alovudine profile

Alovudine is a nucleoside reverse transcriptase inhibitor (NRTI) that was developed for the treatment of HIV infection. It is a prodrug that is converted to the active metabolite, alovudine triphosphate, inside cells. Alovudine triphosphate inhibits HIV reverse transcriptase by competing with the natural substrate, deoxythymidine triphosphate, for incorporation into the growing DNA chain. Alovudine has shown good antiviral activity in vitro and in vivo, but it was discontinued in clinical development due to toxicity concerns. The primary toxicity of alovudine was peripheral neuropathy, which is damage to the nerves in the hands and feet. Alovudine was also associated with other side effects, such as nausea, vomiting, and diarrhea. The development of other NRTIs with better safety profiles led to the discontinuation of alovudine.'

ID Source	ID
PubMed CID	33039
CHEMBL ID	105318
CHEBI ID	177762
SCHEMBL ID	133722
MeSH ID	M0043649

Synonym
1-[(2r,4s,5r)-4-luoro-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione
CHEBI:177762
nsc-140025
25526-93-6
cl-184824
alovudine (usan/inn)
D02830
fddt
alovudine
fddthd
1-[(2r,4s,5r)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-methyl-pyrimidine-2,4-dione
miv-310
3'-fddt
FLT ,
3'-fluoro-3'-deoxythymidine
3'f-tdr
3'-flt
3'-deoxy-3'-fluorothymidine, 97%
brn 0754299
alovudine [usan:inn]
drg-0097
cl 184824
nsc 140025
1-(3'-deoxy-3'-fluoro-beta-d-pentofuranosyl)thymine
bdbm50132287
3''-fluoro-2'',3''-dideoxythymidine
1-((2r,5r)-4-fluoro-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1h-pyrimidine-2,4-dione
1-((2r,4s,5r)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1h,3h)-dione
1-[(2r,4s,5r)-4-fluoro-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione
CHEMBL105318 ,
cl-184,824
cl 184,824
cas-25526-93-6
dtxsid4046579 ,
tox21_112376
dtxcid2026579
A817893
AKOS015917785
unii-pg53r0dwdq
3'-deoxy-3'-18f fluorothymidine
pg53r0dwdq ,
alovudine [usan]
alovudine [who-dd]
alovudine [inn]
S6848
3'-deoxy-3'-fluoro thymidine
SCHEMBL133722
tox21_112376_1
NCGC00166256-02
1-(3-fluoro-2,3-dideoxy-beta-d-erythro-pentofuranosyl)thymine
UXCAQJAQSWSNPQ-XLPZGREQSA-N
1-[(2r,4s,5r)-4-fluoro-5-(hydroxymethyl)oxolan-2-yl]-5-methyl-1,2,3,4-tetrahydropyrimidine-2,4-dione
AS-60404
3-deoxy-3-fluorothymidine
Q4734671
DB06198
HY-B1516
CS-0013305
3'-fluoro-3'-deoxythymidine (alovudine)

Excerpt	Reference	Relevance
"beta-D-Uridine protected human granulocyte-macrophage lineage cells in both semi-solid (granulocyte-macrophage colony-forming units, CFU-GM) and liquid cultures against the toxic effects of 3'-azido-3'-deoxythymidine (AZT), 3'-fluoro-3'-deoxythymidine (FLT) and a combination of AZT and FLT, without impairment of the activities of these respective drugs against human immunodeficiency virus (HIV) replication."	( Selective protection of toxicity of 2',3'-dideoxypyrimidine nucleoside analogs by beta-D-uridine in human granulocyte-macrophage progenitor cells. Faraj, A; Gosselin, G; Imbach, JL; Perigaud, C; Schinazi, RF; Sommadossi, JP; Xie, MY, 1996)	0.29
"FLT is a safe radiotracer for quantifying proliferation in the human cancer setting."	( NCI-sponsored trial for the evaluation of safety and preliminary efficacy of FLT as a marker of proliferation in patients with recurrent gliomas: safety studies. Eary, JF; Hoffman, JM; Krohn, KA; Link, JM; Muzi, M; Spence, AM, 2008)	0.35

Excerpt	Reference	Relevance
" The pharmacokinetic properties of these compounds in rhesus monkeys after intravenous, oral, and subcutaneous administration of the drug were compared."	( Pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-deoxy-2',3'-didehydrothymidine in rhesus monkeys. Boudinot, FD; Doshi, KJ; McClure, HM; Schinazi, RF, 1990)	0.28
" Secondly, the calculation of pharmacokinetic parameter estimates is discussed including an algorithm for dealing with multicompartment models and direct studies of transfer rate constants."	( Microdialysis in pharmacokinetics. Ståhle, L, )	0.13
" The concentrations attained in blood and muscle were similar for each drug, with a Cmax of 57 microM (blood) and 54 microM (muscle) for alovudine and 38 and 46 microM, respectively, for zidovudine."	( Pharmacokinetics and extracellular distribution to blood, brain, and muscle of alovudine (3'-fluorothymidine) and zidovudine in the rat studied by microdialysis. Guzenda, E; Ljungdahl-Ståhle, E; Ståhle, L, 1993)	0.72
" Here, we describe preclinical characterization of alisertib (MLN8237), a selective AAK inhibitor, incorporating these novel pharmacodynamic assays."	( Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays. Bolen, JB; Chakravarty, A; Chen, W; Claiborne, CF; Ecsedy, JA; Germanos, MS; Gershman, RE; Hoar, KM; Huck, JJ; Hyer, ML; Janowick, DA; Leroy, PJ; Manfredi, MG; Sells, TB; Shinde, V; Silva, MD; Silverman, L; Stroud, SG; Wysong, DR; Zhang, M, 2011)	0.37
" VEGF levels and sunitinib pharmacokinetic (PK) data were assessed at the same time points."	( Pharmacodynamic study using FLT PET/CT in patients with renal cell cancer and other solid malignancies treated with sunitinib malate. Carmichael, L; Chao, B; Eickhoff, J; Harrison, M; Ivy, P; Jeraj, R; Kolesar, J; Liu, G; Marnocha, R; Perlman, S; Simoncic, U; Vanderhoek, M; Wilding, G, 2011)	0.37
"Sixteen patients (8 patients on 4/2 schedule and 8 patients on 2/1 schedule) completed all three planned FLT PET/CT scans and were evaluable for pharmacodynamic imaging evaluation."	( Pharmacodynamic study using FLT PET/CT in patients with renal cell cancer and other solid malignancies treated with sunitinib malate. Carmichael, L; Chao, B; Eickhoff, J; Harrison, M; Ivy, P; Jeraj, R; Kolesar, J; Liu, G; Marnocha, R; Perlman, S; Simoncic, U; Vanderhoek, M; Wilding, G, 2011)	0.37
" The whole-body and tumor pharmacokinetic (PK) parameters of this model can be noninvasively measured with molecular imaging, providing a means of comparing potential TRT agents."	( Application of a whole-body pharmacokinetic model for targeted radionuclide therapy to NM404 and FLT. Burnette, RR; Floberg, JM; Grudzinski, JJ; Jeffery, JJ; Jeraj, R; Mudd, SR; Nomura, A; Peterson, ET; Tomé, WA; Weichert, JP, 2012)	0.38
" In this study, we aimed to investigate the effect of early frame sampling and reconstruction method on pharmacokinetic parameters obtained from a 2-tissue model, in terms of bias and uncertainty (SD)."	( A Monte Carlo study of the dependence of early frame sampling on uncertainty and bias in pharmacokinetic parameters from dynamic PET. Axelsson, J; Garpebring, A; Häggström, I; Johansson, L; Karlsson, M; Larsson, A; Schmidtlein, CR; Sörensen, J, 2015)	0.42
" Plasma VEGF and axitinib pharmacokinetic levels were also assessed at specified time points."	( Pharmacodynamic study of axitinib in patients with advanced malignancies assessed with (18)F-3'deoxy-3'fluoro-L-thymidine positron emission tomography/computed tomography. Bruce, JY; Carmichael, LL; Eickhoff, JC; Heideman, JL; Jeraj, R; Kolesar, JM; Liu, G; Perlman, SB; Scully, PC, 2015)	0.42
" In this study we investigate the safety/tolerability and pharmacodynamic effects of docetaxel used in sequential combination with the novel VEGFR-TKI X-82."	( Pharmacodynamic study using FLT PET/CT in advanced solid malignancies treated with a sequential combination of X-82 and docetaxel. Binger, K; Bruce, JY; Carmichael, L; Dukart, G; Eickhoff, J; Harrow, K; Heideman, J; Jeraj, R; Kolesar, J; Liang, C; Liu, G; Perlman, S; Rampurwala, M; Scarpelli, M, 2018)	0.48
" Further, decrease in FLT uptake during cycle 2 (X-82 plus docetaxel) was greater than in cycle 1 (X-82 alone), suggesting sequential chemotherapy enhances the pharmacodynamic effect of therapy."	( Pharmacodynamic study using FLT PET/CT in advanced solid malignancies treated with a sequential combination of X-82 and docetaxel. Binger, K; Bruce, JY; Carmichael, L; Dukart, G; Eickhoff, J; Harrow, K; Heideman, J; Jeraj, R; Kolesar, J; Liang, C; Liu, G; Perlman, S; Rampurwala, M; Scarpelli, M, 2018)	0.48

Excerpt	Reference	Relevance
" The most potent inhibitor, 3'-fluoro-3'-deoxythymidine, was shown to give synergistic inhibition of HIV-1 replication in combination with the PPi analog phosphonoformate."	( Structure-activity relationships of fluorinated nucleoside analogs and their synergistic effect in combination with phosphonoformate against human immunodeficiency virus type 1. Cox, S; Gilljam, G; Harmenberg, J; Koshida, R; Wahren, B, 1989)	0.28
" Anti-proliferative effects of sorafenib were evidenced by (1)H MRS and (18)F-FLT PET after 2 days of treatment with sorafenib, with no additional effect of the combination with radiation therapy, results that are in agreement with Ki67 staining."	( Multimodal imaging of tumor response to sorafenib combined with radiation therapy: comparison between diffusion-weighted MRI, choline spectroscopy and 18F-FLT PET imaging. Bol, A; Bouzin, C; Danhier, P; Feron, O; Gallez, B; Grégoire, V; Jordan, BF; Karmani, L; Karroum, O; Kengen, J; Labar, D; Levêque, P; Magat, J; Mignion, L, )	0.13
" We hypothesized that the combination with rationally selected other therapeutic agents may improve response."	( Temsirolimus combined with cisplatin or bevacizumab is active in osteosarcoma models. Boerman, OC; Fleuren, ED; Flucke, UE; Franssen, GM; Houghton, PJ; Oyen, WJ; Roeffen, MH; van der Graaf, WT; Versleijen-Jonkers, YM, 2014)	0.4

Excerpt	Reference	Relevance
" Oral bioavailability of 3'-deoxy-2',3'-didehydrothymidine was incomplete, with an average of 42% +/- 15% of the dose reaching the systemic circulation."	( Pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-deoxy-2',3'-didehydrothymidine in rhesus monkeys. Boudinot, FD; Doshi, KJ; McClure, HM; Schinazi, RF, 1990)	0.28
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" Neither compound prevented the infection despite dosing prior to virus inoculation."	( Antiviral effects of 3'-fluorothymidine and 3'-azidothymidine in cynomolgus monkeys infected with simian immunodeficiency virus. Böttiger, D; Ljungdahl-Ståhle, E; Lundgren, B; Norrby, E; Oberg, B; Ståhle, L; Wahren, B, 1991)	0.28
" In an initial open-label CCT involving 14 subjects infected with human immunodeficiency virus (HIV), unacceptable hematologic toxicity occurred when the area under the concentration-time curve during a 12-h dosing interval (AUC12) was > or = 300 ng*h/mL."	( Relationship between plasma concentrations of 3'-deoxy-3'-fluorothymidine (alovudine) and antiretroviral activity in two concentration-controlled trials. Armstrong, D; Barditch-Crovo, PA; Baron, PA; Duncanson, F; Flexner, C; Ganes, D; Jacobson, MA; Petty, BG; Powderly, W; van der Horst, C, 1994)	0.52
" Cell lines also underwent 1) [(3)H]NBMPR equilibrium binding assays with or without 5-S-{2-(1-[(fluorescein-5-yl)thioureido]hexanamido)ethyl}-6-N-(4-nitrobenzyl)-5-thioadenosine, a membrane-impermeable NBMPR analog, to determine plasma membrane hENT1 levels, and 2) dose-response NBMPR inhibition of [(3)H]FLT uptake."	( The role of human nucleoside transporters in uptake of 3'-deoxy-3'-fluorothymidine. Cass, CE; Graham, K; Ng, AM; Paproski, RJ; Yao, SY; Young, JD, 2008)	0.35
"PET/CT scans obtained at a median of 2 mo after initial dosing did not demonstrate significant changes in lesion size or (18)F-FDG or (18)F-FLT uptake when focusing on metastatic lesions."	( Imaging of CTLA4 blockade-induced cell replication with (18)F-FLT PET in patients with advanced melanoma treated with tremelimumab. Allen-Auerbach, MS; Benz, MR; Chmielowski, B; Czernin, J; Gomez-Navarro, J; McCarthy, T; Radu, C; Ribas, A; Seja, E; Williams, JL, 2010)	0.36
" On the other hand, HCT8 cells showed a biphasic [(18)F]FLT flare with lacked TK1 induction in response to the dosage of 5-FU."	( Induction of thymidine kinase 1 after 5-fluorouracil as a mechanism for 3'-deoxy-3'-[18F]fluorothymidine flare. Chung, JH; Hong, YS; Kim, SY; Kim, TW; Lee, SJ; Moon, DH; Oh, SJ; Ryu, JS, 2010)	0.36
" Tumor uptake of [(18)F]-FLT was significantly reduced following GDC-0941 dosing in responsive tumors at the acute time point and correlated with pharmacodynamic markers of PI3K signaling inhibition and significant reduction in TK1 expression in U87, but not HCT116, tumors."	( [18F]-FLT positron emission tomography can be used to image the response of sensitive tumors to PI3-kinase inhibition with the novel agent GDC-0941. Babur, M; Brown, G; Burrows, N; Cawthorne, C; Dive, C; Forster, D; Gieling, RG; Gregory, J; Hiscock, D; Hodgkinson, C; McMahon, A; Morrow, CJ; Radigois, M; Simpson, K; Smigova, A; Williams, KJ; Wilson, I, 2013)	0.39
"5 mg continuous daily dosing of sunitinib."	( FDG and FLT-PET for Early measurement of response to 37.5 mg daily sunitinib therapy in metastatic renal cell carcinoma. Agarwal, N; Beardmore, B; Boucher, K; Butterfield, RI; Hoffman, JM; Horn, KP; Kadrmas, DJ; Morton, KA; Yap, JT, 2015)	0.42
" Sixteen patients enrolled in the pharmacodynamic cohort demonstrated significant decreases in SUVs and increases in VEGF during dosing periods."	( Bruce, JY; Carmichael, L; Eickhoff, J; Jeraj, R; Kolesar, J; Liu, G; Perlman, S; Scarpelli, M, 2016)	0.43
"Response to axitinib included diminished FLT uptake during dosing periods followed by increased FLT uptake during drug washout periods."	( Bruce, JY; Carmichael, L; Eickhoff, J; Jeraj, R; Kolesar, J; Liu, G; Perlman, S; Scarpelli, M, 2016)	0.43

Class	Description
pyrimidine 2',3'-dideoxyribonucleoside
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
TDP1 protein	Homo sapiens (human)	Potency	11.7364	0.0008	11.3822	44.6684	AID686978; AID686979
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	21.8761	0.0123	7.9835	43.2770	AID1645841
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	0.0335	0.0030	41.6115	22,387.1992	AID1159552
Histone H2A.x	Cricetulus griseus (Chinese hamster)	Potency	0.0495	0.0391	47.5451	146.8240	AID1224845; AID1224896
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Thymidylate kinase	Mycobacterium tuberculosis H37Rv	Ki	28.0000	4.5000	8.5000	10.0000	AID210904
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	IC50 (µMol)	0.0500	0.0001	1.0768	10.0000	AID197924
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	ED50	0.0010	0.0002	0.9935	9.8000	AID105582
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (125)

Assay ID	Title	Year	Journal	Article
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1610167	Antiviral activity against Human adenovirus 2 infected in human HELF cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by microscopic analysis	2019	European journal of medicinal chemistry, Dec-15, Volume: 184	Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID1141005	Antiretroviral activity against HIV-1 3B infected in human CEM/0 cells expressing thymidine kinase assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis	2014	Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10	Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
AID479437	Antimycobacterial activity against Mycobacterium tuberculosis H37Ra at 100 ug/ml after 6 days by microplate alamar blue assay	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis.
AID1447283	Inhibition of HIV1 BaL dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9	Synthesis and anti-HIV activities of unsymmetrical long chain dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID105578	Concentration required to affect a 50% reduction in the cytopathic effect of HIV for MT-4 cells	1992	Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18	3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine.
AID675197	Ratio of AZT EC50 to compound EC50 for HIV-1 subtype B US/92/727 infected in PBMC	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1447282	Inhibition of HIV1 3B dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9	Synthesis and anti-HIV activities of unsymmetrical long chain dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID105766	Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 5 uM concentration	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID46200	Tested for in vitro drug concentration which produces 50% survival of HIV-1 infected CEM cells relative to uninfected untreated controls	1994	Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21	Synthesis and antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine diastereomers. Potential prodrugs to 3'-fluoro-3'-deoxythymidine.
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID157559	Cytotoxic concentration required to inhibit 50% of HIV-1 in peripheral blood mononuclear cells (PBMC)	1997	Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21	Probing the mechanism of action and decomposition of amino acid phosphomonoester amidates of antiviral nucleoside prodrugs.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID664466	Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
AID675192	Therapeutic index, ratio of TC50 for human PBMC to EC50 for HIV-1 subtype B US/92/727 infected in PBMC	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID32065	Protection of ATH8 cells against the cytopathic effect of HIV.	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID210721	Antiviral activity against thymidine kinase from Herpes simplex virus type-2 (333 Strain) infected HeLa (Bu-25-TK-) cells at 500 uM concentration	1993	Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3	Syntheses and biological evaluations of 3'-deoxy-3'-C-branched-chain-substituted nucleosides.
AID664467	Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
AID105373	Concentration required to reduce the number of viable cells in the untreated MT-4 cell culture	1992	Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18	3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID664469	Antiviral activity against wild type HIV1 clade B 94US3393IN clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround infecti	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID81069	Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells.	1988	Journal of medicinal chemistry, Oct, Volume: 31, Issue:10	Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides.
AID1865335	Antiviral activity against thymidine deficient HIV2 ROD infected in CEM-TK(-) cells assessed as inhibition of HIV induced cytopathogenic effects	2022	Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18	Triphosphate Prodrugs of the Anti-HIV-Active Compound 3'-Deoxy-3'-fluorothymidine (FLT).
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID21032	Partition coefficient which is the ratio of its concentration in octanol to concentration in water	1994	Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21	Synthesis and antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine diastereomers. Potential prodrugs to 3'-fluoro-3'-deoxythymidine.
AID106976	Effective concentration achieving 50% protection of MT-4 cells against the cytopathic effect of HIV-1	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.
AID664470	Antiviral activity against wild type HIV1 clade C 98USMSC5016 clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround infect	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
AID1141006	Antiretroviral activity against HIV-2 ROD infected in human CEM/0 cells expressing thymidine kinase assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis	2014	Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10	Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
AID235480	Selectivity index is the ratio of CC50 to EC50	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID235875	Ratio of CD50 to ED50 rvaluated for inhibition of HIV replication in MT-4 cells	1988	Journal of medicinal chemistry, Oct, Volume: 31, Issue:10	Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides.
AID675188	Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID1865333	Antiviral activity against HIV1 HE strain infected in CEM/0 cells assessed as inhibition of HIV induced cytopathogenic effects	2022	Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18	Triphosphate Prodrugs of the Anti-HIV-Active Compound 3'-Deoxy-3'-fluorothymidine (FLT).
AID1141009	Cytostatic activity against thymidine kinase-deficient human CEM cells assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis	2014	Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10	Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
AID664471	Antiviral activity against NNRTI-resistant HIV1 clade B A-17 clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround infecti	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
AID1141007	Antiretroviral activity against HIV-2 ROD infected in thymidine kinase-deficient human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis	2014	Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10	Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
AID105748	Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.008 uM concentration; Range is 10-40	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID1325061	Cytotoxicity against HEL cells assessed as alteration of cell morphology after 3 days by microscopic analysis	2016	Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21	First discovery of novel 3-hydroxy-quinazoline-2,4(1H,3H)-diones as specific anti-vaccinia and adenovirus agents via 'privileged scaffold' refining approach.
AID105376	Cytotoxic dose in MT-4 cells	1989	Journal of medicinal chemistry, Aug, Volume: 32, Issue:8	3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues.
AID1141008	Cytostatic activity against human CEM/0 cells expressing thymidine kinase assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis	2014	Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10	Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
AID1610153	Cytotoxicity against human HELF cells assessed as minimum cytotoxic concentration by observing alteration in cell morphology incubated for 3 days by microscopic analysis	2019	European journal of medicinal chemistry, Dec-15, Volume: 184	Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID1141013	Ratio of EC50 for HIV-2 ROD infected in thymidine kinase-deficient human CEM cells to EC50 for HIV-2 ROD infected in human CEM/0 cells expressing thymidine kinase	2014	Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10	Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID235486	Selectivity index is the ratio of ED50 and CD50 values against inhibition of HIV-1 in MT-4 cells	1989	Journal of medicinal chemistry, Aug, Volume: 32, Issue:8	3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues.
AID106607	Cytotoxic concentration required to reduce the viability of normal uninfected MT-4 cells by 50%	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.
AID45990	Cytotoxic concentration required to inhibit 50% of HIV-1 in CEM cells	1997	Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21	Probing the mechanism of action and decomposition of amino acid phosphomonoester amidates of antiviral nucleoside prodrugs.
AID81438	Dose required to inhibit cytopathic effect of human immunodeficiency virus replication in MT-4 cells.	1988	Journal of medicinal chemistry, Oct, Volume: 31, Issue:10	Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides.
AID664468	Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID197924	Concentration required to inhibit HIV reverse transcriptase	1992	Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18	3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine.
AID675191	Cytotoxicity against human PBMC	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID105762	Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.2 uM concentration	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID675190	Therapeutic index, ratio of TC50 for human CEM-SS cells to EC50 for HIV-1 subtype 3B infected in CEM-SS cells	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1498117	Antiviral activity against Adenovirus 2 infected in HEL cells assessed as inhibition of virus-induced cytopathicity	2018	Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12	Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
AID675189	Cytotoxicity against human CEM-SS cells by XTT method	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID105759	Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.00032 uM concentration	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID210720	Antiviral activity against thymidine kinase from Herpes simplex virus type-1 (KOS Strain) infected HeLa (Bu-25-TK-) cells at 500 uM concentration	1993	Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3	Syntheses and biological evaluations of 3'-deoxy-3'-C-branched-chain-substituted nucleosides.
AID1447284	Cytotoxicity against human P4R5 MAGI cells after 2 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9	Synthesis and anti-HIV activities of unsymmetrical long chain dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID210719	Antiviral activity against thymidine kinase activity from K562 mammalian cells at 500 uM concentration	1993	Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3	Syntheses and biological evaluations of 3'-deoxy-3'-C-branched-chain-substituted nucleosides.
AID675187	Antiviral activity against HIV-1 subtype B US/92/727 infected in PBMC assessed as inhibition of viral replication after 7 days by XTT assay	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID105761	Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.008 uM concentration; Range is 10-40	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID1427837	Cytotoxicity against virus infected HEL cells assessed as alteration in cell morphology by microscopic method
AID1865336	Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability	2022	Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18	Triphosphate Prodrugs of the Anti-HIV-Active Compound 3'-Deoxy-3'-fluorothymidine (FLT).
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID105746	Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.00032 uM concentration; Range is 10-40	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID210904	Inhibitory activity against thymidine monophosphate kinase (TMPK) in Mycobacterium tuberculosis	2003	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18	Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.
AID199981	Inhibition of HIV-1 reverse transcriptase; + = active	1994	Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16	HIV-1 reverse transcriptase inhibitor design using artificial neural networks.
AID105764	Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 125 uM concentration	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID105582	Inhibitory activity against HIV-1 replication in MT-4 cells	1989	Journal of medicinal chemistry, Aug, Volume: 32, Issue:8	3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues.
AID675196	Ratio of FLT EC50 to compound EC50 for HIV-1 subtype 3B infected in CEM-SS cells	2012	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17	Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors.
AID155102	Effective concentration required to inhibit 50% of HIV-1 in peripheral blood mononuclear cells (PBMC)	1997	Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21	Probing the mechanism of action and decomposition of amino acid phosphomonoester amidates of antiviral nucleoside prodrugs.
AID78749	Compound was tested for anti-HIV activity in H9 cell line; Active	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Fluorinated sugar analogues of potential anti-HIV-1 nucleosides.
AID1865334	Antiviral activity against HIV2 ROD infected in CEM/0 cells assessed as inhibition of HIV induced cytopathogenic effects	2022	Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18	Triphosphate Prodrugs of the Anti-HIV-Active Compound 3'-Deoxy-3'-fluorothymidine (FLT).
AID458192	Activity at Drosophila melanogaster dNK by spectrophotometry	2010	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3	Synthesis of fluorescent nucleoside analogs as probes for 2'-deoxyribonucleoside kinases.
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1325060	Antiviral activity against Human adenovirus 2 infected in HEL cells assessed as inhibition of virus-induced cytopathicity	2016	Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21	First discovery of novel 3-hydroxy-quinazoline-2,4(1H,3H)-diones as specific anti-vaccinia and adenovirus agents via 'privileged scaffold' refining approach.
AID1141010	Cytostatic activity against mouse L1210 cells assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis	2014	Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10	Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
AID1498130	Cytotoxicity against HEL cells assessed as alteration of cell morphology by microscopic analysis	2018	Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12	Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID664472	Antiviral activity against multidrug-resistant HIV1 clade B 4775-5 clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround i	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
AID1427834	Antiviral activity against Human adenovirus 2 infected in HEL cells assessed as reduction in virus-induced cytopathogenicity
AID1079938	Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID234204	Therapeutic index (Ratio = ID50/ED50).	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID32066	Required dose to reduce viability of normal uninfected ATH8 cells.	1987	Journal of medicinal chemistry, Aug, Volume: 30, Issue:8	3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
AID104472	Inhibitory effect on human immunodeficiency virus type-1 (HIV-1) in MT-4 cells	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	Synthesis and antiviral activity of some 3'-C-difluoromethyl and 3'-deoxy-3'-C-fluoromethyl nucleosides.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	11 (1.93)	18.7374
1990's	42 (7.36)	18.2507
2000's	158 (27.67)	29.6817
2010's	336 (58.84)	24.3611
2020's	24 (4.20)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	83 (13.97%)	5.53%
Reviews	47 (7.91%)	6.00%
Case Studies	27 (4.55%)	4.05%
Observational	0 (0.00%)	0.25%
Other	437 (73.57%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (38)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Study of the Effects of Dexamethasone on Non-Small Cell Lung Cancer Using [F-18] FLT for Imaging With Positron Emission Tomography (PET) [NCT02819024]		6 participants (Actual)	Interventional	2016-06-30	Active, not recruiting
A Study of 18F-FLT Positron Emission Tomography/Computed Tomography (PET/CT) Imaging in Cases of Prefibrotic/Early Primary Myelofibrosis (PMF) and Essential Thrombocythemia (ET) [NCT03116542]		21 participants (Anticipated)	Interventional	2017-05-07	Recruiting
Monitoring Treatment Response in Women With Breast Cancer Utilizing FLT-PET/CT [NCT01018251]		0 participants (Actual)	Interventional	2009-03-31	Withdrawn
A Pilot Study of FLT-PET/MRI for Early Response Monitoring to Novel Cancer Therapeutic Agents [NCT02055586]		10 participants (Actual)	Observational	2013-10-22	Completed
A Phase 1 Dose-Escalation Study of ABT-888 (Veliparib) in Combination With Carboplatin in HER2 Negative Metastatic Breast Cancer [NCT01251874]	Phase 1	44 participants (Actual)	Interventional	2010-11-16	Completed
A Pilot Study Investigating ¹⁸F-FLT-PET as a Marker of Response to Preoperative Radiotherapy in Soft Tissue Sarcoma [NCT03613259]	Early Phase 1	0 participants (Actual)	Interventional	2020-06-01	Withdrawn(stopped due to Funding expired)
Could Positon Emission Tomography With Radiolabelled 3'-Deoxy-3'-(18)F-Fluoro-L-Thymidine be a Theranostic Tool During Erlotinib Treatment in Non-small Cell Lung Cancer Patients ? [NCT02069418]	Phase 2	80 participants (Anticipated)	Interventional	2014-02-28	Active, not recruiting
Multi-Institutional Prospective Pilot Study of Lupron to Enhance Lymphocyte Immune Reconstitution Following Allogeneic Bone Marrow Transplantation in Post-Pubertal Children and Adults With Molecular Imaging Evaluation [NCT01338987]	Phase 2	76 participants (Actual)	Interventional	2011-04-19	Completed
Multi-Modality Imaging and Correlative Studies in Patients With Leukemia [NCT03422731]	Early Phase 1	74 participants (Anticipated)	Interventional	2018-02-15	Recruiting
Early Prediction of Clinical Response to Chemotherapy With FLT-PET [NCT00880074]	Phase 1	10 participants (Actual)	Interventional	2009-04-09	Completed
A Study of 18F-FLT Positron Emission Tomography (PET)/Computed Tomography Imaging in Pediatrics With Myeloproliferative Neoplasms [NCT03121599]		3 participants (Actual)	Interventional	2017-06-11	Terminated(stopped due to Delayed study materials, poor recruitment)
Phase II Single-Arm Trial Comparing the Use of FLT PET to Standard Computed Tomography to Assess the Treatment Response of Neoadjuvant Docetaxel and Cisplatin in Stage IB-IIIA Resectable Non-small Cell Lung Cancer [NCT00963807]	Phase 2	26 participants (Actual)	Interventional	2009-09-30	Completed
3'-Deoxy-3'-18F Fluorothymidine PET/CT in Predicting Response To Chemotherapy Before Surgery in Patients With Locally Advanced Breast Cancer [NCT00572728]	Phase 2	90 participants (Actual)	Interventional	2008-12-31	Completed
Pharmacodynamic Study of Sunitinib Malate in Patients With Renal Cell Cancer and Other Advanced Solid Malignancies [NCT00499135]	Phase 1	25 participants (Actual)	Interventional	2007-05-22	Completed
A Contiguous, Sequential Phase I/II Imaging Study of 18F-fluoro-3'-L-fluorothymidine (18F-FLT) in Patients With Known or Suspected Carcinoma of the Lung, Breast, Renal Cell, Pancreas, or Brain, and With Gastrointestinal Malignancies, Neuroendocrine Tumour [NCT01065805]	Phase 1/Phase 2	94 participants (Actual)	Interventional	2009-03-20	Terminated(stopped due to Retirement of former Qualified Investigator and lack of resources to complete study)
An Evaluation of Preoperative Chemotherapy With Irinotecan and Cisplatin for Advanced, But Resectable Gastric Cancer: A Coordinated Multidisciplinary, Multicenter Study Linking Functional Imaging, Genomic Expression Profiles and Histopathology [NCT00062374]	Phase 2	55 participants (Actual)	Interventional	2003-06-30	Completed
Pilot Study of 18F-FLT Pet Imaging in Cancer Patients [NCT00585741]		15 participants (Actual)	Interventional	2006-12-31	Terminated
SARC037: A Phase I/II Study to Evaluate the Safety of Trabectedin Administered as a 1-Hour Infusion in Ewing Sarcoma Patients in Combination With Low Dose Irinotecan and 3'-Deoxy-3'-18F Fluorothymidine (18F-FLT) Imaging [NCT04067115]	Phase 1/Phase 2	48 participants (Anticipated)	Interventional	2021-01-05	Active, not recruiting
Evaluation of 3'-Deoxy-3'-[18F]Fluorothymidine -PET and Diffusion Weighted Imaging -MRI in Patients With Early Stage Non-small Cell Lung Cancer Treated With a Platinum-based Doublet as Preoperative Chemotherapy [NCT02273271]		31 participants (Anticipated)	Interventional	2015-10-31	Recruiting
A Pilot Study to Evaluate the Correlation Between 18F-FLT-PET Uptake, Ki-67 Immunohistochemistry, and Proliferation Signature in Response to Neo-Adjuvant Chemotherapy in Breast Cancer [NCT01015131]	Phase 2	46 participants (Actual)	Interventional	2010-04-08	Completed
A Pilot, Non-Therapeutic NeuroImaging Study of 18F-FLT in Pediatric Patients With Newly Diagnosed Central Nervous System Tumors [NCT00633958]	Phase 1	2 participants (Actual)	Interventional	2008-03-31	Terminated(stopped due to Large phase II opened to accue same patients)
A Phase I, Open Label, Single Center Safety Study of [F-18]FLT [NCT00553748]	Phase 1	11 participants (Actual)	Interventional	2007-11-30	Completed
18-FLT PET/MR Imaging to Predict Graft Failure and Graft Versus Host Disease in Bone Marrow Transplant Patients [NCT03546556]	Early Phase 1	10 participants (Actual)	Interventional	2017-01-01	Terminated(stopped due to Study terminated due to COVID-19 pandemic and not being able to perform PET/MR scans on participants.)
A Phase II Neoadjuvant Study of Encorafenib With Binimetinib in Patients With Resectable Locoregional Metastases From Cutaneous or Unknown Primary Melanoma (Stages III N1B/C/D) [NCT04221438]	Phase 2	3 participants (Actual)	Interventional	2021-09-22	Active, not recruiting
Validation of 18F-MISO-PET and 18F-FLT-PET by Immunohistochemical Assessment of Head and Neck Cancer Resection Specimen [NCT00159978]		21 participants (Actual)	Observational	2005-07-31	Terminated(stopped due to Problems with FMISO supply)
Early Assessment of Treatment Response in AML Using FLT PET/CT Imaging [NCT02392429]	Phase 2	57 participants (Anticipated)	Interventional	2016-04-20	Active, not recruiting
Imaging Early Response of ER+, HER2- Breast Cancer to Aromatase Inhibitor (AI) +/- Ovarian Suppression (OS) Therapy With [18F]Fluorothymidine (FLT) PET [NCT01928186]		28 participants (Actual)	Interventional	2011-09-30	Completed
An Open-Label, Crossover Study to Assess the Effect of Food on the Oral Bioavailability and Pharmacokinetic Profile of 3'-Deoxy-3'-Fluorothymidine (FLT) in Asymptomatic Human Immunodeficiency Virus (HIV)-Infected Subjects [NCT00002260]		0 participants	Interventional		Completed
Use of 18F-FLT Positron Emission Tomography to Evaluate the Suspicious Findings on Mammography and Breast Ultrasound: A Pilot Study [NCT01713049]		70 participants (Anticipated)	Interventional	2010-08-31	Recruiting
An Ascending, Single Oral Dose Pharmacokinetic Study of 3'-Deoxy-3'-Fluorothymidine (FLT) in Asymptomatic Human Immunodeficiency Virus (HIV)-Infected Subjects [NCT00002271]		0 participants	Interventional		Completed
Image-Guided Stereotactic Biopsy of High Grade Gliomas [NCT00979810]		11 participants (Actual)	Interventional	2009-09-16	Completed
Multi-tracer PET Assessment of Response in Various Malignancies in Investigational and Recently Approved Therapeutic Agents [NCT01243333]		26 participants (Actual)	Interventional	2011-02-02	Terminated
A Multi-Center, Open-Label, Ascending, Multiple Oral Dose, Safety, Tolerance and Pharmacokinetic Study of 3'-Deoxy-3'-Fluorothymidine (FLT) in Patients With Acquired Immune Deficiency Syndrome (AIDS) or AIDS-Related Complex (ARC) [NCT00002254]		0 participants	Interventional		Completed
Pilot Study of 18F-FLT-PET Imaging of the Brain in Patients With Metastatic Breast Cancer to the Brain Treated With Whole Brain Radiation Therapy With or Without Sorafenib: Comparison With MR Imaging of the Brain [NCT01621906]		17 participants (Actual)	Interventional	2012-06-13	Completed
A Phase-I Trial for Simultaneous Imaging of Tumor Hypoxia and Proliferation in Patients With Treatment- Naïve High-Grade Glioma [NCT04309552]	Phase 1	30 participants (Anticipated)	Interventional	2021-02-01	Recruiting
Cellular Proliferation Imaging Using [18F] Fluorothymidine (FLT) Positron Emission Tomography (PET) in Brain Tumors [NCT02167204]		9 participants (Actual)	Interventional	2012-11-30	Completed
Randomised, Double Blind, Placebo-controlled Dose Ranging Trial to Determine the Antiviral Activity and Safety of Alovudine in Nucleoside-experienced HIV-infected Subjects Experiencing Virologic Failure [NCT02232581]	Phase 2	72 participants (Actual)	Interventional	2004-04-30	Completed
A Phase II, Multi-center, Open-label Study Evaluating GRN1005 Alone or in Combination With Trastuzumab in Breast Cancer Patients With Brain Metastases [NCT01480583]	Phase 2	85 participants (Actual)	Interventional	2011-10-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00062374 (2) [back to overview]	Disease Free Survival (DFS)
NCT00062374 (2) [back to overview]	Histological Response Determined by FDG Uptake Correlates
NCT00572728 (9) [back to overview]	%Change SUVmax From FLT1-FLT2 to Predict Lymph Node Status at Surgery
NCT00572728 (9) [back to overview]	SUVmax at FLT-2 Comparison Between Residual Cancer Burden (RCB) 0/I and RCB II/III
NCT00572728 (9) [back to overview]	SUVmax at FLT-3 Comparison Between Residual Cancer Burden (RCB) 0/I and RCB II/III
NCT00572728 (9) [back to overview]	%Change in FLT Uptake Between the Baseline (Pre-therapy) and the Early-therapy Imaging Studies to Predict Pathological Complete Response
NCT00572728 (9) [back to overview]	Correlation Between SUVmax and Ki-67 LI at FLT1(Baseline PET)
NCT00572728 (9) [back to overview]	Correlation Between SUVmax and Ki-67 LI at FLT3 (Post-NAC)
NCT00572728 (9) [back to overview]	%Change SUVmax From FLT1-FLT3 to Predict Lymph Node Status at Surgery
NCT00572728 (9) [back to overview]	Change in Uptake Between FLT1 and FLT3 to Predict Pathologic Complete Response (pCR) of the Primary Tumor
NCT00572728 (9) [back to overview]	SUVmax at FLT-1 Comparison Between Residual Cancer Burden (RCB) 0/I and RCB II/III
NCT00963807 (5) [back to overview]	Change in 18F-Fluorodeoxyglucose (FDG) Uptake
NCT00963807 (5) [back to overview]	Change in 18F-Fluorothymidine (FLT) Uptake
NCT00963807 (5) [back to overview]	Change in FLT Uptake
NCT00963807 (5) [back to overview]	Change in FLT Uptake in Responders and Non-responders
NCT00963807 (5) [back to overview]	Overall Response Rate Reported as a Proportion of the Total Number of Patients Who Received at Least One Cycle of Therapy Assessed Using Response Evaluation Criteria in Solid Tumors (RECIST)
NCT01015131 (11) [back to overview]	Change From Baseline in 18F-FLT-PET Mean Standardized Uptake Value (SUVmean) After the First Cycle of Standard of Care (SOC) Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Change From Baseline in Ki-67 Labeling Index After the First Cycle of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Change From Baseline in Proliferation Signature Score (PSS) After the First Cycle of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Spearman's Rank Correlation Coefficient Between Change From Baseline in Ki-67 Labeling Index and Change From Baseline in SUVmax After the First Cycle of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Spearman's Rank Correlation Coefficient Between Change From Baseline in Ki-67 Labeling Index and Change From Baseline in SUVmean After the First Cycle of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Spearman's Rank Correlation Coefficient Between Change From Baseline in Ki-67 LI After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Spearman's Rank Correlation Coefficient Between Change From Baseline in PSS After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Spearman's Rank Correlation Coefficient Between Change From Baseline in SUVmax After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Spearman's Rank Correlation Coefficient Between Change From Baseline in SUVmean After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.
NCT01015131 (11) [back to overview]	Change From Baseline in 18F-FLT-PET Maximum Standardized Uptake Value (SUVmax) After the First Cycle of SOC Neo-adjuvant Chemotherapy.
NCT01338987 (4) [back to overview]	Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria in Adverse Events (CTCAE v4.0)
NCT01338987 (4) [back to overview]	Percentage of B Cells at One Year Post-transplant in Participants Who Did/Did Not Receive Leuprolide Following Bone Marrow Transplant (BMT)
NCT01338987 (4) [back to overview]	Time to Engraftment in First Transplant Recipients Only With Median Thoracic Spine Standardized Uptake Values (SUV) of 1.4 or Greater Than Those Patients With SUV's Less Than 1.4
NCT01338987 (4) [back to overview]	Number of Adverse Events Related to Study Drug Experienced by Participants After Second Bone Marrow Transplant (BMT)
NCT01621906 (2) [back to overview]	Overall Response Rate
NCT01621906 (2) [back to overview]	Change in Avg SUV Max From Baseline to 1 Year
NCT01928186 (11) [back to overview]	Baseline FLT Transport (K1) Values by FLT PET
NCT01928186 (11) [back to overview]	Baseline Ki (Flux Constant) Values by FLT PET
NCT01928186 (11) [back to overview]	Baseline Standardized Uptake Values (SUV) by FLT PET
NCT01928186 (11) [back to overview]	Percent Change in Net Influx Constant (Ki) by FLT PET
NCT01928186 (11) [back to overview]	Percent Change in SUV by FLT PET
NCT01928186 (11) [back to overview]	Percentage Change in K1 (Blood Flow Parameter) by FLT PET
NCT01928186 (11) [back to overview]	Percentage Change in Ki-67 Positive Cells Between Pre-therapy and Post-therapy Tumor Specimens
NCT01928186 (11) [back to overview]	Percentage of Ki-67 Positive Tumor Cells in Surgical (Post-therapy) Sample
NCT01928186 (11) [back to overview]	Post-therapy Ki (Flux Constant) Values by FLT PET
NCT01928186 (11) [back to overview]	Post-treatment FLT Transport (K1) Values by FLT PET
NCT01928186 (11) [back to overview]	Post-treatment Standardized Uptake Values (SUV) by FLT PET
NCT02167204 (4) [back to overview]	Percentage Change in Measure of FLT Flux
NCT02167204 (4) [back to overview]	Percentage Change in Measure of Reflecting Transport
NCT02167204 (4) [back to overview]	Percentage Change in Measure of Standard Uptake Value
NCT02167204 (4) [back to overview]	Survival

Disease Free Survival (DFS)

Overall Survival (OS) and Disease Free Survival (DFS) are the secondary endpoints. Technical problems with measurement of OS leading to unreliable or uniterpretable data. Data adjudication was invalid, and needs to be re-adjudicated. Therefore, only DFS data is being reported. (NCT00062374)
Timeframe: Every 3 mos for the first 2 yrs, then every 6 mos for 2 years and once a year afterwards, up to 5 years

Intervention	months (Median)
Arm I	23.8

Intervention	percent change in SUVmax from FLT1-FLT2 (Mean)
	All Data	0 Positive Nodes	1-3 Positive Nodes	3+ Positive Nodes
Diagnostic (18F-FLT)	44.9	47.7	43.8	42.6

Intervention	Standard Uptake Values (SUVmax) (Mean)
	All Data (FLT3)	RCB 0/I (FLT3)	RCB II/III (FLT3)
Diagnostic (18F-FLT)	1.8	0.7	2.4

Intervention	SUV (Mean)
	Baseline	End of Cycle 1	Change from Baseline
All Participants	2.79	1.78	1.00

Intervention	Labeling Index (Mean)
	Baseline (n = 36)	End of Cycle 1	Change from Baseline
All Participants	57.89	43.81	10.53

Intervention	cm^3 (Mean)
	Baseline	End of Chemotherapy	Change from Baseline
All Participants	22.74	6.14	16.59

Intervention	Participants (Count of Participants)
Males That Did Not Receive Leuprolide for 1st Transplant	10
Males Randomized to Receive Leuprolide for 1st Transplant	8
Females That Received Leuprolide for 1st Transplant	20
Matched Related Donors for Transplant	4
Recipients of 2nd Transplant	2

Intervention	percentage of cells (Median)
	Males that received leuprolide	Males that did not receive leuprolide	Females who all received leuprolide
Transplant Recipient	22.1	21.9	14.3

Intervention	Days (Median)
	Patients with SUV 1.4 or greater	Patients with SUV less than 1.4
Transplant Recipient	5	15

Intervention	participants (Number)
	Not enrolled in FLT-PET study	Decline in avg SUV max of >/= 25% of WBRT + sorafenib participants	No decline in avg SUV max of >/= 25% of WBRT + sorafenib participants	Decline in avg SUV max of >/= 25% of WBRT participants	No decline in avg SUV max of >/= 25% of WBRT participants
Cohort 1	2	9	1	0	0
Cohort 2	0	0	0	2	3

Intervention	percent change (Median)
2 Diagnostic (18F-FLT PET/CT)Scans	-4
2 or 3 Diagnostic (18F-FLT PET/CT) Scans	3

Intervention	SULmax (Mean)
Responders	-1.8
Non-Responders	1.2

Intervention	percent change (Median)
2 Diagnostic (18F-FLT PET/CT) Scans	-11
2 or 3 Diagnostic (18F-FLT PET/CT) Scans	-11

alovudine

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Studies (571)

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Research Demand Index: 19.38

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Clinical Trials (38)

Trial Overview

Trial Outcomes

Disease Free Survival (DFS)

Histological Response Determined by FDG Uptake Correlates

%Change SUVmax From FLT1-FLT2 to Predict Lymph Node Status at Surgery

SUVmax at FLT-2 Comparison Between Residual Cancer Burden (RCB) 0/I and RCB II/III

SUVmax at FLT-3 Comparison Between Residual Cancer Burden (RCB) 0/I and RCB II/III

%Change in FLT Uptake Between the Baseline (Pre-therapy) and the Early-therapy Imaging Studies to Predict Pathological Complete Response

Correlation Between SUVmax and Ki-67 LI at FLT1(Baseline PET)

Correlation Between SUVmax and Ki-67 LI at FLT3 (Post-NAC)

%Change SUVmax From FLT1-FLT3 to Predict Lymph Node Status at Surgery

Change in Uptake Between FLT1 and FLT3 to Predict Pathologic Complete Response (pCR) of the Primary Tumor

SUVmax at FLT-1 Comparison Between Residual Cancer Burden (RCB) 0/I and RCB II/III

Change in 18F-Fluorodeoxyglucose (FDG) Uptake

Change in 18F-Fluorothymidine (FLT) Uptake

Change in FLT Uptake

Change in FLT Uptake in Responders and Non-responders

Overall Response Rate Reported as a Proportion of the Total Number of Patients Who Received at Least One Cycle of Therapy Assessed Using Response Evaluation Criteria in Solid Tumors (RECIST)

Change From Baseline in 18F-FLT-PET Mean Standardized Uptake Value (SUVmean) After the First Cycle of Standard of Care (SOC) Neo-adjuvant Chemotherapy.

Change From Baseline in Ki-67 Labeling Index After the First Cycle of SOC Neo-adjuvant Chemotherapy.

Change From Baseline in Proliferation Signature Score (PSS) After the First Cycle of SOC Neo-adjuvant Chemotherapy.

Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.

Spearman's Rank Correlation Coefficient Between Change From Baseline in Ki-67 Labeling Index and Change From Baseline in SUVmax After the First Cycle of SOC Neo-adjuvant Chemotherapy.

Spearman's Rank Correlation Coefficient Between Change From Baseline in Ki-67 Labeling Index and Change From Baseline in SUVmean After the First Cycle of SOC Neo-adjuvant Chemotherapy.

Spearman's Rank Correlation Coefficient Between Change From Baseline in Ki-67 LI After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.

Spearman's Rank Correlation Coefficient Between Change From Baseline in PSS After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.

Spearman's Rank Correlation Coefficient Between Change From Baseline in SUVmax After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.

Spearman's Rank Correlation Coefficient Between Change From Baseline in SUVmean After the First Cycle of SOC Neo-adjuvant Chemotherapy, and Change From Baseline in Tumor Volume at the End of SOC Neo-adjuvant Chemotherapy.

Change From Baseline in 18F-FLT-PET Maximum Standardized Uptake Value (SUVmax) After the First Cycle of SOC Neo-adjuvant Chemotherapy.

Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria in Adverse Events (CTCAE v4.0)

Percentage of B Cells at One Year Post-transplant in Participants Who Did/Did Not Receive Leuprolide Following Bone Marrow Transplant (BMT)

Time to Engraftment in First Transplant Recipients Only With Median Thoracic Spine Standardized Uptake Values (SUV) of 1.4 or Greater Than Those Patients With SUV's Less Than 1.4

Number of Adverse Events Related to Study Drug Experienced by Participants After Second Bone Marrow Transplant (BMT)

Overall Response Rate

Change in Avg SUV Max From Baseline to 1 Year

Baseline FLT Transport (K1) Values by FLT PET

Baseline Ki (Flux Constant) Values by FLT PET

Baseline Standardized Uptake Values (SUV) by FLT PET

Percent Change in Net Influx Constant (Ki) by FLT PET

Percent Change in SUV by FLT PET

Percentage Change in K1 (Blood Flow Parameter) by FLT PET

Percentage Change in Ki-67 Positive Cells Between Pre-therapy and Post-therapy Tumor Specimens

Percentage of Ki-67 Positive Tumor Cells in Surgical (Post-therapy) Sample

Post-therapy Ki (Flux Constant) Values by FLT PET

Post-treatment FLT Transport (K1) Values by FLT PET

Post-treatment Standardized Uptake Values (SUV) by FLT PET

Percentage Change in Measure of FLT Flux

Percentage Change in Measure of Reflecting Transport

Percentage Change in Measure of Standard Uptake Value

Survival

Related Drugs (203)

Related Conditions (301)