPK pathway. In this study, A375 and FO-1, BRAF-mutated melanoma cell lines, were treated for 4-5 months with RAF inhibitor dabrafenib or AZ628, leading to drug resistance over time.
View Article and Find Full Text PDFFirst Case of HIV Seroconversion With Integrase Resistance Mutations on Long-Acting Cabotegravir for Prevention in Routine Care.
Open Forum Infect Dis
September 2024
University of Pittsburgh, Pittsburgh, Pennsylvania, USA.
Article Synopsis
- Long-acting cabotegravir (CAB-LA) is effective for preventing HIV, but there have been instances of delayed diagnoses and resistance to integrase inhibitors in trials.
- A case study involving a 23-year-old gender-nonbinary individual showed that after a brief interruption in CAB-LA, HIV became detectable with an INSTI resistance mutation only identified through a sensitive research assay.
- The findings highlight the need for faster HIV testing and access to CAB-LA, even without insurance, to improve early detection and reduce the risk of resistance.
Physicochemical Stability of Doravirine (Pifeltro): Characterization of Main Degradation Products and Assessment of Stability of Tablets Repackaged in Single-Dose Unit Containers.
Pharmaceutics
July 2024
Department of Pharmacy, Hôpitaux Universitaires Pitié-Salpêtrière, AP-HP, 75013 Paris, France.
Doravarine (DOR) is an antiviral drug with a marketed authorization for the management of occupational blood and body fluid exposure. The currently existing packaging, consisting of multiple unit bottles comprising 30 tablets, is not fully appropriate for daily nominative dispensing at the hospital. This study aims at assessing the impact of the change in packaging on the key attributes of the drug: assay, impurity profile, and dissolution.
View Article and Find Full Text PDFSimultaneous quantification of five antiretrovirals in human tissues using ultra-high performance liquid chromatography-tandem mass spectrometry methods for therapeutic drug monitoring at the sites of action.
J Chromatogr B Analyt Technol Biomed Life Sci
July 2024
Center for Clinical Pharmaceutical Sciences, Department of Pharmacy & Therapeutics, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA, USA. Electronic address:
Although antiretroviral therapy (ART) is highly effective for the treatment of HIV-1 infection to suppress virus in the blood, HIV persists in tissues. HIV persistence in the tissues is due to numerous factors, and one of those factors are antiretroviral (ARV) concentrations. ARV concentrations in tissues must be adequate to suppress HIV at the sites of action.
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