Compounds > apricitabine
Page last updated: 2024-12-08

apricitabine

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Description

apricitabine: BCH-10619 is the (+)-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID455041
CHEMBL ID210651
SCHEMBL ID1101075
MeSH IDM0502430

Synonyms (56)

Synonym
160707-69-7
avx-754
(-)-bch-10652
bch-270
4-amino-1-[(2r,4r)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]pyrimidin-2-one
bch-10652
(+/-)-cis-1-[2-(hydroxymethyl)-5-(1,3-oxathiolanyl)]cytosine
(+/-)dotc
(+/-)-2'-deoxy-3'-oxa-4'-thiocytidine
spd754
(-)-dotc
bch-10618
avx754
(-)-2'-deoxy-3'-oxa-4'-thiocytidine
spd-754
apricitabine
bch-10619
CHEMBL210651
bch-10652, (-)-
spd -754
apricitabine, (+/-)-
dnd9y3g72c ,
143338-12-9
2(1h)-pyrimidinone, 4-amino-1-((2r,4r)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-, rel-
unii-k1yx059ml1
avx 754
spd 754
2(1h)-pyrimidinone, 4-amino-1-(2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-, (2r-cis)-
bch 10618
apricitabine [inn]
bch10619
2(1h)-pyrimidinone, 4-amino-1-((2r,4r)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-
(-)-bch 10652
k1yx059ml1 ,
apricitabine [mi]
4-amino-1-((2r,4r)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)pyrimidin-2(1h)-one
AKOS022181355
4-amino-1-[(2r,4r)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]-2(1h)-pyrimidinone
RYMCFYKJDVMSIR-RNFRBKRXSA-N
2-(r)-hydroxymethyl-4-(r)-(cytosin-1-yl)-1,3-oxathiolane
AS-2749
SCHEMBL1101075
DTXSID60166974
DB12855
BCP07907
Q621846
HY-14913
bch10618
gtpl12677
mfcd09837753
(-)-2'-deoxy-3'-oxa-4'-thiocytidine (apricitabine)
spd754;avx754
2'-deoxy-3'-oxa-4'-thiocytidine, cis-
dotc, cis-(+/-)-
CS-0003629
2(1h)-pyrimidinone, 4-amino-1-[(2r,4r)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]-

Research Excerpts

Overview

Apricitabine is a novel deoxycytidine analogue reverse transcriptase inhibitor that is under development for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. It has clinical efficacy against both wild-type and drug-resistant HIV.

ExcerptReferenceRelevance
"Apricitabine is a novel deoxycytidine analog reverse transcriptase inhibitor. "( Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
Holdich, T; Sawyer, J; Shiveley, LA, 2007)		2.01
"Apricitabine is a novel deoxycytidine analogue reverse transcriptase inhibitor that is under development for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. "( In vitro interactions between apricitabine and other deoxycytidine analogues.
Bethell, R; Collins, P; De Muys, J; Hamelin, B; Lippens, J; Ren, C; Richard, A, 2007)		2.07
"Apricitabine is a novel deoxycytidine analogue reverse transcriptase inhibitor with clinical efficacy against both wild-type and drug-resistant HIV. "( Influence of food on the pharmacokinetics of apricitabine, a novel deoxycytidine analogue reverse transcriptase inhibitor.
Holdich, T; Sawyer, J, 2008)		2.05
"Apricitabine (ATC) is a nucleoside reverse transcriptase inhibitor (NRTI) being developed for the treatment of HIV. "( Apricitabine--a novel nucleoside reverse transcriptase inhibitor for the treatment of HIV infection that is refractory to existing drugs.
Cox, S; Southby, J, 2009)		3.24
"Apricitabine is a prodrug that is phosphorylated to its active triphosphate form intracellularly, which ultimately results in chain termination and inhibition of reverse transcription. "( Apricitabine: a nucleoside reverse transcriptase inhibitor for HIV infection.
Belliveau, PP; Gaffney, MM; Spooner, LM, 2009)		3.24
"Apricitabine is a deoxycytidine analogue nucleoside reverse transcriptase inhibitor for the treatment of HIV infection. "( Comparison of the pharmacokinetics of apricitabine in the presence and absence of ritonavir-boosted tipranavir: a phase I, open-label, controlled, single-centre study.
Borin, M; Cox, S; Linet, O; Perry, K; Southby, J; Tackwell, K, 2009)		2.07
"Apricitabine is a novel deoxycytidine nucleoside reverse transcriptase inhibitor (NRTI) currently in clinical development for the treatment of HIV infection. "( Resistance profile of the new nucleoside reverse transcriptase inhibitor apricitabine.
Cahn, P; Wainberg, MA, 2010)		2.03
"Apricitabine (ATC) is a novel deoxycytidine analogue nucleoside reverse transcriptase inhibitor (NRTI) with significant antiviral activity in vitro, including activity against HIV-1 with reverse transcriptase mutations that confer resistance to other NRTIs. "( Antiviral activity of apricitabine in treatment-experienced HIV-1-infected patients with M184V who are failing combination therapy.
Altclas, J; Cahn, P; Cassetti, I; Cooper, DA; Cox, S; Losso, M; Martins, M, 2011)		2.13
"Apricitabine (ATC) is a novel nucleoside reverse transcriptase inhibitor undergoing phase 2/3 clinical development for the treatment of HIV infection. "( Renal excretion of apricitabine in rats: ex vivo and in vivo studies.
Babayeva, M; Cox, S; Taft, DR; White, MP, 2011)		2.14
"Apricitabine (ATC) is a novel deoxycytidine analog reverse transcriptase inhibitor in development for the treatment of human immunodeficiency virus infection. "( Effects of trimethoprim on the clearance of apricitabine, a deoxycytidine analog reverse transcriptase inhibitor, and Lamivudine in the isolated perfused rat kidney.
Babayeva, M; Dontabhaktuni, A; Nakatani-Freshwater, T; Taft, DR, 2006)		2.04
"Apricitabine is a novel deoxycytidine analogue reverse transcriptase inhibitor that is undergoing clinical development for the treatment of HIV-1 infection. "( Pharmacokinetics of single oral doses of apricitabine, a novel deoxycytidine analogue reverse transcriptase inhibitor, in healthy volunteers.
Holdich, T; Sawyer, J; Shiveley, L, 2006)		2.04
"Apricitabine is a novel deoxycytidine analogue reverse transcriptase inhibitor under development for the treatment of human immunodeficiency virus-1 infection. "( Pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers treated with trimethoprim-sulphamethoxazole.
Cox, S; Sawyer, J; Shiveley, L; Struthers-Semple, C, 2008)		2.11

Effects

ExcerptReferenceRelevance
"Apricitabine has shown activity in treatment-experienced HIV-1-infected patients with NRTI resistance (with M184V and up to five TAMs) as well as in treatment-naive patients."( Resistance profile of the new nucleoside reverse transcriptase inhibitor apricitabine.
Cahn, P; Wainberg, MA, 2010)		1.31

Pharmacokinetics

The aim of this phase I study was to investigate whether administration of apricitabine with the HIV protease inhibitor tipranavir (ritonavir-boosted) affects the pharmacokinetic profile. This study was performed to investigate potential pharmacokinetics interactions between apricitABine and trimethoprim-sulphamethoxazole.

ExcerptReferenceRelevance
" Plasma concentrations declined in a log-linear manner over at least 12 hours, with an elimination half-life of approximately 3 hours."( Pharmacokinetics of single oral doses of apricitabine, a novel deoxycytidine analogue reverse transcriptase inhibitor, in healthy volunteers.
Holdich, T; Sawyer, J; Shiveley, L, 2006)		0.6
" On days 1 and 8, blood and urine samples were collected over 24 hours for pharmacokinetic analysis."( Multiple-dose pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in patients with HIV-1 infection.
Cahn, P; Cassetti, I; Holdich, T; Rolon, M; Sawyer, J; Shiveley, L, 2008)		0.63
" This study was performed to investigate potential pharmacokinetic interactions between apricitabine and trimethoprim-sulphamethoxazole."( Pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers treated with trimethoprim-sulphamethoxazole.
Cox, S; Sawyer, J; Shiveley, L; Struthers-Semple, C, 2008)		0.89
" The aim of this phase I study was to investigate whether administration of apricitabine with the HIV protease inhibitor tipranavir (ritonavir-boosted) affects the pharmacokinetic profile of apricitabine."( Comparison of the pharmacokinetics of apricitabine in the presence and absence of ritonavir-boosted tipranavir: a phase I, open-label, controlled, single-centre study.
Borin, M; Cox, S; Linet, O; Perry, K; Southby, J; Tackwell, K, 2009)		0.85
" Following dosing on days 1, 9 and 10, pharmacokinetic sampling was undertaken over 12 hours post-dosing to determine the plasma concentrations of apricitabine and tipranavir."( Comparison of the pharmacokinetics of apricitabine in the presence and absence of ritonavir-boosted tipranavir: a phase I, open-label, controlled, single-centre study.
Borin, M; Cox, S; Linet, O; Perry, K; Southby, J; Tackwell, K, 2009)		0.82

Bioavailability

ExcerptReferenceRelevance
" ATC is well absorbed orally, with a bioavailability of 65-80%."( Apricitabine: a novel deoxycytidine analogue nucleoside reverse transcriptase inhibitor for the treatment of nucleoside-resistant HIV infection.
Bethell, RC; Cahn, P; Cox, S; Sawyer, J; Wainberg, MA, 2007)		1.78

Dosage Studied

No adjustment of apricitabine dosing is required when administered with ritonavir-boosted tipranavir. Following dosing on days 1, 9 and 10, pharmacokinetic sampling was undertaken over 12 hours post-dosing.

ExcerptRelevanceReference
" Following dosing on days 1, 9 and 10, pharmacokinetic sampling was undertaken over 12 hours post-dosing to determine the plasma concentrations of apricitabine and tipranavir."( Comparison of the pharmacokinetics of apricitabine in the presence and absence of ritonavir-boosted tipranavir: a phase I, open-label, controlled, single-centre study.
Borin, M; Cox, S; Linet, O; Perry, K; Southby, J; Tackwell, K, 2009)		0.82
" No adjustment of apricitabine dosing is required when administered with ritonavir-boosted tipranavir."( Comparison of the pharmacokinetics of apricitabine in the presence and absence of ritonavir-boosted tipranavir: a phase I, open-label, controlled, single-centre study.
Borin, M; Cox, S; Linet, O; Perry, K; Southby, J; Tackwell, K, 2009)		0.96
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (62)

Assay IDTitleYearJournalArticle
AID546147Selectivity ratio of IC50 for 20 week drug adapted HIV1 HXB-2D harboring reverse transcriptase M184V, M41L, T215Y mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V, M41L, T215Y mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340669AUC (0 to 24 hrs) in healthy human at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340683Cmin in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546136Selectivity ratio of IC50 for 17 week drug adapted HIV1 HXB-2D harboring reverse transcriptase S68S/G mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546142Selectivity ratio of IC50 for 38 week drug adapted HIV1 HXB-2D harboring reverse transcriptase I50T/II, D237N/D mutant gene to IC50 for HIV1 HXB-2D harboring wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID341751Drug level in human resting PBMC assessed as apricitabine triphosphate level at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID340676AUC (0 to 24 hrs) in healthy human at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546152Antiviral activity against HIV1 HXB-2D harboring reverse transcriptase M184V, M41L and T215Y mutant gene infected in human cord blood mononuclear cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546144Selectivity ratio of IC50 for 51 week drug adapted HIV1 HXB-2D harboring reverse transcriptase M184V, K65R mutant gene to IC50 for HIV1 HXB-2D harboring wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546149Selectivity ratio of IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V, M41L and T215Y mutant gene to IC50 for wild type HIV1 HXB-2D infected in human cord blood mononuclear cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340687Tmax in healthy human PBMC assessed as intracellular apricitabine triphosphate level at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340671Renal clearance in healthy human at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340689Cmin in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340680Apparent terminal half life in healthy human at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID341744Antiviral activity against HIV in T cells assessed as inhibition of viral replication2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID546156Selectivity ratio of IC50 for 38 week drug adapted HIV1 HXB-2D harboring reverse transcriptase V101I/V, D177N, E194G mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340692Half life in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID341754Drug level in human phytohemagglutininin-activated PBMC assessed as apricitabine monophosphate level at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID340679Volume of distribution at steady state in healthy human at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546137Selectivity ratio of IC50 for 8 week drug adapted HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546153Antiviral activity against HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene infected in human cord blood mononuclear cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340691AUC (0 to 12 hrs) in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340688Cmax in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546151Selectivity ratio of IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V mutant gene to IC50 for wild type HIV1 HXB-2D infected in human cord blood mononuclear cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340685AUC (0 to 12 hrs) in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID341760Antiviral activity against HIV1 with reverse transcriptase M184V mutation in human phytohemagglutininin-activated PBMC assessed as inhibition of viral replication2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID341747Drug level in human resting PBMC assessed as apricitabine monophosphate level at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID340673Apparent terminal half life in healthy human at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340678Renal clearance in healthy human at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340690Ratio of Cmax to Cmin in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546146Selectivity ratio of IC50 for 8 week drug adapted HIV1 HXB-2D harboring reverse transcriptase M184V, M41L, T215Y mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V, M41L, T215Y mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546154Antiviral activity against HIV1 HXB-2D harboring reverse transcriptase M184V mutant gene infected in human cord blood mononuclear cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID341756Drug level in human phytohemagglutininin-activated PBMC assessed as apricitabine diphosphate level at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID546138Selectivity ratio of IC50 for 38 week drug adapted HIV1 HXB-2D harboring reverse transcriptase S68S/G mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340682Cmax in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546148Selectivity ratio of IC50 for 28 week drug adapted HIV1 HXB-2D harboring reverse transcriptase M184V, M41L, T215Y mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V, M41L, T215Y mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546139Selectivity ratio of IC50 for 17 week drug adapted HIV1 HXB-2D harboring reverse transcriptase D237N mutant gene to IC50 for HIV1 HXB-2D harboring wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340668Tmax in healthy human at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID341758Drug level in human phytohemagglutininin-activated PBMC assessed as apricitabine triphosphate level at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID546140Selectivity ratio of IC50 for 8 week drug adapted HIV1 HXB-2D harboring reverse transcriptase D237N mutant gene to IC50 for HIV1 HXB-2D harboring wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546157Selectivity ratio of IC50 for 32 week drug adapted HIV1 HXB-2D harboring reverse transcriptase V101I/V, D177N, E194G mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID341749Drug level in human resting PBMC assessed as apricitabine diphosphate level at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID546158Selectivity ratio of IC50 for 8 week drug adapted HIV1 HXB-2D harboring reverse transcriptase F87L/F mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340667Cmax in healthy human at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340686Half life in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID341746Drug level in human resting PBMC at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID546155Antiviral activity against wild type HIV1 HXB-2D infected in human cord blood mononuclear cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID341745Antiviral activity against HIV in PBMCs assessed as inhibition of viral replication2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID546150Selectivity ratio of IC50 for HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene to IC50 for wild type HIV1 HXB-2D infected in human cord blood mononuclear cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546135Selectivity ratio of IC50 for 32 week drug adapted HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase K65R mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340681Tmax in healthy human PBMC assessed as intracellular apricitabine triphosphate level at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340675Tmax in healthy human at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546143Selectivity ratio of IC50 for 48 week drug adapted HIV1 HXB-2D harboring reverse transcriptase M184V mutant gene to IC50 for HIV1 HXB-2D harboring wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID546141Selectivity ratio of IC50 for 32 week drug adapted HIV1 HXB-2D harboring wild type reverse transcriptase to IC50 for HIV1 HXB-2D harboring wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340672Volume of distribution at steady state in healthy human at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340677Apparent total oral clearance in healthy human at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340670Apparent total oral clearance in healthy human at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID340684Ratio of Cmax to Cmin in healthy human PBMC assessed as intracellular apricitabine triphosphate level per 10'6 cells at 600 mg, po administered twice daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID546145Selectivity ratio of IC50 for 51 week drug adapted HIV1 HXB-2D harboring reverse transcriptase M184V/M, K65R mutant gene to IC50 for HIV1 HXB-2D harboring wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
AID340674Cmax in healthy human at 600 mg, po twice daily coadministered with 300 mg, po Lamivudine once daily for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of Lamivudine on the plasma and intracellular pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers.
AID341753Drug level in human phytohemagglutininin-activated PBMC at 2.6 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro interactions between apricitabine and other deoxycytidine analogues.
AID546159Selectivity ratio of IC50 for 17 week drug adapted HIV1 HXB-2D harboring reverse transcriptase D177N/D, E194E/G mutant gene to IC50 for HIV1 HXB-2D harboring reverse transcriptase M184V mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's21 (87.50)29.6817
2010's3 (12.50)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.38

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.38 (24.57)
Research Supply Index3.50 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (33.33%)5.53%
Reviews5 (20.83%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (45.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.44206-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
ag-1549
capravirine: a non-nucleoside reverse transcriptase inhibitor		3.1210
benzophenone
benzophenone : The simplest member of the class of benzophenones, being formaldehyde in which both hydrogens are replaced by phenyl groups.		3.1210benzophenonesphotosensitizing agent;
plant metabolite
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		7.0310aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
cytidine triphosphate
Cytidine Triphosphate: Cytidine 5'-(tetrahydrogen triphosphate). A cytosine nucleotide containing three phosphate groups esterified to the sugar moiety.		3.1210cytidine 5'-phosphate;
pyrimidine ribonucleoside 5'-triphosphate		Escherichia coli metabolite;
mouse metabolite
deoxycytidine
[no description available]		10.18248pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		2.0510dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
zalcitabine
Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.		3.1210pyrimidine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		2.4420azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
lamivudine
[no description available]		4.1131monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
emtricitabine
Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection.		3.5320monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone		antiviral drug;
HIV-1 reverse transcriptase inhibitor
dexelvucitabine
dexelvucitabine: inhibits human hepatitis B virus (HBV) and human immunodeficiency virus (HIV) in vitro		3.1210
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		2.4420divalent inorganic anion;
phosphite ion
etravirine
[no description available]		3.1210aminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound		antiviral agent;
HIV-1 reverse transcriptase inhibitor
darunavir
Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.		3.1210carbamate ester;
furofuran;
sulfonamide		antiviral drug;
HIV protease inhibitor
trimethoprim, sulfamethoxazole drug combination
Trimethoprim, Sulfamethoxazole Drug Combination: A drug combination with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.. co-trimoxazole : A two-component mixture comprising trimethoprim and sulfamethoxazole.		3.4311
bevirimat
bevirimat: an HIV inhibitor; disrupts late step in processing HIV Major Core Protein p24, preventing the capsid precursor p25 from being converted to mature capsid p24. bevirimat : A pentacyclic triterpenoid obtained by the formal condensation of 2,2-dimethylsuccinic acid with the 3-hydroxy group of betulinic acid. It is isolated from the Chinese herb Syzygium claviflorum. The first in the class of HIV-1 maturation inhibitors to be studied in humans, bevirimat was identified as a potent HIV drug candidate and several clinical trials were conducted, but development into a new drug was plagued by numerous resistance-related problems.		2.0410dicarboxylic acid monoester;
monocarboxylic acid;
pentacyclic triterpenoid		HIV-1 maturation inhibitor;
metabolite
tenofovir
tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.		2.4420nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
sulfur
Sulfur: An element that is a member of the chalcogen family. It has an atomic symbol S, atomic number 16, and atomic weight [32.059; 32.076]. It is found in the amino acids cysteine and methionine.		3.1210chalcogen;
nonmetal atom		macronutrient
rilpivirine
[no description available]		2.0410aminopyrimidine;
nitrile		EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor
racivir
[no description available]		3.1210
tipranavir
tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor.		9.9221sulfonamideantiviral drug;
HIV protease inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
HIV Coinfection
[description not available]		07.99103
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		19.99103
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		02.9410
Bilateral Headache
[description not available]		03.4311
Bilateral Nasal Obstruction
[description not available]		03.4311
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		03.4311
Nasal Obstruction
Any hindrance to the passage of air into and out of the nose. The obstruction may be unilateral or bilateral, and may involve any part of the NASAL CAVITY.		03.4311