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). |