Dabigatran in cardiovascular disease management: A comprehensive review

Javed, Ayesha; Ajmal, Muhammad; Wolfson, A.M.

doi:10.4330/wjc.v13.i12.710

Cited by 7 publications

(3 citation statements)

References 49 publications

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“…Another ensemble model was built on all 11 models, which required testing on a smaller held-out test set due to the limited overlap of data. Evaluation metrics for all models are given in 84 Supporting Information Table S5 .…”

Section: Resultsmentioning

confidence: 99%

Insights into Drug Cardiotoxicity from Biological and Chemical Data: The First Public Classifiers for FDA Drug-Induced Cardiotoxicity Rank

Seal,

Spjuth,

Hosseini-Gerami

et al. 2024

J. Chem. Inf. Model.

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Drug-induced cardiotoxicity (DICT) is a major concern in drug development, accounting for 10−14% of postmarket withdrawals. In this study, we explored the capabilities of chemical and biological data to predict cardiotoxicity, using the recently released DICTrank data set from the United States FDA. We found that such data, including protein targets, especially those related to ion channels (e.g., hERG), physicochemical properties (e.g., electrotopological state), and peak concentration in plasma offer strong predictive ability for DICT. Compounds annotated with mechanisms of action such as cyclooxygenase inhibition could distinguish between mostconcern and no-concern DICT. Cell Painting features for ER stress discerned most-concern cardiotoxic from nontoxic compounds. Models based on physicochemical properties provided substantial predictive accuracy (AUCPR = 0.93). With the availability of omics data in the future, using biological data promises enhanced predictability and deeper mechanistic insights, paving the way for safer drug development. All models from this study are available at https://broad.io/DICTrank_Predictor.

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Section: Resultsmentioning

confidence: 99%

Insights into Drug Cardiotoxicity from Biological and Chemical Data: The First Public Classifiers for FDA Drug-Induced Cardiotoxicity Rank

Seal,

Spjuth,

Hosseini-Gerami

et al. 2024

J. Chem. Inf. Model.

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“…Since the thrombin antagonist dabigatran, which prevents blood clots and stroke in patients with atrial fibrillation, is a widely used anticoagulant [ 32 ], we tested the ability of rEcarin (0.16 mU/4 mL blood) to clot a patient’s blood who is prescribed dabigatron. The patient was on a dose of 100 mg of dabigatran with blood collected 5 h after the morning dose for a clotting assay twice a week ( Figure 5 A,B).…”

Section: Resultsmentioning

confidence: 99%

Potential Application of Recombinant Snake Prothrombin Activator Ecarin in Blood Diagnostics

et al. 2022

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We describe here the purification and cloning of a codon-optimized form of the snake prothrombin activator ecarin from the saw scaled viper (Echis carinatus) expressed in mammalian cells. Expression of recombinant ecarin (rEcarin) was carried out in human embryonic kidney cells (HEK) cells under conditions for the development and performance of a novel and scalable recombinant snake ecarin to industry standards. Clotting performance of the rEcarin was established in recalcified citrated whole blood, plasma, and fresh whole blood and found to be comparable to native ecarin (N-Ecarin). Furthermore, hemolysis was observed with N-Ecarin at relatively high doses in both recalcified citrated and fresh whole blood, while clotting was not observed with rEcarin, providing an important advantage for the recombinant form. In addition, rEcarin effectively clotted both recalcified citrated whole blood and fresh whole blood containing different anticoagulants including heparin, warfarin, dabigatran, Fondaparinux, rivaroxaban and apixaban, forming firm clots in the blood collection tubes. These results demonstrate that rEcarin efficiently clots normal blood as well as blood spiked with high concentrations of anticoagulants and has great potential as an additive to blood collection tubes to produce high quality serum for analyte analysis in diagnostic medicine.

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“…Der direkte orale Thrombininhibitor (DTI) Dabigatran-Etexilat befindet sich seit 2008 im klinischen Einsatz. Die initiale Zulassung erfolgte zur Antikoagulation bei Patienten mit nicht-valvulärem Vorhofflimmern sowie zur VTE-Prophylaxe im Rahmen der Implantation einer Knie- oder Hüft-Totalendoprothese (TEP); diese Zulassung wurde später auf die Therapie und Langzeitprophylaxe der tiefen Beinvenenthrombose und der Lungenembolie ausgeweitet 6 . Bei Patienten mit mechanischem Herzklappenersatz ist Dabigatran, ebenso wie alle anderen NOAK, kontraindiziert 7 .…”

Section: Nicht-vitamin K-abhängige Orale Antikoagulanzien (Noak)unclassified

Aktuelle Aspekte und Strategien zum Einsatz oraler Antikoagulantien und Plättchenfunktionshemmer in der Praxis

Sucker

Dörner

2022

Aktuelle Rheumatologie

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ZusammenfassungAufgrund erhöhter venöser und arterieller Risiken und Begleiterkrankungen bei entzündlich-rheumatischen Erkrankungen sind die Grundprinzipien der adäquaten medikamentösen Behandlung auch von Bedeutung in der rheumatologischen Praxis. Bei der oralen Antikoagulation haben die innovativen Nicht-Vitamin K-abhängigen oralen Antikoagulanzien (NOAK) die „klassischen“ Antikoagulanzien, die Vitamin K-Antagonisten (VKA), in vielen Indikationen weitgehend verdrängt; allerdings finden sich weiterhin Gründe, Patienten anstelle von NOAK mit VKA zu antikoagulieren. Bei der medikamentösen Hemmung der Plättchenfunktion werden neben ASS die Thienopyridine Clopidogrel und Prasugrel sowie Ticagrelor eingesetzt; von besonderer Bedeutung ist eine duale Plättchenfunktionshemmung (DAPT) mit Kombination verschiedener Plättchenhemmer. In dieser Übersichtsarbeit wird auf wichtige Aspekte der oralen Antikoagulation und der oralen Plättchenfunktionshemmung eingegangen.

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Dabigatran in cardiovascular disease management: A comprehensive review

Cited by 7 publications

References 49 publications

Insights into Drug Cardiotoxicity from Biological and Chemical Data: The First Public Classifiers for FDA Drug-Induced Cardiotoxicity Rank

Insights into Drug Cardiotoxicity from Biological and Chemical Data: The First Public Classifiers for FDA Drug-Induced Cardiotoxicity Rank

Potential Application of Recombinant Snake Prothrombin Activator Ecarin in Blood Diagnostics

Aktuelle Aspekte und Strategien zum Einsatz oraler Antikoagulantien und Plättchenfunktionshemmer in der Praxis

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