stiripentol: structure
ID Source | ID |
---|---|
PubMed CID | 5311454 |
CHEMBL ID | 1983350 |
CHEBI ID | 94435 |
SCHEMBL ID | 216436 |
SCHEMBL ID | 2533815 |
MeSH ID | M0075555 |
Synonym |
---|
me-2080 |
bcx-2600 |
diacomit |
stiripentol [usan:inn] |
1-penten-3-ol, 4,4-dimethyl-1-(3,4-methylenedioxyphenyl)- |
1-(1,3-benzodioxol-5-yl)-4,4-dimethyl-1-penten-3-ol |
stiripentolum [inn-latin] |
brn 1313047 |
einecs 256-480-9 |
estiripentol [inn-spanish] |
bcx 2600 |
4,4-dimethyl-1-((3,4-methylenedioxy)phenyl)-1-penten-3-ol |
diacomit (tn) |
D05928 |
stiripentol (jan/usan/inn) |
MLS001424144 |
stiripentol |
MLS000758313 |
smr000449279 |
cpd000449279 |
49763-96-4 |
HMS2052K07 |
NCGC00185769-01 |
cas-49763-96-4 |
dtxsid6049068 , |
tox21_113622 |
dtxcid1028994 |
HMS2232P06 |
CHEMBL1983350 |
CCG-101092 |
estiripentol |
stiripentolum |
5-19-02-00640 (beilstein handbook reference) |
S5266 |
(1e)-1-(2h-1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ol |
gtpl5469 |
131206-47-8 |
stiripentol [orange book] |
SCHEMBL216436 |
NC00342 |
(e)-1-(benzo[d][1,3]dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol |
SCHEMBL2533815 |
AKOS025149123 |
mfcd00869310 |
DB09118 |
AKOS027255159 |
CHEBI:94435 |
137767-55-6 |
bdbm50504273 |
stiripentol, >=98% (hplc) |
CS-7801 |
HY-103392 |
Q412182 |
1-(benzo[d][1,3]dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol |
BS-16863 |
bcx2600; bcx-2600; bcx 2600 |
BCP10434 |
HMS3886M17 |
CCG-266819 |
NCGC00185769-02 |
bcx2600 |
W10731 |
DTXSID80860609 |
(1e)-1-(1,3-benzodioxol-5-yl)-4,4-dimethyl-1-penten-3-ol |
(1e)-1-(1,3-dioxaindan-5-yl)-4,4-dimethylpent-1-en-3-ol |
EN300-7393003 |
n03ax17 |
stiripentolum (inn-latin) |
estiripentol (inn-spanish) |
(1e,3rs)-1-(benzo(d)(1,3)dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol |
stiripentol (mart.) |
Stiripentol is safe and effective during long-term use in patients with DS in routine clinical practice. In infants with Dravet syndrome, stiripents significantly reduce long-lasting seizures including status epilepticus.
Stiripentol showed a significant degree of tolerance to the anticonvulsant and neurotoxic effects following subacute treatment with the racemic compound. Study undertook to define the overall pharmacokinetic profile of stiripentl in rhesus monkey prior to its efficacy evaluation.
Cannabidiol was investigated in an experimental model of stroke. Study looked at impact of cannabidio on steady-state pharmacokinetics of clobazam, stiripentol, and valproate.
Excerpt | Reference | Relevance |
---|---|---|
"The anticonvulsant and acute adverse (neurotoxic) effects of STP in combination with the various conventional antiepileptic drugs (AEDs), at fixed ratios of 1:3, 1:1, and 3:1, were evaluated in the PTZ and chimney tests in mice using the isobolographic analysis." | ( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis. Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006) | 0.33 |
"Phase I, open-label, randomized, single-dose, 3-period crossover study assessing pharmacokinetics (PK) and safety of ZX008, a liquid oral formulation of fenfluramine (FFA) under development for adjunctive treatment of Dravet syndrome and Lennox-Gastaut syndrome, administered with and without a combined antiepileptic drug (AED) regimen of stiripentol (STP), valproate (VPA), and clobazam (CLB) (STP regimen)." | ( A phase I, randomized, open-label, single-dose, 3-period crossover study to evaluate the drug-drug interaction between ZX008 (fenfluramine HCl oral solution) and a regimen of stiripentol, clobazam, and valproate in healthy subjects
. Boyd, B; Farfel, GM; Galer, BS; Gammaitoni, A; Smith, S, 2019) | 0.51 |
" This open-label, fixed-sequence, drug-drug interaction, healthy volunteer trial investigated the impact of cannabidiol on steady-state pharmacokinetics of clobazam (and N-desmethylclobazam), stiripentol, and valproate; the reciprocal effect of clobazam, stiripentol, and valproate on cannabidiol and its major metabolites (7-hydroxy-cannabidiol [7-OH-CBD] and 7-carboxy-cannabidiol [7-COOH-CBD]); and cannabidiol safety and tolerability when coadministered with each antiepileptic drug." | ( A Phase 1, Open-Label, Pharmacokinetic Trial to Investigate Possible Drug-Drug Interactions Between Clobazam, Stiripentol, or Valproate and Cannabidiol in Healthy Subjects. Blakey, G; Crockett, J; Morrison, G; Sommerville, K, 2019) | 0.51 |
" It is important to consider the possibility of drug-drug interactions (DDIs)." | ( Clinical implications of trials investigating drug-drug interactions between cannabidiol and enzyme inducers or inhibitors or common antiseizure drugs. Critchley, D; Gidal, B; Morrison, G; Patsalos, PN; Szaflarski, JP; VanLandingham, K, 2020) | 0.56 |
" Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model." | ( Study of the metabolic stability profiles of perampanel, rufinamide and stiripentol and prediction of drug interactions using HepaRG cells as an in vitro human model. Alves, G; Falcão, A; Fortuna, A; Meirinho, S; Rodrigues, M, 2022) | 0.72 |
" In the current study, we have investigated the neuroprotective effect of stiripentol (STP) and trans integrated stress response inhibitor (ISRIB) alone and in combination with rat bone marrow derived mesenchymal stem cells (BM-MSCs) secretome in an experimental model of stroke." | ( Rat BM-MSCs secretome alone and in combination with stiripentol and ISRIB, ameliorated microglial activation and apoptosis in experimental stroke. Attri, SV; Bhattacharyya, S; Das Radotra, B; Dhir, N; Jain, A; Mahendru, D; Malik, D; Medhi, B; Patial, A; Prakash, A; Sharma, AR; Sharma, S, 2023) | 0.91 |
"STP and trans ISRIB, alone and in combination with rat BM-MSCs secretome, significantly improved neurological, motor function and memory deficits along with significant reduction in pyknotic neurons in the brain of post MCAO rats." | ( Rat BM-MSCs secretome alone and in combination with stiripentol and ISRIB, ameliorated microglial activation and apoptosis in experimental stroke. Attri, SV; Bhattacharyya, S; Das Radotra, B; Dhir, N; Jain, A; Mahendru, D; Malik, D; Medhi, B; Patial, A; Prakash, A; Sharma, AR; Sharma, S, 2023) | 0.91 |
"STP and trans ISRIB, alone and in combination with rat BM-MSCs secretome, might be considered as potential neuroprotective agents in the acute ischemic stroke (AIS) management." | ( Rat BM-MSCs secretome alone and in combination with stiripentol and ISRIB, ameliorated microglial activation and apoptosis in experimental stroke. Attri, SV; Bhattacharyya, S; Das Radotra, B; Dhir, N; Jain, A; Mahendru, D; Malik, D; Medhi, B; Patial, A; Prakash, A; Sharma, AR; Sharma, S, 2023) | 0.91 |
Stiripentol was very highly bound to plasma proteins in plasma from dosed subjects as well as spiked human plasma (free fraction of 1 per cent) This suggests in vivo activation to a metabolic intermediate forming a complex with cerebral cytochrome P-450.
Excerpt | Relevance | Reference |
---|---|---|
"The inhibitory effect of stiripentol (STP) on disposition of carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZE) was quantitated to establish CBZ dosage reduction guidelines for future clinical add-on efficacy trials of STP." | ( Carbamazepine dose requirements during stiripentol therapy: influence of cytochrome P-450 inhibition by stiripentol. Eddy, AC; Kerr, BM; Levy, RH; Martinez-Lage, JM; Tor, J; Viteri, C, ) | 0.13 |
" Blood and urine samples in the studies were collected during a dosing interval at steady state." | ( Effects of polytherapy with phenytoin, carbamazepine, and stiripentol on formation of 4-ene-valproate, a hepatotoxic metabolite of valproic acid. Acheampong, A; Anderson, GD; Baillie, TA; Friel, PN; Guyot, M; Levy, RH; Loiseau, P; Rettenmeier, AW; Tor, J; Wilensky, AJ, 1990) | 0.28 |
" Dose-response studies were performed after acute intraperitoneal injection and subacute oral drug treatment." | ( Efficacy of stiripentol in the intravenous pentylenetetrazol infusion seizure model in the rat. Levy, RH; Moor, MJ; Savitch, JL; Shen, DD, ) | 0.13 |
" From a quantitative standpoint, the most important pathway of biotransformation of I following both acute and chronic dosing involved opening of the methylenedioxy ring to generate catechol derivatives." | ( The metabolic fate of stiripentol in man. Astoin, J; Baillie, TA; Lepage, F; Levy, RH; Moreland, TA; Tombret, F, ) | 0.13 |
" This suggests in vivo activation to a metabolic intermediate forming a complex with cerebral cytochrome P-450, which 2 hr after dosing is fully insensitive to stiripentol added to incubates." | ( Ex vivo inhibition of rat brain cytochrome P-450 activity by stiripentol. Jenner, P; Mesnil, M; Testa, B, 1988) | 0.27 |
" Stiripentol was very highly bound to plasma proteins in plasma from dosed subjects as well as spiked human plasma (free fraction of 1 per cent)." | ( Pharmacokinetics of stiripentol in normal man: evidence of nonlinearity. Blehaut, HM; Levy, RH; Lin, HS; Tor, JA, ) | 0.13 |
" Stiripentol was administered orally three times a day in dosage increments of 600, 1,200, and 1,800 mg/day for consecutive periods of 3, 4, and 7 days, respectively." | ( Michaelis-Menten kinetics of stiripentol in normal humans. Blehaut, HM; Guyot, M; Levy, RH; Loiseau, P; Moreland, TA; Tor, J, 1984) | 0.27 |
" The frequency of congenital defects in PHT-treated animals was dosage dependent, ranging from 7 to 55%." | ( Protection from phenytoin-induced congenital malformations by coadministration of the antiepileptic drug stiripentol in a mouse model. Finnell, RH; Kerr, BM; Levy, RH; Steward, RL; van Waes, M, ) | 0.13 |
"05), compared with mice dosed with CBZ alone (1,000 mg/kg/day)." | ( Effect of treatment with phenobarbital and stiripentol on carbamazepine-induced teratogenicity and reactive metabolite formation. Amore, BM; Bajpai, M; Bennett, GD; Finnell, RH; Levy, RH; Slattery, JT, 1995) | 0.29 |
"l-1 and the dosage of CBZ should simultaneously be decreased in steps by more than 50% to minimize the change in CBZ plasma concentration." | ( Effect of stiripentol on carbamazepine plasma concentration and metabolism in epileptic children. Chiron, C; d'Athis, P; Dulac, O; Olive, G; Pous, G; Renard, F; Rey, E; Tran, A; Vauzelle-Kervroedan, F, 1996) | 0.29 |
" This study sought to determine the lowest dosage of stiripentol (STP) protective against phenytoin-induced teratogenesis in a mouse model, and to determine mechanistically if inhibition of oxidative metabolism by STP in vitro decreased production of reactive phenytoin (PHT) metabolites." | ( Effect of stiripentol dose on phenytoin-induced teratogenesis in a mouse model. Bajpai, M; Bennett, GD; Finnell, RH; Levy, RH; Mather, GG; Wlodarczyk, B, ) | 0.13 |
" They could be so severe in patients over 12 years of age that the stiripentol dosage could not be increased to 50 mg kg-1 j-1." | ( [Long-term efficacy and tolerance of stiripentaol in severe myoclonic epilepsy of infancy (Dravet's syndrome)]. Chiron, C; Dellatolas, G; Dulac, O; Pons, G; Rey, E; Thanh, TN; Vincent, J, 2002) | 0.31 |
"The aim of this study was to characterize the anticonvulsant effects of stiripentol (STP) in combination with clobazam [CLB], and valproate [VPA]) in the mouse maximal electroshock (MES)-induced seizure model using the type I isobolographic analysis for parallel and non-parallel dose-response relationship curves (DRRCs)." | ( Interactions of stiripentol with clobazam and valproate in the mouse maximal electroshock-induced seizure model. Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N; Trojnar, MK, 2010) | 0.36 |
" They were also offered an increased dosage of stiripentol if treatment with carnitine improved the encephalopathy." | ( Starting stiripentol in adults with Dravet syndrome? Watch for ammonia and carnitine. Andrade, DM; Marques, P; Sadoway, T; Selvarajah, A; Tabarestani, S; Zulfiqar Ali, Q, 2020) | 0.56 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 22.4301 | 0.0072 | 15.7588 | 89.3584 | AID1224835; AID624030 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 35.4813 | 0.0184 | 6.8060 | 14.1254 | AID624172 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 22.6874 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
AR protein | Homo sapiens (human) | Potency | 32.2543 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 29.1142 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 23.7101 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 6.9178 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 29.8493 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 25.6770 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1259401 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 29.8493 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
G | Vesicular stomatitis virus | Potency | 3.0901 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 10.9640 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 12.6082 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
Interferon beta | Homo sapiens (human) | Potency | 3.0901 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.0901 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.0901 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.0901 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[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) |
---|---|---|---|---|---|---|---|
Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | EC50 (µMol) | 46.0000 | 0.0011 | 2.0009 | 10.0000 | AID1517295 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | EC50 (µMol) | 46.0000 | 0.0014 | 1.9578 | 10.0000 | AID1517295 |
Gamma-aminobutyric acid receptor subunit beta-2 | Homo sapiens (human) | EC50 (µMol) | 46.0000 | 0.0014 | 1.7768 | 10.0000 | AID1517295 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID696708 | Neurotoxicity in Swiss albino mouse assessed as effect on hindlimb grip strength at 747 umol/kg, sc administered measured every 15 mins for 2 hrs | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID696703 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as maximal electroshock-induced seizures administered 30 mins before electroshock challenge | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID696696 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 640 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID696698 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 747 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1517295 | Agonist activity at GABA alpha1beta2gamma2 receptor in human HEK293T at -50 mV holding potential by whole cell voltage clamp assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1868303 | Cytotoxicity against hyperoxaluric-primary hepatocyte isolated from Hoga1-knockdown PH3 C57BL/6 mouse assessed as cell death at 10 uM by MTS assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production. |
AID696709 | Neurotoxicity in Swiss albino mouse assessed as climbing response to inverted mesh at at 747 umol/kg, sc administered measured every 15 mins for 2 hrs by wire mesh grasping test | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1517332 | Inhibition of human LDH5 at 2 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID696692 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 427 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1323834 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
AID1517254 | Anticonvulsant activity in Kunming mouse assessed as MES-induced hind limb extension at 100 mg/kg, ip administered 0. 5 to 2 hrs before MES stimulation | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1868301 | Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Hoga1-knockdown PH3 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 24 hrs in the presence of hydroxyproline relative to control | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production. |
AID696691 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 384 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1868305 | Cytotoxicity against hyperoxaluric-primary hepatocyte isolated from Agxt1-knockdown PH1 C57BL/6 mouse assessed as cell death at 10 uM by MTS assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production. |
AID1517288 | Inhibition of human LDH1 at 2 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID696702 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1517286 | Inhibition of human LDH1 at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1868302 | Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Hoga1-knockdown PH3 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 48 hrs in the presence of hydroxyproline relative to control | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production. |
AID1517287 | Inhibition of human LDH5 at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1868300 | Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Grhpr-knockdown PH2 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 48 hrs in the presence of glycolate relative to control | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production. |
AID1323835 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
AID696693 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 491 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID696694 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 534 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1868304 | Cytotoxicity against hyperoxaluric-primary hepatocyte isolated from Grhpr-knockdown PH2 C57BL/6 mouse assessed as cell death at 10 uM by MTS assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production. |
AID696695 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures at 576 umol/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1517296 | Agonist activity at GABA alpha1beta2gamma2 receptor in human HEK293T at 3.3 to 300 uM at -50 mV holding potential by whole cell voltage clamp assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1868299 | Inhibition of GO/LDHA in hyperoxaluric-primary hepatocyte isolated from Grhpr-knockdown PH2 C57BL/6 mouse assessed as relative oxalate output at 10 uM measured at 24 hrs in the presence of glycolate relative to control | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | New salicylic acid derivatives, double inhibitors of glycolate oxidase and lactate dehydrogenase, as effective agents decreasing oxalate production. |
AID696697 | Anticonvulsant activity in Swiss albino mouse assessed as maximal electroshock-induced seizures at 640 umol/kg, ip administered 30 mins before electroshock challenge | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Design and synthesis of novel stiripentol analogues as potential anticonvulsants. |
AID1517256 | Neurotoxicity against Kunming mouse assessed as time remained in rod at 100 mg/kg, ip administered 0.5 to 2 hrs by rotarod test | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
[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 (6.43) | 18.7374 |
1990's | 17 (9.94) | 18.2507 |
2000's | 22 (12.87) | 29.6817 |
2010's | 78 (45.61) | 24.3611 |
2020's | 43 (25.15) | 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 | 18 (9.63%) | 5.53% |
Reviews | 45 (24.06%) | 6.00% |
Case Studies | 10 (5.35%) | 4.05% |
Observational | 3 (1.60%) | 0.25% |
Other | 111 (59.36%) | 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 | ||
---|---|---|---|---|---|---|---|
Pharmacokinetic Study of Stiripentol and Its Metabolites After Multiple Dose Oral Administration in Healthy Male Volunteers [NCT03866928] | Phase 1 | 14 participants (Actual) | Interventional | 2019-02-12 | Completed | ||
Expanded Access Use of Stiripentol in Participants With Dravet Syndrome or Epileptic Encephalopathies Associated With Sodium Channel Mutations [NCT02239276] | 0 participants | Expanded Access | No longer available | ||||
Evaluation of the Efficacy of Stiripentol (Diacomit) as Monotherapy for the Treatment of Primary Hyperoxaluria [NCT03819647] | Phase 2 | 15 participants (Actual) | Interventional | 2019-05-21 | Completed | ||
A Randomised Controlled Trial of the Ketogenic Diet in the Treatment of Epilepsy in Children Under the Age of Two Years [NCT02205931] | Phase 4 | 160 participants (Anticipated) | Interventional | 2015-01-31 | Recruiting | ||
Study of the Interest of the Combination of Stiripentol (Diacomit®) and Carbamazepine in the Treatment of Patients With Pharmacoresistant Focal Epilepsies [NCT05419180] | Phase 4 | 100 participants (Anticipated) | Interventional | 2022-10-13 | Recruiting | ||
Treatment Plan to Provide Expanded Access to Stiripentol for Patients With Dravet Syndrome [NCT01983722] | 0 participants | Expanded Access | Approved for marketing | ||||
Compassionate Use of Stiripentol in Intractable Epilepsy Due to Dravet Syndrome [NCT01533506] | 0 participants | Expanded Access | 2012-02-29 | No longer available | |||
Open Label, Phase I Study to Assess and Compare the Pharmacokinetic Parameters After Multiple Oral Administration of Stiripentol 1000 mg in Renal Impaired Patients and Matching Controls With Normal Renal Function [NCT05735951] | Phase 1 | 48 participants (Anticipated) | Interventional | 2023-03-25 | Not yet recruiting | ||
Population Pharmacokinetics of Antiepileptic in Pediatrics [NCT03196466] | 1,000 participants (Anticipated) | Observational | 2017-06-19 | Recruiting | |||
Compassionate Use of Stiripentol in Dravet Syndrome [NCT01835314] | 0 participants | Expanded Access | No longer available | ||||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |