orbofiban: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 178080 |
| CHEMBL ID | 64706 |
| SCHEMBL ID | 7854981 |
| MeSH ID | M0332100 |
| Synonym |
|---|
| 3-{3-[1-(4-carbamimidoyl-phenyl)-2-oxo-pyrrolidin-3-yl]-ureido}-propionic acid ethyl ester (sc-57099b (orbofiban)) |
| bdbm50092109 |
| 3-{(s)-3-[1-(4-carbamimidoyl-phenyl)-2-oxo-pyrrolidin-3-yl]-ureido}-propionic acid ethyl ester |
| orbofiban |
| CHEMBL64706 , |
| ethyl 3-[[(3s)-1-(4-carbamimidoylphenyl)-2-oxopyrrolidin-3-yl]carbamoylamino]propanoate |
| 163250-90-6 |
| fgj53js7pt , |
| unii-fgj53js7pt |
| orbofiban [inn] |
| beta-alanine, n-((((3s)-1-(4-(aminoiminomethyl)phenyl)-2-oxo-3- pyrrolidinyl)amino)carbonyl)-, ethyl ester |
| .beta.-alanine, n-((((3s)-1-(4-(aminoiminomethyl)phenyl)-2-oxo-3-pyrrolidinyl)amino)carbonyl)-, ethyl ester |
| orbofiban [who-dd] |
| SCHEMBL7854981 |
| DTXSID20167543 |
| Q27277978 |
| HY-10304 |
| CS-0002538 |
Orbofiban is a unique antiplatelet agent that inhibits the binding of fibrinogen to gycoprotein (GP) IIb/IIIa integrin receptors and thus prevents platelet aggregation induced by various agents.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Orbofiban is a unique antiplatelet agent that inhibits the binding of fibrinogen to gycoprotein (GP) IIb/IIIa integrin receptors and thus prevents platelet aggregation induced by various agents. " | ( Role of oral blockade of platelet glycoprotein IIb/IIIa on neutrophil activation in patients with acute coronary syndromes. Anders, RJ; Baracioli, LM; Cannon, CP; Nicolau, JC; Ramires, JA; Serrano, CV; Venturinelli, M, 2003) | 1.76 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Roxifiban has pharmacokinetic and pharmacodynamic properties believed to be more favorable than the earlier oral agents." | ( Effects of glycoprotein IIb/IIIa antagonists on platelet activation: development of a transfer method to mimic peak to trough receptor occupancy. Billheimer, JT; He, B; Seiffert, D; Spitz, SM; Stern, AM, 2002) | 0.31 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " It is predicted that the high oral bioavailability for these compounds in multiple species should translate into lower intra- and intersubject variability in man." | ( Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. Heath, JA; Hollenbach, SJ; Lambing, JL; Mehrotra, MM; Nannizzi-Alaimo, L; Pandey, A; Park, GL; Rose, JW; Scarborough, RM; Seroogy, JM; Smyth, MS; Volkots, DL, 2004) | 0.32 |
| " Superoxide is known to alter the bioavailability of NO, and its contribution to the GPIIb/IIIa dependent increase in NO release was determined." | ( Glycoprotein IIb/IIIa inhibition enhances platelet nitric oxide release. Chakrabarti, S; Clutton, P; Cox, D; Freedman, JE; Mascelli, MA; Varghese, S, 2004) | 0.32 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Depending on the degree of the precipitation, which was dosage dependent, and the location, which differed somewhat between the two compounds, the lesions varied from acute obstruction with tubule cell necrosis, nephron dilation, and sudden death with no inflammation to severe chronic pyogranulomatous inflammation." | ( Lesions and identification of crystalline precipitates of glycoprotein IIb-IIIa antagonists in the rat kidney. Cortez, E; Fouant, M; Friedman, RM; Hribar, J; Khan, N; Levin, S; Nicholas, M; Schlessinger, S, ) | 0.13 |
| " Oral GP IIb/IIIa inhibitors have been associated with an increased incidence of bleeding, but additional experience may permit the design of dosing regimens that decrease this risk." | ( Learning from the recently completed oral glycoprotein IIb/IIIa receptor antagonist trials. Cannon, CP, 2000) | 0.31 |
| " Nevertheless, none of these fibans was able to effectively block shear-induced platelet adhesion at targeted clinical dosing regimens except for abciximab." | ( Comparative analysis of various platelet glycoprotein IIb/IIIa antagonists on shear-induced platelet activation and adhesion. Barbera, FA; Dorsam, RT; Feuerstein, GZ; Friedman, SM; Gibbs, S; Lauver, A; Savion, N; Varon, D; Wang, H; Wang, X, 2002) | 0.31 |
| " Site occupancy studies combined with clot retraction experiments addressed whether high affinity and slow off-rate compounds can alter clot retraction during the dosing interval." | ( Regulation of clot retraction by glycoprotein IIb/IIIa antagonists. Billheimer, JT; He, B; Kieras, CJ; Pedicord, DL; Seiffert, D; Stern, AM, 2002) | 0.31 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Integrin beta-3 | Homo sapiens (human) | IC50 (µMol) | 0.1462 | 0.0001 | 0.6323 | 10.0000 | AID219711; AID221915; AID72990; AID93131; AID93132; AID93141 |
| Integrin alpha-IIb | Homo sapiens (human) | IC50 (µMol) | 0.1462 | 0.0001 | 0.7309 | 10.0000 | AID219711; AID221915; AID72990; AID93131; AID93132; AID93141 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID27703 | biological half-life was measured on dog | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
| AID73596 | Inhibition of Human umbilical vein endothelial cells (HUVEC) adhesion to fibronectin (not determined) | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID93138 | Inhibition of citreated human platelet (h-PRP) aggregation induced by 4 ug/mL collagen (not determined) | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID93136 | Inhibition of platelet aggregation induced by 20 uM adenosine 5-diphosphate (ADP) in citreated human platelet rich plasma (h-PRP) | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID18840 | Oral bioavailability in dog | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
| AID217292 | Inhibition of Human umbilical vein endothelial cells (HUVEC) adhesion to vitronectin (not determined) | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID217302 | Inhibition of vitronectin binding to Vitronectin receptor (alpha V beta 3) (not determined) | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID93131 | Inhibition of human platelet (h-PRP) aggregation induced by 20 uM ADP with PPACK | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID219711 | Inhibition of collagen-induced platelet aggregation | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
| AID93140 | Inhibition of human platelet (h-PRP) aggregation induced by 4 ug/mL collagen with PPACK (not determined) | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID72990 | Tested for inhibition of the binding of fibrinogen to purified human GPIIb-IIIa in a 96-well format (ELISA assay) | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID221915 | Inhibition of human gel filtered platelet aggregation induced by ADP | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
| AID93132 | Inhibition of human platelet (h-PRP) aggregation induced by 5 uM TRAP6 with PPACK | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| AID93141 | Inhibition of citreated human (h-PRP) platelet aggregation induced by 5 uM TRAP6 | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
| [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 (2.13) | 18.2507 |
| 2000's | 45 (95.74) | 29.6817 |
| 2010's | 1 (2.13) | 24.3611 |
| 2020's | 0 (0.00) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (19.74) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 17 (35.42%) | 5.53% |
| Reviews | 9 (18.75%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 22 (45.83%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||