Approved HIV reverse transcriptase inhibitors in the past decade.
3TC, (−)-2′,3′-dideoxy-3′-thiacytidine (common name, lamivudine)
ABC, abacavir
ATV, atazanavir
AZT, 3′-azido-3′-deoxy-thymidine (common name, zidovudine)
BIC, bictegravir
CAB, cabotegravir
CC50, the 50% cytotoxic concentration
COBI, cobicistat
Clinical efficacy
DOR, doravirine
DPV, dapivirine
DRV, darunavir
DTG, dolutegravir
EACS, European AIDS Clinical Society
EC50, half maximal effective concentration
EFV, efavirenz
ESV, elsulfavirine
EVG, elvitegravir
F, bioavailability
FDA, US Food and Drug Administration
FTC, (−)-2′,3′-dideoxy-5-fluoro-3′-thiacytidine (common name, emtricitabine)
HAART
HAART, highly active antiretroviral therapy
HIV treatment
HIV, human immunodeficiency virus
IAS-USA, International Antiviral Society-USA
IC50, half maximal inhibitory concentration
MSM, men who have sex with men
NNRTI
NNRTI, non-nucleoside reverse transcriptase inhibitor
NRTI
NRTI, nucleoside/nucleotide reverse transcriptase inhibitor
RPV, rilpivirine
TAF, tenofovir alafenamide
TDF, tenofovir disoproxil fumarate
t1/2, elimination half-life
Journal
Acta pharmaceutica Sinica. B
ISSN: 2211-3835
Titre abrégé: Acta Pharm Sin B
Pays: Netherlands
ID NLM: 101600560
Informations de publication
Date de publication:
Apr 2022
Apr 2022
Historique:
received:
07
07
2021
revised:
13
10
2021
accepted:
08
11
2021
entrez:
18
7
2022
pubmed:
19
7
2022
medline:
19
7
2022
Statut:
ppublish
Résumé
HIV reverse transcriptase (RT) inhibitors are the important components of highly active antiretroviral therapies (HAARTs) for anti-HIV treatment and pre-exposure prophylaxis in clinical practice. Many RT inhibitors and their combination regimens have been approved in the past ten years, but a review on their drug discovery, pharmacology, and clinical efficacy is lacking. Here, we provide a comprehensive review of RT inhibitors (tenofovir alafenamide, rilpivirine, doravirine, dapivirine, azvudine and elsulfavirine) approved in the past decade, regarding their drug discovery, pharmacology, and clinical efficacy in randomized controlled trials. Novel RT inhibitors such as islatravir, MK-8504, MK-8507, MK8583, IQP-0528, and MIV-150 will be also highlighted. Future development may focus on the new generation of novel antiretroviral inhibitors with higher bioavailability, longer elimination half-life, more favorable side-effect profiles, fewer drug-drug interactions, and higher activities against circulating drug-resistant strains.
Identifiants
pubmed: 35847492
doi: 10.1016/j.apsb.2021.11.009
pii: S2211-3835(21)00443-3
pmc: PMC9279714
doi:
Types de publication
Journal Article
Review
Langues
eng
Pagination
1567-1590Commentaires et corrections
Type : ErratumIn
Informations de copyright
© 2022 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
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