Thrombin inhib News - LARVOL Sigma

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|||||||||| [VIRTUAL] Combining Heparin with a FX/FXa Aptamer to Reduce Thrombin Generation in Models of Cardiopulmonary Bypass and COVID-19 Associated Coagulopathy (Room 3) - Jun 9, 2021 - Abstract #ISTH2021ISTH_380;
Similar anticoagulation and reduced thrombin generation was observed when blood from severely ill COVID-19 patients on heparin therapy was treated with 2μM 11F7t (Figure 2). Conclusions : This study demonstrates that combining UFH with a FX/Xa aptamer produces potent anticoagulation with reduced thrombin generation and has the potential to address CPB-associated AEs and has potential utility in other procoagulant settings such as CoAC.

|||||||||| [VIRTUAL] Polycationic Molecules Towards the Inhibition of Procoagulant and Antifibrinolytic Properties of Nucleic Acids (Room 3) - Jun 9, 2021 - Abstract #ISTH2021ISTH_371;
PNBIs also enhance the effectiveness of tPA-mediated clot lysis attributed to nucleic acids. Studies are ongoing to determine the efficacy of PNBIs in inhibiting thrombosis in relevant animal models.

|||||||||| desmopressin / Generic mfg.
[VIRTUAL] The FV East Texas Variant Causes Bleeding in a Three Generation Family from Indiana (Room 3) - Jun 9, 2021 - Abstract #ISTH2021ISTH_368;
Results : Over 13 years, a proband (male) presented with undiagnosed mild mucocutaneous bleeding symptoms, and significant post-surgical and post-traumatic hemorrhage, treated with rFVIIa due to failure of universal hemostatic agents including DDAVP and antifibrinolytics...Evaluation of rare bleeding disorders should include measurement of plasma TFPIα and DNA sequencing of FV B-domain. In vitro thrombin generation assays suggest that antibodies directed against the TFPI K2 domain, which are in development for hemophilia prophylaxis, may be therapeutically effective in FVET patients or others with mutations producing FVshort.

|||||||||| dabigatran etexilate / Generic mfg., apixaban / Generic mfg.
Clinical, Journal: Improved efficacy/safety profile of factor XIa inhibitor BMS-724296 versus factor Xa inhibitor apixaban and thrombin inhibitor dabigatran in cynomolgus monkeys. (Pubmed Central) - Jun 8, 2021
BMS-724296 produced similar antithrombotic efficacy as apixaban and dabigatran but with no increase in KBT in NHPs. These findings suggest that FXIa inhibitors may provide safe and effective antithrombotic therapy.

|||||||||| Journal: Quercetin Phytosome® as a potential drug for Covid-19. (Pubmed Central) - Jun 4, 2021
It has been also observed that the presence of specific glucuronidase could yield free systemic quercetin in human body. Taking also into considerations its anti-inflammatory and thrombin-inhibitory actions, a bioavailable form of quercetin, like Quercetin Phytosome®, should be considered a possible candidate to clinically face COVID-19.

|||||||||| Clinical, Journal: The relationship between insulin sensitivity and serum antithrombin 3 activity in patients with type 2 diabetes. (Pubmed Central) - Jun 3, 2021
Taking also into considerations its anti-inflammatory and thrombin-inhibitory actions, a bioavailable form of quercetin, like Quercetin Phytosome®, should be considered a possible candidate to clinically face COVID-19. Reduced basal and systemic insulin sensitivity are associated with decreased serum AT3 activity in patients with T2D.

|||||||||| aspirin / Generic mfg., argatroban / Generic mfg.
Journal: MicroRNA-126 is a regulator of platelet-supported thrombin generation. (Pubmed Central) - May 29, 2021
Finally, the plasma levels of miR-126, but not a control platelet-derived miRNA, correlated with markers of in vivo thrombin generation in a cohort of 185 cardiovascular patients. Our results from three complementary approaches support a key role for miR-126 in platelet-supported thrombin generation and open new avenues in the tailoring of antithrombotic treatment.

|||||||||| dabigatran etexilate / Generic mfg.
Review, Journal: Alzheimer's Disease-Rationales for Potential Treatment with the Thrombin Inhibitor Dabigatran. (Pubmed Central) - May 28, 2021
Beneficial effects of dabigatran on CAA and AD have recently been shown in preclinical studies and in retrospective observer studies on patients. Therefore, clinical studies are warranted, in order to possibly expand dabigatran approval for repositioning for AD treatment.

|||||||||| Preclinical, Review, Journal: Overview of the Therapeutic Potential of Aptamers Targeting Coagulation Factors. (Pubmed Central) - May 26, 2021
Although no aptamers targeting blood coagulation factors have been approved for clinical use, several aptamers have been evaluated in clinical trials and many more have demonstrated encouraging preclinical results. This review summarized our knowledge of the aptamers targeting proteins involved in coagulation, anticoagulation, fibrinolysis, their extensive applications as therapeutics and diagnostics tools, and the challenges they face for advancing to clinical use.

|||||||||| Journal: Iron-Deficiency and Estrogen Are Associated with Ischemic Stroke by Up-Regulating Transferrin to Induce Hypercoagulability. (Pubmed Central) - May 25, 2021
In contrast, anti-transferrin antibodies, transferrin knockdown, and peptide inhibitors of transferrin-thrombin/FXIIa interaction exerted anti-IS effects in vivo. Our findings revealed that certain factors (i.e., ID and CC) up-regulating transferrin are risk factors of thromboembolic diseases decipher a previously unrecognized mechanistic association among ID, CC and IS and provide a novel strategy for the development of anti-IS medicine by interfering with transferrin-thrombin/FXIIa interactions.

|||||||||| bivalirudin / Generic mfg.
Journal: Phenolic-amine chemistry mediated synergistic modification with polyphenols and thrombin inhibitor for combating the thrombosis and inflammation of cardiovascular stents. (Pubmed Central) - May 25, 2021
In this work, a plant-inspired phenolic-amine chemistry strategy was developed to combine the biological functions of a plant polyphenol, tannic acid (TA), and the thrombin inhibitor bivalirudin (BVLD) for tailoring the desired multiple surface functionalities of cardiovascular stents...Meanwhile, BVLD provided an antithrombogenic and endothelial-friendly microenvironment. As a result, the combined functions of the TA and BVLD facilitate the rapid stent re-endothelialization for reduced intimal hyperplasia in vivo, and may be a promising strategy to address the clinical complications associated with restenosis and late stent thrombosis.

|||||||||| dabigatran etexilate / Generic mfg.
Clinical, PK/PD data, Journal: Pharmacokinetic Modeling and Simulation Support for Age- and Weight-Adjusted Dosing of Dabigatran Etexilate in Children with Venous Thromboembolism. (Pubmed Central) - May 22, 2021
As a result, the combined functions of the TA and BVLD facilitate the rapid stent re-endothelialization for reduced intimal hyperplasia in vivo, and may be a promising strategy to address the clinical complications associated with restenosis and late stent thrombosis. Using a population PK model of DE for children with VTE, simulations showed that the final dosing algorithms were appropriate for all DE formulations; no dose titration was needed.

|||||||||| Clinical, Clinical data, Journal: Middle East Treatment Strategies and Clinical Outcomes in Patients with Atrial Fibrillation: One-Year Follow-up Data from Garfield-AF Study. (Pubmed Central) - May 22, 2021
P=N/A
We have found that rates of stroke and bleeding were lower, although mortality was higher, in the Middle East population. This paper describes the baseline characteristics, patterns of antithrombotic treatment and 1-year outcomes in Middle East AF patients.

|||||||||| dabigatran etexilate / Generic mfg.
Journal: The Research Progress of Direct Thrombin Inhibitors. (Pubmed Central) - May 20, 2021
The other part is derived from the design, synthesis and activity studies of small molecule inhibitors. This review discusses the progress of direct thrombin inhibitors in recent years.

|||||||||| Fanhdi (human plasma derived coagulation factor VIII) / Grifols
Journal: FVIII/VWF complex displays a greater pro-haemostatic activity than FVIII preparations devoid of VWF: Study in plasma and cell-based models. (Pubmed Central) - May 20, 2021
This review discusses the progress of direct thrombin inhibitors in recent years. The greater pro-haemostatic activity of FVIII/VWF complex, either in haemophilic plasma with inhibitor or in the presence of endothelial cells, may offer therapeutic advantages.

|||||||||| Journal: Molecular docking-assisted screening reveals tannic acid as a natural protein disulphide isomerase inhibitor with antiplatelet and antithrombotic activities. (Pubmed Central) - May 20, 2021
Therefore, we identified TA from natural polyphenols as a novel inhibitor of PDI function. TA inhibits platelet activation and thrombus formation, suggesting it as a potential antithrombotic agent.

|||||||||| argatroban / Generic mfg.
Journal: Early Identification of Argatroban Resistance and the Consideration of Factor VIII. (Pubmed Central) - May 15, 2021
This case supports early assessment of factor VIII levels and the consideration of argatroban resistance and in patients who have a subtherapeutic aPTT, despite multiple increases in dose with an elevated factor VIII level. Early identification should prompt the use of an alternative anticoagulant to ensure efficacy.

|||||||||| Savaysa (edoxaban) / Daiichi Sankyo
Journal: Unveiling the complex effects of direct oral anticoagulants on dilute Russell's viper venom time assays. (Pubmed Central) - May 15, 2021
The dRVVT ratios are unaffected for some reagents and this can be explained by an equal dose-dependent effect on both screen and confirm assays. The phospholipid type and content of the different reagents may contribute to the observed differences.

|||||||||| rivaroxaban / Generic mfg.
Preclinical, Journal: Effect of myeloperoxidase on the anticoagulant activity of low-molecular-weight heparin and rivaroxaban in an in-vitro tumor model. (Pubmed Central) - May 15, 2021
MPO release may partially attenuate the anticoagulant activity of trough levels of dalteparin and tinzaparin in the context of paraneoplastic leukocyte activation. However, this effect is likely not sufficient to explain the improved efficacy of rivaroxaban, and possibly other oral factor Xa inhibitors, in CAT treatment.

|||||||||| Journal: Paper Diagnostic for Direct Measurement of Fibrinogen Concentration in Whole Blood. (Pubmed Central) - May 15, 2021
Furthermore, diluting blood samples not only increases the test's sensitivity but also eliminates the effect of hematocrit and thrombin inhibitors. The test can be completed in 3-4 min, making it suitable for diagnosing early hypofibrinogenemia and allowing for fibrinogen replacement therapy in critically bleeding patients.

|||||||||| Journal: Skeletal muscle myosin and cardiac myosin attenuate heparin's antithrombin-dependent anticoagulant activity. (Pubmed Central) - May 15, 2021
In addition to the chain length, the type and extent of sulfation of glycosaminoglycans influenced the ability of skeletal muscle myosin to neutralize the polysaccharide's ability to enhance antithrombin's activity. In summary, these studies show that skeletal muscle myosin and cardiac myosin can influence antithrombin's anticoagulant activity against factor Xa and thrombin, implying that they may significantly influence the hemostatic balance involving bleeding versus clotting.

|||||||||| dabigatran etexilate / Generic mfg.
Journal: Introduction of a thrombin sensor based on its interaction with dabigatran as an oral direct thrombin inhibitor. (Pubmed Central) - May 15, 2021
The calibration plot was linear in the concentration range of 1 to 70 nM (R = 0.9992) by LSV technique with a detection limit of 0.3 nM. The applicability of the proposed sensor was evaluated by the determination of thrombin in human serum as a real sample.

|||||||||| argatroban / Generic mfg.
Clinical, Journal: Evaluating the safety and efficacy of argatroban locking solution in the prevention of the dysfunction of haemodialysis central venous catheters: a study protocol for a randomized controlled trial. (Pubmed Central) - May 15, 2021
At present, there is no clinical study of argatroban as a CVC lock solution. This study will explore the efficacy and safety of the argatroban as locking solution in the prevention of the dysfunction of HD CVCs to provide evidence for further research.

|||||||||| Journal: Development of MALDI MS peptide array for thrombin inhibitor screening. (Pubmed Central) - May 15, 2021
MALDI MS imaging results showed that the fractions of proanthocyanidins with the mean DP of 4.61-6.82 had good thrombin inhibitory activity and their half-maximal inhibitory concentration (IC) were below 10 μg/mL. Therefore, the developed peptide array is a reliable platform for the discovery of natural thrombin inhibitors.

|||||||||| Journal: Response to: Time frame for withholding direct thrombin inhibitor therapy before neurosurgery. (Pubmed Central) - May 14, 2021
Therefore, the developed peptide array is a reliable platform for the discovery of natural thrombin inhibitors. No abstract available

|||||||||| Journal: Time frame for withholding direct thrombin inhibitor therapy before neurosurgery. (Pubmed Central) - May 14, 2021
No abstract available No abstract available

|||||||||| Review, Journal: The Potency of Seaweed Sulfated Polysaccharides for the Correction of Hemostasis Disorders in COVID-19. (Pubmed Central) - May 14, 2021
The combination of the anticoagulant, thrombolytic, and fibrinolytic properties, along with low toxicity and relative cheapness of production, open up prospects for the clinical use of PSs as alternative sources of new anticoagulant and antithrombotic compounds. However, further investigation and clinical trials are needed to confirm their efficacy.

|||||||||| [VIRTUAL] Research of influence of virus inactivating agent on the activity of Thrombin () - May 12, 2021 - Abstract #BSH2021BSH_501;
The Thrombin activity recovered when removing them from the reaction mixture. These properties allow to effectively use these virus-activating reagents in one technological scheme of purification of plasma proteins using pre-fractionation and dye-ligand affinity chromatography on silica sorbents, which will significantly improve the safety of concentrate.

|||||||||| warfarin / Generic mfg., enoxaparin sodium / Generic mfg.
[VIRTUAL] Management of Spontaneous Intra-Cranial Haemorrhage whilst on a Direct Oral Anticoagulant is less well known than Warfarin () - May 12, 2021 - Abstract #BSH2021BSH_469;
Despite this, mortality was higher in those on Warfarin. Further work is required to educate clini- cians on the management of ICH in patients on DOACs and to encourage earlier, appropriate administration of PCC, Vitamin K and Idarucizumab.

|||||||||| [VIRTUAL] Abnormal serum protein electrophoretic pattern of patients with severe SARS-CoV-2 infection in the Intensive Care Unit reveals very high levels of dimeric form of alpha-2- macroglobulin () - May 12, 2021 - Abstract #BSH2021BSH_314;
Mass spectrometry evaluation is needed for confirm- ing this specific alteration, opening the case for having this test run as a routine in severely affected patients. We finally hypothesise that this notable A2M serum protein profile shift may explain, at least in part, the pro-thrombotic state seen in patients with severe COVID- 19 infection.

|||||||||| dabigatran etexilate / Generic mfg.
Journal: Dabigatran ameliorates airway smooth muscle remodeling in asthma by modulating Yes-associated protein. (Pubmed Central) - May 11, 2021
Mechanistically, thrombin promoted actin stress fibre polymerization through the PAR1/RhoA/ROCK/MLC2 axis to activate YAP and then interacted with SMAD2 in the nucleus to induce downstream target genes, ultimately aggravating HASMCs remodeling. Our study provides experimental evidence that dabigatran ameliorates airway smooth muscle remodeling in asthma by inhibiting YAP signalling, and dabigatran may have therapeutic potential for the treatment of asthma.

|||||||||| Journal: Regenerating Antithrombotic Surfaces through Nucleic Acid Displacement. (Pubmed Central) - May 11, 2021
The surface-bound ODNs inhibit thrombin activity to significantly reduce fibrinogen cleavage and fibrin formation, and this effect is sustained after ODN exchange of the surface-bound strands with a fresh antithrombotic payload. This study presents a unique strategy for achieving a continuous antithrombotic state for blood-contacting devices using an ODN-based regeneration method.

|||||||||| Heparin+AT+Thrombin making a trimolar complex exerts its anticoagulant effect. Hence, Heparin is an “Indirect Thrombin Inhibitor” as opposed to the “BANs” which are the DTIs. LMWH also binds AT but more inhibitory to Xa than Thrombin. Don’t check AT level while on Heparin. (Twitter) - May 8, 2021

|||||||||| argatroban / Generic mfg.
Clinical, Journal: Argatroban Increased the Basal Vein Drainage and Improved Outcomes in Acute Paraventricular Ischemic Stroke Patients. (Pubmed Central) - May 6, 2021
No difference was found in the incidence of adverse reactions between the 2 groups. CONCLUSIONS These observations indicate that vein drainage change may contribute to the acute phase of brain edema and the outcomes of ischemic stroke patients.

|||||||||| Journal: Salvia miltiorrhiza-derived miRNAs suppress vascular remodeling through regulating OTUD7B/KLF4/NMHC IIA axis. (Pubmed Central) - May 6, 2021
These results add important knowledge to the pharmacological actions and bioactive components of Salvia miltiorrhiza. Sal-miR-1 and 3-regulated OTUD7B/KLF4/NMHC IIA axis may represent a therapeutic target for vascular remodeling.

|||||||||| The recent ECATEM (using ecarin, ie similar to ecarin clotting time) tests for direct thrombin inhibitors If you want to use it for research, TEG is not very sensitive, so it can be a supporting technique but never the main technique (eg. LTA if you want to measure platelet Fx) (Twitter) - May 4, 2021

|||||||||| Review, Journal: Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review. (Pubmed Central) - May 4, 2021
Therefore, by collecting and summarizing publications from the recent two decades, the pharmacological activities, pharmacokinetics, novel preparations and derivatives, as well as toxicity of hirudin were systematically reviewed in this paper. In addition, the clinical application, the underlying mechanisms of pharmacological effects, the dose-effect relationship, and the development potential in new drug research of hirudin were discussed on the purpose of providing new ideas for application of hirudin in treating related diseases.

|||||||||| Review, Journal: Proton Bridging in Catalysis by and Inhibition of Serine Proteases of the Blood Cascade System. (Pubmed Central) - May 1, 2021
The principal conclusion of this review is that proton sharing at distances below the sum of van der Waals radii of the hydrogen and both donor and acceptor atoms contribute to the remarkable catalytic prowess of serine proteases of the blood clotting system and other enzymes that employ acid-base catalysis. Proton bridges also play a role in tight binding in proteins and at exosites, i.e., allosteric sites, of enzymes.

|||||||||| bivalirudin / Generic mfg.
Clinical, Review, Journal: Role of Bivalirudin for Anticoagulation in Adult Perioperative Cardiothoracic Practice. (Pubmed Central) - Apr 28, 2021
Through a triple mechanism of action-inhibition of plasma thrombin, clot bound thrombin, and collagen-induced platelet activation-bivalirudin may perform better than heparin by attenuating the immediate postoperative prothrombotic state and thus positively impacting the early coronary graft patency after off-pump coronary artery bypass grafting. Further studies are necessary to better evaluate this niche field and discover further applications for this unique anticoagulant.

|||||||||| Clinical, Journal, Real-world evidence: Real-World Direct Oral Anticoagulants Experience in Atrial Fibrillation: Falls Risk and Low Dose Anticoagulation are Predictive of both Bleeding and Stroke Risk. (Pubmed Central) - Apr 28, 2021
Low dose anticoagulation and falls risk are associated with increased bleeding and thrombotic risk demonstrating overlapping risk factors. Careful individualised patient risk assessment is still required as low dose anticoagulation is not without risks.

|||||||||| Journal: The pleiotropic effects of antithrombotic drugs in the metabolic-cardiovascular-neurodegenerative disease continuum: impact beyond reduced clotting. (Pubmed Central) - Apr 22, 2021
Overall, we attempt to provide an up-to-date comprehensive review of the less-recognized, beneficial molecular aspects of antithrombotic therapy beyond reduced thrombus formation. We also make a solid argument for the need of further mechanistic analysis of the pleiotropic effects of antithrombotic drugs in the future.

|||||||||| Review, Journal: Protease Nexin-1 in the Cardiovascular System: Wherefore Art Thou? (Pubmed Central) - Apr 20, 2021
Overall, PN-1 appears to serve as a "hand brake" for protease activities during cardiovascular remodeling. This review will thus highlight the role of PN-1 in the cardiovascular system and deliver a comprehensive assessment of its position among serpins.

|||||||||| argatroban / Generic mfg.
Clinical, Journal: Lung transplantation using argatroban in severe heparin-induced thrombocytopenia during extracorporeal membrane oxygenation: a case series. (Pubmed Central) - Apr 15, 2021
Argatroban was successfully used during lung transplant surgery in patients who developed HIT type II during ECMO support. Further studies on the feasibility and safety of lung transplantation using a direct thrombin inhibitor in patients with HIT during ECMO are required.

|||||||||| dabigatran etexilate / Generic mfg., apixaban / Generic mfg.
The German study used dabigatran which is a direct thrombin inhibitor and showed harm. Apixaban works through a different pathway (Xa inhibitor), which is more important in VADs. @bradbumm https://t.co/AfBooSRWlP (Twitter) - Apr 14, 2021

|||||||||| Zontivity (vorapaxar) / Merck (MSD)
Corey Tabit and @NirUrielMD showed that bleeding is associated with thrombin-induced Ang-2 expression and this expression can by reduced by inhibiting thrombin using Vorapaxar. Maybe in the future we will use a thrombin receptor antagonist instead of ASA. https://t.co/dd2sMbuTrt (Twitter) - Apr 14, 2021

|||||||||| argatroban / Generic mfg.
Review, Journal: Thrombin Inhibition by Argatroban: Potential Therapeutic Benefits in COVID-19. (Pubmed Central) - Apr 7, 2021
It also appears to lack a significant risk of drug-drug interactions with therapeutics currently being evaluated for COVID-19. Thus, argatroban presents a substantial promise in treating severe cases of COVID-19; however, this promise is yet to be established in randomized, controlled clinical trials.

|||||||||| warfarin / Generic mfg.
Review, Journal: Updates in Anticoagulation Therapy Monitoring. (Pubmed Central) - Apr 7, 2021
In the past six decades, heparin and warfarin were the primary anticoagulants prescribed for treatment and prophylaxis of venous thromboembolism worldwide...While this has perhaps streamlined the process for physicians and is often desirable for patients, it has also left a knowledge and resource gap in clinical scenarios for which urgent reversal and monitoring is necessary. An overview of the currently available anticoagulants with a focus on the guidelines and available tests for anticoagulant monitoring will be discussed in this article.

|||||||||| Journal: Stepwise Reversion of Multiply Mutated Recombinant Antitrypsin Reveals a Selective Inhibitor of Coagulation Factor XIa as Active as the M358R Variant. (Pubmed Central) - Apr 7, 2021
Structural modeling of the AAT-RC-2/FXIa encounter complex suggested that both E (Glu) substitutions at P3 and P3' may promote FXIa binding via hydrogen bonding to K192 in FXIa. AAT-RC-2 is the most selective and active AAT variant reported to date for FXIa inhibition and will be tested in animal models of thrombosis and bleeding.

|||||||||| Clinical, Review, Journal: COVID-19 and cardiovascular problems in elderly patients: Food for thought. (Pubmed Central) - Apr 7, 2021
This segment of the population will be a key issue and probably of primary interest to all. Biomarkers appear to be extremely useful as an indicator of what is happening from a pathophysiological point of view in the heart, allowing us to better stratify the prognosis of our patients affected by COVID-19, especially in the most severe cases and those with comorbidities.

|||||||||| dabigatran etexilate / Generic mfg.
Preclinical, Journal: The impact of dabigatran treatment on sinusoidal protection against hepatic ischemia-reperfusion injury in mice. (Pubmed Central) - Apr 1, 2021
In conclusion, thrombin exacerbated hepatic IRI, and excessive extracellular HMGB-1 caused severe inflammation- and apoptosis-induced liver damage. In this situation, dabigatran treatment improved vascular integrity via sinusoidal protection, and degraded HMGB-1 by endogenous TM enhancement on SECs, finally ameliorated hepatic IRI.



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