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Article
Insights into the Substrate Specificity, Inhibitors, Regulation, and Polymorphisms and the Clinical Impact of Human Cytochrome P450 1A2
Human CYP1A2 is one of the major CYPs in human liver and metabolizes a variety of clinically important drugs (e.g., clozapine, tacrine, tizanidine, and theophylline), a number of procarcinogens (e.g. benzo[a]pyre...
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Article
Prediction of Deleterious Non-synonymous Single-Nucleotide Polymorphisms of Human Uridine Diphosphate Glucuronosyltransferase Genes
UDP glucuronosyltransferases (UGTs) are an important class of Phase II enzymes involved in the metabolism and detoxification of numerous xenobiotics including therapeutic drugs and endogenous compounds (e.g. b...
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Article
Role of P-glycoprotein in Limiting the Brain Penetration of Glabridin, An Active Isoflavan from the Root of Glycyrrhiza glabra
Glabridin is a major active constituent of Glycyrrhiza glabra which is commonly used in the treatment of cardiovascular and central nervous system (CNS) diseases. Recently, we have found that glabridin is a subst...
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Article
Intra- and Inter-ethnic Differences in the Allele Frequencies of Cytochrome P450 2B6 Gene in Chinese
This study aimed to investigate the allele frequencies of CYP2B6 gene in 193 Han Chinese and compared with 91 Uygur Chinese. Five single nucleotide polymorphisms of CYP2B6, 64C>T, 516G>T, 777C>A, 785A>G and 1459C...
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Article
Use of in Vitro Critical Inhibitory Concentration, a Novel Approach to Predict in Vivo Synergistic Bactericidal Effect of Combined Amikacin and Piperacillin Against Pseudomonas aeruginosa in a Systemic Rat Infection Model
This study was undertaken to explore the use of in vitro critical inhibitory concentration (CIC) as a surrogate marker relating the pharmacokinetic (PK) parameters to in vivo bactericidal synergistic effect [phar...
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Article
Alteration of the Pharmacokinetics of COL-3, a Matrix Metalloproteinase Inhibitor, Due to Acute Gastrointestinal Toxicity of Doxorubicin
Combination of COL-3, a matrix metalloproteinase inhibitor, and doxorubicin (DOX) might be a promising anticancer regimen. The present study was to examine the potential pharmacokinetic interactions and toxici...
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Article
Human Multidrug Resistance Associated Protein 4 Confers Resistance to Camptothecins
The multidrug resistance associated protein (MRP) 4 is a member of the adenosine triphosphate (ATP)-binding cassette transporter family. Camptothecins (CPTs) have shown substantial anticancer activity against ...
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Article
St. John’s Wort Modulates the Toxicities and Pharmacokinetics of CPT-11 (Irinotecan) in Rats
CPT-11 is a DNA topoisomerase I inhibitor for the therapy of colorectal cancer, whereas St. John’s Wort (Hypericum perforatum, SJW) is a widely used herbal anti-depressant. This study aimed to investigate the eff...
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Article
Herb-Drug Interactions
Herbs are often administered in combination with therapeutic drugs, raising the potential of herb-drug interactions. An extensive review of the literature identified reported herb-drug interactions with clinic...
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Article
Significant Intestinal Excretion, One Source of Variability in Pharmacokinetics of COL-3, a Chemically Modified Tetracycline
This study was undertaken to examine the disposition of COL-3, a chemically modified tetracycline, in order to elucidate its major route of elimination as one possible source of the variability in pharmacokine...
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Article
Transport of thalidomide by the human intestinal Caco-2 monolayers
Studies in patients have indicated that the oral absorption of thalidomide is considerably variable at high doses (>200 mg/day). The aim of this study was to investigate the transport of racemic thalidomide us...
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Article
Mechanism-Based Inhibition of Cytochrome P450 3A4 by Therapeutic Drugs
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the metabolism of about 60% of currently known drugs. However, this unusual low substrate specificity also makes CYP...
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Article
Evidence for Dissolution Rate-Limited Absorption of COL-3, a Matrix Metalloproteinase Inhibitor, Leading to the Irregular Absorption Profile in Rats After Oral Administration
Purpose. This study was undertaken to elucidate the underlying mechanism of the irregular absorption profiles of COL-3, a matrix metalloproteinase inhibitor, with a double- or plateau-peak concentration after a ...