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Volumn 16, Issue 2, 2016, Pages 119-127

Effect of rifampin on the pharmacokinetics of apixaban, an oral direct inhibitor of factor xa

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE AMINOTRANSFERASE; APIXABAN; ASPARTATE AMINOTRANSFERASE; RIFAMPICIN; BLOOD CLOTTING FACTOR 10A INHIBITOR; CYTOCHROME P450 3A; MULTIDRUG RESISTANCE PROTEIN; PYRAZOLE DERIVATIVE; PYRIDONE DERIVATIVE;

EID: 84953404552     PISSN: 11753277     EISSN: 1179187X     Source Type: Journal    
DOI: 10.1007/s40256-015-0157-9     Document Type: Article
Times cited : (93)

References (41)
  • 1
    • 35848929515 scopus 로고    scopus 로고
    • Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa
    • Pinto DJ, Orwat MJ, Koch S, et al. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. J Med Chem. 2007;50: 5339-56.
    • (2007) J Med Chem , vol.50 , pp. 5339-5356
    • Pinto, D.J.1    Orwat, M.J.2    Koch, S.3
  • 2
    • 42149172523 scopus 로고    scopus 로고
    • Apixaban, an oral, direct and highly selective factor Xa inhibitor: In vitro, antithrombotic and antihemostatic studies
    • Wong PC, Crain EJ, Xin B, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost. 2008;6: 820-9.
    • (2008) J Thromb Haemost , vol.6 , pp. 820-829
    • Wong, P.C.1    Crain, E.J.2    Xin, B.3
  • 3
    • 68249158084 scopus 로고    scopus 로고
    • Apixaban or enoxaparin for thromboprophylaxis after knee replacement
    • Lassen MR, Raskob GE, Gallus A, et al. Apixaban or enoxaparin for thromboprophylaxis after knee replacement. N Engl J Med. 2009;361: 594-604.
    • (2009) N Engl J Med , vol.361 , pp. 594-604
    • Lassen, M.R.1    Raskob, G.E.2    Gallus, A.3
  • 4
    • 78650587760 scopus 로고    scopus 로고
    • Apixaban versus enoxaparin for thromboprophylaxis after hip replacement
    • Lassen MR, Gallus A, Raskob GE, et al. Apixaban versus enoxaparin for thromboprophylaxis after hip replacement. N Engl J Med. 2010;363: 2487-98.
    • (2010) N Engl J Med , vol.363 , pp. 2487-2498
    • Lassen, M.R.1    Gallus, A.2    Raskob, G.E.3
  • 5
    • 77649113258 scopus 로고    scopus 로고
    • Apixaban versus enoxaparin for thromboprophylaxis after knee replacement (ADVANCE-2): A randomised double-blind trial
    • Lassen MR, Raskob GE, Gallus A, et al. Apixaban versus enoxaparin for thromboprophylaxis after knee replacement (ADVANCE-2): a randomised double-blind trial. Lancet. 2010;375: 807-15.
    • (2010) Lancet , vol.375 , pp. 807-815
    • Lassen, M.R.1    Raskob, G.E.2    Gallus, A.3
  • 6
    • 79952301326 scopus 로고    scopus 로고
    • Apixaban in patients with atrial fibrillation
    • Connolly SJ, Eikelboom J, Joyner C, et al. Apixaban in patients with atrial fibrillation. N Engl J Med. 2011;364: 806-17.
    • (2011) N Engl J Med , vol.364 , pp. 806-817
    • Connolly, S.J.1    Eikelboom, J.2    Joyner, C.3
  • 7
    • 80052825103 scopus 로고    scopus 로고
    • Apixaban versus warfarin in patients with atrial fibrillation
    • Granger CB, Alexander JH, McMurray JJ, et al. Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med. 2011;365: 981-92.
    • (2011) N Engl J Med , vol.365 , pp. 981-992
    • Granger, C.B.1    Alexander, J.H.2    McMurray, J.J.3
  • 8
    • 84880327613 scopus 로고    scopus 로고
    • AMPLIFY Investigators. Oral apixaban for the treatment of acute venous thromboembolism
    • Agnelli G, Buller HR, Cohen, et al. AMPLIFY Investigators. Oral apixaban for the treatment of acute venous thromboembolism. N Engl J Med. 2013;369: 799-808.
    • (2013) N Engl J Med , vol.369 , pp. 799-808
    • Agnelli, G.1    Buller, H.R.2    Cohen3
  • 9
    • 84873596181 scopus 로고    scopus 로고
    • AMPLIFY-EXT Investigators. Apixaban for extended treatment of venous thromboembolism
    • Agnelli G, Buller HR, Cohen A, et al. AMPLIFY-EXT Investigators. Apixaban for extended treatment of venous thromboembolism. N Engl J Med. 2013;368: 699-708.
    • (2013) N Engl J Med , vol.368 , pp. 699-708
    • Agnelli, G.1    Buller, H.R.2    Cohen, A.3
  • 10
    • 84878952383 scopus 로고    scopus 로고
    • Safety, pharmacokinetics and pharmacodynamics of multiple oral doses of apixaban, a factor Xa inhibitor, in healthy subjects
    • Frost C, Nepal S, Wang J, et al. Safety, pharmacokinetics and pharmacodynamics of multiple oral doses of apixaban, a factor Xa inhibitor, in healthy subjects. Br J Clin Pharmacol. 2013;76: 776-86.
    • (2013) Br J Clin Pharmacol , vol.76 , pp. 776-786
    • Frost, C.1    Nepal, S.2    Wang, J.3
  • 11
    • 84872260247 scopus 로고    scopus 로고
    • Apixaban, an oral, direct factor Xa inhibitor: Single-dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects
    • Frost C, Wang J, Nepal S, et al. Apixaban, an oral, direct factor Xa inhibitor: single-dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects. Br J Clin Pharmacol. 2013;75: 476-87.
    • (2013) Br J Clin Pharmacol , vol.75 , pp. 476-487
    • Frost, C.1    Wang, J.2    Nepal, S.3
  • 12
    • 57449113800 scopus 로고    scopus 로고
    • Apixaban, a direct factor Xa inhibitor: Single-dose pharmacokinetics and pharmacodynamics of an intravenous formulation [abstract 148]
    • Frost C, Yu Z, Nepal S, et al. Apixaban, a direct factor Xa inhibitor: single-dose pharmacokinetics and pharmacodynamics of an intravenous formulation [abstract 148]. J Clin Pharmacol. 2008;48: 1132.
    • (2008) J Clin Pharmacol , vol.48 , pp. 1132
    • Frost, C.1    Yu, Z.2    Nepal, S.3
  • 13
    • 58149458160 scopus 로고    scopus 로고
    • Apixaban metabolism and pharmacokinetics after oral administration to humans
    • Raghavan N, Frost CE, Yu Z, et al. Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos. 2009;37: 74-81.
    • (2009) Drug Metab Dispos , vol.37 , pp. 74-81
    • Raghavan, N.1    Frost, C.E.2    Yu, Z.3
  • 14
    • 79251511891 scopus 로고    scopus 로고
    • Tissue distribution and elimination of [14C]apixaban in rats
    • Wang L, He K, Maxwell B, et al. Tissue distribution and elimination of [14C]apixaban in rats. Drug Metab Dispos. 2011;39: 256-64.
    • (2011) Drug Metab Dispos , vol.39 , pp. 256-264
    • Wang, L.1    He, K.2    Maxwell, B.3
  • 15
    • 84875844889 scopus 로고    scopus 로고
    • Investigating the enteroenteric recirculation of apixaban, a factor Xa inhibitor: Administration of activated charcoal to bile duct-cannulated rats and dogs receiving an intravenous dose and use of drug transporter knockout rats
    • Zhang D, Frost CE, He K, et al. Investigating the enteroenteric recirculation of apixaban, a factor Xa inhibitor: administration of activated charcoal to bile duct-cannulated rats and dogs receiving an intravenous dose and use of drug transporter knockout rats. Drug Metab Dispos. 2013;41: 906-15.
    • (2013) Drug Metab Dispos , vol.41 , pp. 906-915
    • Zhang, D.1    Frost, C.E.2    He, K.3
  • 16
    • 67650809062 scopus 로고    scopus 로고
    • Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans
    • Zhang D, He K, Raghavan N, et al. Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans. Drug Metab Dispos. 2009;37: 1738-48.
    • (2009) Drug Metab Dispos , vol.37 , pp. 1738-1748
    • Zhang, D.1    He, K.2    Raghavan, N.3
  • 17
    • 63849186171 scopus 로고    scopus 로고
    • Sulfation of o-demethyl apixaban: Enzyme identification and species comparison
    • Wang L, Raghavan N, He K, et al. Sulfation of o-demethyl apixaban: enzyme identification and species comparison. Drug Metab Dispos. 2009;37: 802-8.
    • (2009) Drug Metab Dispos , vol.37 , pp. 802-808
    • Wang, L.1    Raghavan, N.2    He, K.3
  • 18
    • 76749166335 scopus 로고    scopus 로고
    • In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies
    • Wang L, Zhang D, Raghavan N, et al. In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies. Drug Metab Dispos. 2010;38: 448-58.
    • (2010) Drug Metab Dispos , vol.38 , pp. 448-458
    • Wang, L.1    Zhang, D.2    Raghavan, N.3
  • 19
    • 84856389296 scopus 로고    scopus 로고
    • Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor
    • He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor. Eur J Drug Metab Pharmacokinet. 2011;36: 129-39.
    • (2011) Eur J Drug Metab Pharmacokinet , vol.36 , pp. 129-139
    • He, K.1    Luettgen, J.M.2    Zhang, D.3
  • 20
    • 84875859352 scopus 로고    scopus 로고
    • Characterization of efflux transporters involved in distribution and disposition of apixaban
    • Zhang D, He K, Herbst JJ, et al. Characterization of efflux transporters involved in distribution and disposition of apixaban. Drug Metab Dispos. 2013;41: 827-35.
    • (2013) Drug Metab Dispos , vol.41 , pp. 827-835
    • Zhang, D.1    He, K.2    Herbst, J.J.3
  • 22
    • 0035478419 scopus 로고    scopus 로고
    • The drug efflux-metabolism alliance: Biochemical aspects
    • Benet LZ, Cummins CL. The drug efflux-metabolism alliance: biochemical aspects. Adv Drug Deliv Rev. 2001;50(Suppl 1): S3-11.
    • (2001) Adv Drug Deliv Rev , vol.50 , pp. S3-11
    • Benet, L.Z.1    Cummins, C.L.2
  • 23
    • 84928312539 scopus 로고    scopus 로고
    • Effect of ketoconazole and diltiazem on the pharmacokinetics of apixaban, an oral direct factor Xa inhibitor
    • Frost CE, Byon W, Song Y, et al. Effect of ketoconazole and diltiazem on the pharmacokinetics of apixaban, an oral direct factor Xa inhibitor. Br J Clin Pharmacol. 2015;79: 838-46.
    • (2015) Br J Clin Pharmacol , vol.79 , pp. 838-846
    • Frost, C.E.1    Byon, W.2    Song, Y.3
  • 24
    • 0032754284 scopus 로고    scopus 로고
    • The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin
    • Greiner B, Eichelbaum M, Fritz P, et al. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest. 1999;104: 147-53.
    • (1999) J Clin Invest , vol.104 , pp. 147-153
    • Greiner, B.1    Eichelbaum, M.2    Fritz, P.3
  • 25
    • 84979156144 scopus 로고    scopus 로고
    • Accessed 2 Feb 2015
    • Sanofi-Aventis U.S. LLC. Rifadin (rifampin) package insert. 2013. http://products.sanofi.us/rifadin/Rifadin.pdf. Accessed 2 Feb 2015.
    • (2013)
  • 26
    • 0026464616 scopus 로고
    • Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes
    • Kolars JC, Schmiedlin-Ren P, Schuetz JD, et al. Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes. J Clin Invest. 1992;90: 1871-8.
    • (1992) J Clin Invest , vol.90 , pp. 1871-1878
    • Kolars, J.C.1    Schmiedlin-Ren, P.2    Schuetz, J.D.3
  • 27
    • 84908018905 scopus 로고    scopus 로고
    • LC-MS/MS determination of apixaban (BMS-562247) and its major metabolite in human plasma: An application of polarity switching and monolithic HPLC column
    • Pursley J, Shen JX, Schuster A, et al. LC-MS/MS determination of apixaban (BMS-562247) and its major metabolite in human plasma: an application of polarity switching and monolithic HPLC column. Bioanalysis. 2014;6: 2071-82.
    • (2014) Bioanalysis , vol.6 , pp. 2071-2082
    • Pursley, J.1    Shen, J.X.2    Schuster, A.3
  • 28
    • 0020117866 scopus 로고
    • General derivation of the equation for time to reach a certain fraction of steady state
    • Perrier D, Gibaldi M. General derivation of the equation for time to reach a certain fraction of steady state. J Pharm Sci. 1982;71: 474-5.
    • (1982) J Pharm Sci , vol.71 , pp. 474-475
    • Perrier, D.1    Gibaldi, M.2
  • 29
    • 0042163137 scopus 로고    scopus 로고
    • Pharmacokinetic interactions with rifampicin: Clinical relevance
    • Niemi M, Backman JT, Fromm MF, et al. Pharmacokinetic interactions with rifampicin: clinical relevance. Clin Pharmacokinet. 2003;42: 819-50.
    • (2003) Clin Pharmacokinet , vol.42 , pp. 819-850
    • Niemi, M.1    Backman, J.T.2    Fromm, M.F.3
  • 30
    • 33645551838 scopus 로고    scopus 로고
    • Relationship between excretion clearance of rhodamine 123 and P-glycoprotein (Pgp) expression induced by representative Pgp inducers
    • Kageyama M, Fukushima K, Togawa T, et al. Relationship between excretion clearance of rhodamine 123 and P-glycoprotein (Pgp) expression induced by representative Pgp inducers. Biol Pharm Bull. 2006;29: 779-84.
    • (2006) Biol Pharm Bull , vol.29 , pp. 779-784
    • Kageyama, M.1    Fukushima, K.2    Togawa, T.3
  • 31
    • 73849094765 scopus 로고    scopus 로고
    • Effects of the P-glycoprotein inducer carbamazepine on fexofenadine pharmacokinetics
    • Yamada S, Uasui-Furukori N, Akamine Y, et al. Effects of the P-glycoprotein inducer carbamazepine on fexofenadine pharmacokinetics. Ther Drug Monit. 2009;31: 764-8.
    • (2009) Ther Drug Monit , vol.31 , pp. 764-768
    • Yamada, S.1    Uasui-Furukori, N.2    Akamine, Y.3
  • 32
    • 84898969855 scopus 로고    scopus 로고
    • Effect of activated charcoal on apixaban pharmacokinetics in healthy subjects
    • Wang X, Mondal S, Wang J, et al. Effect of activated charcoal on apixaban pharmacokinetics in healthy subjects. Am J Cardiovasc Drugs. 2014;14: 147-54.
    • (2014) Am J Cardiovasc Drugs , vol.14 , pp. 147-154
    • Wang, X.1    Mondal, S.2    Wang, J.3
  • 33
    • 84904013662 scopus 로고    scopus 로고
    • Safety, tolerability, pharmacokinetics, and pharmacodynamics of multiple doses of apixaban in healthy Japanese male subjects
    • Yamahira N, Frost C, Fukase H, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of multiple doses of apixaban in healthy Japanese male subjects. Int J Clin Pharmacol Ther. 2014;52: 564-73.
    • (2014) Int J Clin Pharmacol Ther , vol.52 , pp. 564-573
    • Yamahira, N.1    Frost, C.2    Fukase, H.3
  • 34
    • 84927938274 scopus 로고    scopus 로고
    • Model-based exposure-response analysis of apixaban to quantify bleeding risk in special populations of subjects undergoing orthopedic surgery
    • Leil TA, Frost C, Wang X, Pfister M, LaCreta F. Model-based exposure-response analysis of apixaban to quantify bleeding risk in special populations of subjects undergoing orthopedic surgery. CPT Pharmacomet Syst Pharmacol. 2014;3: e136.
    • (2014) CPT Pharmacomet Syst Pharmacol , vol.3
    • Leil, T.A.1    Frost, C.2    Wang, X.3    Pfister, M.4    LaCreta, F.5
  • 35
    • 84930086872 scopus 로고    scopus 로고
    • Effects of age and sex on the single-dose pharmacokinetics and pharmacodynamics of apixaban
    • Frost CE, Song Y, Shenker A, et al. Effects of age and sex on the single-dose pharmacokinetics and pharmacodynamics of apixaban. Clin Pharmacokinet. 2015;54: 651-62.
    • (2015) Clin Pharmacokinet , vol.54 , pp. 651-662
    • Frost, C.E.1    Song, Y.2    Shenker, A.3
  • 36
    • 33845493309 scopus 로고    scopus 로고
    • Pharmacokinetics and metabolic drug interactions
    • Leucuta SE, Vlase L. Pharmacokinetics and metabolic drug interactions. Curr Clin Pharmacol. 2006;1: 5-20.
    • (2006) Curr Clin Pharmacol , vol.1 , pp. 5-20
    • Leucuta, S.E.1    Vlase, L.2
  • 38
    • 0031959294 scopus 로고    scopus 로고
    • The area under the plasma concentration-time curve for oral midazolam is 400-fold larger during treatment with itraconazole than with rifampicin
    • Backman JT, Kivistö KT, Olkkola KT, et al. The area under the plasma concentration-time curve for oral midazolam is 400-fold larger during treatment with itraconazole than with rifampicin. Eur J Clin Pharmacol. 1998;54: 53-8.
    • (1998) Eur J Clin Pharmacol , vol.54 , pp. 53-58
    • Backman, J.T.1    Kivistö, K.T.2    Olkkola, K.T.3
  • 39
    • 51649119903 scopus 로고    scopus 로고
    • Pharmacokinetics of intravenous and oral midazolam in plasma and saliva in humans: Usefulness of saliva as matrix for CYP3A phenotyping
    • Link B, Haschke M, Grignaschi N, et al. Pharmacokinetics of intravenous and oral midazolam in plasma and saliva in humans: usefulness of saliva as matrix for CYP3A phenotyping. Br J Clin Pharmacol. 2008;66: 473-84.
    • (2008) Br J Clin Pharmacol , vol.66 , pp. 473-484
    • Link, B.1    Haschke, M.2    Grignaschi, N.3
  • 40
    • 84928321421 scopus 로고    scopus 로고
    • May, Accessed 21 Aug 2015
    • Bristol-Myers Squibb, Pfizer EEIG. Eliquis (apixaban tablets) Summary of product characteristics. 2013 May. http://www.ema. europa.eu/docs/en_GB/document_library/EPAR_-_Product_Infor mation/human/002148/WC500107728.pdf. Accessed 21 Aug 2015.
    • (2013) Eliquis (apixaban tablets) Summary of product characteristics
  • 41
    • 84979150387 scopus 로고    scopus 로고
    • Eliquis (apixaban tablets)
    • August, Accessed 21 Aug 2015
    • Bristol-Myers Squibb. Eliquis (apixaban tablets). Prescribing information. 2014 August. http://www.accessdata.fda.gov/ drugsatfda_docs/label/2014/202155s009lbl.pdf. Accessed 21 Aug 2015.
    • (2014) Prescribing information


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