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In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition
In conclusion, B-01 ester compounds may be safe PK boosters with antedrug characteristics.PMID:38663182 | DOI:10.1016/j.dmpk.2024.101005 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Makoto Kataoka Sae Takenaka Shota Fujii Takato Masada Keiko Minami Toshihide Takagi Masaaki Omote Kentaro Kawai Shinji Yamashita Source Type: research
Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery
Drug Metab Pharmacokinet. 2024 Mar 11;56:101008. doi: 10.1016/j.dmpk.2024.101008. Online ahead of print.ABSTRACTWe aimed at predicting the drug-drug interaction (DDI) risk of P-glycoprotein (P-gp) substrates by using P-gp expressing LLC-PK1 cells and its knockout mice (KO). The area under the curve (AUC) of 16 marketed drugs and plasma concentration (Cplasma) of 207 screening compounds, with corrected efflux ratio (CER) ≥ 2, were compared between P-gp KO mice and wild type mice (WT). At permeability (Papp) ≥ 10 × 10-6 cm/s in parent LLC-PK1 cells, AUC ratios (KO/WT) and Cplasma ratios (KO/WT) of these compounds were w...
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Yasuto Kido Isamu Nanchi Takanobu Matsuzaki Ryosuke Watari Hayato Kiyohara Naomi Seki Tomohiko Okuda Source Type: research
In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition
In conclusion, B-01 ester compounds may be safe PK boosters with antedrug characteristics.PMID:38663182 | DOI:10.1016/j.dmpk.2024.101005 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Makoto Kataoka Sae Takenaka Shota Fujii Takato Masada Keiko Minami Toshihide Takagi Masaaki Omote Kentaro Kawai Shinji Yamashita Source Type: research
Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery
Drug Metab Pharmacokinet. 2024 Mar 11;56:101008. doi: 10.1016/j.dmpk.2024.101008. Online ahead of print.ABSTRACTWe aimed at predicting the drug-drug interaction (DDI) risk of P-glycoprotein (P-gp) substrates by using P-gp expressing LLC-PK1 cells and its knockout mice (KO). The area under the curve (AUC) of 16 marketed drugs and plasma concentration (Cplasma) of 207 screening compounds, with corrected efflux ratio (CER) ≥ 2, were compared between P-gp KO mice and wild type mice (WT). At permeability (Papp) ≥ 10 × 10-6 cm/s in parent LLC-PK1 cells, AUC ratios (KO/WT) and Cplasma ratios (KO/WT) of these compounds were w...
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Yasuto Kido Isamu Nanchi Takanobu Matsuzaki Ryosuke Watari Hayato Kiyohara Naomi Seki Tomohiko Okuda Source Type: research
In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition
In conclusion, B-01 ester compounds may be safe PK boosters with antedrug characteristics.PMID:38663182 | DOI:10.1016/j.dmpk.2024.101005 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Makoto Kataoka Sae Takenaka Shota Fujii Takato Masada Keiko Minami Toshihide Takagi Masaaki Omote Kentaro Kawai Shinji Yamashita Source Type: research
Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery
Drug Metab Pharmacokinet. 2024 Mar 11;56:101008. doi: 10.1016/j.dmpk.2024.101008. Online ahead of print.ABSTRACTWe aimed at predicting the drug-drug interaction (DDI) risk of P-glycoprotein (P-gp) substrates by using P-gp expressing LLC-PK1 cells and its knockout mice (KO). The area under the curve (AUC) of 16 marketed drugs and plasma concentration (Cplasma) of 207 screening compounds, with corrected efflux ratio (CER) ≥ 2, were compared between P-gp KO mice and wild type mice (WT). At permeability (Papp) ≥ 10 × 10-6 cm/s in parent LLC-PK1 cells, AUC ratios (KO/WT) and Cplasma ratios (KO/WT) of these compounds were w...
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Yasuto Kido Isamu Nanchi Takanobu Matsuzaki Ryosuke Watari Hayato Kiyohara Naomi Seki Tomohiko Okuda Source Type: research
In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition
In conclusion, B-01 ester compounds may be safe PK boosters with antedrug characteristics.PMID:38663182 | DOI:10.1016/j.dmpk.2024.101005 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Makoto Kataoka Sae Takenaka Shota Fujii Takato Masada Keiko Minami Toshihide Takagi Masaaki Omote Kentaro Kawai Shinji Yamashita Source Type: research
Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery
Drug Metab Pharmacokinet. 2024 Mar 11;56:101008. doi: 10.1016/j.dmpk.2024.101008. Online ahead of print.ABSTRACTWe aimed at predicting the drug-drug interaction (DDI) risk of P-glycoprotein (P-gp) substrates by using P-gp expressing LLC-PK1 cells and its knockout mice (KO). The area under the curve (AUC) of 16 marketed drugs and plasma concentration (Cplasma) of 207 screening compounds, with corrected efflux ratio (CER) ≥ 2, were compared between P-gp KO mice and wild type mice (WT). At permeability (Papp) ≥ 10 × 10-6 cm/s in parent LLC-PK1 cells, AUC ratios (KO/WT) and Cplasma ratios (KO/WT) of these compounds were w...
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Yasuto Kido Isamu Nanchi Takanobu Matsuzaki Ryosuke Watari Hayato Kiyohara Naomi Seki Tomohiko Okuda Source Type: research
In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition
In conclusion, B-01 ester compounds may be safe PK boosters with antedrug characteristics.PMID:38663182 | DOI:10.1016/j.dmpk.2024.101005 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Makoto Kataoka Sae Takenaka Shota Fujii Takato Masada Keiko Minami Toshihide Takagi Masaaki Omote Kentaro Kawai Shinji Yamashita Source Type: research
Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery
Drug Metab Pharmacokinet. 2024 Mar 11;56:101008. doi: 10.1016/j.dmpk.2024.101008. Online ahead of print.ABSTRACTWe aimed at predicting the drug-drug interaction (DDI) risk of P-glycoprotein (P-gp) substrates by using P-gp expressing LLC-PK1 cells and its knockout mice (KO). The area under the curve (AUC) of 16 marketed drugs and plasma concentration (Cplasma) of 207 screening compounds, with corrected efflux ratio (CER) ≥ 2, were compared between P-gp KO mice and wild type mice (WT). At permeability (Papp) ≥ 10 × 10-6 cm/s in parent LLC-PK1 cells, AUC ratios (KO/WT) and Cplasma ratios (KO/WT) of these compounds were w...
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Yasuto Kido Isamu Nanchi Takanobu Matsuzaki Ryosuke Watari Hayato Kiyohara Naomi Seki Tomohiko Okuda Source Type: research
In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition
In conclusion, B-01 ester compounds may be safe PK boosters with antedrug characteristics.PMID:38663182 | DOI:10.1016/j.dmpk.2024.101005 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Makoto Kataoka Sae Takenaka Shota Fujii Takato Masada Keiko Minami Toshihide Takagi Masaaki Omote Kentaro Kawai Shinji Yamashita Source Type: research
Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery
Drug Metab Pharmacokinet. 2024 Mar 11;56:101008. doi: 10.1016/j.dmpk.2024.101008. Online ahead of print.ABSTRACTWe aimed at predicting the drug-drug interaction (DDI) risk of P-glycoprotein (P-gp) substrates by using P-gp expressing LLC-PK1 cells and its knockout mice (KO). The area under the curve (AUC) of 16 marketed drugs and plasma concentration (Cplasma) of 207 screening compounds, with corrected efflux ratio (CER) ≥ 2, were compared between P-gp KO mice and wild type mice (WT). At permeability (Papp) ≥ 10 × 10-6 cm/s in parent LLC-PK1 cells, AUC ratios (KO/WT) and Cplasma ratios (KO/WT) of these compounds were w...
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Yasuto Kido Isamu Nanchi Takanobu Matsuzaki Ryosuke Watari Hayato Kiyohara Naomi Seki Tomohiko Okuda Source Type: research
Unveiling the intra-tumor fate of trastuzumab deruxtecan in a xenograft model to support its mechanism of action
Drug Metab Pharmacokinet. 2024 Jan 23;56:101001. doi: 10.1016/j.dmpk.2024.101001. Online ahead of print.ABSTRACTTrastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate used for cancer treatment comprising an anti-human epidermal growth factor receptor type 2 (HER2) antibody and the topoisomerase I inhibitor DXd. The present study investigated the intratumor fate of T-DXd. Fluorescence-labeled T-DXd was found to accumulate in tumors of HER2-positive tumor xenograft mice and was observed to be distributed within lysosomes of in vitro tumor cells in accordance with their HER2 expression. DXd was released by cysteine prot...
Source: Drug Metabolism and Pharmacokinetics - April 21, 2024 Category: Drugs & Pharmacology Authors: Yoko Nagai Masataka Oitate Takahiro Shibayama Hideo Takakusa Nobuaki Watanabe Source Type: research