disufenton sodium: a nitrone benzene bissulfonate in development for stroke; has neuroprotective activity; structure in first source
ID Source | ID |
---|---|
PubMed CID | 6440181 |
CHEMBL ID | 1627056 |
SCHEMBL ID | 678345 |
MeSH ID | M0496532 |
Synonym |
---|
cerovive |
cpi-22 |
arl-16556 |
disufenton sodium |
cxy-059 |
okn-007 |
168021-79-2 |
D03875 , |
disufenton sodium (usan/inn) |
disufenton sodium [inn] |
nxy 059 |
disodium 4-(((1,1-dimethylethyl)imino)methyl)benzene-1,3-disulfonate n-oxide |
hpn-07 |
nxy059 |
sodium 4-(2-tert-butyl-1,2-oxaziridin-3-yl)benzene-1,3-disulfonate |
A25442 |
CHEMBL1627056 |
7m1j3hn9vo , |
disufenton sodium salt |
AKOS015890930 |
S6002 |
SCHEMBL678345 |
disufenton sodium [usan] |
disufenton sodium salt [mi] |
disufenton sodium [mart.] |
disodium 4-((tert-butylimino)methyl)benzene-1,3-disulphonate n-oxide |
1,3-benzenedisulfonic acid, 4-(((1,1-dimethylethyl)oxidoimino)methyl), disodium salt |
disufenton sodium [who-dd] |
disodium 4-(((1,1-dimethylethyl)imino)methyl)benzene-1,3-disulphonate n-oxide |
disodium 4-((tert-butylimino)methyl)benzene-1,3-disulfonate n-oxide |
disodium,4-[(z)-[tert-butyl(oxido)azaniumylidene]methyl]benzene-1,3-disulfonate |
4-[[(1,1-dimethylethyl)oxoimino]methyl]-1,3-benzenedisulfonic acid disodium salt |
sodium 4-((tert-butyloxidoimino)methyl)benzene-1,3-disulfonate |
AC-33143 |
mfcd09833648 |
cerovive (nxy-059) |
J-010424 |
hpn-07, >=98% (hplc) |
SW219403-1 |
Q5283598 |
nxy-059 (disufenton sodium) |
HMS3678O19 |
AS-16949 |
disodium;4-[(z)-[tert-butyl(oxido)azaniumylidene]methyl]benzene-1,3-disulfonate |
HMS3886D09 |
CCG-268419 |
1,3-benzenedisulfonic acid, 4-[[(1,1-dimethylethyl)oxidoimino]methyl]-, sodium salt (1:2) |
l-glutamicacidgamma-(beta-naphthylamide) |
bdbm50531970 |
Excerpt | Reference | Relevance |
---|---|---|
" The objectives of this study were to develop a population pharmacokinetic model for NXY-059 in acute stroke patients and to estimate individualised dosing strategies for NXY-059 using preclinical pharmacological and clinical pharmacokinetic information and knowledge of characteristics of the patient population." | ( Population pharmacokinetic modelling and estimation of dosing strategy for NXY-059, a nitrone being developed for stroke. Cheng, YF; Edenius, C; Jönsson, S; Karlsson, MO; Lees, KR; Odergren, T, 2005) | 0.33 |
" Population pharmacokinetic models were derived using NONMEM software." | ( Population pharmacokinetic modelling and estimation of dosing strategy for NXY-059, a nitrone being developed for stroke. Cheng, YF; Edenius, C; Jönsson, S; Karlsson, MO; Lees, KR; Odergren, T, 2005) | 0.33 |
"The results illustrate how an individualised dosing strategy, given a pharmacokinetic target, for NXY-059 was successfully optimised through estimation using the increasing pharmacokinetic and pharmacodynamic knowledge during a clinical drug development programme." | ( Population pharmacokinetic modelling and estimation of dosing strategy for NXY-059, a nitrone being developed for stroke. Cheng, YF; Edenius, C; Jönsson, S; Karlsson, MO; Lees, KR; Odergren, T, 2005) | 0.33 |
" The pharmacokinetic results indicate proportional exposure of 8-h and 24-h infusions of NXY-059 resulting in mean unbound steady state plasma concentrations up to 417 micromol/L and 379 micromol/L, respectively." | ( A phase 1, placebo-controlled, randomised, double-blind (within dose panels) study evaluating the safety, tolerability and pharmacokinetics of intravenous NXY-059 in Japanese subjects. Cheng, YF; Itoh, Y; Kumagai, Y; Nilsson, D; Watabe, M, 2007) | 0.34 |
"The primary objectives of this study were to determine the pharmacokinetic (PK) properties of an 8-hour IV infusion of NXY-059 in healthy Chinese volunteers and to compare those data with those previously reported in the white population, therefore exploring any differences in PK properties between the 2 ethnic groups." | ( Pharmacokinetics of 8-hour intravenous infusion of NXY-059: a phase I, randomized, double-blind (within dose panels), placebo-controlled study in healthy Chinese volunteers. Asenblad, N; Cheng, YF; Guo, W; Hu, P; Jiang, J; Nilsson, D; Reinholdsson, I, 2008) | 0.35 |
Excerpt | Relevance | Reference |
---|---|---|
"This was a randomized, double-blind, placebo-controlled, parallel group, multicenter study that evaluated the safety and tolerability of 2 NXY-059 dosing regimens compared with placebo within 24 hours of acute stroke." | ( Tolerability and pharmacokinetics of the nitrone NXY-059 in patients with acute stroke. Barer, D; Cheng, YF; Ford, GA; Kostulas, V; Lees, KR; Odergren, T; Sharma, AK, 2001) | 0.31 |
"This was a randomized, double-blind, placebo-controlled, parallel-group, dose-escalation, multicenter study that evaluated safety, tolerability, and plasma concentrations of 2 NXY-059 dosing regimens within 24 hours of acute stroke." | ( Tolerability of NXY-059 at higher target concentrations in patients with acute stroke. Barer, D; Ford, GA; Hacke, W; Kostulas, V; Lees, KR; Odergren, T; Sharma, AK, 2003) | 0.32 |
" However, there is little information available concerning the dose-response profiles or therapeutic window for NXY-059 in a validated embolic stroke model, nor is there information available pertaining to the effects of combining NXY-059 with tenecteplase." | ( Coadministration of NXY-059 and tenecteplase six hours following embolic strokes in rabbits improves clinical rating scores. Lapchak, PA; Song, D; Wei, J; Zivin, JA, 2004) | 0.32 |
" Data from the permanent MCAO model and an embolic stroke model suggested a bell shaped dose-response curve." | ( Free radical trapping as a therapeutic approach to neuroprotection in stroke: experimental and clinical studies with NXY-059 and free radical scavengers. Ashwood, T; Green, AR, 2005) | 0.33 |
" The objectives of this study were to develop a population pharmacokinetic model for NXY-059 in acute stroke patients and to estimate individualised dosing strategies for NXY-059 using preclinical pharmacological and clinical pharmacokinetic information and knowledge of characteristics of the patient population." | ( Population pharmacokinetic modelling and estimation of dosing strategy for NXY-059, a nitrone being developed for stroke. Cheng, YF; Edenius, C; Jönsson, S; Karlsson, MO; Lees, KR; Odergren, T, 2005) | 0.33 |
" Optimal dosing strategies, individualised based on CL(CR) or bodyweight, were estimated using the population pharmacokinetic models, empirical covariate distributions relevant for the target population, and a target definition." | ( Population pharmacokinetic modelling and estimation of dosing strategy for NXY-059, a nitrone being developed for stroke. Cheng, YF; Edenius, C; Jönsson, S; Karlsson, MO; Lees, KR; Odergren, T, 2005) | 0.33 |
" The preferred dosing strategy for NXY-059 comprised an initial loading infusion (the same for all patients) followed by an individualised maintenance infusion on the basis of CL(CR) (three dosing categories) with cut-off values (at which infusion rates are incremented or decremented) of 50 and 80 mL/min." | ( Population pharmacokinetic modelling and estimation of dosing strategy for NXY-059, a nitrone being developed for stroke. Cheng, YF; Edenius, C; Jönsson, S; Karlsson, MO; Lees, KR; Odergren, T, 2005) | 0.33 |
"The results illustrate how an individualised dosing strategy, given a pharmacokinetic target, for NXY-059 was successfully optimised through estimation using the increasing pharmacokinetic and pharmacodynamic knowledge during a clinical drug development programme." | ( Population pharmacokinetic modelling and estimation of dosing strategy for NXY-059, a nitrone being developed for stroke. Cheng, YF; Edenius, C; Jönsson, S; Karlsson, MO; Lees, KR; Odergren, T, 2005) | 0.33 |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Lipoxygenase | Glycine max (soybean) | IC50 (µMol) | 57.5000 | 0.5000 | 4.8650 | 9.2300 | AID1624746 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1624774 | Neuroprotective activity in C57BL/6 mouse model of ischemia-induced cerebral ischemia model assessed as reduction in apoptosis in hippocampal CA1 region at 40 mg/kg, ip administered at onset of reperfusion period and measured at 5 days reperfusion post is | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1624741 | Antioxidant activity assessed as DPPH free radical scavenging activity at 0.1 mM measured after 20 to 60 mins | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1623862 | Antioxidant activity assessed as hydroxyl radical scavenging activity by measuring inhibition of damage to 2-deoxy-D-ribose after 3 mins by TBA-based Fenton reaction assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Antioxidant-Inspired Drug Discovery: Antitumor Metabolite Is Formed in Situ from a Hydroxycinnamic Acid Derivative upon Free-Radical Scavenging. |
AID1624748 | Antioxidant activity assessed as superoxide anion scavenging activity at 0.1 mM pH 7.4 after 10 mins by NBT assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1624743 | Antioxidant activity assessed as inhibition of linoleic acid peroxidation activity at 10 uL | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1624737 | Neuroprotective activity against oxygen-glucose deprivation-induced cell death in Sprague-Dawley rat primary neuronal cells assessed as cell viability at 250 uM treated at onset of recovery period and measured at 24 hrs of recovery by MTT assay relative t | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1239291 | Neuroprotection in Wistar rat model of ischemia assessed as reduction ischemia-induced neuronal apoptosis in cortical regions at 40 mg/kg, ip dosed at onset of reperfusion period and measured on 5 days of reperfusion by TUNEL assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID1239281 | Neuroprotection in Wistar rat model of ischemia assessed as reduction in neurological deficit score at 40 mg/kg measured after 5 days of reperfusion | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID1624772 | Neuroprotective activity in C57BL/6 mouse model of ischemia-induced cerebral ischemia model assessed reduction in neuronal cell death in hippocampal CA1 region at 40 mg/kg, ip administered at onset of reperfusion period and measured at 5 days reperfusion | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID247808 | In vitro inhibitory concentration against NO (nitrous oxide); (na: not active) | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Nitrone derivatives of trolox as neuroprotective agents. |
AID248625 | In vitro inhibitory concentration against peroxynitrite (ONOO-): using pyrogallol red bleaching assay; (na: not active) | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Nitrone derivatives of trolox as neuroprotective agents. |
AID1624755 | Neuroprotective activity in C57BL/6 mouse model of ischemia-induced cerebral ischemia model assessed reduction in neurodeficit score at 40 mg/kg, ip administered at onset of reperfusion period and measured at 5 days reperfusion post ischemia | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1239272 | Protection against oxygen-glucose deprivation-induced cytotoxicity in Sprague-Dawley rat cerebral cortex primary neuronal cell cultures assessed as increase in cell viability at 250 uM added after 48 hrs post recovery period and measured during recovery f | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID248216 | In vitro inhibitory concentration against Total peroxyl radical-trapping antioxidant parameter(TRAP) | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Nitrone derivatives of trolox as neuroprotective agents. |
AID1239284 | Neuroprotection in Wistar rat model of ischemia assessed as reduction ischemia-induced neuronal death in cortical regions at 40 mg/kg, ip dosed at onset of reperfusion period and measured on 5 days of reperfusion by fluoro jade B staining based fluorescen | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID1239271 | Protection against oxygen-glucose deprivation-induced cytotoxicity in Sprague-Dawley rat cerebral cortex primary neuronal cell cultures assessed as increase in cell viability at 250 uM added at onset of recovery period and measured during recovery for 5 d | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID247569 | In vitro inhibitory concentration against hydroxyl radical (-OH) | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Nitrone derivatives of trolox as neuroprotective agents. |
AID1624746 | Inhibition of soybean lipoxygenase using sodium linoleate as substrate by UV-based analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1239290 | Neuroprotection in Wistar rat model of ischemia assessed as reduction ischemia-induced neuronal apoptosis in hippocampal CA1 regions at 40 mg/kg, ip dosed at onset of reperfusion period and measured on 5 days of reperfusion by TUNEL assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID1624773 | Neuroprotective activity in C57BL/6 mouse model of ischemia-induced cerebral ischemia model assessed reduction in neuronal cell death in cortical region at 40 mg/kg, ip administered at onset of reperfusion period and measured at 5 days reperfusion post is | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1624744 | Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalents at 10 uL after 1 min | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1624763 | Neuroprotective activity in C57BL/6 mouse model of transient middle cerebral artery occlusion-induced ttransient focal cerebral ischemia assessed decrease in motor deficit by measuring improvement in grip strength at 40 mg/kg, ip measured after 48 hrs pos | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1239270 | Protection against oxygen-glucose deprivation-induced cytotoxicity in Sprague-Dawley rat cerebral cortex primary neuronal cell cultures assessed as increase in cell viability at 250 uM added at onset of recovery period by MTT assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID247576 | In vitro inhibitory concentration against lipid peroxidation (LPO) | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Nitrone derivatives of trolox as neuroprotective agents. |
AID1624742 | Antioxidant activity assessed as hydroxyl radical scavenging activity at 0.1 mM measured after 30 mins | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1239282 | Neuroprotection in Wistar rat model of ischemia assessed as reduction ischemia-induced neuronal death in hippocampal CA1 regions at 40 mg/kg, ip dosed at onset of reperfusion period and measured on 5 days of reperfusion by fluoro jade B staining based flu | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | CholesteroNitrones for Stroke. |
AID1624765 | Neuroprotective activity in C57BL/6 mouse model of transient middle cerebral artery occlusion-induced ttransient focal cerebral ischemia assessed decrease in size of ischemic lesion at 40 mg/kg, ip measured after 48 hrs post dose relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1624775 | Neuroprotective activity in C57BL/6 mouse model of ischemia-induced cerebral ischemia model assessed as reduction in apoptosis in cortical region at 40 mg/kg, ip administered at onset of reperfusion period and measured at 5 days reperfusion post ischemia | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1624747 | Antiinflammatory activity assessed as NO release at 100 uM after 60 mins in presence of L-cysteine by Griess reagent-based relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (0.88) | 18.2507 |
2000's | 98 (85.96) | 29.6817 |
2010's | 14 (12.28) | 24.3611 |
2020's | 1 (0.88) | 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 | 19 (16.67%) | 5.53% |
Reviews | 31 (27.19%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 64 (56.14%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Randomized, Placebo-controlled, Double-blind, Dose Escalation Study to Determine the Safety, Tolerability, and Pharmacokinetic Profile of HPN-07 and HPN-07 Plus NAC in Single Doses in Male and Female Subjects [NCT02259595] | Phase 1 | 32 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
CHANT (Cerebral Hemorrhage And NXY Treatment) A Double-Blind, Randomized, Placebo-Controlled, Parallel Group, Multicenter, Phase IIb Study to Assess the Safety and Tolerability of Intravenous Infusion of NXY-059 in Adult Patients With Acute Intracerebral [NCT00075959] | Phase 2 | 600 participants | Interventional | 2004-08-31 | Completed | ||
SAINT I (Stroke - Acute Ischemic - NXY Treatment) A Double Blind, Randomized, Placebo Controlled, Parallel Group, Multicenter, Phase IIb/III Study to Assess the Efficacy and Safety of Intravenous NXY-059 in Acute Ischemic Stroke. [NCT00119626] | Phase 3 | 1,700 participants | Interventional | 2003-06-30 | Completed | ||
SAINT (Stroke - Acute Ischemic - NXY Treatment) A Double Blind, Randomized, Placebo Controlled, Parallel Group, Multicenter, Phase IIb/III Study to Assess the Efficacy and Safety of Intravenous NXY-059 in Acute Ischemic Stroke [NCT00061022] | Phase 3 | 3,200 participants | Interventional | 2003-05-31 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |