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1. 直接経口抗凝固薬（DOAC）と非経口直接作用型抗凝固薬：用量および副作用direct oral anticoagulants doacs and parenteral direct acting anticoagulants dosing and adverse effects [show details]
… and serum creatinine . P-glycoprotein inhibitors or inducers – Dabigatran is a substrate for P-glycoprotein. Concomitant use of dabigatran with P-glycoprotein inducers (eg, rifampin) reduces the …
2. 痛風発作の治療treatment of gout flares [show details]
… result in adverse interactions, with increased colchicine levels, include: P-gp inhibitors – More commonly used inhibitors of P-gp include macrolide antibiotics (azithromycin, clarithromycin, erythromycin) …
3. 急性骨髄性白血病の予後prognosis of acute myeloid leukemia [show details]
… combination was more common in the older patient. There are a number of inhibitors of PgP mediated drug efflux that have been evaluated in randomized clinical trials. Unfortunately, these studies did not …
4. 心房細動：血栓塞栓症予防のための抗凝固療法atrial fibrillation anticoagulant therapy to prevent thromboembolism [show details]
…substrates of P-glycoprotein (P-gp) efflux pump and subject to pharmacokinetic drug interactions, although fewer in number than warfarin interactions. Drugs that inhibit CYP3A4 metabolism or P-gp efflux can …
5. ジゴキシンによる治療：初回投与、モニタリング、および用量変更treatment with digoxin initial dosing monitoring and dose modification [show details]
… no dose adjustment is necessary. There are a number of important drug interactions: Inhibitors of P-glycoprotein efflux transporters (eg, amiodarone, dronedarone, propafenone, quinidine, and verapamil) …

English Journal

Molecular pharmacokinetic mechanism of the drug-drug interaction between genistein and repaglinide mediated by P-gp.

Jin H, Zhu Y, Wang C, Meng Q, Wu J, Sun P, Ma X, Sun H, Huo X, Liu K, Tan A.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2020 May;125()110032.
This study was devised to investigate if P-glycoprotein (P-gp) mediated the drug-drug interaction (DDI) between genistein and repaglinide. When genistein was added, the plasma concentrations of repaglinide in rats were increased. The maximum plasma concentration (Cmax) of repaglinide increased from
PMID 32187961

Donepezil, a cholinesterase inhibitor used in Alzheimer's disease therapy, is actively exported out of the brain by abcb1ab p-glycoproteins in mice.

Spieler D, Namendorf C, Namendorf T, von Cube M, Uhr M.
Journal of psychiatric research. 2020 May;124()29-33.
Polymorphisms in the drug transporter gene ABCB1 predict the treatment response of selected antidepressants and limit anticonvulsive medication's effectiveness. The ABCB1 locus encodes the energy-dependent transporter P-glycoprotein (P-gp) of the blood brain barrier (BBB), which serves as an efflux
PMID 32114029

The characteristics and mechanism of co-administration of lovastatin solid dispersion with kaempferol to increase oral bioavailability.

Li J, Di L, Cheng X, Ji W, Piao H, Cheng G, Zou M.
Xenobiotica; the fate of foreign compounds in biological systems. 2020 May;50(5)593-601.
Lovastatin shows low bioavailability (lower than 5%) after oral administration because of the poor aqueous solubility and widely metabolized by CYP3A4.Lovastatin solid dispersion was designed to enhance the dissolution. The intestinal absorption study indicated an increase in the apparent permeabil
PMID 31505985

Japanese Journal

Preliminary in Vitro Assessment of the Potential of EST64454, a Sigma-1 Receptor Antagonist, for Pharmacokinetic Drug–Drug Interactions

Yeste Sandra,Reinoso Raquel F.,Ayet Eva,Pretel Maria Jose,Balada Ariadna,Serafini Maria Teresa
Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 43(1), 68-76, 2020
… EST64454 is a selective sigma-1 receptor ligand intended for orally administered pain treatment that showed a promising profile in the lead optimization process. … between 100 and 1000 µM) and as time-dependent inhibitor (IC50 … EST64454 was not a P-glycoprotein (P-gp) substrate and was highly permeable in Caco-2 cells. …
NAID 130007779199

Continuous Cytostatic Effects of BCR-ABL Tyrosine Kinase Inhibitors (TKIs) after Washout in Human Leukemic K562 Cells

Aoyama Tsuyoshi,Shibayama Yoshihiko,Furukawa Tatsuhiko,Sugawara Mitsuru,Takekuma Yoh
Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 42(11), 1805-1813, 2019
… Tyrosine kinase inhibitors (TKIs) are used as the first choice for chronic myeloid leukemia (CML) pharmacotherapeutics. … These results suggest that a good response in patients with a low serum concentration of imatinib, nilotinib or dasatinib may be due to the cytostatic effect of that drug continues even after its disappearance in plasma. …
NAID 130007740590

胆汁酸トランスポーター阻害薬エロビキシバット（グーフィス®錠5 mg）の薬理学的特性及び臨床試験成績

池田尚紀,谷口真也,関光徳
日本薬理学雑誌 153(3), 129-138, 2019
… エロビキシバット（グーフィス®錠5 mg）は，胆汁酸の再吸収に係わるトランスポーター（IBAT）の阻害作用を有する新規低分子化合物であり，慢性便秘症を適応として世界で初めて日本で承認された．エロビキシバットはin vitroで選択的にIBATを阻害し，in vivoで用量依存的に胆汁酸の吸収抑制作用を示し，ラットロペラミド誘発便秘モデルにおいて糞便湿重量を用量依存的に増加させた．エロビキ …
NAID 130007610697