PMC:7600245 / 18273-21986 JSONTXT 9 Projects

Annnotations TAB TSV DIC JSON TextAE

Id Subject Object Predicate Lexical cue
T136 0-4 Sentence denotes 2.5.
T137 5-94 Sentence denotes Emtricitabine (Emtriva) in Combination with Tenofovir Disoproxil or Tenofovir Alafenamide
T138 95-248 Sentence denotes Emtricitabine is a cytosine nucleoside analog (Figure 3) that is a competitive inhibitor of human immunodeficiency virus-1 (HIV-1) reverse transcriptase.
T139 249-337 Sentence denotes It is metabolized by cellular kinases-mediated phosphorylation to the triphosphate form.
T140 338-565 Sentence denotes Emtricitabine triphosphate is the active form that blocks the HIV replication by terminating its genetic chain elongation, and thus, it prevents the generation of complementary DNA from the viral RNA and reduces the viral load.
T141 566-605 Sentence denotes The drug was first approved by the U.S.
T142 606-676 Sentence denotes FDA as an orally bioavailable, once-daily antiretroviral drug in 2003.
T143 677-784 Sentence denotes It is now used in combination with other antiretroviral drugs for the treatment of HIV-1 infection [62,63].
T144 785-1011 Sentence denotes Combinations with tenofovir disoproxil fumarate (Truvada), tenofovir alafenamide (Descovy; 2016), rilpivirine, and tenofovir alafenamide (Odefsey; 2016), or bictegravir and tenofovir alafenamide (Biktarvy; 2018) are available.
T145 1012-1270 Sentence denotes In particular, tenofovir disoproxil (Viread; 2001) is an adenine-based acyclic nucleotide analog (Figure S1) that, following activation, acts as a competitive inhibitor of reverse transcriptase, and subsequently, it leads to DNA chain elongation termination.
T146 1271-1595 Sentence denotes Activation of the drug starts with the hydrolysis of the external esters followed by spontaneous release of carbon dioxide and formaldehyde to form the corresponding tenofovir, a nucleoside monophosphate, which subsequently undergoes two phosphorylation steps to form tenofovir diphosphate, the active drug (Figure S1) [64].
T147 1596-1637 Sentence denotes It was first approved in 2001 by the U.S.
T148 1638-1724 Sentence denotes FDA and is prescribed for the oral treatment of HIV-1 and chronic HBV infections [65].
T149 1725-1908 Sentence denotes It is also available in many other combinations with emtricitabine, lamivudine (Cimduo; 2018), doravirine and lamivudine (Delstrigo; 2018), and efavirenz and lamivudine (Symfi; 2018).
T150 1909-2187 Sentence denotes The efficacy of emtricitabine and tenofovir disoproxil as a prophylactic combination against SARS-CoV-2 infection is being evaluated in a large randomized, double-blind, controlled with placebo clinical trial for health care providers exposed to COVID-19 patients (NCT04334928).
T151 2188-2360 Sentence denotes The two drugs have been reported by a recent computational work as potential inhibitors of RdRp of SARS-CoV-2 [55,66], yet this potential is to be experimentally confirmed.
T152 2361-2577 Sentence denotes Likewise, tenofovir alafenamide (Vemlidy; 2016) is an adenine-based acyclic nucleotide analog that, following activation, acts as a competitive inhibitor of reverse transcriptase and DNA chain elongation termination.
T153 2578-2756 Sentence denotes The activation of the drug is, however, different and it usually takes place in infected cells by a series of bio-transformations similar to those of remdesivir (Figure S2) [67].
T154 2757-2973 Sentence denotes The main advantage of the prodrug, relative to the former prodrug, is that it increases the drug’s oral bioavailability, intestinal diffusion, selectivity of targeting the infected cells, and intracellular half-life.
T155 2974-3055 Sentence denotes It also decreases the potential renal toxicity of the monophosphate intermediate.
T156 3056-3116 Sentence denotes Tenofovir alafenamide was first approved in 2016 by the U.S.
T157 3117-3184 Sentence denotes FDA and is prescribed for the oral treatment of HBV infection [68].
T158 3185-3423 Sentence denotes It is also available in many other combinations with emtricitabine (Descovy; 2016), bictegravir and emtricitabine (Biktarvy; 2018), emtricitabine and rilpivirine (Odefsey; 2016), and darunavir/cobicistat and emtricitabine (Symtuza; 2018).
T159 3424-3713 Sentence denotes The efficacy of emtricitabine and tenofovir alafenamide as a prophylactic combination against SARS-CoV-2 infection is being evaluated in a large randomized, double-blind, controlled with placebo clinical trial for health care providers exposed to COVID-19 patients (NCT04405271; n = 1378).