Page last updated: 2024-12-11

ro 48-3657

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

sibrafiban: prodrug of Ro-44-3888; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5491394
CHEMBL ID435176
CHEBI ID177667
MeSH IDM0264707

Synonyms (13)

Synonym
CHEBI:177667
ethyl 2-[1-[(2s)-2-[[4-[(e)-n'-hydroxycarbamimidoyl]benzoyl]amino]propanoyl]piperidin-4-yl]oxyacetate
sibrafiban
172927-65-0
bdbm50092123
(1-{2-[4-(n-hydroxycarbamimidoyl)-benzoylamino]-propionyl}-1,2,3,4-tetrahydro-pyridin-4-yloxy)-acetic acid ethyl ester(ro 48-3657(sibrafiban))
((s)-1-{2-[4-(n-hydroxycarbamimidoyl)-benzoylamino]-propionyl}-piperidin-4-yloxy)-acetic acid ethyl ester
CHEMBL435176 ,
ethyl [z]-(s)-[[1-[2-[[4-(amino-hydroximino-methyl)-benzoyl]amino]-1-oxopropyl]-4-piperidinyl]oxy]acetate
WBNUCLPUOSXSNJ-ZDUSSCGKSA-N
ethyl [z]-(s)-[[1-[2-[[4-(amino-hydroximino-methyl)-benzoyl]amino]-1 -oxopropyl]-4-piperidinyl]oxy]acetate
ro483657
Q7507267

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Particular emphasis was placed on intersubject variability of the pharmacokinetic and pharmacodynamic parameters of Ro 44-3888."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
" Part II, a double-blind, placebo-controlled, parallel-group study, addressed the intersubject variability of pharmacokinetic and pharmacodynamic parameters of the active principle at a sibrafiban dose achieving an intermediate effect."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
" The interindividual coefficients of variation of the integrated pharmacokinetic and pharmacodynamic parameters (AUC and AUE) were below 20%, thus lying well within the pre-set level of acceptance."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
"With a low intersubject variability of its pharmacokinetic and pharmacodynamic parameters, linear pharmacokinetics and pharmacodynamic effects closely related to its plasma concentrations, Ro 44-3888 has good pharmacological prerequisites for a well controllable therapy of secondary prevention of arterial thrombosis in patients with acute coronary syndrome."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
"The addition of ticlopidine/aspirin to sibrafiban did not significantly alter the pharmacokinetic parameters of Ro 44-3888."( Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin.
Birnböck, H; Chung, J; Ensor, H; Ertel, SI; Lausecker, B; Machin, SJ; MacKie, IJ; Wittke, B, 2000
)
0.31
"This study shows a significant pharmacodynamic interaction between sibrafiban and ticlopidine/aspirin."( Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin.
Birnböck, H; Chung, J; Ensor, H; Ertel, SI; Lausecker, B; Machin, SJ; MacKie, IJ; Wittke, B, 2000
)
0.31
" No pharmacodynamic interaction was seen with coadministration of heparin."( Pharmacokinetics and pharmacodynamics of sibrafiban, an orally administered GP IIb/IIIa antagonist, following coadministration of aspirin and heparin.
Modi, NB; Novotny, W; Reimann, JD, 2000
)
0.31
" 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

Compound-Compound Interactions

ExcerptReferenceRelevance
" Using the unique features of column-switching HPLC combined with MS/MS, it was possible to develop the method in a short period of time."( Column-switching high-performance liquid chromatography combined with ionspray tandem mass spectrometry for the simultaneous determination of the platelet inhibitor Ro 44-3888 and its pro-drug and precursor metabolite in plasma.
Hopfgartner, G; Husser, C; Zell, M, 1997
)
0.3
" Concentrations of the active metabolite of sibrafiban, Ro 44-3888, in plasma and urine were determined by column-switching liquid chromatography combined with tandem mass spectrometry."( Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin.
Birnböck, H; Chung, J; Ensor, H; Ertel, SI; Lausecker, B; Machin, SJ; MacKie, IJ; Wittke, B, 2000
)
0.31

Dosage Studied

ExcerptRelevanceReference
" In the PK/PD cohort of TIMI 12, 106 patients were randomized to receive one of seven dosing regimens of sibrafiban, ranging from 5 mg daily to 10 mg twice daily for 28 days."( Randomized trial of an oral platelet glycoprotein IIb/IIIa antagonist, sibrafiban, in patients after an acute coronary syndrome: results of the TIMI 12 trial. Thrombolysis in Myocardial Infarction.
Ault, K; Borzak, S; Braunwald, E; Cannon, CP; Feldman, R; Hamilton, SA; Henry, TD; McCabe, CH; Mueller, HS; Novotny, WF; Palmeri, ST; Rothman, JM; Tischler, MD, 1998
)
0.3
"The oral glycoprotein IIb/IIIa antagonist sibrafiban achieved effective, long-term platelet inhibition with a clear dose-response but at the expense of a relatively high incidence of minor bleeding."( Randomized trial of an oral platelet glycoprotein IIb/IIIa antagonist, sibrafiban, in patients after an acute coronary syndrome: results of the TIMI 12 trial. Thrombolysis in Myocardial Infarction.
Ault, K; Borzak, S; Braunwald, E; Cannon, CP; Feldman, R; Hamilton, SA; Henry, TD; McCabe, CH; Mueller, HS; Novotny, WF; Palmeri, ST; Rothman, JM; Tischler, MD, 1998
)
0.3
" This large trial uses twice daily dosage regimens to produce the plasma concentrations which were associated with less bleeding in the earlier dose-ranging trial."( Sibrafiban.
Dooley, M; Goa, KL, 1999
)
0.3
" At the higher doses, ADP-induced platelet aggregation was almost completely inhibited while a clear dose-response could be observed with TRAP-induced inhibition of platelet aggregation at sibrafiban doses of 5 to 12 mg."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
" Once-daily dosing resulted in high peak-trough excursions in active drug concentrations: trough concentrations were 21% +/- 6% of peak."( Pharmacokinetics and pharmacodynamics of sibrafiban, an orally administered IIb/IIIa antagonist, in patients with acute coronary syndrome.
Braunwauld, E; Cannon, CP; Modi, NB; Novotny, W; Reimann, JD, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
N-acylglycineAn N-acyl-amino acid in which amino acid specified is glycine.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (40)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (35.00)18.2507
2000's26 (65.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.23

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.23 (24.57)
Research Supply Index4.03 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials14 (34.15%)5.53%
Reviews12 (29.27%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (36.59%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]