Page last updated: 2024-12-06

lisofylline

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Lisofylline is a synthetic xanthine derivative with bronchodilator and anti-inflammatory properties. It is structurally similar to theophylline, another xanthine derivative, but with a unique chemical structure. It is studied for its potential therapeutic benefits in respiratory diseases like asthma and chronic obstructive pulmonary disease (COPD). Lisofylline acts as a phosphodiesterase (PDE) inhibitor, leading to increased levels of cyclic adenosine monophosphate (cAMP) in cells. This increased cAMP levels contribute to bronchodilation, reducing airway inflammation and improving lung function. Its specific mechanism of action involves inhibiting PDE4, which is primarily expressed in inflammatory cells. By inhibiting PDE4, lisofylline suppresses the production of pro-inflammatory mediators, such as cytokines and leukotrienes. This, in turn, helps to reduce airway inflammation and improve respiratory symptoms.'
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1-(5-hydroxyhexyl)-3,7-dimethylxanthine: the primary metabolite of pentoxifyline; CTP-499 is a partially deuterated form [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dione : A dimethylxanthine that is 3,7-dihydro-1H-purine-2,6-dione which is substituted at positions 1,3 and 7 by a 5-hydroxyhexyl group, methyl group and methyl group, respectively. [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]

lisofylline: metabolite of pentoxifylline; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

(R)-lisofylline : A 1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dione that has (R)-configuration. A synthetic small molecule which was under development for the treatment of type 1 diabetes mellitus. [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]

Cross-References

ID SourceID
PubMed CID57782
CHEMBL ID1514176
CHEBI ID143565
SCHEMBL ID680306
MeSH IDM0084266
PubMed CID501254
CHEMBL ID1411
CHEBI ID143527
SCHEMBL ID39131
MeSH IDM0084266

Synonyms (109)

Synonym
xanthine, 1-(5'-hydroxyhexyl)-3,7-dimethyl
lsf
SMP2_000274
NCGC00163298-01
3,7-dimethyl-1-(5-hydroxyhexyl)xanthine
lisofylline [usan:inn]
1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1h-purine-2,6-dione
1h-purine-2,6-dione, 3,7-dihydro-1-(5-hydroxyhexyl)-3,7-dimethyl-
1-(5'-hydroxyhexyl)-3,7-dimethylxanthine
bl 194
1h-purine-2,6-dione, 3,7-dihydro-1-(5-hydroxyhexyl)-3,7-dimethyl-, (r)-
1-(5r-hydroxyhexyl)-3,7-dimethylxanthine
1-(5-hydroxyhexyl)-3,7-dimethylpurine-2,6-dione
pentoxifylline alcohol
hydroxy pentoxifylline
(+/-)-1-(5-hydroxyhexyl)-3,7-dimethylxanthine
CHEBI:143565
lisophylline
(+/-)-lisofylline
(r)-lisophylline
l1f2q2x956 ,
unii-l1f2q2x956
dtxsid6046343 ,
dtxcid4026343
cas-6493-06-7
tox21_112043
6493-06-7
lisofylline, (+/-)-
theobromine, 1-(5-hydroxyhexyl)-
penthydroxyfylline
r99ee080js ,
penthydroxyfylline alcohol
unii-r99ee080js
FT-0670822
FT-0670823
5-hydroxypentoxyfylline
5'-hydroxypentoxyphylline
bl-194
hydroxypentoxifylline
1h-purine-2,6-dione, 3,7-dihydro-1-(5-hydroxyhexyl)-3,7-dimethyl-theobromine, 1-(5-hydroxyhexyl)-
(+/-)-lisophylline
SCHEMBL680306
NCGC00163298-02
tox21_112043_1
CHEMBL1514176
mfcd00871850
(+/-)-lisofylline, analytical standard
HY-126042
1-(5-hydroxyhexyl)-3,7-dimethylxanthine
1-(5-hydroxyhexyl)-3,7-dimethyl-1h-purine-2,6(3h,7h)-dione
FT-0670824
SB18959
AS-6130
1-[5-hydroxyhexyl]-3,7-dimethyl-3,7-dihydro-1h-purine-2,6-dione
alcool metabolite, pentoxifylline
6493-06-7 (racemic)
lisofylline (raceimic)
Q27288004
AT25342
( inverted exclamation marka)-lisofylline
AKOS037645541
1-(5-hydroxyhexyl)-3,7-dimethyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione
lisofylline (r,s)
penthydroxifillyne
also see
CS-0090310
ct1501r
1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-purine-2,6-dione
ct-1501r
r-1-(5-hydroxyhexyl)-3,7-dimethylxanthine
lisofylline
protec
protec (tn)
lisofylline (usan/inn)
D04748
100324-81-0
ct 1501r
1-[(5r)-5-hydroxyhexyl]-3,7-dimethylpurine-2,6-dione
CHEMBL1411
lisofylline, (r)-
3,7-dihydro-1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-1h-purine-2,6-dione
1-[(r)-5-hydroxyhexyl]theobromine
CHEBI:143527
(r)-lsf
1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-3,7-dihydro-1h-purine-2,6-dione
1-[(5r)-5-hydroxyhexyl]-3,7-dimethyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione
(-)-lisofylline
lisofyllinum
lisofilina
(r)-1-(5-hydroxyhexyl)-3,7-dimethylxanthine
(r)-lisofylline
NCGC00186630-01
SCHEMBL39131
lisofylline [usan]
lisofylline [inn]
lisofylline [mi]
lisofylline [who-dd]
DTXSID7058709
gtpl9225
AKOS025394050
J-000102
1-(5-r-hydroxyhexyl)-3,7-dimethylxanthine
DB12406
HY-109854A
Q15409404
CS-0034091
(r)-1-(5-hydroxyhexyl)-3,7-dimethyl-1h-purine-2,6(3h,7h)-dione
MS-23979
EX-A6722

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" CTP-499 was well tolerated with no serious or severe adverse events, or adverse events leading to discontinuation."( A First-in-Patient, Multicenter, Double-Blind, 2-Arm, Placebo-Controlled, Randomized Safety and Tolerability Study of a Novel Oral Drug Candidate, CTP-499, in Chronic Kidney Disease.
Braman, V; Cheng, C; Dao, M; Graham, P; Liu, J; Neutel, J; Sabounjian, L; Shipley, J; Wu, L, 2016
)
0.43

Pharmacokinetics

Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug. The aim of this study was to develop pharmacokinetic models for pentoxifylline (PTX) and the R(-)-enantiomer of the PTX metabolite 1,.

ExcerptReferenceRelevance
" The pharmacokinetic parameters evaluated were area under the concentration-time curve from time zero extrapolated to infinity (AUC(0-infinity)), maximum concentration (Cmax), time to maximum concentration (Tmax), elimination rate constant (k(el)), and half-life (t1/2)."( Pharmacokinetics of intranasal and intratracheal pentoxifylline in rabbits.
Adcock, KG; Deaton, JS; Hogan, SM; Kyle, PB; Olivier, JH, 2007
)
0.34
"The pharmacokinetic profiles after intranasal and intratracheal administration of pentoxifylline appear similar to those after intravenous administration."( Pharmacokinetics of intranasal and intratracheal pentoxifylline in rabbits.
Adcock, KG; Deaton, JS; Hogan, SM; Kyle, PB; Olivier, JH, 2007
)
0.34
"The aim of this study was to develop pharmacokinetic models for pentoxifylline (PTX) and the R(-)-enantiomer of the PTX metabolite 1, lisofylline (LSF), in order to identify some factors influencing the absorption of these compounds from the intestines and to clarify mechanisms involved in their non-linear pharmacokinetics."( Pharmacokinetic modelling of pentoxifylline and lisofylline after oral and intravenous administration in mice.
Obruśnik, A; Pekala, E; Szymura-Oleksiak, J; Wyska, E, 2007
)
0.34
" The application of the assay to a pilot pharmacokinetic study and tissue distribution of the compounds in rats after intraperitoneal dosing of 50 mg x kg(-1) of PTX was described."( Validation of a high-performance liquid chromatography method for pharmacokinetic evaluation of pentoxifylline and lisofylline in rat serum and tissues.
Pekala, E; Szymura-Oleksiak, J; Walczak, M,
)
0.13
" This hypothesis was supported by the outcomes of pharmacokinetic analysis."( Pharmacokinetic interaction between verapamil and methylxanthine derivatives in mice.
Wyska, E, 2010
)
0.36
" The aim of the study was to develop a physiologically based pharmacokinetic (PBPK) model of LSF in mice and to perform simulations in order to predict LSF concentrations in human serum and tissues following intravenous and oral administration."( Physiologically based modeling of lisofylline pharmacokinetics following intravenous administration in mice.
Pociecha, K; Przejczowska-Pomierny, K; Świerczek, A; Wyska, E, 2016
)
0.43
"Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug, pentoxifylline (PTX) resulting in very poor pharmacokinetic (PK) parameters, necessitating high dose and dosing frequency."( Nanoparticulate tablet dosage form of lisofylline-linoleic acid conjugate for type 1 diabetes: in situ single-pass intestinal perfusion (SPIP) studies and pharmacokinetics in rat.
Chitkara, D; Italiya, KS; Mittal, A; Singh, AK, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
"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
" Its high solubility and rapid metabolism results in poor bioavailability and short half-life, limiting its clinical utility."( Self-assembling lisofylline-fatty acid conjugate for effective treatment of diabetes mellitus.
Chitkara, D; Italiya, KS; Mahato, RI; Mazumdar, S; Mittal, A; Sharma, S, 2019
)
0.51
" A subcutaneous route of (±)-LSF administration to rats is more favourable than an oral one due to a high bioavailability and a fast absorption of both LSF enantiomers."( Influence of inflammatory disorders on pharmacokinetics of lisofylline in rats: implications for studies in humans.
Baś, S; Mlynarski, J; Pociecha, K; Świerczek, A; Wyska, E, 2019
)
0.51

Dosage Studied

Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug, pentoxifylline (PTX) It has poor pharmacokinetic (PK) parameters, necessitating high dose and dosing frequency.

ExcerptRelevanceReference
"Prospective, randomized, and blinded survival studies were performed with two lisofylline dosing regimens added to fluid resuscitation in a shock model."( Lisofylline decreases white cell adhesiveness and improves survival after experimental hemorrhagic shock.
Aswani, S; Daughters, K; Rice, G; Waxman, K, 1996
)
0.29
" Dosing was continued for 20 days or until the patient achieved 48 hrs of unassisted breathing."( Randomized, placebo-controlled trial of lisofylline for early treatment of acute lung injury and acute respiratory distress syndrome.
, 2002
)
0.31
" These data provide support for development of pentoxifylline intranasal and intratracheal dosage formulations that would be suitable for use in premature neonates."( Pharmacokinetics of intranasal and intratracheal pentoxifylline in rabbits.
Adcock, KG; Deaton, JS; Hogan, SM; Kyle, PB; Olivier, JH, 2007
)
0.34
" The application of the assay to a pilot pharmacokinetic study and tissue distribution of the compounds in rats after intraperitoneal dosing of 50 mg x kg(-1) of PTX was described."( Validation of a high-performance liquid chromatography method for pharmacokinetic evaluation of pentoxifylline and lisofylline in rat serum and tissues.
Pekala, E; Szymura-Oleksiak, J; Walczak, M,
)
0.13
" The proposed PK/PD model allowed a better understanding of the pharmacological properties of both methylxanthine derivatives and may be helpful in appropriate dosage selection for further studies."( Pharmacokinetic-pharmacodynamic modeling of methylxanthine derivatives in mice challenged with high-dose lipopolysaccharide.
Wyska, E, 2010
)
0.36
"Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug, pentoxifylline (PTX) resulting in very poor pharmacokinetic (PK) parameters, necessitating high dose and dosing frequency."( Nanoparticulate tablet dosage form of lisofylline-linoleic acid conjugate for type 1 diabetes: in situ single-pass intestinal perfusion (SPIP) studies and pharmacokinetics in rat.
Chitkara, D; Italiya, KS; Mittal, A; Singh, AK, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
anti-inflammatory agentAny compound that has anti-inflammatory effects.
immunomodulatorBiologically active substance whose activity affects or plays a role in the functioning of the immune system.
[role 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]

Drug Classes (3)

ClassDescription
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
dimethylxanthine
1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dioneA dimethylxanthine that is 3,7-dihydro-1H-purine-2,6-dione which is substituted at positions 1,3 and 7 by a 5-hydroxyhexyl group, methyl group and methyl group, respectively.
[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 Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency0.77620.002541.796015,848.9004AID1347398
progesterone receptorHomo sapiens (human)Potency33.49150.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency0.50121.000010.475628.1838AID1457
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1815370Antidiabetic activity against STZ-induced diabetic Wistar rat model assessed as decrease in fasting blood glucose level at 15 mg/kg, ip administered once daily for 5 weeks and measured after 3 weeks by glucometric analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815353Clearance in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815345AUMC (0 to t) in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID267569Secretion of insulin in INS1 cells at 20 uM2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes.
AID1815343AUC (0 to infinity) in Wistar rat at 15 mg/kg, iv by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815347AUMC (0 to infinity) in Wistar rat at 15 mg/kg, iv by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815364Binding affinity to bovine serum albumin assessed as decrease in fluorescence intensity measured after 30 mins by fluorescence quenching method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815337Initial plasma concentration in Wistar rat at 15 mg/kg, iv by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815351Volume of distribution in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID267568Protection of cytokine-induced death of pancreatic beta cells at 0.1 uM2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes.
AID1815341AUC (0 to t) in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815366Elimination rate constant in Wistar rat at 15 mg/kg,iv measured after 24 hrs by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815373Protection against STZ-induced pancreatic beta cell destruction in Wistar rat assessed as proper arrangement of islets at 15 mg/kg, ip administered once daily for 5 weeks and measured on day 35 by Hematoxylin and eosin staining based analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815349MRT in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID267571Half life in human liver2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes.
AID1815371Antidiabetic activity against STZ-induced diabetic Wistar rat model assessed as decrease in fasting blood glucose level at 15 mg/kg, ip administered once daily for 5 weeks and measured after 5 weeks by glucometric analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815339Half life in Wistar rat at 15 mg/kg, iv measured after 24 hrs by HPLC analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
AID1815332Cytotoxicity against mouse MIN6 cells assessed as cell viability at 20 uM equiv. LSF measured after 48 hrs by MTT assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Role of Chain Length and Degree of Unsaturation of Fatty Acids in the Physicochemical and Pharmacological Behavior of Drug-Fatty Acid Conjugates in Diabetes.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (112)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (7.14)18.7374
1990's38 (33.93)18.2507
2000's34 (30.36)29.6817
2010's23 (20.54)24.3611
2020's9 (8.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.31

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 Index25.31 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (9.09%)5.53%
Trials6 (5.71%)5.53%
Reviews0 (0.00%)6.00%
Reviews5 (4.76%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other10 (90.91%)84.16%
Other94 (89.52%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Safety, Tolerability and Bioavailability Study of Lisofylline After Continuous Subcutaneous (12 mg/kg) and Intravenous (12 mg/kg) Administration in Healthy Subjects and in Subjects With Type 1 Diabetes Mellitus [NCT00896077]Phase 1/Phase 28 participants (Actual)Interventional2009-05-31Completed
Strategies to Improve Long Term Islet Graft Survival [NCT00464555]Phase 25 participants (Actual)Interventional2006-12-31Completed
A Safety, Tolerability and Bioavailability Study of Lisofylline After Continuous Subcutaneous (12 mg/kg) and Intravenous (9 mg/kg) Administration in Subjects With Type 1 Diabetes Mellitus [NCT01603121]Phase 1/Phase 21 participants (Actual)Interventional2012-02-29Terminated(stopped due to Unable to enroll sufficient number of subjects)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]