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Rare but impaired flavin-containing monooxygenase 3 (FMO3) variants reported in a recently updated Japanese mega-databank of genome resources
Drug Metab Pharmacokinet. 2023 Dec 22;55:100539. doi: 10.1016/j.dmpk.2023.100539. Online ahead of print.ABSTRACTGenetic variants of human flavin-containing monooxygenase 3 (FMO3) were investigated using an updated Japanese population panel containing 54,000 subjects (the previous panel contained 38,000 subjects). One stop codon mutation and six amino acid-substituted FMO3 variants were newly identified in the updated databank. Of these, two substituted variants (p.Thr329Ala and p.Arg492Trp) were previously identified in compound haplotypes with p.[(Glu158Lys; Glu308Gly)] and were associated with the metabolic disorder trim...
Source: Drug Metabolism and Pharmacokinetics - January 27, 2024 Category: Drugs & Pharmacology Authors: Makiko Shimizu Miaki Makiguchi Eiji Hishinuma Sakae Saito Masahiro Hiratsuka Hiroshi Yamazaki Source Type: research

Exposure-response analysis of the efficacy and safety of esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker, in hypertensive patients with or without diabetic kidney disease
CONCLUSIONS: The exposure-response analyses supported the esaxerenone recommended doses and the safety benefits of using the up-titration regimen.PMID:38245949 | DOI:10.1016/j.dmpk.2023.100535 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - January 21, 2024 Category: Drugs & Pharmacology Authors: Kazutaka Yoshihara Masato Fukae Helen Kastrissios Russell Wada Takako Shimizu Source Type: research

Cross-species drug metabolism and impact of metabolic stability testing under anaerobic condition on predicting pharmacokinetics of keto-enol containing compound in humans
Drug Metab Pharmacokinet. 2023 Nov 21;55:100538. doi: 10.1016/j.dmpk.2023.100538. Online ahead of print.ABSTRACTAfter oral administration of [14C]-S-1360 in rats and dogs, [14C]-S-1360 was absorbed rapidly and the bioavailability was 93.7% in rats and 75.1% in dogs. Based on the results in animals, good systemic exposure would be expected in humans. In contrast to the expectation, the exposure was low in healthy volunteers compared to the exposure expected. In addition, human mass balance study using [14C]-S1360 revealed that a large amount of metabolites existed in human plasma. The major metabolites in human plasma were ...
Source: Drug Metabolism and Pharmacokinetics - January 20, 2024 Category: Drugs & Pharmacology Authors: Takushi Kanazu Junto Tamada Susumu Kume Tohru Mizutare Source Type: research

Quantification of fluticasone propionate in human plasma by LC-MS/MS and its application in the pharmacokinetic study of nasal spray at clinical doses
Drug Metab Pharmacokinet. 2024 Feb;54:100541. doi: 10.1016/j.dmpk.2023.100541. Epub 2023 Dec 11.ABSTRACTWe developed a method for quantifying fluticasone propionate (FP) using general-purpose liquid chromatography-tandem mass spectrometry equipment to measure the plasma concentration of FP for the pharmacokinetic study of FP following the administration of a prescribed nasal spray dose (100 μg). Using ammonium acetate (0.01 M)-formic acid (pH 2.9; 499:1, v/v) and methanol as the mobile phase, 3 pg/mL of FP was quantified. The relative error and standard deviation of the lower limit of quantification were <3.1%. The int...
Source: Drug Metabolism and Pharmacokinetics - December 27, 2023 Category: Drugs & Pharmacology Authors: Aya Yamagata Rena Adachi Akitomo Yokokawa Tomomi Furihata Hiromi Shibasaki Source Type: research

Quantification of fluticasone propionate in human plasma by LC-MS/MS and its application in the pharmacokinetic study of nasal spray at clinical doses
Drug Metab Pharmacokinet. 2023 Dec 11;54:100541. doi: 10.1016/j.dmpk.2023.100541. Online ahead of print.ABSTRACTWe developed a method for quantifying fluticasone propionate (FP) using general-purpose liquid chromatography-tandem mass spectrometry equipment to measure the plasma concentration of FP for the pharmacokinetic study of FP following the administration of a prescribed nasal spray dose (100 μg). Using ammonium acetate (0.01 M)-formic acid (pH 2.9; 499:1, v/v) and methanol as the mobile phase, 3 pg/mL of FP was quantified. The relative error and standard deviation of the lower limit of quantification were <3.1%....
Source: Drug Metabolism and Pharmacokinetics - December 27, 2023 Category: Drugs & Pharmacology Authors: Aya Yamagata Rena Adachi Akitomo Yokokawa Tomomi Furihata Hiromi Shibasaki Source Type: research