Rivaroxaban: Expanded Role in Cardiovascular Disease Management—A Literature Review

Ajmal, Muhammad; Friedman, Jacob; Sipra, Qurat Ul Ain Riaz; Lassar, Tom

doi:10.1155/2021/8886210

Cited by 20 publications

(15 citation statements)

References 79 publications

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Section: Results and Discussionmentioning

confidence: 99%

“…To demonstrate the synthetic potential of the developed dichromatic photocatalyzed transformation, this method was applied to the late-stage phosphonylation of rivaroxaban, an oral anticoagulant agent for the prevention and treatment of thromboembolic disorders. 56 Thus, the subsequent phosphonylated product (Table 2, entry 3o) was obtained in very good, isolated yields (70%). In addition, the model reaction was submitted at higher scales (from 0.05 to 1 mmol), producing a 66% isolated yield of 3a (86% GC yield) and under outdoor sunlight generating 3a after 8 h in an excellent 94% yield (see all details in the Supporting Information).…”

Section: T H Imentioning

confidence: 99%

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Highly Efficient Production of Heteroarene Phosphonates by Dichromatic Photoredox Catalysis

Herrera-Luna

Díaz

Jiménez

et al. 2021

ACS Appl. Mater. Interfaces

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A new strategy to achieve efficient aerobic phosphorylation of five-membered heteraroenes with excellent yields using dichromatic photoredox catalysis in a gel-based nanoreactor is described here. The procedure involves visible aerobic irradiation (cold white LEDs) of a mixture containing the heteroarene halide, trisubstituted phospite, N , N -diisopropylethylamine (DIPEA) as sacrificial agent, and catalytic amounts of 9,10-dicyanoanthracene ( DCA ) in the presence of an adequate gelator, which permits a faster process than at the homogeneous phase. The methodology, which operates by a consecutive photoinduced electron transfer (ConPET) mechanism, has been successfully applied to the straightforward and clean synthesis of a number of different heteroarene (furan, thiophene, selenophene, pyrrole, oxazole, or thioxazole) phosphonates, extending to the late-stage phosphonylation of the anticoagulant rivaroxaban. Strategically, employment of cold white light is critical since it provides both selective wavelengths for exciting first DCA (blue region) and subsequently its corresponding radical anion DCA •– (green region). The resultant strongly reducing excited agent DCA •– * is capable of even activate five-membered heteroarene halides (Br, Cl) with high reduction potentials (∼−2.7 V) to effect the C(sp 2 )–P bond formation. Spectroscopic and thermodynamic studies have supported the proposed reaction mechanism. Interestingly, the rate of product formation has been clearly enhanced in gel media because reactants can be presumably localized not only in the solvent pools but also through to the fibers of the viscoelastic gel network. This has been confirmed by field-emission scanning electron microscopy images where a marked densification of the network has been observed, modifying its fibrillary morphology. Finally, rheological measurements have shown the resistance of the gel network to the incorporation of the reactants and the formation of the desired products.

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Section: Results and Discussionmentioning

confidence: 99%

Section: T H Imentioning

confidence: 99%

Highly Efficient Production of Heteroarene Phosphonates by Dichromatic Photoredox Catalysis

Herrera-Luna

Díaz

Jiménez

et al. 2021

ACS Appl. Mater. Interfaces

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“…Nevertheless, moderate or minor bleeding of rivaroxaban still puzzles doctors, especially for patients with high bleeding risk. 12 , 13 Therefore, it is of scientific significance to develop new-generation anticoagulants with few or no bleeding side effects to improve the prevention and treatment of thrombotic diseases.…”

Section: Introductionmentioning

confidence: 99%

The Antithrombotic Effect of Recombinant Neorudin on Thrombi

Liu¹,

Zhang²,

Zhou³

et al. 2022

DDDT

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Introduction Recombinant neorudin (EPR-hirudin, EH) was developed through the addition of an EPR (Glu-Pro-Arg) peptide to the amino terminus of hirudin, which can be recognized and cut by coagulation factors XIa (FXIa) and/or Xa (FXa). In this study, the low-bleeding antithrombotic effects of EH were evaluated utilizing experimental models of thrombosis in rabbits and rats to provide a test basis for clinical trials. Methods The bleeding risks of EH and hirudin were first compared in mice by the tail-clipping method, and then the antithrombotic activity of EH was investigated in a rabbit model of arteriovenous bypass thrombosis and a rat model of thrombotic cerebral infarction. Results In mice, intravenous administration of EH at 1.5 mg/kg and 3 mg/kg did not affect the bleeding time compared with normal saline, while the administration of hirudin at 1.5 mg/kg prolonged the bleeding time by over 3 times the administration of normal saline. Furthermore, intravenous administration of EH had a significant dose-dependent inhibitory effect on the formation and development of arteriovenous bypass thrombosis and thrombotic cerebral infarction. Compared with an equimolar dose of hirudin, the antithrombotic effect of EH was similar, while the bleeding side effects were significantly attenuated. Moreover, when the antithrombotic effects were similar, EH had a shorter bleeding time and was associated with less bleeding than low molecular weight heparin (LMWH). EH had a therapeutic effect on thrombotic cerebral infarction without increasing the occurrence of cerebral hemorrhage. Conclusion The findings from the preclinical animal models used in this study showed that EH could not only effectively inhibit thrombus formation but also reduce the risk of bleeding.

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“…Rivaroxaban, a direct oral anticoagulant (DOAC), inhibits factors Ⅹa, thus preventing the blood clotting cascade and inhibiting thrombosis ( Ajmal et al, 2021 ). Rivaroxaban is used in clinical practice to treat venous thromboembolism after elective hip and knee arthroplasty ( Huang et al, 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Herb–Drug Interaction Between Danshen and Rivaroxaban in Rat and Human Liver Microsomes

Wang

Zhang

et al. 2022

Front. Pharmacol.

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The combination of Salvia miltiorrhiza (Danshen) and rivaroxaban is a promising treatment option in clinical practice in China, but the herb–drug interaction between Danshen and rivaroxaban remains unclear. Therefore, this study aims to reveal the interaction between Danshen and rivaroxaban. We not only investigated the inhibitory properties of Danshen tablet on rivaroxaban metabolism in rat and human liver microsomes but also evaluated the inhibitory effects of Danshen tablet and its eight active components (dihydrotanshinone I, tanshinone I, tanshinone IIA, cryptotanshinone, danshensu, salvianolic acid A, salvianolic acid B, and salvianolic acid C) on cytochrome P450 (CYP) enzymes. The results showed that Danshen tablet potently inhibited the metabolism of rivaroxaban in rat and human liver microsomes. In the CYP inhibition study, we found that dihydrotanshinone I, the active component of Danshen tablet, potently inhibited the activities of rat CYP3A and CYP2J, with IC50 values at 13.85 and 6.39 μM, respectively. In further inhibition kinetic study, we found that Danshen tablet is a mixed inhibitor in rivaroxaban metabolism in rat and human liver microsomes, with the Ki value at 0.72 and 0.25 mg/ml, respectively. In conclusion, there is a potential interaction between Danshen tablet and rivaroxaban. Danshen tablet inhibits the metabolism of rivaroxaban, which may be because its lipid-soluble components such as dihydrotanshinone I strongly inhibit the activities of CYP enzymes, especially CYP3A and CYP2J. Therefore, when Danshen tablet and rivaroxaban are used simultaneously in the clinic, it is necessary to strengthen the drug monitoring of rivaroxaban and adjust the dosage.

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Rivaroxaban: Expanded Role in Cardiovascular Disease Management—A Literature Review

Cited by 20 publications

References 79 publications

Highly Efficient Production of Heteroarene Phosphonates by Dichromatic Photoredox Catalysis

Highly Efficient Production of Heteroarene Phosphonates by Dichromatic Photoredox Catalysis

The Antithrombotic Effect of Recombinant Neorudin on Thrombi

Evaluation of Herb–Drug Interaction Between Danshen and Rivaroxaban in Rat and Human Liver Microsomes

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