In Silico Prediction of Pharmacokinetic Profile for Human Oral Drug Candidates Which Lack Clinical Pharmacokinetic Experiment Data
ConclusionIn conclusion, we generated practical guidance on applying two mainstream software packages, ADMET Predictor and SimCYP, to construct PBPK models for drugs or drug candidates that lack ADME parameters in model construction. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 16, 2022 Category: Drugs & Pharmacology Source Type: research

Population Pharmacokinetic Model for Tramadol and O-desmethyltramadol in Older Patients
ConclusionExposure to tramadol increased with increased frailty and reduced CrCL. Prescribers should consider patients frailty status and CrCL to minimise the risk of tramadol toxicity in such cohort of patients. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 15, 2022 Category: Drugs & Pharmacology Source Type: research

Clinical and Nonclinical Disposition and In Vitro Drug-Drug Interaction Potential of Felcisetrag, a Highly Selective and Potent 5-HT4 Receptor Agonist
ConclusionsFelcisetrag is primarily cleared in humans through renal excretion. Although the metabolism of felcisetrag is primarily through CYP3A, the potential for clinically relevant DDI as a victim is significantly reduced as metabolism plays a minor role in the overall clearance.Graphical Abstract (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 14, 2022 Category: Drugs & Pharmacology Source Type: research

Inhibition of Cytochrome P450s by Strobilanthes crispus Sub-Fraction (F3): Implication for Herb –Drug Interaction
ConclusionTaken together, the results revealed a low probability of inhibition by F3 on CYP enzymes involved in tamoxifen metabolism. However, further in vivo investigation is necessary for potential F3 interaction with CYP2C9. The utility of a preliminary in vitro approach in the assessment of potential HDI was demonstrated in this study. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 11, 2022 Category: Drugs & Pharmacology Source Type: research

Predicting the Drug Clearance Pathway with Structural Descriptors
ConclusionThe developed model can be used to find the clearance pathways of new drug candidates with acceptable accuracy. The main descriptors that are used to evaluate this parameter are the hydrophobicity and the number of hydrogen-bonding functional groups of the compound. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 11, 2022 Category: Drugs & Pharmacology Source Type: research

Prediction of Drug –Drug Interaction Between Dabrafenib and Irinotecan via UGT1A1-Mediated Glucuronidation
ConclusionDabrafenib is a potent noncompetitive inhibitor of UGT1A1 and may bring potential risk of DDI when combined with irinotecan. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 11, 2022 Category: Drugs & Pharmacology Source Type: research

Inhibition of Cytochrome P450s by Strobilanthes crispus Sub-Fraction (F3): Implication for Herb –Drug Interaction
ConclusionTaken together, the results revealed a low probability of inhibition by F3 on CYP enzymes involved in tamoxifen metabolism. However, further in vivo investigation is necessary for potential F3 interaction with CYP2C9. The utility of a preliminary in vitro approach in the assessment of potential HDI was demonstrated in this study. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 11, 2022 Category: Drugs & Pharmacology Source Type: research

Predicting the Drug Clearance Pathway with Structural Descriptors
ConclusionThe developed model can be used to find the clearance pathways of new drug candidates with acceptable accuracy. The main descriptors that are used to evaluate this parameter are the hydrophobicity and the number of hydrogen-bonding functional groups of the compound. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 11, 2022 Category: Drugs & Pharmacology Source Type: research

Prediction of Drug –Drug Interaction Between Dabrafenib and Irinotecan via UGT1A1-Mediated Glucuronidation
ConclusionDabrafenib is a potent noncompetitive inhibitor of UGT1A1 and may bring potential risk of DDI when combined with irinotecan. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 11, 2022 Category: Drugs & Pharmacology Source Type: research

The Effects of AT-533 and AT-533 gel on Liver Cytochrome P450 Enzymes in Rats
ConclusionsAT-533 and AT-533 gel did not have any effect on CYP activity and may be considered safe for external use in gel form, as an alternative to conventional treatment. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 9, 2022 Category: Drugs & Pharmacology Source Type: research

Effects and Mechanism of Action of Panax notoginseng Saponins on the Pharmacokinetics of Warfarin
ConclusionPNS can increase the blood concentration of warfarin, as well as the exposure time, and it can enhance the anticoagulant effect of warfarin by inhibiting the expression of the liver enzyme CYP3A4. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 9, 2022 Category: Drugs & Pharmacology Source Type: research

The Effects of AT-533 and AT-533 gel on Liver Cytochrome P450 Enzymes in Rats
ConclusionsAT-533 and AT-533 gel did not have any effect on CYP activity and may be considered safe for external use in gel form, as an alternative to conventional treatment. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 9, 2022 Category: Drugs & Pharmacology Source Type: research