tbc-11251 has been researched along with lu 208075 in 32 studies
| Studies (tbc-11251) | Trials (tbc-11251) | Recent Studies (post-2010) (tbc-11251) | Studies (lu 208075) | Trials (lu 208075) | Recent Studies (post-2010) (lu 208075) |
|---|---|---|---|---|---|
| 167 | 32 | 58 | 298 | 54 | 227 |
| Protein | Taxonomy | tbc-11251 (IC50) | lu 208075 (IC50) |
|---|---|---|---|
| Endothelin receptor type B | Rattus norvegicus (Norway rat) | 0.195 | |
| Endothelin receptor type B | Homo sapiens (human) | 0.6925 | |
| Endothelin-1 receptor | Homo sapiens (human) | 0.0114 |
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 14 (43.75) | 29.6817 |
| 2010's | 17 (53.13) | 24.3611 |
| 2020's | 1 (3.13) | 2.80 |
| Authors | Studies |
|---|---|
| Barnes, JC; Bradley, P; Day, NC; Fourches, D; Reed, JZ; Tropsha, A | 1 |
| Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
| Bolli, MH; Boss, C; Gatfield, J | 1 |
| Humbert, M; Simonneau, G | 1 |
| Hoeper, MM | 1 |
| Langleben, D | 1 |
| Dupuis, J; Hoeper, MM | 1 |
| Amoura, Z; Cacoub, P; Langleben, D | 1 |
| Batyraliev, TA; Ekinsi, E; Makhmutkhodzhaev, SA; Pataraia, SA; Pershukov, IV; Preobrazhenskiĭ, DV; Sidorenko, BA | 1 |
| Howard, LS; Price, LC | 1 |
| Ewert, R; Kirch, W; Opitz, CF; Pittrow, D | 1 |
| Coghlan, G; Kabunga, P | 1 |
| Badesch, DB; Despain, DJ; Dufton, C; Frost, AE; Galie, N; Gerber, MJ; McGoon, MD; McLaughlin, VV; Olschewski, H; Oudiz, RJ; Rubin, LJ | 1 |
| Stähler, G | 1 |
| Preston, IR; Steiner, MK | 1 |
| Mucke, HA | 1 |
| Dranitsaris, G; Mehta, S | 1 |
| Humbert, M; Montani, D | 1 |
| Hunsche, E; Lefebvre, MC | 1 |
| Brouwer, K; Gorczynski, R; Hartman, JC; Mandagere, A; Melvin, L | 1 |
| Derk, CT; Shetty, N | 1 |
| Safdar, Z | 1 |
| French, B; Gabler, NB; Halpern, SD; Kawut, SM; Liu, Z; Palevsky, HI; Strom, BL; Taichman, DB | 1 |
| Alexander, GJ; Davenport, AP; Davie, NJ; Gibbs, P; Kuc, RE; Ling, L; Maguire, JJ; Webb, DJ | 1 |
| Blenkhorn, F; Eisenberg, MJ; Fox, B; Hirsch, AM; Joyal, D; Langleben, D; Lesenko, L; Schlesinger, RD | 1 |
| Boico, A; Hamilton, K; Hanna, G; Irwin, D; Palmer, G; Piantadosi, CA; Radiloff, DR; Schroeder, T; Shan, S; Wu, C; Zhao, Y | 1 |
| Luo, N; Ryan, JJ | 1 |
| Catalá-López, F; de la Fuente Honrubia, C; Macías Saint-Gerons, D; Montero Corominas, D | 1 |
| Barbaro Foschino, MP; Brunetti, ND; Correale, M; Di Biase, M; Lacedonia, D; Montrone, D; Totaro, A | 1 |
| Brouwer, KR; Gillies, H; Hao, J; Hubert, C; Lepist, EI; Ray, AS; Smith, W; St Claire, RL | 1 |
| Andersson, LC; Bergare, J; Billger, M; Eakins, JA; Elebring, M; Elmore, CS; Foster, AJ; Kenna, JG; Stahl, SH; Thompson, RA | 1 |
| Bahmany, S; Danser, AHJ; Hitzerd, E; Koch, BCP; van de Velde, D; van Domburg, B; Versmissen, J | 1 |
17 review(s) available for tbc-11251 and lu 208075
| Article | Year |
|---|---|
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk | 2016 |
From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
Topics: Bosentan; Chemistry, Pharmaceutical; Dose-Response Relationship, Drug; Humans; Molecular Structure; Pyrimidines; Receptors, Endothelin; Structure-Activity Relationship; Sulfonamides | 2016 |
Drug Insight: endothelin-receptor antagonists for pulmonary arterial hypertension in systemic rheumatic diseases.
Topics: Endothelin Receptor Antagonists; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pulmonary Wedge Pressure; Pyridazines; Rheumatic Diseases; Thiophenes; Treatment Outcome | 2005 |
[Treatment of pulmonary arterial hypertension: endothelin-receptor antagonists].
Topics: Algorithms; Antihypertensive Agents; Bosentan; Drug Interactions; Endothelin Receptor Antagonists; Endothelin-1; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pyridazines; Sulfonamides; Survival Rate; Thiophenes | 2006 |
Endothelin receptor antagonists in the treatment of pulmonary arterial hypertension.
Topics: Antihypertensive Agents; Bosentan; Drug Therapy, Combination; Endothelin Receptor Antagonists; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pyridazines; Randomized Controlled Trials as Topic; Sulfonamides; Thiophenes | 2007 |
Endothelin receptor antagonists in pulmonary arterial hypertension.
Topics: Animals; Bosentan; Clinical Trials, Phase III as Topic; Endothelin A Receptor Antagonists; Endothelin B Receptor Antagonists; Endothelin Receptor Antagonists; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Prognosis; Pyridazines; Randomized Controlled Trials as Topic; Receptor, Endothelin A; Receptor, Endothelin B; Receptors, Endothelin; Severity of Illness Index; Sulfonamides; Survival Rate; Thiophenes; Treatment Outcome | 2008 |
[Treatment of pulmonary arterial hypertension by endothelin receptor antagonists in 2008].
Topics: Antihypertensive Agents; Bosentan; Endothelin Receptor Antagonists; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pyridazines; Sulfonamides; Thiophenes | 2008 |
[Pulmonary hypertension and right ventricular failure. Part XI. Endothelin receptor blockers in the treatment of primary pulmonary arterial hypertension].
Topics: Antihypertensive Agents; Bosentan; Endothelin Receptor Antagonists; Heart Failure; Hemodynamics; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pyridazines; Sulfonamides; Thiophenes; Ventricular Dysfunction, Right | 2007 |
Endothelin receptor antagonists for pulmonary arterial hypertension: rationale and place in therapy.
Topics: Antihypertensive Agents; Bosentan; Clinical Trials, Phase III as Topic; Drug Interactions; Endothelin Receptor Antagonists; Endothelins; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pyridazines; Sulfonamides; Thiophenes | 2008 |
Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: does selectivity matter?
Topics: Antihypertensive Agents; Bosentan; Endothelin Receptor Antagonists; Endothelin-1; Female; Humans; Hypertension, Pulmonary; Isoxazoles; Male; Phenylpropionates; Pulmonary Artery; Pyridazines; Randomized Controlled Trials as Topic; Sulfonamides; Thiophenes; Treatment Outcome; Vascular Resistance; Walking | 2008 |
Endothelin receptor antagonism: role in the treatment of pulmonary arterial hypertension related to scleroderma.
Topics: Antihypertensive Agents; Bosentan; Drug Therapy, Combination; Endothelin Receptor Antagonists; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pyridazines; Receptors, Endothelin; Scleroderma, Systemic; Sulfonamides; Thiophenes; Treatment Outcome | 2008 |
[Specific drugs for the treatment of pulmonary arterial hypertension - current status].
Topics: Antihypertensive Agents; Bosentan; Endothelin Receptor Antagonists; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Phosphodiesterase 5 Inhibitors; Phosphodiesterase Inhibitors; Piperazines; Prostaglandins; Purines; Pyridazines; Sildenafil Citrate; Sulfonamides; Sulfones; Survival Rate; Thiophenes; Vasodilator Agents | 2008 |
Optimizing endothelin receptor antagonist use in the management of pulmonary arterial hypertension.
Topics: Animals; Antihypertensive Agents; Bosentan; Drug Therapy, Combination; Endothelin Receptor Antagonists; Humans; Hypertension, Pulmonary; Isoxazoles; Patient Compliance; Patient Satisfaction; Phenylpropionates; Pyridazines; Quality of Life; Receptors, Endothelin; Sulfonamides; Thiophenes; Treatment Outcome | 2008 |
Small-molecule endothelin receptor antagonists: a review of patenting activity across therapeutic areas.
Topics: Animals; Antihypertensive Agents; Bosentan; Drug Design; Endothelin Receptor Antagonists; Endothelins; Humans; Hypertension, Pulmonary; Isoxazoles; Patents as Topic; Phenylpropionates; Pyridazines; Sulfonamides; Thiophenes | 2009 |
Endothelin receptor antagonists as disease modifiers in systemic sclerosis.
Topics: Animals; Antihypertensive Agents; Bosentan; Endothelin Receptor Antagonists; Endothelins; Familial Primary Pulmonary Hypertension; Fibrosis; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pyridazines; Receptors, Endothelin; Scleroderma, Systemic; Sulfonamides; Thiophenes; Treatment Outcome | 2011 |
[Hepatotoxicity in patients treated with endothelin receptor antagonists: systematic review and meta-analysis of randomized clinical trials].
Topics: Antihypertensive Agents; Biomarkers; Bosentan; Chemical and Drug Induced Liver Injury; Endothelin Receptor Antagonists; Humans; Hypertension; Isoxazoles; Phenylpropionates; Pyridazines; Randomized Controlled Trials as Topic; Safety-Based Drug Withdrawals; Sulfonamides; Thiophenes; Transaminases | 2014 |
Novelty in treatment of pulmonary fibrosis: pulmonary hypertension drugs and others.
Topics: Antihypertensive Agents; Bosentan; Humans; Isoxazoles; Phenylpropionates; Phosphodiesterase Inhibitors; Pulmonary Fibrosis; Pyridazines; Sulfonamides; Thiophenes | 2013 |
2 trial(s) available for tbc-11251 and lu 208075
| Article | Year |
|---|---|
Ambrisentan therapy in patients with pulmonary arterial hypertension who discontinued bosentan or sitaxsentan due to liver function test abnormalities.
Topics: Adolescent; Adult; Aged; Antihypertensive Agents; Bosentan; Child; Disease-Free Survival; Endothelin Receptor Antagonists; Female; Humans; Hypertension, Pulmonary; Isoxazoles; Liver Function Tests; Male; Middle Aged; Phenylpropionates; Pyridazines; Sulfonamides; Thiophenes; Transaminases; Treatment Outcome; Young Adult | 2009 |
Race and sex differences in response to endothelin receptor antagonists for pulmonary arterial hypertension.
Topics: Adolescent; Adult; Aged; Aged, 80 and over; Antihypertensive Agents; Bosentan; Child; Double-Blind Method; Endothelin Receptor Antagonists; Ethnicity; Exercise Test; Familial Primary Pulmonary Hypertension; Female; Follow-Up Studies; Humans; Hypertension, Pulmonary; Isoxazoles; Male; Middle Aged; Phenylpropionates; Prevalence; Prospective Studies; Pulmonary Wedge Pressure; Pyridazines; Sex Factors; Sulfonamides; Thiophenes; Treatment Outcome; United States; Walking; Young Adult | 2012 |
13 other study(ies) available for tbc-11251 and lu 208075
| Article | Year |
|---|---|
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
Topics: Animals; Chemical and Drug Induced Liver Injury; Cluster Analysis; Databases, Factual; Humans; MEDLINE; Mice; Models, Chemical; Molecular Conformation; Quantitative Structure-Activity Relationship | 2010 |
Oral therapies for the treatment of pulmonary arterial hypertension: a population-based cost-minimization analysis.
Topics: Administration, Oral; Antihypertensive Agents; Bosentan; Canada; Costs and Cost Analysis; Drug Costs; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Piperazines; Placebos; Purines; Pyridazines; Randomized Controlled Trials as Topic; Sildenafil Citrate; Sulfonamides; Sulfones; Thiophenes; Treatment Outcome | 2009 |
[Endothelin receptor antagonists in the new European guidelines on pulmonary hypertension].
Topics: Administration, Oral; Antihypertensive Agents; Bosentan; Drug Therapy, Combination; Endothelin Receptor Antagonists; Europe; Evidence-Based Medicine; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Phosphodiesterase 5 Inhibitors; Phosphodiesterase Inhibitors; Piperazines; Practice Guidelines as Topic; Purines; Pyridazines; Sildenafil Citrate; Sulfonamides; Sulfones; Thiophenes | 2010 |
Oral Therapies for the treatment of pulmonary arterial hypertension: a population-based cost-minimization analysis.
Topics: Administration, Oral; Antihypertensive Agents; Bosentan; Canada; Cost Control; Drug Costs; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Piperazines; Purines; Pyridazines; Sildenafil Citrate; Sulfonamides; Sulfones; Thiophenes | 2010 |
Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes.
Topics: Adolescent; Adult; Aged; Antihypertensive Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Bosentan; Cell Culture Techniques; Cells, Cultured; Endothelin Receptor Antagonists; Enkephalin, D-Penicillamine (2,5)-; Estradiol; Female; Hepatocytes; Humans; Isoxazoles; Male; Middle Aged; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Organic Anion Transporters; Organic Anion Transporters, Sodium-Dependent; Phenylpropionates; Pyridazines; Pyrimidines; Sulfonamides; Symporters; Taurocholic Acid; Thiophenes; Young Adult | 2010 |
Effect of transition from sitaxsentan to ambrisentan in pulmonary arterial hypertension.
Topics: Adult; Aged; Antihypertensive Agents; Blood Pressure; Drug Substitution; Dyspnea; Edema; Endothelin A Receptor Antagonists; Exercise Test; Exercise Tolerance; Familial Primary Pulmonary Hypertension; Female; Humans; Hypertension, Pulmonary; Isoxazoles; Liver Function Tests; Male; Middle Aged; Natriuretic Peptide, Brain; Oxygen; Phenylpropionates; Pyridazines; Retrospective Studies; Texas; Thiophenes; Time Factors; Treatment Outcome; Walking | 2011 |
Comparison of endothelin receptors in normal versus cirrhotic human liver and in the liver from endothelial cell-specific ETB knockout mice.
Topics: Animals; Autoradiography; Binding, Competitive; Hepatic Artery; Humans; Isoxazoles; Liver; Liver Cirrhosis; Mice; Mice, Knockout; Microscopy, Fluorescence; Phenylpropionates; Portal Vein; Pyridazines; Receptor, Endothelin A; Receptor, Endothelin B; Thiophenes; Up-Regulation | 2012 |
Hemodynamic stability after transitioning between endothelin receptor antagonists in patients with pulmonary arterial hypertension.
Topics: Administration, Oral; Aged; Antihypertensive Agents; Bosentan; Endothelin Receptor Antagonists; Familial Primary Pulmonary Hypertension; Female; Humans; Hypertension, Pulmonary; Isoxazoles; Middle Aged; Phenylpropionates; Pulmonary Wedge Pressure; Pyridazines; Retrospective Studies; Sulfonamides; Thiophenes; Treatment Outcome; Vascular Resistance | 2013 |
The combination of theophylline and endothelin receptor antagonism improves exercise performance of rats under simulated high altitude.
Topics: Altitude; Animals; Arterial Pressure; Cyclic Nucleotide Phosphodiesterases, Type 5; Drug Synergism; Endothelin Receptor Antagonists; Female; Heart Rate; Hemodynamics; Hemoglobins; Hypoxia; Isoxazoles; Oxygen; Phenylpropionates; Physical Conditioning, Animal; Piperazines; Pulmonary Artery; Purines; Pyridazines; Random Allocation; Rats; Rats, Sprague-Dawley; Receptors, Endothelin; Renal Circulation; Respiration; Sildenafil Citrate; Sulfones; Task Performance and Analysis; Theophylline; Thiophenes; Vasoconstriction | 2012 |
Transitioning between endothelin receptor blockers: monitoring to ensure a smooth transition.
Topics: Bosentan; Endothelin Receptor Antagonists; Familial Primary Pulmonary Hypertension; Female; Humans; Hypertension, Pulmonary; Isoxazoles; Phenylpropionates; Pulmonary Wedge Pressure; Pyridazines; Sulfonamides; Thiophenes; Vascular Resistance | 2013 |
Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes.
Topics: Adult; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Bile; Bile Acids and Salts; Bosentan; Endothelin Receptor Antagonists; Female; Hepatocytes; Humans; Isoxazoles; Liver; Liver-Specific Organic Anion Transporter 1; Male; Membrane Transport Proteins; Middle Aged; Multidrug Resistance-Associated Proteins; Neoplasm Proteins; Organic Anion Transporters; Organic Anion Transporters, Sodium-Dependent; Organic Anion Transporters, Sodium-Independent; Phenylpropionates; Pyridazines; Pyrimidines; Receptors, Endothelin; Solute Carrier Organic Anion Transporter Family Member 1B3; Sulfonamides; Symporters; Taurocholic Acid; Thiophenes | 2014 |
Multiple compound-related adverse properties contribute to liver injury caused by endothelin receptor antagonists.
Topics: ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Sub-Family B Member 4; ATP-Binding Cassette Transporters; Bosentan; Cell Line; Cell Survival; Chemical and Drug Induced Liver Injury; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Endothelin Receptor Antagonists; Epithelial Cells; Hepatocytes; Humans; Isoxazoles; Mitochondria; Molecular Structure; Oxygen Consumption; Phenylpropionates; Pyridazines; Sulfonamides; Thiophenes | 2015 |
Simultaneous quantification of ambrisentan, macitentan and sitaxentan in human plasma using UPLC-MS/MS.
Topics: Antihypertensive Agents; Chromatography, High Pressure Liquid; Humans; Isoxazoles; Linear Models; Phenylpropionates; Pyridazines; Pyrimidines; Reproducibility of Results; Sensitivity and Specificity; Sulfonamides; Tandem Mass Spectrometry; Thiophenes | 2020 |