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WARFARIN Drug Record

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  • Interactions
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  • WARFARIN chembl:CHEMBL1464 Approved

    Alternate Names:

    WARFARIN
    NSC-59813
    PANWARFIN
    4-HYDROXY-3-(3-OXO-1-PHENYLBUTYL)COUMARIN
    MAREVAN®
    ZOOCOUMARIN
    COUMAFENE
    COUMADIN®
    rxcui:11289
    chembl:CHEMBL1464
    pubchem.compound:54678486
    chemidplus:81-81-2
    drugbank:00682

    Drug Info:

    Year of Approval approved before 1982
    Drug Class anticoagulants
    Drug Categories rodenticides
    FDA Approval Approved before 1982
    Drug Class small molecule
    Drug Indications Anticoagulants
    Drug Categories compounds used in a research, industrial, or household setting
    Drug Categories cytochrome p-450 cyp1a2 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 cyp2c18 substrates
    Drug Categories cytochrome p-450 cyp2c18 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 cyp2c19 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2c19 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2c9 inducers
    Drug Categories cytochrome p-450 cyp2c9 inducers (weak)
    Drug Categories cytochrome p-450 cyp3a inducers
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inducers
    Drug Categories cytochrome p-450 cyp3a4 inducers (weak)
    Drug Categories cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 enzyme inducers
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories drugs that are mainly renally excreted
    Drug Categories drugs that are mainly renally excreted with narrow therapeutic index
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories narrow therapeutic index drugs
    Drug Categories vitamin k inhibitors
    (6 More Sources)

    Publications:

    Luo Z et al., 2017, Identification of novel variants associated with warfarin stable dosage by use of a two-stage extreme phenotype strategy., J Thromb Haemost
    An SH et al., 2015, Influence of UDP-Glucuronosyltransferase Polymorphisms on Stable Warfarin Doses in Patients with Mechanical Cardiac Valves., Cardiovasc Ther
    Bhatt DK et al., 2019, Age- and Genotype-Dependent Variability in the Protein Abundance and Activity of Six Major Uridine Diphosphate-Glucuronosyltransferases in Human Liver., Clin Pharmacol Ther
    Cavallari LH et al., 2010, Genetic and clinical predictors of warfarin dose requirements in African Americans., Clin Pharmacol Ther
    Zambon CF et al., 2011, VKORC1, CYP2C9 and CYP4F2 genetic-based algorithm for warfarin dosing: an Italian retrospective study., Pharmacogenomics
    Choi JR et al., 2011, Proposal of pharmacogenetics-based warfarin dosing algorithm in Korean patients., J Hum Genet
    Mandic D et al., 2015, VKORC1 gene polymorphisms and adverse events in Croatian patients on warfarin therapy., Int J Clin Pharmacol Ther
    Li et al., 2004, Identification of the gene for vitamin K epoxide reductase., Nature
    Limdi NA et al., 2008, Warfarin pharmacogenetics., Pharmacotherapy
    Mitchell C et al., 2011, Novel CYP2C9 and VKORC1 gene variants associated with warfarin dosage variability in the South African black population., Pharmacogenomics
    Kadian-Dodov DL et al., 2013, Warfarin pharmacogenetics: a controlled dose-response study in healthy subjects., Vasc Med
    Wypasek E et al., 2014, Genetic determinants of acenocoumarol and warfarin maintenance dose requirements in Slavic population: a potential role of CYP4F2 and GGCX polymorphisms., Thromb Res
    Gaikwad T et al., 2013, Influence of CYP2C9 and VKORC1 gene polymorphisms on warfarin dosage, over anticoagulation and other adverse outcomes in Indian population., Eur J Pharmacol
    Schwarz UI et al., 2006, Genetic determinants of dose and clinical outcomes in patients receiving oral anticoagulants., Clin Pharmacol Ther
    Lee KE et al., 2017, Influence of NR3C1 and VDR polymorphisms on stable warfarin dose in patients with mechanical cardiac valves., Int J Cardiol
    Nowak-Göttl U et al., 2010, In pediatric patients, age has more impact on dosing of vitamin K antagonists than VKORC1 or CYP2C9 genotypes., Blood
    Loebstein R et al., 2007, A coding VKORC1 Asp36Tyr polymorphism predisposes to warfarin resistance., Blood
    Wei M et al., 2012, A new algorithm to predict warfarin dose from polymorphisms of CYP4F2 , CYP2C9 and VKORC1 and clinical variables: derivation in Han Chinese patients with non valvular atrial fibrillation., Thromb Haemost
    Gage BF, 2006, Pharmacogenetics-based coumarin therapy., Hematology Am Soc Hematol Educ Program
    Sconce EA et al., 2006, Appraisal of current vitamin K dosing algorithms for the reversal of over-anticoagulation with warfarin: the need for a more tailored dosing regimen., Eur J Haematol
    Chan SL et al., 2012, Translational aspects of genetic factors in the prediction of drug response variability: a case study of warfarin pharmacogenomics in a multi-ethnic cohort from Asia., Pharmacogenomics J
    Liang R et al., 2012, Impact of CYP2C9*3, VKORC1-1639, CYP4F2rs2108622 genetic polymorphism and clinical factors on warfarin maintenance dose in Han-Chinese patients., J Thromb Thrombolysis
    Nakagita K et al., 2018, Effects of vitamin K epoxide reductase complex 1 gene polymorphisms on warfarin control in Japanese patients with left ventricular assist devices (LVAD)., Eur J Clin Pharmacol
    Shaw K et al., 2014, VKORC1 and CYP2C9 genotypes are predictors of warfarin-related outcomes in children., Pediatr Blood Cancer
    D'Andrea G et al., 2005, A polymorphism in the VKORC1 gene is associated with an interindividual variability in the dose-anticoagulant effect of warfarin., Blood
    Li S et al., 2015, Warfarin dosage response related pharmacogenetics in Chinese population., PLoS One
    Montes et al., 2006, The c.-1639G > A polymorphism of the VKORC1 gene is a major determinant of the response to acenocoumarol in anticoagulated patients., Br. J. Haematol.
    Pourgholi L et al., 2016, Gene polymorphisms and the risk of warfarin-induced bleeding complications at therapeutic international normalized ratio (INR)., Toxicol Appl Pharmacol
    Wakamiya T et al., 2016, Effect of VKORC1, CYP2C9, CFP4F2, and GGCX Gene Polymorphisms on Warfarin Dose in Japanese Pediatric Patients., Mol Diagn Ther
    Jeong E et al., 2015, Impact of GATA4 variants on stable warfarin doses in patients with prosthetic heart valves., Pharmacogenomics J
    Ferrari M et al., 2017, Assessing the relative potency of (S)- and (R)-warfarin with a new PK-PD model, in relation to VKORC1 genotypes., Eur J Clin Pharmacol
    Zhong SL et al., 2011, The influence of genetic polymorphisms and interacting drugs on initial response to warfarin in Chinese patients with heart valve replacement., Eur J Clin Pharmacol
    Tham LS et al., 2006, A warfarin-dosing model in Asians that uses single-nucleotide polymorphisms in vitamin K epoxide reductase complex and cytochrome P450 2C9., Clin Pharmacol Ther
    Veenstra DL et al., 2005, Association of Vitamin K epoxide reductase complex 1 (VKORC1) variants with warfarin dose in a Hong Kong Chinese patient population., Pharmacogenet Genomics
    Limdi NA et al., 2008, Influence of CYP2C9 and VKORC1 on warfarin dose, anticoagulation attainment and maintenance among European-Americans and African-Americans., Pharmacogenomics
    Krishna Kumar D et al., 2015, An acenocoumarol dosing algorithm exploiting clinical and genetic factors in South Indian (Dravidian) population., Eur J Clin Pharmacol
    de Oliveira Almeida VC et al., 2014, Polymorphisms of CYP2C9, VKORC1, MDR1, APOE and UGT1A1 genes and the therapeutic warfarin dose in Brazilian patients with thrombosis: a prospective cohort study., Mol Diagn Ther
    Stepien E et al., 2009, A vitamin K epoxide reductase-oxidase complex gene polymorphism (-1639G>A) and interindividual variability in the dose-effect of vitamin K antagonists., J Appl Genet
    Aquilante CL et al., 2006, Influence of coagulation factor, vitamin K epoxide reductase complex subunit 1, and cytochrome P450 2C9 gene polymorphisms on warfarin dose requirements., Clin Pharmacol Ther
    Anderson JL et al., 2007, Randomized trial of genotype-guided versus standard warfarin dosing in patients initiating oral anticoagulation., Circulation
    Mushiroda T et al., 2006, Association of VKORC1 and CYP2C9 polymorphisms with warfarin dose requirements in Japanese patients., J Hum Genet
    Bader L et al., 2020, The effect of genetic and nongenetic factors on warfarin dose variability in Qatari population., Pharmacogenomics J
    Yoshizawa M et al., 2009, Effect of VKORC1-1639 G>A polymorphism, body weight, age, and serum albumin alterations on warfarin response in Japanese patients., Thromb Res
    Kamali F, 2006, Genetic influences on the response to warfarin., Curr Opin Hematol
    Eriksson N et al., 2016, Genetic determinants of warfarin maintenance dose and time in therapeutic treatment range: a RE-LY genomics substudy., Pharmacogenomics
    Johnson JA et al., 2011, Clinical Pharmacogenetics Implementation Consortium Guidelines for CYP2C9 and VKORC1 genotypes and warfarin dosing., Clin Pharmacol Ther
    Fuchshuber-Moraes M et al., 2009, Exploring warfarin pharmacogenomics with the extreme-discordant-phenotype methodology: impact of FVII polymorphisms on stable anticoagulation with warfarin., Eur J Clin Pharmacol
    Zhang W et al., 2012, Genetic polymorphisms are associated with variations in warfarin maintenance dose in Han Chinese patients with venous thromboembolism., Pharmacogenomics
    Kimura R et al., 2006, Polymorphisms in vitamin K-dependent gamma-carboxylation-related genes influence interindividual variability in plasma protein C and protein S activities in the general population., Int J Hematol
    Cini M et al., 2012, A new warfarin dosing algorithm including VKORC1 3730 G > A polymorphism: comparison with results obtained by other published algorithms., Eur J Clin Pharmacol
    Cain D et al., 1998, Warfarin resistance is associated with a protein component of the vitamin K 2,3-epoxide reductase enzyme complex in rat liver., Thromb Haemost
    Caldwell MD et al., 2007, Evaluation of genetic factors for warfarin dose prediction., Clin Med Res
    Wadelius M et al., 2007, Pharmacogenetics of warfarin: current status and future challenges., Pharmacogenomics J
    Sandanaraj E et al., 2009, VKORC1 diplotype-derived dosing model to explain variability in warfarin dose requirements in Asian patients., Drug Metab Pharmacokinet
    Cho HJ et al., 2007, Factors affecting the interindividual variability of warfarin dose requirement in adult Korean patients., Pharmacogenomics
    Chung JE et al., 2015, Effects of NAD(P)H quinone oxidoreductase 1 polymorphisms on stable warfarin doses in Korean patients with mechanical cardiac valves., Eur J Clin Pharmacol
    de Oliveira Magalhães Mourão A et al., 2020, Algorithm for predicting low maintenance doses of warfarin using age and polymorphisms in genes CYP2C9 and VKORC1 in Brazilian subjects., Pharmacogenomics J
    Limdi NA et al., 2010, Warfarin pharmacogenetics: a single VKORC1 polymorphism is predictive of dose across 3 racial groups., Blood
    Osman et al., 2007, Plasma S/R ratio of warfarin co-varies with VKORC1 haplotype., Blood Coagul. Fibrinolysis
    Cavallari LH et al., 2011, Pharmacogenomics of warfarin dose requirements in Hispanics., Blood Cells Mol Dis
    Wadelius M et al., 2009, The largest prospective warfarin-treated cohort supports genetic forecasting., Blood
    Pathare A et al., 2012, Warfarin pharmacogenetics: development of a dosing algorithm for Omani patients., J Hum Genet
    Serna MJ et al., 2018, Pharmacogenetics of vitamin K antagonists and bleeding risk prediction in atrial fibrillation., Eur J Clin Invest
    Orsi FA et al., 2010, VKORC1 V66M mutation in African Brazilian patients resistant to oral anticoagulant therapy., Thromb Res
    Sermsathanasawadi N et al., 2015, The Influence of VKORC1 Polymorphisms on Warfarin Doses in Thai Patients with Deep Vein Thrombosis., J Med Assoc Thai
    Kosaki K et al., 2006, 1173C>T polymorphism in VKORC1 modulates the required warfarin dose., Pediatr Cardiol
    Zhang J et al., 2015, The influence of VKORC1 gene polymorphism on warfarin maintenance dosage in pediatric patients: A systematic review and meta-analysis., Thromb Res
    Zhao L et al., 2014, Verification of pharmacogenetics-based warfarin dosing algorithms in Han-Chinese patients undertaking mechanic heart valve replacement., PLoS One
    Santos PC et al., 2013, CYP2C9 and VKORC1 polymorphisms influence warfarin dose variability in patients on long-term anticoagulation., Eur J Clin Pharmacol
    Tang XY et al., 2017, The association between GGCX, miR-133 genetic polymorphisms and warfarin stable dosage in Han Chinese patients with mechanical heart valve replacement., J Clin Pharm Ther
    Maddison J et al., 2013, The pharmacokinetics and pharmacodynamics of single dose (R)- and (S)-warfarin administered separately and together: relationship to VKORC1 genotype., Br J Clin Pharmacol
    Özer M et al., 2013, Impact of genetic factors (CYP2C9, VKORC1 and CYP4F2) on warfarin dose requirement in the Turkish population., Basic Clin Pharmacol Toxicol
    Geisen C et al., 2005, VKORC1 haplotypes and their impact on the inter-individual and inter-ethnical variability of oral anticoagulation., Thromb Haemost
    Mega JL et al., 2015, Genetics and the clinical response to warfarin and edoxaban: findings from the randomised, double-blind ENGAGE AF-TIMI 48 trial., Lancet
    Nakai K et al., 2007, Ethnic differences in the VKORC1 gene polymorphism and an association with warfarin dosage requirements in cardiovascular surgery patients., Pharmacogenomics
    Nguyen N et al., 2013, Genetic and clinical determinants influencing warfarin dosing in children with heart disease., Pediatr Cardiol
    Zhu et al., 2007, Estimation of warfarin maintenance dose based on VKORC1 (-1639 G>A) and CYP2C9 genotypes., Clin. Chem.
    Cho HJ et al., 2011, Development and comparison of a warfarin-dosing algorithm for Korean patients with atrial fibrillation., Clin Ther
    Ozer N et al., 2010, The impact of CYP2C9 and VKORC1 genetic polymorphism and patient characteristics upon warfarin dose requirements in an adult Turkish population., Heart Vessels
    Ferder NS et al., 2010, Ability of VKORC1 and CYP2C9 to predict therapeutic warfarin dose during the initial weeks of therapy., J Thromb Haemost
    Michaud V et al., 2008, Combination of phenotype assessments and CYP2C9-VKORC1 polymorphisms in the determination of warfarin dose requirements in heavily medicated patients., Clin Pharmacol Ther
    Yuan HY et al., 2005, A novel functional VKORC1 promoter polymorphism is associated with inter-individual and inter-ethnic differences in warfarin sensitivity., Hum Mol Genet
    Ohno M et al., 2009, Influence of clinical and genetic factors on warfarin dose requirements among Japanese patients., Eur J Clin Pharmacol
    Lee CH et al., 2005, Venous thromboembolism: diagnosis and management of pulmonary embolism., Med J Aust
    Kimura R et al., 2007, Genotypes of vitamin K epoxide reductase, gamma-glutamyl carboxylase, and cytochrome P450 2C9 as determinants of daily warfarin dose in Japanese patients., Thromb Res
    Hamberg AK et al., 2010, A pharmacometric model describing the relationship between warfarin dose and INR response with respect to variations in CYP2C9, VKORC1, and age., Clin Pharmacol Ther
    Wadelius M et al., 2005, Common VKORC1 and GGCX polymorphisms associated with warfarin dose., Pharmacogenomics J
    Esmerian MO et al., 2011, Influence of CYP2C9 and VKORC1 polymorphisms on warfarin and acenocoumarol in a sample of Lebanese people., J Clin Pharmacol
    Carlquist JF et al., 2006, Genotypes of the cytochrome p450 isoform, CYP2C9, and the vitamin K epoxide reductase complex subunit 1 conjointly determine stable warfarin dose: a prospective study., J Thromb Thrombolysis
    Sridharan K et al., 2016, Association of Genetic Polymorphisms of CYP2C9 and VKORC1 with Bleeding Following Warfarin: A Case-Control Study., Curr Clin Pharmacol
    Valentín II et al., 2014, Pharmacogenetic association study of warfarin safety endpoints in Puerto Ricans., P R Health Sci J
    Vandell AG et al., 2017, Genetics and clinical response to warfarin and edoxaban in patients with venous thromboembolism., Heart
    Limdi et al., 2008, Influence of CYP2C9 and VKORC1 1173C/T genotype on the risk of hemorrhagic complications in African-American and European-American patients on warfarin., Clin. Pharmacol. Ther.
    Gebauer, 2007, Synthesis and structure-activity relationships of novel warfarin derivatives., Bioorg. Med. Chem.
    Wells PS et al., 2010, A regression model to predict warfarin dose from clinical variables and polymorphisms in CYP2C9, CYP4F2, and VKORC1: Derivation in a sample with predominantly a history of venous thromboembolism., Thromb Res
    Hawcutt DB et al., 2014, Pharmacogenetics of warfarin in a paediatric population: time in therapeutic range, initial and stable dosing and adverse effects., Pharmacogenomics J
    Rettie AE et al., 2006, The pharmocogenomics of warfarin: closing in on personalized medicine., Mol Interv
    Sconce EA et al., 2005, The impact of CYP2C9 and VKORC1 genetic polymorphism and patient characteristics upon warfarin dose requirements: proposal for a new dosing regimen., Blood
    Shikata E et al., 2006, Multiple gene polymorphisms and warfarin sensitivity., Eur J Clin Pharmacol
    Schelleman H et al., 2007, Warfarin response and vitamin K epoxide reductase complex 1 in African Americans and Caucasians., Clin Pharmacol Ther
    Pavani A et al., 2014, Methodological issues in the development of a pharmacogenomic algorithm for warfarin dosing: comparison of two regression approaches., Pharmacogenomics
    Montes R et al., 2008, The influence of polymorphisms of VKORC1 and CYP2C9 on major gastrointestinal bleeding risk in anticoagulated patients., Br J Haematol
    Higashi MK et al., 2002, Association between CYP2C9 genetic variants and anticoagulation-related outcomes during warfarin therapy., JAMA
    Takahashi H et al., 2003, Pharmacogenetics of CYP2C9 and interindividual variability in anticoagulant response to warfarin., Pharmacogenomics J
    Cha PC et al., 2010, Genome-wide association study identifies genetic determinants of warfarin responsiveness for Japanese., Hum Mol Genet
    Zambon CF et al., 2018, Pharmacokinetic and pharmacodynamic re-evaluation of a genetic-guided warfarin trial., Eur J Clin Pharmacol
    Jiménez-Varo E et al., 2014, Pharmacogenetics role in the safety of acenocoumarol therapy., Thromb Haemost
    Moon HW et al., 2011, The effect of CYP2C9, VKORC1 genotypes and old age on warfarin pharmacologic sensitivity in korean patients with thromboembolic disease., Ann Clin Lab Sci
    Huang SW et al., 2009, Validation of VKORC1 and CYP2C9 genotypes on interindividual warfarin maintenance dose: a prospective study in Chinese patients., Pharmacogenet Genomics
    You JH et al., 2011, Warfarin dosing algorithm using clinical, demographic and pharmacogenetic data from Chinese patients., J Thromb Thrombolysis
    Pautas E et al., 2010, Genetic factors (VKORC1, CYP2C9, EPHX1, and CYP4F2) are predictor variables for warfarin response in very elderly, frail inpatients., Clin Pharmacol Ther
    Lund K et al., 2012, Polymorphisms in VKORC1 have more impact than CYP2C9 polymorphisms on early warfarin International Normalized Ratio control and bleeding rates., Br J Haematol
    Limdi NA et al., 2009, Influence of CYP2C9 and VKORC1 on warfarin response during initiation of therapy., Blood Cells Mol Dis
    Stehle S et al., 2008, Pharmacogenetics of oral anticoagulants: a basis for dose individualization., Clin Pharmacokinet
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Obayashi K et al., 2006, VKORC1 gene variations are the major contributors of variation in warfarin dose in Japanese patients., Clin Pharmacol Ther
    Meckley LM et al., 2008, An analysis of the relative effects of VKORC1 and CYP2C9 variants on anticoagulation related outcomes in warfarin-treated patients., Thromb Haemost
    Tomek A et al., 2013, The bleeding risk during warfarin therapy is associated with the number of variant alleles of CYP2C9 and VKORC1 genes., Cardiology
    Pavani A et al., 2012, Retrospective evidence for clinical validity of expanded genetic model in warfarin dose optimization in a South Indian population., Pharmacogenomics
    Skov J et al., 2013, The influence of VKORC1 and CYP2C9 gene sequence variants on the stability of maintenance phase warfarin treatment., Thromb Res
    Biss TT et al., 2012, VKORC1 and CYP2C9 genotype and patient characteristics explain a large proportion of the variability in warfarin dose requirement among children., Blood
    Shahabi P et al., 2016, An expanded pharmacogenomics warfarin dosing table with utility in generalised dosing guidance., Thromb Haemost
    Kawai VK et al., 2014, Genotype and risk of major bleeding during warfarin treatment., Pharmacogenomics
    Sconce EA et al., 2006, APOE genotype makes a small contribution to warfarin dose requirements., Pharmacogenet Genomics
    Giansante C et al., 2012, Oral anticoagulation and VKORC1 polymorphism in patients with a mechanical heart prosthesis: a 6-year follow-up., J Thromb Thrombolysis
    Krishna Kumar D et al., 2014, Effect of CYP2C9, VKORC1, CYP4F2 and GGCX genetic variants on warfarin maintenance dose and explicating a new pharmacogenetic algorithm in South Indian population., Eur J Clin Pharmacol
    Wang LS et al., 2013, Influence of ORM1 polymorphisms on the maintenance stable warfarin dosage., Eur J Clin Pharmacol
    Wadelius M et al., 2004, Warfarin sensitivity related to CYP2C9, CYP3A5, ABCB1 (MDR1) and other factors., Pharmacogenomics J
    Rost S et al., 2004, Mutations in VKORC1 cause warfarin resistance and multiple coagulation factor deficiency type 2., Nature
    Ma C et al., 2012, Influence of warfarin dose-associated genotypes on the risk of hemorrhagic complications in Chinese patients on warfarin., Int J Hematol
    Tan SL et al., 2013, Cytochrome P450 oxidoreductase genetic polymorphisms A503V and rs2868177 do not significantly affect warfarin stable dosage in Han-Chinese patients with mechanical heart valve replacement., Eur J Clin Pharmacol
    Kim HS et al., 2009, Effect of CYP2C9 and VKORC1 genotypes on early-phase and steady-state warfarin dosing in Korean patients with mechanical heart valve replacement., Pharmacogenet Genomics
    Gaikwad T et al., 2018, Warfarin Dose Model for the Prediction of Stable Maintenance Dose in Indian Patients., Clin Appl Thromb Hemost
    Vecsler M et al., 2006, Combined genetic profiles of components and regulators of the vitamin K-dependent gamma-carboxylation system affect individual sensitivity to warfarin., Thromb Haemost
    Šupe S et al., 2015, Clinical Application of Genotype-guided Dosing of Warfarin in Patients with Acute Stroke., Arch Med Res
    Chung JE et al., 2018, Polymorphisms of vitamin K-related genes (EPHX1 and VKORC1L1) and stable warfarin doses., Gene
    Bryk AH et al., 2018, Bleeding predictors in patients following venous thromboembolism treated with vitamin K antagonists: Association with increased number of single nucleotide polymorphisms., Vascul Pharmacol
    Brehm K et al., 2013, Mechanical heart valve recipients: anticoagulation in patients with genetic variations of phenprocoumon metabolism., Eur J Cardiothorac Surg
    Hamberg AK et al., 2014, Characterizing variability in warfarin dose requirements in children using modelling and simulation., Br J Clin Pharmacol
    Yang J et al., 2011, Contribution of 1173C > T polymorphism in the VKORC1 gene to warfarin dose requirements in Han Chinese patients receiving anticoagulation., Int J Clin Pharmacol Ther
    Li T et al., 2006, Polymorphisms in the VKORC1 gene are strongly associated with warfarin dosage requirements in patients receiving anticoagulation., J Med Genet
    Misasi S et al., 2016, VKORC1 and CYP2C9 polymorphisms related to adverse events in case-control cohort of anticoagulated patients., Medicine (Baltimore)
    McMillin GA et al., 2010, Gene-based warfarin dosing compared with standard of care practices in an orthopedic surgery population: a prospective, parallel cohort study., Ther Drug Monit
    Lal et al., 2006, Pharmacogenetics of target genes across the warfarin pharmacological pathway., Clin Pharmacokinet
    Ho WK et al., 2005, Venous thromboembolism: diagnosis and management of deep venous thrombosis., Med J Aust
    Gage BF et al., 2008, Pharmacogenetics of warfarin: regulatory, scientific, and clinical issues., J Thromb Thrombolysis
    Schalekamp et al., 2006, VKORC1 and CYP2C9 genotypes and acenocoumarol anticoagulation status: interaction between both genotypes affects overanticoagulation., Clin. Pharmacol. Ther.
    Rieder MJ et al., 2005, Effect of VKORC1 haplotypes on transcriptional regulation and warfarin dose., N Engl J Med
    Herman D et al., 2006, The influence of sequence variations in factor VII, gamma-glutamyl carboxylase and vitamin K epoxide reductase complex genes on warfarin dose requirement., Thromb Haemost
    Kato Y et al., 2011, Effect of the VKORC1 genotype on warfarin dose requirements in Japanese pediatric patients., Drug Metab Pharmacokinet
    Shahabi P et al., 2019, Nuclear receptor gene polymorphisms and warfarin dose requirements in the Quebec Warfarin Cohort., Pharmacogenomics J
    Gao L et al., 2011, Extremely low warfarin dose in patients with genotypes of CYP2C9*3/*3 and VKORC1-1639A/A., Chin Med J (Engl)
    Bodin et al., 2005, Cytochrome P450 2C9 (CYP2C9) and vitamin K epoxide reductase (VKORC1) genotypes as determinants of acenocoumarol sensitivity., Blood
    Margaglione M et al., 2000, Genetic modulation of oral anticoagulation with warfarin., Thromb Haemost
    Lee KE et al., 2012, Effects of CYP4F2 gene polymorphisms on warfarin clearance and sensitivity in Korean patients with mechanical cardiac valves., Ther Drug Monit
    Yin et al., 2007, Warfarin dose and the pharmacogenomics of CYP2C9 and VKORC1 - rationale and perspectives., Thromb. Res.
    D'Andrea G et al., 2008, Oral anticoagulants: Pharmacogenetics Relationship between genetic and non-genetic factors., Blood Rev
    Gan GG et al., 2011, Contribution of VKORC1 and CYP2C9 polymorphisms in the interethnic variability of warfarin dose in Malaysian populations., Ann Hematol
    Nutescu EA, 2004, Emerging options in the treatment of venous thromboembolism., Am J Health Syst Pharm
    Biss TT et al., 2013, The VKORC1 and CYP2C9 genotypes are associated with over-anticoagulation during initiation of warfarin therapy in children., J Thromb Haemost
    Yang J et al., 2013, Influence of CYP2C9 and VKORC1 genotypes on the risk of hemorrhagic complications in warfarin-treated patients: a systematic review and meta-analysis., Int J Cardiol
    Oner Ozgon G et al., 2008, VKORC1 and CYP2C9 polymorphisms are associated with warfarin dose requirements in Turkish patients., Eur J Clin Pharmacol
    Wienkers LC et al., 1996, Formation of (R)-8-hydroxywarfarin in human liver microsomes. A new metabolic marker for the (S)-mephenytoin hydroxylase, P4502C19., Drug Metab Dispos
    Lilja JJ et al., 2007, Effects of daily ingestion of cranberry juice on the pharmacokinetics of warfarin, tizanidine, and midazolam--probes of CYP2C9, CYP1A2, and CYP3A4., Clin Pharmacol Ther
    Zhang Z et al., 1995, Human cytochromes P4501A1 and P4501A2: R-warfarin metabolism as a probe., Drug Metab Dispos
    Zhang JE et al., 2017, Effect of Genetic Variability in the <i>CYP4F2</i>, <i>CYP4F11</i>, and <i>CYP4F12</i> Genes on Liver mRNA Levels and Warfarin Response., Front Pharmacol
    Moon JY et al., 2015, Combined effects of hepatocyte nuclear factor 4α and constitutive androstane receptor on stable warfarin doses., Pharmacogenet Genomics
    Byrne et al., 2004, Warfarin skin necrosis associated with protein S deficiency and a mutation in the methylenetetrahydrofolate reductase gene., Clin. Exp. Dermatol.
    Kudo et al., 1998, Evidence for modulation of osteocalcin containing gamma-carboxyglutamic acid residues synthesis by insulin-like growth factor-I and vitamin K2 in human osteosarcoma cell line MG-63., Eur. J. Endocrinol.
    Tavares LC et al., 2018, Association Between <i>ABCB1</i> Polymorphism and Stable Warfarin Dose Requirements in Brazilian Patients., Front Pharmacol
    Thorarensen A et al., 2007, Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor., Bioorg Med Chem Lett
    An SH et al., 2014, Association of gene polymorphisms with the risk of warfarin bleeding complications at therapeutic INR in patients with mechanical cardiac valves., J Clin Pharm Ther
    Rettie et al., 1985, Stereoselective and regioselective hydroxylation of warfarin and selective O-dealkylation of phenoxazone ethers in human placenta., Biochem. Biophys. Res. Commun.
    Cavallari LH et al., 2011, Association of apolipoprotein E genotype with duration of time to achieve a stable warfarin dose in African-American patients., Pharmacotherapy
    Ngui JS et al., 2001, In vitro stimulation of warfarin metabolism by quinidine: increases in the formation of 4'- and 10-hydroxywarfarin., Drug Metab Dispos
    Nagai et al., 2005, Gas6 induces Akt/mTOR-mediated mesangial hypertrophy in diabetic nephropathy., Kidney Int.
    Lip et al., 1995, Increased markers of thrombogenesis in chronic atrial fibrillation: effects of warfarin treatment., Br Heart J
    Siguret et al., 2004, [Cytochrome P450 2C9 polymorphisms (CYP2C9) and warfarin maintenance dose in elderly patients]., Rev Med Interne
    Jorgensen AL et al., 2009, Genetic and environmental factors determining clinical outcomes and cost of warfarin therapy: a prospective study., Pharmacogenet Genomics
    Lane S et al., 2012, The population pharmacokinetics of R- and S-warfarin: effect of genetic and clinical factors., Br J Clin Pharmacol
    Liang Y et al., 2013, Association of genetic polymorphisms with warfarin dose requirements in Chinese patients., Genet Test Mol Biomarkers
    Chang M et al., 2015, CYP2C19*17 affects R-warfarin plasma clearance and warfarin INR/dose ratio in patients on stable warfarin maintenance therapy., Eur J Clin Pharmacol
    Zhang H et al., 2016, Impact of CYP2C19 gene polymorphism on warfarin maintenance doses in patients with non-valvular atrial fibrillation., Gene
    Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
    Rulcova A et al., 2010, Stereoselective interactions of warfarin enantiomers with the pregnane X nuclear receptor in gene regulation of major drug-metabolizing cytochrome P450 enzymes., J Thromb Haemost
  • WARFARIN   VKORC1

    Interaction Score: 23.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Specific Action of the Ligand Inhibition

    PMIDs:
    20072124 21174619 21326313 26445138 14765195 18752379 21635147 24029542 25042728 23602689 16815312 28262345 20833980 17110455 22534826 17124101 17042764 21383771 22528326 29781049 24474498 15358623 25594941 16611310 27581200 27262824 25026456 28382498 21318593 17015052 16141794 18466099 25519826 25312789 19875892 16580898 17989110 16432637 31653973 19135231 16888441 27488176 21900891 19387626 22248286 17189218 22349464 9684798 17456829 16983400 19745563 17391071 26257249 31395958 20203262 17413769 21185752 18574025 22854539 29577257 20615525 26219158 17031720 26433837 24728385 22990331 28429387 22616655 23061746 16270629 25769357 18240904 23183958 17510308 21981797 20339978 19874474 18030307 15888487 26223945 19582440 15938684 17049586 20410877 15883587 21148049 17111199 26777610 25244877 28689179 17653141 17275317 20421126 25001883 16960144 15947090 16821005 17329985 25084205 18950464 11926893 12931134 20833655 29396738 24919870 22075505 19177029 20585834 19794411 22571356 19297219 18698879 11752352 16890578 18690342 23774101 22676192 23159229 22010099 27121899 25521356 16847429 22592842 24019055 23208322 14676821 14765194 23104259 23949431 19077919 28049362 16493479 25989350 29054760 29432897 23423913 24330000 21176721 16611750 28033245 20386359 17112295 15865594 17906972 16815313 15930419 16676068 21273734 29298995 22040439 15790782 11127854 22549502 17161452 18234403 21110192 15597574 23279643 23932037 18542936


    Sources:
    TEND FDA PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • WARFARIN   NEDD4

    Interaction Score: 3.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27488176


    Sources:
    PharmGKB

  • WARFARIN   VKORC1L1

    Interaction Score: 3.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    29054760


    Sources:
    TEND PharmGKB TdgClinicalTrial

  • WARFARIN   DDHD1

    Interaction Score: 3.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27488176


    Sources:
    PharmGKB

  • WARFARIN   CYP4F11

    Interaction Score: 3.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28620303


    Sources:
    PharmGKB

  • WARFARIN   STX1B

    Interaction Score: 3.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27740732


    Sources:
    PharmGKB

  • WARFARIN   GAS6

    Interaction Score: 1.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16014032


    Sources:
    NCI

  • WARFARIN   ASPH

    Interaction Score: 1.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27488176


    Sources:
    PharmGKB

  • WARFARIN   PRSS53

    Interaction Score: 1.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • WARFARIN   GATA4

    Interaction Score: 0.92

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25026456 29298995


    Sources:
    PharmGKB

  • WARFARIN   STX4

    Interaction Score: 0.77

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • WARFARIN   DNMT3A

    Interaction Score: 0.51

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27740732


    Sources:
    PharmGKB

  • WARFARIN   THBD

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24602049


    Sources:
    PharmGKB

  • WARFARIN   PROS1

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA PharmGKB

  • WARFARIN   FPGS

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • WARFARIN   NQO1

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27581200 26257249 21923605 27740732


    Sources:
    PharmGKB

  • WARFARIN   CYP3A7

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    3977899


    Sources:
    NCI

  • WARFARIN   APOE

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21923605 29432897


    Sources:
    PharmGKB

  • WARFARIN   VWF

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    7626351


    Sources:
    NCI

  • WARFARIN   CYP1A1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27740732 8689941


    Sources:
    PharmGKB

  • WARFARIN   HNF4A

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25356900


    Sources:
    PharmGKB

  • WARFARIN   NR1I3

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25356900 29298995


    Sources:
    PharmGKB

  • WARFARIN   PROC

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA

  • WARFARIN   MTHFR

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14723717


    Sources:
    NCI

  • WARFARIN   UGT1A1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26223945 29737521


    Sources:
    PharmGKB

  • WARFARIN   BGLAP

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9578515


    Sources:
    NCI

  • WARFARIN   ALB

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17560104


    Sources:
    DTC

  • WARFARIN   APOB

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • WARFARIN   ABCB1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25312789 29875668 22248286 29432897


    Sources:
    PharmGKB

  • WARFARIN   CYP3A5

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18695978


    Sources:
    PharmGKB

  • WARFARIN   CYP2C19

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19752777 18574025 8723744 21692828 23941071 25652102 27356304


    Sources:
    PharmGKB

  • WARFARIN   NR1I2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20735727


    Sources:
    DrugBank

  • WARFARIN   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15050794


    Sources:
    NCI FDA

  • WARFARIN   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8723744 17392729 8689941


    Sources:
    PharmGKB

  • WARFARIN   VDR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29298995


    Sources:
    PharmGKB

  • WARFARIN   TP53

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • WARFARIN   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11353757


    Sources:
    PharmGKB

  • DrugBank: DB00682

    • Version: 5.1.7

    Alternate Names:
    81-81-2 CAS Number
    Apo-warfarin Drug Brand
    Coumadin Drug Brand

    Drug Info:
    Drug Groups approved
    Drug Type small molecule
    Drug Categories 4-hydroxycoumarins

    Publications:
    Rulcova A et al., 2010, Stereoselective interactions of warfarin enantiomers with the pregnane X nuclear receptor in gene regulation of major drug-metabolizing cytochrome P450 enzymes., J Thromb Haemost
    Osman et al., 2007, Plasma S/R ratio of warfarin co-varies with VKORC1 haplotype., Blood Coagul. Fibrinolysis
    Zhu et al., 2007, Estimation of warfarin maintenance dose based on VKORC1 (-1639 G>A) and CYP2C9 genotypes., Clin. Chem.

  • TdgClinicalTrial: WARFARIN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Anticoagulants
    Drug Class small molecule
    FDA Approval Approved before 1982

    Publications:

  • TEND: WARFARIN

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Drug Class anticoagulants
    Year of Approval approved before 1982

    Publications:

  • NCI: WARFARIN

    • Version: 14-September-2017

    Alternate Names:
    C945 NCI drug code

    Drug Info:

    Publications:
    Nagai et al., 2005, Gas6 induces Akt/mTOR-mediated mesangial hypertrophy in diabetic nephropathy., Kidney Int.
    Siguret et al., 2004, [Cytochrome P450 2C9 polymorphisms (CYP2C9) and warfarin maintenance dose in elderly patients]., Rev Med Interne
    Rettie et al., 1985, Stereoselective and regioselective hydroxylation of warfarin and selective O-dealkylation of phenoxazone ethers in human placenta., Biochem. Biophys. Res. Commun.

  • DTC: WARFARIN

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1464 ChEMBL Drug ID

    Drug Info:

    Publications:
    Thorarensen A et al., 2007, Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor., Bioorg Med Chem Lett

  • PharmGKB: warfarin

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Luo Z et al., 2017, Identification of novel variants associated with warfarin stable dosage by use of a two-stage extreme phenotype strategy., J Thromb Haemost
    Wienkers LC et al., 1996, Formation of (R)-8-hydroxywarfarin in human liver microsomes. A new metabolic marker for the (S)-mephenytoin hydroxylase, P4502C19., Drug Metab Dispos
    Lilja JJ et al., 2007, Effects of daily ingestion of cranberry juice on the pharmacokinetics of warfarin, tizanidine, and midazolam--probes of CYP2C9, CYP1A2, and CYP3A4., Clin Pharmacol Ther

  • TTD: Warfarin

    • Version: 2020.06.01

    Alternate Names:
    D0E3OF TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1464

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Warfarin

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • GuideToPharmacology: 178103459

    • Version: 29-September-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21