Pharmacokinetics and Pharmacogenetics of Apixaban

Savinova, A. V.; Добродеева, В. С.; Петрова, М. М.; Насырова, Р. Ф.; Shnayder, N. А.

doi:10.20996/1819-6446-2020-10-17

Cited by 5 publications

(4 citation statements)

References 58 publications

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“…By inhibiting factor Xa, apixaban reduces the formation of thrombin and the development of blood clots. It has no direct effect on platelet aggregation, but indirectly inhibits thrombin-induced platelet aggregation [ 64 ].…”

Section: Apixabanmentioning

confidence: 99%

“…It should be noted that the frequency of CYP3A5 gene SNVs’ carriership varies significantly depending on patients’ ethnicity. For example, most Europeans are not expressors, while many people of African descent are CYP3A5 expressors [ 64 , 75 ]. Higher concentrations of the active component of drugs, metabolized with participation of isoenzyme CYP3A5, in blood plasma are higher in non-expressors of CYP3A5 compared with expressors [ 76 ].…”

Section: Apixabanmentioning

confidence: 99%

See 1 more Smart Citation

Using Pharmacogenetics of Direct Oral Anticoagulants to Predict Changes in Their Pharmacokinetics and the Risk of Adverse Drug Reactions

et al. 2021

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Dabigatran, rivaroxaban, apixaban, and edoxaban are direct oral anticoagulants (DOACs) that are increasingly used worldwide. Taking into account their widespread use for the prevention of thromboembolism in cardiology, neurology, orthopedics, and coronavirus disease 2019 (COVID 19) as well as their different pharmacokinetics and pharmacogenetics dependence, it is critical to explore new opportunities for DOACs administration and predict their dosage when used as monotherapy or in combination with other drugs. In this review, we describe the details of the relative pharmacogenetics on the pharmacokinetics of DOACs as well as new data concerning the clinical characteristics that predetermine the needed dosage and the risk of adverse drug reactions (ADRs). The usefulness of genetic information before and shortly after the initiation of DOACs is also discussed. The reasons for particular attention to these issues are not only new genetic knowledge and genotyping possibilities, but also the risk of serious ADRs (primarily, gastrointestinal bleeding). Taking into account the effect of the carriership of single nucleotide variants (SNVs) of genes encoding biotransformation enzymes and DOACs metabolism, the use of these measures is important to predict changes in pharmacokinetics and the risk of ADRs in patients with a high risk of thromboembolism who receive anticoagulant therapy.

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Section: Apixabanmentioning

confidence: 99%

Section: Apixabanmentioning

confidence: 99%

Using Pharmacogenetics of Direct Oral Anticoagulants to Predict Changes in Their Pharmacokinetics and the Risk of Adverse Drug Reactions

et al. 2021

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show abstract

“…By inhibiting factor Xa, apixaban reduces formation of thrombin and development of blood clots. It has no direct effect on platelet aggregation, but indirectly inhibits thrombin-induced platelet aggregation [63].…”

Section: Apixabanmentioning

confidence: 99%

“…It should be noted that frequency of carriage of SNVs of CYP3A5 gene varies significantly depending on ethnicity of patients. For example, most Europeans are not expressors, while many people of African descent are CYP3A5 expressors [63,74]. Higher concentrations of active component of drugs, metabolized with participation of isoenzyme CYP3A5, in blood plasma are higher in non-expressors of CYP3A5 compared with expressors [75].…”

Section: Apixabanmentioning

confidence: 99%

Pharmacogenetics of Direct Oral Anticoagulants

Shnayder¹,

Петрова²,

Bochanova³

et al. 2021

Pharmacogenetics

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For more than 50 years, oral vitamin K antagonists were the choice of anticoagulant for the long-term treatment and prevention of arterial and venous thromboembolic events. In recent years, four direct oral anticoagulants (DOACs), dabigatran, rivaroxaban, apixaban and edoxaban have been compared with warfarin for thromboembolism prevention. These anticoagulants directly inhibit specific proteins within the coagulation cascade; in contrast, oral vitamin K antagonists inhibit the synthesis of vitamin K-dependent clotting factors. Dabigatran, a direct thrombin inhibitor, and rivaroxaban, apixaban and edoxaban, the factor Xa inhibitors, produce a more predictable, less labile anticoagulant effect. DOACs do not have limitations inherent vitamin K antagonists. DOACs have a predictable pharmacokinetic profile and are free of advers drugs reactions inherent in vitamin K antagonists. However, it is necessary to take into account the pharmacogenetic characteristics of the individual that can affect effectiveness and safety of use of DOACs. The results carried out to the present fundamental and clinical studies of DOACs studies demonstrate an undeniable the influence of genome changes on the pharmacokinetics and pharmacodynamics of DOACs. However, the studies need to be continued. There is a need to plan and conduct larger studies in various ethnic groups with the inclusion of sufficient associative genetic studies of the number of patients in each of the documented groups treatments with well-defined phenotypes.

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Anticoagulant therapy with apixaban based on a pharmacogenetic approach: a course to safety

Fedina,

Sychev,

Denisenko

et al. 2023

Medicinskij sovet

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For the past 60 years, vitamin K antagonists (VKAs) have been the main drugs used for long-term oral anticoagulant therapy. Because of the significant limitations of AVCs, direct-acting oral anticoagulants (DOAKs) have been developed over the past decade. DOAKs have a predictable pharmacokinetic profile and lack the disadvantages of vitamin K antagonists. Apixaban is an oral direct-acting factor Xa inhibitor used for the prevention of thromboembolic complications in patients with non-valvular atrial fibrillation (AF) and deep vein thrombosis. Despite the use of recommended dosages, some patients may still experience bleeding or lack the desired anticoagulant effect. With this in mind, it is critical to explore new uses for direct oral anticoagulants and to predict their dosage when used in monotherapy or in combination with other drugs. In addition, recent studies have documented individual variability in plasma POAC levels. DOAC pharmacogenetics is a relatively new area of research. There is a need to understand the role of pharmacogenetics in adapting anticoagulant therapy according to a patient’s genetic characteristics. In this scientific review of current data, we detail the pharmacokinetics and pharmacogenetics of apixaban as well as new data concerning the clinical characteristics that predetermine the necessary dosage and risk of adverse drug reactions (ADRs). Indeed, the results obtained to date from basic and clinical studies certainly indicate an undeniable influence of genomic changes on the pharmacokinetics of POACs.

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Pharmacokinetics and Pharmacogenetics of Apixaban

Cited by 5 publications

References 58 publications

Using Pharmacogenetics of Direct Oral Anticoagulants to Predict Changes in Their Pharmacokinetics and the Risk of Adverse Drug Reactions

Using Pharmacogenetics of Direct Oral Anticoagulants to Predict Changes in Their Pharmacokinetics and the Risk of Adverse Drug Reactions

Pharmacogenetics of Direct Oral Anticoagulants

Anticoagulant therapy with apixaban based on a pharmacogenetic approach: a course to safety

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