Ecarin clotting time (ECT) is currently developed for the specific monitoring of antithrombin drugs, such as hirudin, argatroban, and hirulog. Aqueous reagent and dry chemistry technology have become available for ECT monitoring of antithrombin agents. Currently, many heparinoids and heparinomimetic drugs are being developed. These agents activate heparin cofactor 11 (HCII) and primarily mediate their effects by inhibiting thrombin. Atthough the test is specific for antithrombin agents, heparin cofactor II-mediated thrombin inhibitors are capable of prolonging the ECT. In order to study the relative effects of some of these agents, ECT was measured in human plasma supplemented with PI-88 (a sutfated pentomanose ; Progen Industries Limited. Sydney, Australia), aprosulate, pentosan polysulfate, dermatan Sulfate, unfractionated heparin (UFH), and recombinant hirudin (r-hirtadin). All agents were supplemented to the citrited-pooled plasma prepared from 10 healthy volunteers at a graded dosage of 0 to 100 These techniques gave comparable results for all of the agents used (PI-88. r2 = 0.99; r-hirudin, r2= 0.98, UFH. r2 =0.98; dermatan sutfate, r2 = 0.95; aprosulate, r2 = 0.95; pentosan polysulfate, r2 = 0.94). The relative anticoagulant effects of various agents used on ECT varied widely, exhibiting their potency in the following order: r-hirudin = pentosan polysulfate > dermatan sulfate > PI-88 > aprosulate > UFH. The sensitivity of ECT was adjusted by varying the concentration of the ecarin reagent. The results suggest that HCIImediated inhibition of thrombin can be detected by using ECT reagents.

01 Jul 1999·Clinical and Applied Thrombosis/HemostasisQ4 · MEDICINE

Effects of Aprosulate, a Novel Synthetic Glycosaminoglycan, on Coagulation and Platelet Function Parameters: A Prospective, Randomized Phase I Study

Q4 · MEDICINE

Article

Author: Eckenberger, Peter ; Breddin, Hans K. ; Mörsdorf, Stefan ; Radziwon, Piotr ; Schenk, Joachim F.

In a phase I clinical trial the effect of the highly sulfated polyanion "Aprosulate" was studied in healthy volun teers using different coagulation and platelet function param eters. Eighteen healthy volunteers aged 21 to 30 years received two single subcutaneous doses of aprosulate (0.5 mg/kg body weight; 1.0 mg/kg body weight), or unfractionated heparin (Calciparin® 7,500 IU). The washout period between the dif ferent drugs/doses was at least 7 days. Coagulation and platelet function parameters (activated partial thromboplastin time, Heptest, fibrinogen, von Willebrand factor, ristocetin cofactor, platelet adhesion to siliconized glass, and platelet-induced thrombin generation time [a new method for measuring throm bin generation in platelet-rich plasma in the presence of plate lets]) were assessed during 24 hours after each injection. Aprosulate led to a significant and dose-dependent prolonga tion of activated partial thromboplastin time and Heptest. This effect lasted for 4 hours (activated partial thromboplastin time) to 8 hours (Heptest). Activated partial thromboplastin time was not prolonged after the injection of unfractionated heparin (7,500 IU). Fibrinogen, von Willebrand factor, and ristocetin cofactor remained unchanged with both drugs. Platelet induced thrombin generation time was slightly prolonged and platelet adhesion was slightly diminished up to 2 hours using 0.5 mg/kg aprosulate, and up to 4 hours using 1.0 mg/kg aprosulate while the platelet induced thrombin generation time system was not influenced by the subcutaneous injection (7,500 IU) of unfrac tionated heparin. Both drugs and doses were well tolerated. Plasma transaminase concentrations alanin aminotransferase and aspartate aminotransferase serum values were slightly in creased in some volunteers but returned to normal during or after the study (<4 weeks). Further clinical trials will have to establish whether aprosulate is an effective drug for the pro phylaxis of deep venous thrombosis.

01 Mar 1996·International angiology : a journal of the International Union of AngiologyQ3 · MEDICINE

Physical and pharmacologic manipulation of the vascular system as measured by the release of TFPI and other mediators of antithrombotic actions.

Q3 · MEDICINE

Article

Author: Jeske, W ; Fareed, J ; Hoppensteadt, D A ; Nicolaides, A N

Utilizing highly sensitive monoclonal based assays, we have measured various mediators of antithrombotic action including t-PA, prostacyclin and tissue factor pathway inhibitor (TFPI). To evaluate the pharmacologic stimulation of these mediators, blood from patients treated with heparin and low molecular weight heparin in (LMWH) at various dosages, group of patients treated with oral polydeoxyribonucleotide (defibrotide), a synthetic analogue of heparin, namely aprosulate (Luitpold Pharma, Munich, Germany) were analyzed for various vascular mediators. Similarly, to evaluate patients treated with physical modalities such as the sequential compression devices alone and sequential compression devices in combination with LMWHs were tested for these same parameters. Heparin produced a marked release of TFPI and t-PA after i.v. administration. After subcutaneous administration, a relatively smaller elevation of these parameters were seen. Several of the LMWHs produced varying effects on the release of TFPI and t-PA and the area under the curve after the s.c. injection was found to be much higher than i.v. administration. Defibrotide administration after i.v. and oral administration also resulted in a significant increase in the TFPI and t-PA antigen levels. However, the prostacyclin metabolite 6-keto-PGF1 alpha was much higher than the values obtained the heparins. Repeated administration of a hypersulfated heparin analogue produced marked increase in TFPI in both i.v. and s.c. studies. These results indicate that besides directly acting on plasmatic mediators, antithrombotic drugs are capable of releasing endogenous mediators of antithrombotic actions. Physical manipulation of the vascular system can also produce these effects. Thus, both physical and pharmacologic means can be used to produce an antithrombotic state to mediate their prophylactic and therapeutic effects.

100 Deals associated with Aprosulate sodium

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Thromboembolism	Phase 1	DE	American Regent, Inc.	-
Thromboembolism	Phase 1	-	Daiichi Sankyo Co., Ltd.	-
Thrombosis	Phase 1	DE	American Regent, Inc.	-
Thrombosis	Phase 1	-	Daiichi Sankyo Co., Ltd.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

Aprosulate sodium

Overview

Basic Info

Structure

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation