ID Source | ID |
---|---|
PubMed CID | 152951 |
CHEMBL ID | 59461 |
SCHEMBL ID | 4375 |
MeSH ID | M0100029 |
Synonym |
---|
BIDD:GT0748 |
2-piperidinecarboxylic acid, 1-(5-((aminoiminomethyl)amino)-1-oxo-2-(((1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl)amino)pentyl)-4-methyl-, (2r-(1(s*(r*)),2alpha,4beta))- |
CHEMBL59461 |
(2r,4r)-1-[(2s)-5-(diaminomethylideneamino)-2-[[(3r)-3-methyl-1,2,3,4-tetrahydroquinolin-8-yl]sulfonylamino]pentanoyl]-4-methylpiperidine-2-carboxylic acid |
(21r)-argatroban |
unii-0dw7mih1vx |
0dw7mih1vx , |
cas-74863-84-6 |
dtxsid7046467 , |
tox21_112218 |
dtxcid5026467 |
(2r,4r)-1-[(2s)-5-[(diaminomethylidene)amino]-2-[(3r)-3-methyl-1,2,3,4-tetrahydroquinoline-8-sulfonamido]pentanoyl]-4-methylpiperidine-2-carboxylic acid |
SCHEMBL4375 |
tox21_112218_1 |
NCGC00166413-02 |
argatroban anhydrous, (21r)- |
21r-argatroban anhydrous |
argatroban anhydrous, 21r- |
Q474880 |
21(r)-argatroban |
EX-A4205 |
PD010129 |
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Pathway | Proteins | Compounds |
---|---|---|
Argatroban Action Pathway | 20 | 3 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
AR protein | Homo sapiens (human) | Potency | 20.4947 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 13.8029 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 13.3332 | 0.0376 | 17.0823 | 61.1927 | AID1259364 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
[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 | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 3 (33.33) | 24.3611 |
2020's | 6 (66.67) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (73.50) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 9 (100.00%) | 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 | ||
---|---|---|---|---|---|---|---|
A Prospective Randomized Pilot Trial on Safety and Feasibility of Argatroban as Anticoagulant in Patients With Extracorporeal Membrane Oxygenation (ECMO) [NCT05226442] | Phase 2/Phase 3 | 40 participants (Anticipated) | Interventional | 2021-12-01 | Recruiting | ||
SAICoDis - Safety of Argatroban Infusion in Conduction Disturbances. A Prospective, Open, Multicenter Safety Study to Investigate Conduction Disturbances in Patients Receiving Argatroban Therapy. [NCT05740371] | Phase 4 | 50 participants (Actual) | Interventional | 2017-04-18 | Completed | ||
Argatroban Combined With Antiplatelet Versus Antiplatelet for Acute Mild or Moderate Ischemic Stroke With Large-artery Atherosclerosis: a Prospective, Single Center Study [NCT03552354] | Phase 4 | 120 participants (Actual) | Interventional | 2017-10-25 | Completed | ||
Argatroban Plus R-tPA for Acute Ischemic Stroke: a Prospective, Random, Open Label, Blinded Assessment of Outcome Multi-center Study [NCT03740958] | Phase 4 | 808 participants (Actual) | Interventional | 2018-12-21 | Completed | ||
Fondaparinux in Patients With Acute Heparin-Induced Thrombocytopenia [NCT00603824] | Phase 4 | 0 participants (Actual) | Interventional | 2008-01-31 | Withdrawn(stopped due to PI relocated) | ||
ARTSS-IA: A Pilot, Phase IIa, Safety and Feasibility Study of ARgatroban in Combination With Recombinant Tissue Plasminogen Activator Stroke Study - Intra-Arterial [NCT02448069] | Phase 2 | 10 participants (Actual) | Interventional | 2015-05-31 | Completed | ||
A Phase I, Open-Label, Randomized, Three-Period, Three-Sequence Crossover Study of the Effects of Co-administration of Intravenous VLX-1005 With Argatroban on Pharmacokinetics, Pharmacodynamics and Safety in Healthy Adult Subjects [NCT05325346] | Phase 1 | 12 participants (Actual) | Interventional | 2022-03-07 | Completed | ||
Multi-arm Optimization of Stroke Thrombolysis (MOST): a Single Blinded, Randomized Controlled Adaptive, Multi-arm, Adjunctive-thrombolysis Efficacy Trial in Ischemic Stroke [NCT03735979] | Phase 3 | 514 participants (Actual) | Interventional | 2019-10-15 | Active, not recruiting | ||
An Open-label, Multi-centre, Clinical Study to Collect Information on the Clinical Use of Argatroban in Patients With Heparin Induced Thrombocytopenia (HIT) Type II Who Require Parenteral Antithrombotic Therapy [NCT00861692] | Phase 2 | 20 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
Open-Label, Randomised, Active Controlled, Multi-Centre Ph 3 Study to Evaluate the Safety and Efficacy of Danaparoid vs Argatroban in Acute HIT [NCT03809481] | Phase 3 | 7 participants (Actual) | Interventional | 2019-05-16 | Terminated(stopped due to Prolonged delay as a result of impact of Covid19 pandemic) | ||
Argatroban Versus Lepirudin in Critically Ill Patients - A Randomized Double-blind Trial [NCT00798525] | Phase 4 | 70 participants (Actual) | Interventional | 2009-01-31 | Terminated(stopped due to Supply of Lepirudin ended on 01. April 2012, thus trial terminated on 31. March 2012) | ||
A Pilot Trial to Assess the Efficacy of Argatroban (Argatra®) in Critically Ill Patients With Heparin Resistance [NCT01734252] | Phase 2 | 44 participants (Actual) | Interventional | 2012-07-29 | Completed | ||
Direct Thrombin Inhibitors Versus LMWH in Staphylococcus Aureus Bacteraemia. A Prospective Randomized Controlled Academic Single-centre Feasibility Study. [NCT01911624] | Phase 2 | 94 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
Phase 4 Study of Argatroban for Preventing Restenosis After Extracranial Vertebral Artery Stenting [NCT01980316] | Phase 4 | 114 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
Monitoring Anticoagulation With Argatroban in Patients on Extracorporeal Membrane Oxygenation for Severe Lung Failure Using Anti-FIIa. Monitoring Anticoagulation With Unfractionated Heparin in Patients on Extracorporeal Membrane Oxygenation for Severe Lun [NCT06038682] | 100 participants (Actual) | Observational | 2020-04-01 | Completed | |||
InterMediate ProphylACtic Versus Therapeutic Dose Anticoagulation in Critically Ill Patients With COVID-19: A Prospective Randomized Study (The IMPACT Trial) [NCT04406389] | Phase 4 | 14 participants (Actual) | Interventional | 2020-10-13 | Terminated(stopped due to Low accrual) | ||
Evaluation of Argatroban Injection in Pediatric Patients Requiring Anticoagulant Alternatives to Heparin [NCT00039858] | Phase 4 | 24 participants | Interventional | 2003-09-30 | Completed | ||
A Randomised, Open, Parallel-group, Multicentre Study to Examine the Safety and Effectiveness of Three Doses of Argatroban as Anticoagulant in Combination With Clopidogrel and Aspirin in Patients Undergoing Elective Percutaneous Coronary Intervention in C [NCT00508924] | Phase 2 | 140 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
Open-Label Trial to Evaluate the Efficacy and Safety of the Use of Argatroban in Patients With Heparin-Induced Thrombocytopenia [NCT00198588] | Phase 3 | 8 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
ARTSS-2: A Pilot, Phase 2b, Randomized, Multi-center Trial of Argatroban in Combination With Recombinant Tissue Plasminogen Activator for Acute Stroke [NCT01464788] | Phase 2 | 90 participants (Actual) | Interventional | 2011-10-31 | Terminated(stopped due to The study was halted prematurely at 90 of 105 planned patients due to the beneficial results of embolectomy clinical trials.) | ||
Effectiveness and Safety of Thromboprophylaxis After Surgery for Gynecologic Malignancy in China [NCT02935530] | Phase 3 | 315 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
A Comparative Clinical and Pharmacoeconomic Study Comparing Argatroban® IV vs Desirudin SC for Patients With Suspected Heparin-Induced Thrombocytopenia (HIT)With or Without Thrombosis Syndrome (HIT/TS) [NCT00787332] | Phase 4 | 16 participants (Actual) | Interventional | 2008-09-30 | Terminated(stopped due to Low enrollment) | ||
Phase 4 Study of Argatroban for Preventing Occlusion and Restenosis After Intracranial and Extracranial Artery Stenting [NCT01163604] | Phase 4 | 114 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
Systematische Dokumentation Von Patienten Mit Akutem HIT-Verdacht [NCT01304238] | 195 participants (Actual) | Observational | 2009-02-28 | Completed | |||
Significance of Antibodies to Heparin/Platelet Factor 4 Complex in Vein Graft Patency and Potential Role of Argatroban for Prevention of Vein Graft Occlusion [NCT01246011] | Phase 4 | 9 participants (Actual) | Interventional | 2010-11-30 | Terminated(stopped due to Enrollment was too slow.) | ||
Pharmacokinetics and Pharmacodynamics of Argatroban Injection in End-Stage Renal Disease (ESRD) Patients Undergoing Hemodialysis [NCT00035178] | Phase 4 | 12 participants | Interventional | 2002-05-31 | Completed | ||
Efficacy of Argatroban in Acute Ischemic Stroke With Early Neurological Deterioration [NCT04275180] | Phase 4 | 628 participants (Actual) | Interventional | 2020-03-21 | Completed | ||
A Pilot Study To Determine The Safety Of Argatroban Injection In Combination With Tissue Plasmingen Activator (TPA) In Patients With Acute Ischemic Stroke [NCT00268762] | Phase 1/Phase 2 | 65 participants (Actual) | Interventional | 2003-02-28 | Completed | ||
Safety and Efficacy of Argatroban Applicated in Anticoagulation of V-V ECMO: A Randomized Controlled Study [NCT04925167] | 174 participants (Anticipated) | Interventional | 2021-07-06 | Recruiting | |||
Argatroban Plus R-tPA for Acute Posterior Circulation Infarction (AR-PCI): a Prospective, Random, Blinded Assessment of Outcome and Open Label Multi-center Study [NCT03506009] | Phase 4 | 3 participants (Actual) | Interventional | 2018-07-11 | Terminated(stopped due to it is very difficult to recruit qualified patients) | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |