Edurant (rilpivirine) / J&J 
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  • ||||||||||  Edurant (rilpivirine) / J&J
    Journal:  Genetic characteristics of CRF12_BF first identified in Guangdong Province, China. (Pubmed Central) -  Aug 20, 2021   
    Additionally, this CRF12_BF strain was confirmed to contain the non-nucleoside reverse transcriptase inhibitor mutation E138A associated with potential low-level resistance against efavirenz and low-level resistance against rilpivirine by the Stanford University HIV Drug Resistance Database program. The analysed sequence data in this study will provide more information on the HIV epidemic in China.
  • ||||||||||  Edurant (rilpivirine) / J&J, Rekambys (rilpivirine LA) / J&J
    Journal:  Metabolism of Long-Acting Rilpivirine Following Intramuscular Injection: HIV Prevention Trials Network Study 076 (HPTN 076). (Pubmed Central) -  Aug 20, 2021   
    P2
    A total of 8 missense variants of UGT1A4 were detected, whereas 2 variants were detected for UGT1A1; however, these variants did not appear to account for the observed interindividual variability in metabolite levels. These findings provide insight into the metabolism of long-acting RPV and contribute to overall understanding of metabolism following oral dosing versus injection.
  • ||||||||||  Pifeltro (doravirine) / Merck (MSD), doravirine/islatravir (MK-8591A) / Merck (MSD), islatravir (MK-8591) / Merck (MSD)
    Preclinical, Journal:  Cell culture selections reveal favourable drug resistance profiles for doravirine and islatravir. (Pubmed Central) -  Aug 12, 2021   
    Doravirine showed a more robust resistance profile compared with other NNRTIs. The long intracellular half-life of islatravir and delayed acquisition of resistance in dual selections provide an opportunity for long-acting treatment options.
  • ||||||||||  Edurant (rilpivirine) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
    Clinical, Review, Journal:  Three-Drug Regimens Containing Integrase Inhibitor Show Good Efficacy and Safety in Treatment-Naive Patients With HIV-1: A Bayesian Analysis. (Pubmed Central) -  Aug 10, 2021   
    For virologic suppression at 48 weeks, odds ratios (95% credible intervals) were 0.6 (0.43, 0.82) for EFV+ tenofovir disoproxil fumarate (TDF)+emtricitabine (FTC) versus DTG+ abacavir+ lamivudine (3TC) and 0.52 (0.36, 0.75) for EFV+TDF+FTC vs. DTG+TDF+FTC/3TC...Outcomes associated with death were unsuitable for network meta-analysis due to low event rates. 3-drug regimens containing INI demonstrate better efficacy and safety than those containing RPV or EFV.
  • ||||||||||  Journal:  LONG-ACTING DRUGS AND FORMULATIONS FOR THE TREATMENT AND PREVENTION OF HIV. (Pubmed Central) -  Aug 8, 2021   
    GS-6207 is a novel HIV capsid inhibitor that is injected subcutaneously every 3 months...These approaches appear to be especially attractive for patients complaining of pill fatigue, and for those experiencing HIV-associated stigma. As these formulations are shown to be safe, well-tolerated, and economical, they are likely to gain broader appeal.
  • ||||||||||  Edurant (rilpivirine) / J&J, Pifeltro (doravirine) / Merck (MSD), Intelence (etravirine) / J&J
    Journal:  Small Molecules of Natural Origin as Potential Anti-HIV Agents: A Computational Approach. (Pubmed Central) -  Aug 7, 2021   
    Three natural products (ZINC37538901, ZINC38321654, and ZINC67912677) containing oxan and oxolan rings with hydroxyl substituents and one (ZINC2103242) having 3,6,7,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-1,4-dione core exhibited comparable profiles to etravirine and doravirine, with ZINC2103242 being the most promising anti-HIV candidate in terms of drug metabolism and safety profile. These findings may open new avenues to guide the rational design of novel HIV-1 NNRTIs.
  • ||||||||||  Edurant (rilpivirine) / J&J
    Trial completion, Enrollment change:  Short Cycle Therapy in ART Regimens Containing Rilpivirine: Assessment of Patients' Satisfaction (clinicaltrials.gov) -  Jul 30, 2021   
    P=N/A,  N=33, Completed, 
    Mass spectrometry data were consistent with the covalent modification of the RT, although off-target reactivity constitutes a major limitation for further development of the described inhibitors. Not yet recruiting --> Completed | N=60 --> 33
  • ||||||||||  Edurant (rilpivirine) / J&J, Cabenuva (cabotegravir long acting/rilpivirine long acting) / J&J, GSK, ViiV Healthcare, Pfizer, Shionogi
    Journal:  Cabotegravir/rilpivirine (Cabenuva) for HIV-1 infection. (Pubmed Central) -  Jul 14, 2021   
    This action may be of relevance for the molecular mechanisms of hepatoprotection exerted by RPV. No abstract available
  • ||||||||||  [VIRTUAL] HIV minority resistance variants partially explain genotypic-phenotypic discordance () -  May 27, 2021 - Abstract #IASHIV2021IAS_HIV_995;    
    Discordance, mostly represented by genotypic DR overestimation, was partially explained by NGS minority DR variants. This suggests that minority DR variants might help refine genotypic interpretation algorithms to avoid inappropriate choice of drugs; but also, existence of alternative explanations.
  • ||||||||||  Edurant (rilpivirine) / J&J
    Journal:  Rilpivirine-associated aggregation-induced emission enables cell-based nanoparticle tracking. (Pubmed Central) -  May 15, 2021   
    The intact drug crystals were easily detected in CD4 T cells and macrophages, the natural viral target cells, by flow cytometry and ultraperformance liquid chromatography tandem mass spectrometry. We conclude that AIE can be harnessed to monitor cell biodistribution of selective antiretroviral drug nanocrystals.
  • ||||||||||  Pifeltro (doravirine) / Merck (MSD)
    Clinical, Review, Journal:  Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development. (Pubmed Central) -  Apr 10, 2021   
    Overall, minimal cross-resistance across NNRTIs was observed for doravirine, as well as limited development of doravirine-related resistance. These data should assist clinicians in further understanding the resistance profile of doravirine, so appropriate treatment decisions can be made for their patients.