Apixaban: An oral anticoagulant having unique mechanism of action with better safety and efficacy profile

Za, Fazeel

doi:10.4103/2394-7438.182723

Cited by 7 publications

(8 citation statements)

References 2 publications

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“…Its main mechanism of action is through reversible inhibition of factor Xa. It specifically binds and inhibits both free and bound factor Xa which ultimately results in reduction in the levels of thrombin formation [75].…”

Section: Apixabanmentioning

confidence: 99%

“…Some of the important pharmacokinetic features of apixaban include 50% bioavailability, peak levels reached within 1–2 h, 87% bound to plasma proteins, 21 L volume of distribution, a half-life of 12 h, hepatic CYP450 metabolism, and 25% renal excretion [73,75,76]. Apixaban is mainly metabolized by CYP3A4 with minor contributions from CYP1A2, CYP2C8, CYP2C9, CYP2C19 and CYP2J2 isoenzymes [54].…”

Section: Apixabanmentioning

confidence: 99%

“…Apixaban is a substrate for p-gp and CYP450 enzymes (3A4) and thus caution should be exercised during concomitant administration of strong inducers and inhibitors of both metabolic pathways [50,75]. Strong inducers of CYP3A4 and p-gp such as rifampicin/rifampin, carbamazepine, phenytoin, and phenobarbital can reduce the plasma levels of apixaban and result in a decrease in its therapeutic effect.…”

Section: Apixabanmentioning

confidence: 99%

“…Strong inducers of CYP3A4 and p-gp such as rifampicin/rifampin, carbamazepine, phenytoin, and phenobarbital can reduce the plasma levels of apixaban and result in a decrease in its therapeutic effect. Conversely, strong inhibitors of CYP3A4 and p-gp such as ketoconazole, itraconazole, ritonavir, and clarithromycin can lead to supra-therapeutic levels of apixaban and excessive bleeding tendencies [50,75]. Moderate CYP3A4 and p-gp inhibitors such as erythromycin and clarithromycin can be co-administered with apixaban as their clinical impact is not clearly defined.…”

Section: Apixabanmentioning

confidence: 99%

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Pharmacogenomics of Novel Direct Oral Anticoagulants: Newly Identified Genes and Genetic Variants

Kanuri

Kreutz

2019

JPM

105

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Direct oral anticoagulants (DOAC) have shown an upward prescribing trend in recent years due to favorable pharmacokinetics and pharmacodynamics without requirement for routine coagulation monitoring. However, recent studies have documented inter-individual variability in plasma drug levels of DOACs. Pharmacogenomics of DOACs is a relatively new area of research. There is a need to understand the role of pharmacogenomics in the interpatient variability of the four most commonly prescribed DOACs, namely dabigatran, rivaroxaban, apixaban, and edoxaban. We performed an extensive search of recently published research articles including clinical trials and in-vitro studies in PubMed, particularly those focusing on genetic loci, single nucleotide polymorphisms (SNPs), and DNA polymorphisms, and their effect on inter-individual variation of DOACs. Additionally, we also focused on commonly associated drug-drug interactions of DOACs. CES1 and ABCB1 SNPs are the most common documented genetic variants that contribute to alteration in peak and trough levels of dabigatran with demonstrated clinical impact. ABCB1 SNPs are implicated in alteration of plasma drug levels of rivaroxaban and apixaban. Studies conducted with factor Xa, ABCB1, SLCOB1, CYP2C9, and VKORC1 genetic variants did not reveal any significant association with plasma drug levels of edoxaban. Pharmacokinetic drug-drug interactions of dabigatran are mainly mediated by p-glycoprotein. Strong inhibitors and inducers of CYP3A4 and p-glycoprotein should be avoided in patients treated with rivaroxaban, apixaban, and edoxaban. We conclude that some of the inter-individual variability of DOACs can be attributed to alteration of genetic variants of gene loci and drug-drug interactions. Future research should be focused on exploring new genetic variants, their effect, and molecular mechanisms that contribute to alteration of plasma levels of DOACs.

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Section: Apixabanmentioning

confidence: 99%

Section: Apixabanmentioning

confidence: 99%

Section: Apixabanmentioning

confidence: 99%

Section: Apixabanmentioning

confidence: 99%

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Pharmacogenomics of Novel Direct Oral Anticoagulants: Newly Identified Genes and Genetic Variants

Kanuri

Kreutz

2019

JPM

105

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“…Another problem arising in cancer is enhanced coagulation, leading to stroke and heart attacks, due to chemotherapy or disease progression. While aspirin can reduce coagulation, other compounds specifically designed to control clotting, such as apixaban (Eliquis), a factor Xa inhibitor developed to treat atrial fibrillation, 89 may be preferable as cancer progresses. Apixaban does not have the same effect on platelet interaction as warfarin and heparin and may thus be a safer alternative.…”

Section: Introductionmentioning

confidence: 99%

Repurposing approved drugs for cancer therapy

Schein

2021

British Medical Bulletin

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Background Many drugs approved for other indications can control the growth of tumor cells and limit adverse events (AE). Data sources Literature searches with keywords ‘repurposing and cancer’ books, websites: https://clinicaltrials.gov/, for drug structures: https://pubchem.ncbi.nlm.nih.gov/ Areas of agreement Introducing approved drugs, such as those developed to treat diabetes (Metformin) or inflammation (Thalidomide), identified to have cytostatic activity, can enhance chemotherapy or even replace more cytotoxic drugs. Also, anti-inflammatory compounds, cytokines and inhibitors of proteolysis can be used to control the side effects of chemo- and immuno-therapies or as second-line treatments for tumors resistant to kinase inhibitors (KI). Drugs specifically developed for cancer therapy, such as interferons (IFN), the tyrosine KI abivertinib TKI (tyrosine kinase inhibitor) and interleukin-6 (IL-6) receptor inhibitors, may help control symptoms of Covid-19. Areas of controversy Better knowledge of mechanisms of drug activities is essential for repurposing. Chemotherapies induce ER stress and enhance mutation rates and chromosome alterations, leading to resistance that cannot always be related to mutations in the target gene. Metformin, thalidomide and cytokines (IFN, tumor necrosis factor (TNF), interleukin-2 (IL-2) and others) have pleiomorphic activities, some of which can enhance tumorigenesis. The small and fragile patient pools available for clinical trials can cloud the data on the usefulness of cotreatments. Growing points Better understanding of drug metabolism and mechanisms should aid in repurposing drugs for primary, adjuvant and adjunct treatments. Areas timely for developing research Optimizing drug combinations, reducing cytotoxicity of chemotherapeutics and controlling associated inflammation.

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Synthesis and characterization of impurities of Apixaban drug substance—An anticoagulant

Satheesh

Sreenivasulu

Reddy

et al. 2022

Journal of Heterocyclic Chem

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Apixaban is an anticoagulant used to treat venous thromboembolic disorders. The present work describes the origin and synthesis of related substances of Apixaban PG ester‐1 and PG ester‐2. These impurities arise in the process of Apixaban drug substance, later these impurities are transformed into the final Apixaban drug substance. These novel synthesized impurities were characterized by 1H NMR, 13C NMR, HPLC, and HRMS analysis.

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Apixaban: An oral anticoagulant having unique mechanism of action with better safety and efficacy profile

Cited by 7 publications

References 2 publications

Pharmacogenomics of Novel Direct Oral Anticoagulants: Newly Identified Genes and Genetic Variants

Pharmacogenomics of Novel Direct Oral Anticoagulants: Newly Identified Genes and Genetic Variants

Repurposing approved drugs for cancer therapy

Synthesis and characterization of impurities of Apixaban drug substance—An anticoagulant

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