The Efficacy and Safety of Hirudin Plus Aspirin Versus Warfarin in the Secondary Prevention of Cardioembolic Stroke Due to Nonvalvular Atrial Fibrillation: a Prospective Cohort Study

To investigate the efficacy and safety of hirudin plus aspirin therapy compared with warfarin in the secondary prevention of cardioembolic stroke due to nonvalvular atrial fibrillation.

Start Date01 Jun 2014

Sponsor / Collaborator

Xijing Hospital

[+6]

NCT00913133 / CompletedPhase 4

Multi-Center Trial of Desirudin for the Prophylaxis of Thrombosis: an Alternative to Heparin-Based Anticoagulation (DESIR-ABLE)

The objective of this trial is to demonstrate the clinical utility of fixed-dose SC Desirudin for the prophylaxis of thrombosis as an alternative to heparin-based anticoagulation.

Start Date01 Mar 2010

Sponsor / Collaborator

Canyon Pharmaceuticals, Inc.

NL-OMON35683 / CompletedPhase 2

Canyon-I-Pilot Trial a dose-ranging study of bolus-only Desirudin in patients undergoing PCI - CANYON-PCI pilot study

Start Date04 Sep 2009

Sponsor / Collaborator

Canyon Pharmaceuticals, Inc.

100 Clinical Results associated with Desirudin Recombinant

100 Translational Medicine associated with Desirudin Recombinant

100 Patents (Medical) associated with Desirudin Recombinant

373

Literatures (Medical) associated with Desirudin Recombinant

01 Mar 2024·Proteins

Tyrosine phosphorylation of recombinant hirudin increases affinity to thrombin and antithrombotic activity

Article

Author: Volkova, Alina ; Semenyuk, Pavel

Abstract:

Thrombin is one of the key enzymes of the blood coagulation system and a promising target for the development of anticoagulants. One of the most specific natural thrombin inhibitors is hirudin, contained in the salivary glands of medicinal leeches. The medicinal use of recombinant hirudin is limited because of the lack of sulfation on Tyr63, resulting in a 10‐fold decrease in activity compared to native (sulfated) hirudin. In the present work, a set of hirudin derivatives was tested for affinity to thrombin: phospho‐Tyr63, Tyr63(carboxymethyl)Phe, and Tyr63Glu mutants, which mimic Tyr63 sulfation and Gln65Glu mutant and lysine‐succinylated hirudin, which enhance the overall negative charge of hirudin, as well as sulfo‐hirudin and desulfo‐hirudin as references. Using steered molecular dynamics simulations with subsequent umbrella sampling, phospho‐hirudin was shown to exhibit the highest affinity to thrombin among all hirudin analogs, including native sulfo‐hirudin; succinylated hirudin was also prospective. Phospho‐hirudin exhibited the highest antithrombotic activity in in vitro assay in human plasma. Taking into account the modern methods for obtaining phospho‐hirudin and succinylated hirudin, they are prospective as anticoagulants in clinical practice.

01 Jan 2023·Analytical biochemistry

LC-MS/MS method for determination of r-RGD-hirudin in human plasma and its application in pharmacokinetic study

Article

Author: Xiao, Li ; Peng, Ai ; Yang, Lin ; Xiang, Jin ; Yi, Xiaoqin

OBJECTIVE:

This study aimed to develop a simple, sensitive, and selective Liquid chromatography with a Mass spectroscopic method for simultaneous quantification of a recombinant bifunctional hirudin (r-RGD-Hirudin, Bifunctional Hirudin, BFH) in human plasma and verify its effectiveness.

METHODS:

The analytes and the internal standards from human plasma were extracted using the solid-phase extraction technique. The reconstituted samples were chromatographed on Waters C₁₈ column (BEH 50 × 2.1 mm, 1.7 μm) using a mixture of 0.1% formic acid/acetonitrile (85%/15%, v/v) with gradient elution as the initial mobile phase at a flow rate of 0.3 mL/min.

RESULTS:

The effectiveness of the proposed method was verified over the concentration range of 10-2000 ng/mL for r-RGD-Hirudin. A linear calibration curve was obtained. The precision and accuracy of BFH in the intra- and inter-day runs fell within the range of ±15% at LQC, GMQC, MQC and HQC concentrations. The extraction recoveries and matrix effect at two quality control (QC) levels for BFH were confirmed to conform to the relevant requirement.

CONCLUSION:

The proposed method was successfully adapted to examine the pharmacokinetics of BFH in 40 Chinese healthy volunteers, respectively.

01 Nov 2022·British journal of pharmacologyQ2 · MEDICINE

A novel oncotherapy strategy: Direct thrombin inhibitors suppress progression, dissemination and spontaneous metastasis in non‐small cell lung cancer

Q2 · MEDICINE

Article

Author: Wu, Mengfang ; Wang, Qi ; Yu, Min ; Ma, Yixin ; Zhao, Bing ; Wang, Huijie ; Yu, Jinchao ; Wang, Tianfa ; Li, Yaran ; Hu, Zhihuang ; Mo, Wei ; Zhang, Yanling ; Li, Tianyu ; Chen, Di

Background and Purpose:

Cancer cachexia and cancer‐associated thrombosis are potentially fatal outcomes of advanced cancer. Nevertheless, thrombin expression in non‐small cell lung cancer (NSCLC) primary tumour tissues and the association between prognosis of NSCLC patients remain largely unknown.

Experimental Approach:

Clinical pathological analysis was performed to determine the relationship between thrombin and tumour progression. Effects of r‐hirudin and direct thrombin inhibitor peptide (DTIP) on cancer progression were evaluated. Western blotting, immunohistochemistry, and immunofluorescence were used to explore the inhibition mechanism of r‐hirudin and DTIP. The therapeutic effect of the combination of DTIP and chemotherapy was determined.

Key Results:

Thrombin expression in NSCLC tissues was closely related to clinicopathological features and the prognosis of patients. Thrombin deficiency inhibited tumour progression. The novel thrombin inhibitors, r‐hirudin and DTIP, inhibited cell invasion and metastasis in vitro. They inhibited tumour growth and metastasis in orthotopic lung cancer model, inhibited cell invasion, and prolonged survival after injection of tumour cells via the tail vein. They also inhibited angiogenesis and spontaneous metastases from subcutaneously inoculated tumours. The promotion by thrombin of invasion and metastasis was abolished in PAR‐1‐deficient NSCLC cells. r‐hirudin and DTIP inhibited tumour progression through the thrombin‐PAR‐1‐mediated RhoA and NF‐κB signalling cascades via inhibiting MMP9 and IL6 expression. DTIP potentiated chemotherapy‐induced growth and metastatic inhibition and inhibited chemotherapy‐induced resistance in mice.

Conclusions and Implications:

Thrombin makes a substantial contribution, together with PAR‐1, to NSCLC malignancy. The anti‐coagulants, r‐hirudin and DTIP, could be used in anti‐tumour therapy and a combination of DTIP and chemotherapy might improve therapeutic effects.

News (Medical) associated with Desirudin Recombinant

24 Nov 2016

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Hybio Pharmaceutical Co., Ltd. 300199 Financial and Strategic SWOT Analysis Review Prices from USD $300

Summary Hybio Pharmaceutical Co., Ltd. Hybio is a biopharmaceutical company that develops polypeptide drugs. The company manufactures and develops peptide finished dosage products and peptide active pharmaceutical ingredients. Its finished dosage products include desmopressin for injection, terlipressin for injection, sodium ozagrel for injection, oxytocin for injection, omeprazole sodium for injection,and others. Hybio provides active pharmaceutical ingredients such as abarelix, calcitonin, copaxone, antide, desmopression, alarelin, bivalirudin, desirudin, elecatonin, fertirelin, ganadorelin, histrelin, leuprorelin, vapreotide and haxapeptide. The company conducts research and development to advance its products. Hybio is headquartered in Shenzhen, China. This comprehensive SWOT profile of Hybio Pharmaceutical Co., Ltd. provides you an indepth strategic analysis of the company's businesses and operations. The profile has been compiled by GlobalData to bring to you a clear and an unbiased view of the company's key strengths and weaknesses and the potential opportunities and threats. The profile helps you formulate strategies that augment your business by enabling you to understand your partners, customers and competitors better. This company report forms part of GlobalData's Profile on Demand' service, covering over 50,000 of the world's leading companies. Once purchased, GlobalData's highly qualified team of company analysts will comprehensively research and author a full financial and strategic analysis of Hybio Pharmaceutical Co., Ltd. including a detailed SWOT analysis, and deliver this direct to you in pdf format within two business days. excluding weekends. The profile contains critical company information including*, x000D x000D Business description A detailed description of the company's operations and business divisions.x000D Corporate strategy Analyst's summarization of the company's business strategy.x000D SWOT Analysis A detailed analysis of the company's strengths, weakness, opportunities and threats.x000D Company history Progression of key events associated with the company.x000D Major products and services A list of major products, services and brands of the company.x000D Key competitors A list of key competitors to the company.x000D Key employees A list of the key executives of the company.x000D Executive biographies A brief summary of the executives' employment history.x000D Key operational heads A list of personnel heading key departments/functions.x000D Important locations and subsidiaries A list and contact details of key locations and subsidiaries of the company.x000D Key manufacturing facilities A list of key manufacturing facilities of the company.x000D Detailed financial ratios for the past five years The latest financial ratios derived from the annual financial statements published by the company with 5 years history.x000D Interim ratios for the last five interim periods The latest financial ratios derived from the quarterly/semiannual financial statements published by the company for 5 interims history.x000D x000D Note*: Some sections may be missing if data is unavailable for the company. Key benefits of buying this profile include,x000D x000D You get detailed information about the company and its operations to identify potential customers and suppliers.x000D The profile analyzes the company's business structure, operations, major products and services, prospects, locations and subsidiaries, key executives and their biographies and key competitors.x000D x000D Understand and respond to your competitors' business structure and strategies, and capitalize on their weaknesses. Stay up to date on the major developments affecting the company.x000D The company's core strengths and weaknesses and areas of development or decline are analyzed and presented in the profile objectively. Recent developments in the company covered in the profile help you track important events. x000D x000D Equip yourself with information that enables you to sharpen your strategies and transform your operations profitably.x000D Opportunities that the company can explore and exploit are sized up and its growth potential assessed in the profile. Competitive and/or technological threats are highlighted.x000D x000D Scout for potential investments and acquisition targets, with detailed insight into the companies' strategic, financial and operational performance.x000D Financial ratio presented for major public companies in the profile include the revenue trends, profitability, growth, margins and returns, liquidity and leverage, financial position and efficiency ratios.x000D x000D Gain key insights into the company for academic or business research.x000D Key elements such as SWOT analysis, corporate strategy and financial ratios and charts are incorporated in the profile to assist your academic or business research needs.

Financial StatementAcquisition

100 Deals associated with Desirudin Recombinant

External Link

KEGG	Wiki	ATC	Drug Bank
-	Desirudin Recombinant	B01AE01	DB11095

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Venous Thrombosis	EU	Canyon Pharmaceuticals, Inc.	09 Jul 1997
Venous Thrombosis	IS	Canyon Pharmaceuticals, Inc.	09 Jul 1997
Venous Thrombosis	LI	Canyon Pharmaceuticals, Inc.	09 Jul 1997
Venous Thrombosis	NO	Canyon Pharmaceuticals, Inc.	09 Jul 1997

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00913133 (DESIR-ABLE, CTgov)	Phase 4	Thrombosis	516	Desirudin	ngiyqrcbxe(fhfytsmjgn) = tpyasmoemv hhtafyzxri (cmmxwrdzfn, mrjwjfcssa - osijsyajoz) View more	-	03 Jan 2013
NCT00787332 (HIT, CTgov)	Phase 4	Leriche Syndrome \| Heparin-induced thrombocytopenia \| Spastic Paraplegia 20, Autosomal Recessive	16	Desirudin or Argatroban® (Desirudin)	isqesylawe(kouuawhcba) = nnnbikjkmi uhvapheotq (keispmdmwx, ftyjohynbg - ywlaeohbeg) View more	-	31 Dec 2012
NCT00787332 (HIT, CTgov)	Phase 4		16	Desirudin or Argatroban® (Argatroban®)	isqesylawe(kouuawhcba) = zzwgcdubwr uhvapheotq (keispmdmwx, bgrcawkleo - djoeoduqbi) View more	-	31 Dec 2012
NCT00329433 (CTgov)	Phase 2/3	Venous Thrombosis	120	Heparin	tfxzurcayi(xrenvlvbtr) = dnawmhtzoe kdafkyiygt (uknlnqyrsr, eyfvvkfzzb - ydbbawsnmw) View more	-	13 Jun 2011

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