Strategies to overcome simultaneous P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of drugs

Pharmacogenomics

Volumn 2, Issue 4, 2001, Pages 401-415

  Patel, J ^a   Mitra, A K ^a  

^a UNIVERSITY OF MISSOURI KANSAS CITY   (United States)

Author keywords

Cytochrome P450; Efflux; Inhibitors; Metabolism; Oral bioavailability; P glycoprotein; Substrates

Indexed keywords

ALKALOID; AMPRENAVIR; ANTIBIOTIC AGENT; ANTIFUNGAL AGENT; BEPRIDIL; CALCIUM CHANNEL BLOCKING AGENT; CARDIOVASCULAR AGENT; CYTOCHROME P450 3A4; CYTOCHROME P450 INHIBITOR; DEXAMETHASONE; DILTIAZEM; ERYTHROMYCIN; ESTRADIOL; GLYCOPROTEIN P; HYDROCORTISONE; INDINAVIR; KETOCONAZOLE; PROTEINASE INHIBITOR; QUINIDINE; RESERPINE; RHODAMINE 123; RITONAVIR; STEROID; TESTOSTERONE; UNINDEXED DRUG; VERAPAMIL; VINBLASTINE; VINCRISTINE; XENOBIOTIC AGENT; CYP3A PROTEIN, HUMAN; CYTOCHROME P450; DRUG;

CLINICAL STUDY; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG METABOLISM; EFFUSION; FOOD DRUG INTERACTION; HUMAN; HUMAN CELL; HYPOTHESIS; INTESTINE CELL; LIVER; MULTIDRUG RESISTANCE; PROTEIN EXPRESSION; REVIEW; BIOAVAILABILITY; DRUG INTERACTION; INTESTINE ABSORPTION; METABOLISM; ORAL DRUG ADMINISTRATION; PROTEIN BINDING;

ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; DRUG RESISTANCE, MULTIPLE; FOOD-DRUG INTERACTIONS; HUMAN; INTESTINAL ABSORPTION; P-GLYCOPROTEIN; PHARMACEUTICAL PREPARATIONS; PROTEIN BINDING; XENOBIOTICS;

EID: 0035198013     PISSN: 14622416     EISSN: None     Source Type: Journal    
DOI: 10.1517/14622416.2.4.401     Document Type: Review

References (133)

1. Novel formulation strategies for improving oral bioavailability of drugs with poor membrane permeation or presystemic metabolism
2. Metabolism of drugs and other xenobiotics in the gut lumen and wall
3. Extrahepatic metabolism of drugs in humans
4. Individual variation in first-pass metabolism
5. Cytochrome P 450 isoenzymes, epoxide hydrolase and glutathione transferases in rat and human hepatic and extrahepatic tissues
6. CYP3A gene expression in human gut epithelium
7. Molecular cloning and sequence analysis of cDNA containing the entire coding region for human fetal liver cytochrome P-450
8. Characterisation of CYP3A gene subfamily expression in human gastrointestinal tissues
9. The immunocytochemical localisation and distribution of cytochrome P-450 in normal human hepatic and extrahepatic tissues with a monoclonal antibody to human cytochrome P-450
10. Cytochromes P-450 in the intestinal mucosa of man
11. Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man
12. Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes
13. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: Implications for drug delivery and activity in cancer chemotherapy
14. P-glycoprotein and pharmacokinetics
15. Modulation of oral bioavailability of anticancer drugs: From mouse to man
16. Multidrug-resistant transport proteins in yeast: Complete inventory and phylogenetic characterization of yeast open reading frames with the major facilitator superfamily
17. Prevention of drug access to bacterial targets: Permeability barriers and active efflux
18. Proton-dependent multidrug efflux systems
19. ATP-dependent transport systems in bacteria and humans: Relevance to cystic fibrosis and multidrug resistance
20. Effect of ATP binding cassette/multidrug resistance proteins on ATP efflux of Saccharomyces cerevisiae
21. Transmembrane organization of mouse P-glycoprotein determined by epitope insertion and immunofluorescence
22. P-glycoprotein. Associations between domains and between domains and molecular chaperones
23. Phosphatidylcholine translocase: A physiological role for the mdr2 gene
24. Homozygous disruption of the murine mdr2 P-glycoprotein gene leads to a complete absence of phospholipid from bile and to liver disease
25. The human MDR3 P-glycoprotein promotes translocation of phosphatidylcholine through the plasma membrane of fibroblasts from transgenic mice
26. ABC transporters: From microorganisms to man
27. Uptake of antineoplastic agents into large unilamellar vesicles in response to a membrane potential
28. The P-glycoprotein efflux pump: How does it transport drugs?
29. Volume-regulated chloride channels associated with the human multidrug-resistance P-glycoprotein
30. The multidrug resistance (mdr1) gene product functions as an ATP channel
31. Identification of 6′,7′-dihydroxybergamottin, a cytochrome P450 inhibitor, in grapefruit juice
32. Functional expression of P-glycoproteins in secretory vesicles
33. The role of passive transbilayer drug movement in multidrug resistance and its modulation
34. Human P-glycoprotein transports cortisol, aldosterone and dexamethasone, but not progesterone
35. Effect of quercetin on Hoechst 33342 transport by purified and reconstituted P-glycoprotein
36. Selective biotransformation of the human immunodeficiency virus protease inhibitor saquinavir by human small-intestinal cytochrome P4503A4: Potential contribution to high first-pass metabolism
37. Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine
38. Epithelial secretion of vinblastine by human intestinal adenocarcinoma cell (HCT-8 and T84) layers expressing P-glycoprotein
39. ATP-dependent transport of glutathione S-conjugates by the multidrug resistance-associated protein
40. The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates
41. Overexpression of the gene encoding the multidrug resistance-associated protein results in increased ATP-dependent glutathione S-conjugate transport
42. The human hepatic cytochromes P450 involved in drug metabolism
43. The human drug metabolizing cytochromes P450
44. Drug metabolizing enzymes related to laboratory medicine: Cytochromes P-450 and UDP-glucuronosyl transferases
45. P450 superfamily: Update on new sequences, gene mapping, accession numbers and nomenclature
46. P-glycoprotein-mediated multidrug resistance is modulated by pretreatment with chemosensitizers in HCT-8 carcinoma cells in vitro
47. HIV protease inhibitors: Advances in therapy and adverse reactions, including metabolic complications
48. Enzyme-catalyzed processes of first-pass hepatic and intestinal drug extraction
49. The mdr1 gene product, P-glycoprotein, mediates the transport of the cardiac glycoside, digoxin
50. Reversal of drug resistance by erythromycin: Erythromycin increases the accumulation of actinomycin D and doxorubicin in multidrug-resistant cells
51. First-pass metabolism of cyclosporin by the gut
52. Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by the erythromycin breath test
53. Expression of CYP3A4, CYP3A5 and CYP3A7 in human duodenal tissue
54. Selective expression of CYP3A5 and not CYP3A4 in human blood
55. Characterization of microsomal cytochrome P450 enzymes involved in the oxidation of xenobiotic chemicals in human fetal liver and adult lungs
56. Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: Studies with liver microsomes of 30 Japanese and 30 Caucasians
57. Protease inhibitors for the treatment of human immunodeficiency virus infection
58. Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition
59. Interaction between grapefruit juice and midazolam in humans
60. Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein
61. Effect of saquinavir on the pharmacokinetics and pharmacodynamics of oral and intravenous midazolam
62. Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells
63. Quantitative prediction of in vivo drug clearance and drug interactions from in vitro data on metabolism, together with binding and transport
64. Prediction of pharmacokinetic alterations caused by drug-drug interactions: Metabolic interaction in the liver
65. Role of metabolic enzymes and efflux transporters in the absorption of drugs from the small intestine
66. First-pass metabolism of midazolam by the human intestine
67. Humanized xenobiotic response in mice expressing nuclear receptor SXR
68. The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity
69. The pregnane X receptor: A promiscuous xenobiotic receptor that has diverged during evolution
70. St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor
71. John's wort, a herbal antidepressant, activates the steroid X receptor
72. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux
73. Nuclear receptor response elements mediate induction of intestinal mdr1 by rifampin
74. P-glycoprotein and cytochrome P-450 3A inhibition: Dissociation of inhibitory potencies
75. Grapefruit juice-drug interactions
76. Ketoconazole inhibition of triazolam and alprazolam clearance: Differential kinetic and dynamic consequences
77. Itraconazole drastically increases plasma concentrations of lovastatin and lovastatin acid
78. Simvastatin but not pravastatin is very susceptible to interaction with the CYP3A4 inhibitor itraconazole
79. Pharmacological insights from P-glycoprotein knockout mice
80. In vitro and in vivo drug interactions involving human CYP3A
81. Mechanism-based enzyme inactivators
82. Mechanism-based inactivation of human liver microsomal cytochrome P-450 IIIA4 by gestodene
83. Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression
84. Enhancement of anthracycline growth inhibition in parent and multidrug-resistant Chinese hamster ovary cells by cyclosporin A and its analogues
85. Modulation of P-glycoprotein-induced multidrug resistance in oncology
86. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin
87. Involvement of multiple transporters in the oral absorption of nucleoside analogues
88. Disposition of intravenous and oral cyclosporine after administration with grapefruit juice
89. In vitro identification of the P450 enzymes responsible for the metabolism of ropinirole
90. CYP3A4 drug interactions: Correlation of 10 in vitro probe substrates
91. Cooperativity in oxidations catalyzed by cytochrome P450 3A4
92. Human cytochrome P-450 3A4: In vitro drug-drug interaction patterns are substrate-dependent
93. Effect of quinidine on digoxin bioavailability
94. Inhibition of P-glycoprotein-mediated drug transport: A unifying mechanism to explain the interaction between digoxin and quinidine
95. In vivo modulation of CYP enzymes by quinidine and rifampin
96. Clinical modulation of multidrug resistance in multiple myeloma: Effect of cyclosporine on resistant tumor cells
97. Cyclosporins as drug resistance modifiers
98. Drug-resistance in multiple myeloma and non-Hodgkin's lymphoma: Detection of P-glycoprotein and potential circumvention by addition of verapamil to chemotherapy
99. Overexpression of the mdr1 gene in blast cells from patients with acute myelocytic leukemia is associated with decreased anthracycline accumulation that can be restored by cyclosporin-A
100. Modulation of P-glycoprotein phosphorylation and drug transport by sodium butyrate
101. Characterization of phosphorylation-defective mutants of human P-glycoprotein expressed in mammalian cells
102. Protein kinase C-mediated phosphorylation does not regulate drug transport by the human multidrug resistance P-glycoprotein
103. Staurosporine reduces P-glycoprotein expression and modulates multidrug resistance
104. Transfection of a mutant regulatory subunit gene of cAMP-dependent protein kinase causes increased drug sensitivity and decreased expression of P-glycoprotein
105. The barrier function of CYP3A4 and P-glycoprotein in the small bowel
106. Classical and novel forms of multidrug resistance and the physiological functions of P-glycoproteins in mammals
107. Biochemistry of multidrug resistance mediated by the multidrug transporter
108. From amplification to function: The case of the mdr1 gene
109. Efficient inhibition of P-glycoprotein-mediated multidrug resistance with a monoclonal antibody
110. Modulation of MDR1 and CYP3A expression by dexamethasone: Evidence for an inverse regulation in adrenals
111. Regulation of cytochrome P-450b/e and P-450p gene expression by growth hormone in adult rat hepatocytes cultured on a reconstituted basement membrane
112. Insulin-mediated modulation of cytochrome P450 gene induction profiles in primary rat hepatocyte cultures
113. Phenobarbital induction of cytochromes P-450. High-level long-term responsiveness of primary rat hepatocyte cultures to drug induction and glucocorticoid dependence of the phenobarbital response
114. Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities
115. HIV-protease inhibitors
116. Midazolam metabolism by modified Caco-2 monolayers: Effects of extracellular protein binding
117. Grapefruit juice and drugs. How significant is the interaction?
118. Interaction of citrus juices with felodipine and nifedipine
119. Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram
120. Grapefruit juice alters the systemic bioavailability and cardiac repolarization of terfenadine in poor metabolizers of terfenadine
121. Grapefruit juice-terfenadine single-dose interaction: Magnitude, mechanism and relevance
122. The cardiac effects of terfenadine after inhibition of its metabolism by grapefruit juice
123. Influence of chronic ingestion of grapefruit juice on steady-state blood concentrations of cyclosporine A in renal transplant patients with stable graft function
124. Effect of grapefruit juice on cyclosporine pharmacokinetics in renal transplant patients
125. Grapefruit juice and saquinavir
126. Seville orange juice-felodipine interaction: Comparison with dilute grapefruit juice and involvement of furocoumarins
127. 6′,7′-Dihydroxybergamotin in grapefruit juice and Seville orange juice: Effects on cyclosporine disposition, enterocyte CYP3A4 and P-glycoprotein
128. Inhibition of vinblastine efflux mediated by P-glycoprotein by grapefruit juice components in caco-2 cells
129. Biological effects of resveratrol
130. Resveratrol: A molecule whose time has come? And gone?
131. Mechanism-based inactivation of human cytochrome P450 3A4 by grapefruit juice and red wine
132. Resveratrol, a red wine constituent, is a mechanism-based inactivator of cytochrome P450 3A4
133. Enhancing effects of green tea components on the antitumor activity of adriamycin against M5076 ovarian sarcoma