Genetic polymorphisms in assessing interindividual variability in delivered dose

Regulatory Toxicology and Pharmacology

Volumn 35, Issue 2 I, 2002, Pages 177-197

  Haber, L T ^a   Maier, A ^a   Gentry, P R ^b   Clewell, H J ^b   Dourson, M L ^a  

^a Toxicology Excellence for Risk Assessment   (United States)

^b Environ   (United States)

Author keywords

Dichloroacetic acid; Dichloromethane; Methylene chloride; Parathion; PBPK model; Polymorphism; Risk assessment; Warfarin

Indexed keywords

DICHLOROACETIC ACID; DICHLOROMETHANE; PARATHION; WARFARIN; ENZYME; XENOBIOTIC AGENT;

ALLELISM; ARTICLE; CANCER SUSCEPTIBILITY; CARCINOGENICITY; CHEMICAL ANALYSIS; COMPETITIVE INHIBITION; DOSE RESPONSE; DRUG CLEARANCE; DRUG METABOLISM; ETHNOLOGY; GENE FREQUENCY; GENETIC POLYMORPHISM; GENETIC PREDISPOSITION; GENETIC VARIABILITY; INDIVIDUAL BASED POPULATION MODEL; INHIBITION KINETICS; LIVER TOXICITY; NEUROTOXICITY; PHENOTYPE; PRIORITY JOURNAL; RISK ASSESSMENT; TOXICOKINETICS; ANIMAL; GENETICS; HUMAN; IN VITRO STUDY; METABOLISM; METHODOLOGY; REPRODUCIBILITY; REVIEW; UNCERTAINTY;

ANIMALS; DICHLOROACETATE; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYMES; HUMANS; METHYLENE CHLORIDE; PARATHION; POLYMORPHISM, GENETIC; REPRODUCIBILITY OF RESULTS; RISK ASSESSMENT; UNCERTAINTY; WARFARIN; XENOBIOTICS;

EID: 0036085787     PISSN: 02732300     EISSN: None     Source Type: Journal    
DOI: 10.1006/rtph.2001.1517     Document Type: Article

References (164)

1. A physiologically based pharmacokinetic model for trichloroethylene and its metabolites, chloral hydrate, trichloroacetate, dichloroacetate, trichloroethanol, and trichloroethanol glucuronide in B6C3F1 mice
2. Chondrodysplasi punctata and maternal warfarin treatment
3. Molecular basis for the polymorphic forms of human serum paraoxonase/arylesterase: Glutamine or arginine at position 191, for the respective A or B allozymes
4. Association of polymorphisms in the cytochrome P450 CYP2C9 with warfarin dose requirement and risk of bleeding complications
5. Physiologically based pharmacokinetics and the risk assessment process for methylene chloride
6. Physiologically based pharmacokinetics and cancer risk assessment
7. Probabilistic noncancer risk estimation
8. Noncancer risk assessment: A probablistic alternative to current practice
9. Population distribution and effects on drug metabolism of a genetic variant in the 5′ promoter region of CYP3A4
10. Reference dose (RfD): Description and use in health risk assessments
11. Dichloroacetate (DCA) dosimetry: Interpreting DCA-induced liver cancer dose response and the potential for DCA to contribute to trichloroethylene-induced liver cancer
12. Warfarin-fluconazole. II. A metabolically based drug interaction: In vivo studies
13. Discovery of a functional polymorphism in human glutathione transferase zeta by expressed sequence tag database analysis
14. Interindividual differences in the in vitro conjugation of methylene chloride with glutathione by cytosolic glutathione S-transferase in 22 human liver samples
15. Drinking water disinfection byproducts: Review and approach to toxicity evaluation
16. Concordance between enzyme activity and genotype of glutathione S-transferase theta (GSTT1)
17. Mode of action of liver induction by trichloroethylene and its metabolites trichloroacetate and dichloroacetate
18. Addressing human variability in risk assessment - The robustness of the intraspecies uncertainty factor
19. Biotransformation of parathion in human liver: Participation of CYP3A4 and its inactivation during microsomal parathion oxidation
20. Uncertainty factors and interindividual variation
21. Does the animal-to-human uncertainty factor incorporate interspecies differences in surface area?
22. Lack of total independence of uncertainty factors (UFs): Implications for the size of the total uncertainty factor
23. DNA-protein cross-links (DPX) and cell proliferation in B6C3F1 mice but not Syrian golden hamsters exposed to dichloromethane: Pharmacokinetics and risk assessment with DPX as dosimeter
24. Stereochemical aspects of warfarin drug interactions: Use of a combined pharmacokinetic-pharmacodynamic model
25. Modulation of cytochrome P-450 dependent monooxygenases in streptozotocin-induced diabetic hamster. I. Effects of propofol on defluorination and cytochrome P-450 activities
26. Stereoselective interaction between the R-enantiomer of warfarin and cimetidine
27. 90-Day toxicity study of dichloroacetate in dogs
28. Development of a physiologically based pharmacokinetic model of trichloroethylene and its metabolites for use in risk assessment
29. Use of physiologically based pharmacokinetic modeling to investigate individual versus population risk
30. Inhibition of glutathione S-transferase zeta and tyrosine metabolism by dichloroacetate: A potential unifying mechanism for its altered biotransformation and toxicity
31. Serum paraoxonase and its influence on paraoxon and chlorpyrifos-oxon toxicity in rats
32. The metabolic effects of dichloroacetate
33. The R144C change in the CYP2C9*2 allele alters interaction of the cytochrome P450 with NADPH: Cytochrome P450 oxidoreductase
34. Disposition and pharmacodynamics of dichloroacetate (DCA) and oxalate following oral DCA doses
35. Recent advances in understanding the molecular basis of polymorphisms in genes encoding cytochrome P450 enzymes
36. The impact of exercise and intersubject variability on dose estimates for dichloromethane derived from a physiologically based pharmacokinetic model
37. The effect of the human serum paraoxonase polymorphism is reversed with diazoxon, soman and sarin
38. Interethnic differences in the detoxification of organophosphates: The human serum paraoxonase polymorphism
39. Boron tolerable intake: Re-evaluation of toxicokinetics for data-derived uncertainty factors
40. Regulatory history and experimental support of uncertainty (safety) factors
41. Concise review of the glutathione S-transferases and their significance to toxicology
42. The human serum paraoxonase/arylesterase polymorphism
43. Effects of glutathione transferase theta polymorphism on the risk estimates of dichloromethane to humans
44. Cardiopathic effects of dichloroacetate in the fetal Long-Evans rat
45. Prolonged hypolactatemia and increased total pyruvate dehydrogenase activity by dichloroacetate
46. Human and rabbit paraoxonases: Purification, cloning, sequencing, mapping and role of polymorphism in organophosphate detoxification
47. Genetic polymorphism of CYP2C9 and its effect on warfarin maintenance dose requirement in patients undergoing anticoagulation therapy
48. Metabolism of inhaled dihalomethanes in vivo: Differentiation of kinetic constants for two independent pathways
49. Physiologically based pharmacokinetic and pharmacodynamic model for the inhibition of acetylcholinesterase by diisopropylfluorophosphate
50. Pharmacokinetics and metabolism of dichloroacetate in the F344 rat after prior administration in drinking water
51. Substrate recognition sites in cytochrome P450 family 2 (CYP2) proteins inferred from comparative analyses of amino acid and coding nucleotide sequences
52. Physiologically based pharmacokinetic modeling of inhaled trichloroethylene and its oxidative metabolites in B6C3F1 mice
53. Allelic variants of human cytochrome P450 2C9: Baculovirus-mediated expression, purification, structural characterization, substrate stereoselectivity, and prochiral selectivity of the wild-type and I359L mutant forms
54. Maternal and fetal sequalae of anticoagulation during pregnancy
55. Metabolism of dichloromethane (methylene chloride) to formaldehyde in human erythrocytes: Influence of polymorphism of glutathione transferase theta (GST T1-1)
56. Distributions of individual susceptibility among humans for toxic effects: How much protection does the traditional tenfold factor provide for what fraction of which kinds of chemicals and effects?
57. Human interindividual variability in parameters related to health risks
58. Human interindividual variability in cancer risks-Technical and management challenges
59. Human variability in susceptibility to toxic chemicals - A preliminary analysis of pharmacokinetic data from normal volunteers
60. Human interindividual variability - A major source of uncertainty in assessing risks for noncancer health effects
61. Pharmacokinetic and pharmacodynamic properties of oral anticoagulants, especially phenprocoumon
62. Structural forms of phenprocoumon and warfarin that are metabolized at the active site of CYP2C9
63. Common paraoxonase gene variants, mortality risk and fatal cardiovascular events in elderly subjects
64. Novel mutations of CYP3A4 in Chinese
65. The molecular basis of the human serum paraoxonase activity polymorphism
66. Polymorphic human cytochrome P450 enzymes: An opportunity for individualized drug treatment
67. Characterization of liver microsomal 7-ethoxycoumarin O-deethylation and chlorzoxazone 6-hydroxylation activities in Japanese and Caucasian subjects genotyped for CYP2E1 gene
68. Glutathione-dependent conversion to glyoxylate, a major pathway of dichloroacetate biotransformation in hepatic cytosol from humans and rats, is reduced in dichloroacetate-treated rats
69. Species-related differences in the inhibition of brain acetylcholinesterase by paraoxon and malaoxon
70. A Bayesian analysis of the influence of GSTT1 polymorphism on the cancer risk estimate for dichloromethane
71. Bayesian estimation of variability in adipose tissue blood flow in man by physiologically based pharmacokinetic modeling of inhalation exposure to toulene
72. Physiologically based pharmacokinetic modeling of inhalation exposure of humans to dichloromethane during moderate to heavy exercise
73. Correlation of human cytochrome P4502C substrate specificities with primary structure: Warfarin as a probe
74. Human P450 metabolism of warfarin
75. An evaluation of the safety factor approach in risk assessment
76. Inherited polymorphism in the N-acetyltransferase 1 (NAT1) and 2 (NAT2) genes and susceptibility to gastric and colorectal adenocarcinoma
77. Metabolic enantiomeric interactions: The inhibition of human (S)-warfarin-7-hydroxylase by (R)-warfarin
78. Warfarin-fluconazole. III. A rational approach to management of a metabolically based drug interaction
79. Metabolism and lipoperoxidative activity of trichloroacetate and dichloroacetate in rats and mice
80. Metabolism of trichloroethylene
81. Catalytic efficiency determines the in-vivo efficacy of PON1 for detoxifying organophosphorus compounds
82. Tissue distribution, excretion, and urinary metabolites of dichloroacetic acid in the male Fischer 344 rat
83. Spermatotoxicity of dichloroacetic acid
84. Dichloroacetic acid: Metabolism in cytosol
85. Isothiocyanates, glutathione S-transferase M1 and T1 polymorphisms, and lung-cancer risk: A prospective study of men in Shanghai, China
86. Drug elimination interactions: Analysis using a mathematical model
87. A physiologically based pharmacokinetic computer model for human pregnancy
88. Isolation of a mouse theta glutathione S-transferase active with methylene chloride
89. Approach to assessment of risk to human health for priority substances under the Canadian Environmental Protection Act
90. Guidelines for application of compound specific adjustment factors (CSAF) in dose/concentration response assessment
91. Theta, a new class of glutathione transferases purified from rat and man
92. Workshop report - Health risks of drinking water chlorination by-products: Report of an expert working group
93. Cytochrome P4502C9: An enzyme of major importance in human drug metabolism
94. Human PON2 gene at 7q21.3: Cloning, multiple mRNA forms, and missense polymorphisms in the coding sequence
95. Behavioral evaluation of the neurotoxicity produced by dichloroacetic acid in rats
96. Plasma paraoxonase polymorphism: A new enzyme assay, population, family, biochemical, and linkage studies
97. Population pharmacokinetics of racemic warfarin in adult patients
98. Data-derived uncertainty factors: Boric acid (BA) as a case study
99. Induction of cytochromes P450 2B and 2E1 in rat liver by isomeric picoline N-oxides
100. Interindividual variations in enzymes controlling organophosphate toxicity in man
101. The role of metabolism in determining susceptibility to parathion toxicity in man
102. Ethnic differences in the prevalence of the homozygous deleted genotype of glutathione S-transferase theta
103. Concise review of the cytochrome P450s and their roles in toxicology
104. An approach for modeling noncancer dose responses with an emphasis on uncertainty
105. The human serum paraoxonase/arylesterase gene (PON1) is one member of a multigene family
106. Genetic polymorphisms in human drug-metabolizing enzymes: Potential uses of reverse genetics to identify genes of toxicological relevance
107. Implications of cytochrome P450 2C9 polymorphism on warfarin metabolism and dosing
108. Quantitating the production of biological reactive intermediates in target tissues: Example, dichloromethane
109. In vitro metabolism of methylene chloride in human and animal tissues: Use in physiologically based pharmacokinetic models
110. Safety factors and establishment of acceptable daily intakes
111. Data derived safety factors for the evaluation of food additives and environmental contaminants
112. Human variability and noncancer risk assessment - An analysis of the default uncertainty factor
113. A common genetic basis for idiosyncratic toxicity of warfarin and phenytoin
114. Hydroxylation of warfarin by human cDNA-expressed cytochrome P-450: A role for P-4502C9 in the etiology of (S)-warfarin-drug interactions
115. Impaired (S)-warfarin metabolism catalysed by the R144C allelic variant of CYP2C9
116. CYP2C19 genotype and phenotype determined by omeprazole in a Korean population
117. Evidence for the activation of organophosphate pesticides by cytochromes P450 3A4 and 2D6 in human liver microsomes
118. The codon 55 polymorphism in the paraoxonase 1 gene is not associated with the risk of coronary heart disease in Asian Indians and Chinese
119. CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: Evidence for an allelic variant with altered catalytic activity
120. Analysis of the adequacy of safety factors
121. Evidence that human class Theta glutathione S-transferase T1-1 can catalyse the activation of dichloromethane, a liver and lung carcinogen in the mouse: Comparison of the tissue distribution of GST T1-1 with that of classes Alpha, Mu and Pi GST in human
122. A probabilistic approach for deriving acceptable human intake limits and human health risks from toxicological studies: General framework
123. Developmental toxicity of dichloroacetate in the rat
124. Characteristics of the genetically determined allozymic forms of human serum paraoxonase/arylesterase
125. Interindividual variance of cytochrome P450 forms in human hepatic microsomes: Correlation of individual forms with xenobiotic metabolism and implications in risk assessment
126. The pharmacology of dichloroacetate
127. Dichloroacetate
128. Pharmacokinetics, metabolism and toxicology of dichloroacetate
129. Genetic association between sensitivity to warfarin and expression of CYP2C9*3
130. The role of the CYP2C9-Leu359 allelic variant in the tolbutamide polymorphism
131. Aspects of anticoagulant action: A review of the pharmacology, metabolism and toxicology of warfarin and congeners
132. A probabilistic framework for the reference dose (probabilistic RfD)
133. A theoretical model of the competition between hydrolase and carboxylesterase in protection against organophosphorus poisoning
134. Metabolism of warfarin enantiomers in Japanese patients with heart disease having different CYP2C9 and CYP2C19 genotypes
135. Comparisons between in-vitro and in-vivo metabolism of (S)-warfarin: Catalytic activities of cDNA-expressed CYP2C9, its Leu359 variant and their mixture versus unbound clearance in patients with the corresponding CYP2C9 genotypes
136. Cytochrome P450 2E1: Its clinical and toxicological role
137. Detoxication of paraoxon by rat liver homogenate and serum carboxylesterases and A-esterases
138. Influence of cytochrome P-450 CYP2C9 polymorphisms on warfarin sensitivity and risk of over-anticoagulation in patients on long-term treatment
139. Glutathione transferase zeta catalyses the oxygenation of the carcinogen dichloroacetic acid to glyoxylic acid
140. Glutathione transferase zeta-catalyzed biotransformation of dichloroacetic acid and other alpha-haloacids
141. Polymorphism- and species-dependent inactivation of glutathione transferase zeta by dichloroacetate
142. Differential cytotoxic sensitivity in mouse and human cell lines exposed to organophosphate insecticides
143. Unusually low clearance of two CYP3A substrates, alprazolam and trazodone, in a volunteer subject with wild-type CYP3A4 promoter region
144. CYP3A activity in African American and European American men: Population differences and functional effect of the CYP3A4*1B5′-promoter region polymorphism
145. Purification and characterization of six cytochrome P-450 isozymes from human liver microsomes
146. Polymorphic distribution of glutathione transferase activity with methyl chloride in human blood
147. Interindividual differences in hepatic expression of CYP3A4: Relationship to genetic polymorphism in the 5′-upstream regulatory region
148. Chodrodysplasi punctata after warfarin in early pregnancy: Case report and summary of the literature
149. The hereditary transmission of the glutathione transferase hGSTT1-1 conjugator phenotype in a large family
150. Formation of (R)-8-hydroxywarfarin in human liver microsomes: A new metabolic marker for the (S)-mephenytoin hydroxylase, P4502C19
151. Genetic polymorphisms of human N-acetyltransferase, cytochrome P450, glutathione-S-transferase, and epoxide hydrolase enzymes: Relevance to xenobiotic metabolism and toxicity