Page last updated: 2024-11-12

cgp 39393

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

Description

desirudin: recombinant hirudin; has identical amino acid sequence as the natural hirudin variant 1 but lacks the sulphate group on Tyr(63) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

desirudin : A heterodetic cyclic peptide composed of 65 amino acids joined in sequence and cyclised by three disulfide bridges between cysteine residues 6-14, 16-28 and 22-39. It is a highly specific inhibitor of thrombin and used as an anticoagulant in patients to prevent venous thromboembolism. Its amino acid sequence differs from natural hirudin by lack of sulfate group on Tyr-63. [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]

Cross-References

ID SourceID
PubMed CID16129703
MeSH IDM0167423

Synonyms (21)

Synonym
120993-53-5
desirudin
cgp 39393
recombinant hv1 hirudin
63-desulfohirudin (hirudo medicinalis isoform hv1)
ik-hir02
cgp-39393
hirudin (hirudo medicinalis isoform hv1), 63-desulfo-
63-desulfohirudin
63-desulfohirudin (recombinant)
hirudin desirudin
desirudin [usan:inn:ban]
unii-u0jz726775
u0jz726775 ,
cgp39393
gtpl6458
DTXSID90153094 ,
dtxcid9075585
desirudin (mart.)
63-desulfohirudin(hirudo medicinalis isoform hv1)
b01ae01

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"A principal aim of population pharmacokinetic studies is to estimate the variance components associated with intra- and inter-individual variability in observed drug concentrations."( Statistical methods for population pharmacokinetic modelling.
Racine-Poon, A; Wakefield, J, 1998
)
0.3
" Pharmacodynamic (PD) models describe the relationship between the concentration in the blood (or the dose) and the biologic response."( Errors-in-variables in joint population pharmacokinetic/pharmacodynamic modeling.
Bennett, J; Wakefield, J, 2001
)
0.31

Dosage Studied

ExcerptRelevanceReference
" In the APTT, at concentrations below 5 micrograms/ml, r-hirudin showed a dose-response curve."( Experimental studies on a recombinant hirudin, CGP 39393.
Barrowcliffe, TW; Cesmeli, S; Gray, E; Thomas, DP; Watton, J, 1991
)
0.54
" and the prophylaxis regimen at this dosage level was therefore discontinued."( Direct thrombin inhibition with Rec-hirudin CGP 39393 as prophylaxis of thromboembolic complications after total hip replacement.
Close, P; Ekman, S; Eriksson, BI; Kälebo, P; Kerry, R; Lindbratt, S, 1994
)
0.55
" The study was originally carried out in order to make dosage recommendations."( Errors-in-variables in joint population pharmacokinetic/pharmacodynamic modeling.
Bennett, J; Wakefield, J, 2001
)
0.31
" DTIs have antiplatelet effects, anticoagulant action, and most do not bind to plasma proteins, thereby providing a more consistent dose-response effect than UFH."( Anticoagulation for acute coronary syndromes: from heparin to direct thrombin inhibitors.
Lepor, NE, 2007
)
0.34
" Empiric dosage adjustment and activated partial thromboplastin time (aPTT) monitoring in patients with moderate renal impairment are recommended, but supportive data are lacking."( Desirudin dosing and monitoring in moderate renal impairment.
Bertino, JS; Nafziger, AN, 2010
)
0.36
" Desirudin also offers the advantage of a fixed dosing regimen while being less immunogenic than unfractionated heparin."( Desirudin: a review of the pharmacology and clinical application for the prevention of deep vein thrombosis.
Avidan, MS; Graetz, TJ; Smith, JR; Tellor, BR, 2011
)
0.37
" We found no evidence of a procoagulant effect of C1 INH-nf when studied ex vivo at concentrations up to 10-fold higher than those achieved with clinical dosing in patients with HAE."( Effects of a plasma-derived C1 esterase inhibitor on hemostatic activation, clot formation, and thrombin generation.
Gelone, S; Levy, JH; Szlam, F, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1345816Human coagulation factor II, thrombin (S1: Chymotrypsin)1991Haemostasis, , Volume: 21 Suppl 1Structure-function and refolding studies of the thrombin-specific inhibitor hirudin.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (131)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (2.29)18.7374
1990's89 (67.94)18.2507
2000's24 (18.32)29.6817
2010's14 (10.69)24.3611
2020's1 (0.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials25 (18.38%)5.53%
Reviews18 (13.24%)6.00%
Case Studies5 (3.68%)4.05%
Observational0 (0.00%)0.25%
Other88 (64.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]