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Physiologically based pharmacokinetic modeling to predict complex drug‐drug interactions: a case study of AZD2327 and its metabolite, the competitive and time‐dependent CYP3A inhibitors
In conclusion, this model simulated DDI with less than two‐fold error, indicating that complex clinical DDI associated with multiple mechanisms, pathways, and inhibitors (parent and metabolite) can be predicted using well developed PBPK model. This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - May 1, 2015 Category: Drugs & Pharmacology Authors: Jian Guo, Diansong Zhou, Yan Li, Khanh H. Bui Tags: Original Paper Source Type: research

PBPK modeling of irbesartan: incorporation of hepatic uptake
ABSTRACT Physiological based pharmacokinetic (PBPK) modeling is now commonly used in drug development to integrate human or animal physiological data in order to predict pharmacokinetic profiles. The aim of this work was to construct and refine a PBPK model of irbesartan taking into account its active uptake via OATP1B1/B3 in order to predict more accurately its pharmacokinetic profile using Simcyp®. The activity and expression of the human hepatocyte transporters OATP1B1 and OATP1B3 were studied. RAFs for OATP1B1 and OATP1B3 transporters were calculated, from intrinsic clearances obtained by concentration dependent uptak...
Source: Biopharmaceutics and Drug Disposition - May 1, 2015 Category: Drugs & Pharmacology Authors: Hélène Chapy, Sylvie Klieber, Priscilla Brun, Sabine Gerbal‐Chaloin, Xavier Boulenc, Olivier Nicolas Tags: Original Paper Source Type: research

Verapamil hepatic clearance in four preclinical rat models: towards activity‐based scaling
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - May 1, 2015 Category: Drugs & Pharmacology Authors: J. Nicolaï, T. De Bruyn, P. P. Van Veldhoven, J. Keemink, P. Augustijns, P. Annaert Tags: Original Paper Source Type: research

Plasma vs heart tissue concentration in humans – literature data analysis of drugs distribution
Abstract Little is known about the uptake of drugs into the human heart, although it is of great importance nowadays, when science desires to predict tissue level behavior rather than to measure it. Although the drug concentration in cardiac tissue seems a better predictor for physiological and electrophysiological changes than its level in plasma, knowledge of this value is very limited. Tissue to plasma partition coefficients (Kp) come to rescue since they characterize the distribution of a drug among tissues as being one of the input parameters in physiologically based pharmacokinetic (PBPK) models. The article reviews ...
Source: Biopharmaceutics and Drug Disposition - April 28, 2015 Category: Drugs & Pharmacology Authors: Zofia Tylutki, Sebastian Polak Tags: Invited Review Source Type: research

Safety, Tolerability, and Pharmacokinetics of 2‐Pyridylacetic Acid, a major metabolite of betahistine, in Phase 1 dose escalation study in subjects with ADHD
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 22, 2015 Category: Drugs & Pharmacology Authors: Ganesh Moorthy, Floyd Sallee, Prasad Gabbita, Frank Zemlan, Larry Sallans, Pankaj B. Desai Tags: Original Paper Source Type: research

Induction of Nrf2‐mediated gene expression by dietary phytochemical flavones Apigenin and Luteolin
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 22, 2015 Category: Drugs & Pharmacology Authors: Ximena Paredes‐Gonzalez, Francisco Fuentes, Sundrina Jeffery, Constance Lay‐Lay Saw, Limin Shu, Zheng‐Yuan Su, Ah‐Ng Tony Kong Tags: Original Paper Source Type: research

Projecting human pharmacokinetics of monoclonal antibodies from nonclinical data: comparative evaluation of prediction approaches in early drug development
This article presents a brief overview of the biology and mechanisms of absorption, distribution, metabolism and excretion (ADME) for mAbs. Additionally, we provide a detailed review of mAb human PK/PD prediction from nonclinical data, including allometry for mAbs with linear or nonlinear PK, species‐invariant time method, physiologically based PK (PBPK) modeling and target‐mediated drug disposition (TMDD) model, bioavailability projection and immunogenicity impact on PK prediction. Finally, from an industry perspective a decision tree of mAb human PK projection is proposed to facilitate drug development. This article ...
Source: Biopharmaceutics and Drug Disposition - April 13, 2015 Category: Drugs & Pharmacology Authors: Jing Wang, Suhasini Iyer, Paul J. Fielder, John D. Davis, Rong Deng Tags: Invited Review Source Type: research

Challenges and Advances in the Assessment of the Disposition of Antibody Drug Conjugates
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 1, 2015 Category: Drugs & Pharmacology Authors: Amrita V. Kamath, Suhasini Iyer Tags: Special Issue Article Source Type: research

Gender Differences in the Hepatic Elimination and Pharmacokinetics of Lobeglitazone in Rats
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 1, 2015 Category: Drugs & Pharmacology Authors: Jong‐Hwa Lee, Jun‐Hyeng Son, Yoon‐Jee Chae, Sung Hoon Ahn, Wooin Lee, Dae‐Duk Kim, Suk‐Jae Chung Tags: Short Communication Source Type: research

Pharmacokinetic characterization of BMS‐936561, an anti‐CD70 antibody‐drug conjugate, in preclinical animal species and prediction of its pharmacokinetics in humans
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 1, 2015 Category: Drugs & Pharmacology Authors: Haiqing Wang, Vangipuram S. Rangan, Mei‐Chen Sung, David Passmore, Thomas Kempe, XiaoLi Wang, Lourdes Thevanayagam, Chin Pan, Chetana Rao, Mohan Srinivasan, Sanjeev Gangwar, Shrikant Deshpande, Pina Cardarelli, Punit Marathe, Yang Zheng Tags: Special Issue Article Source Type: research

Investigation of omeprazole and phenacetin first‐pass metabolism in humans using a microscale bioreactor and pharmacokinetic models
Abstract A new in vitro microfluidic platform (integrated insert dynamic microfluidic platform, IIDMP) allowing the co‐culture of intestinal Caco‐2 TC7 cells and of human primary hepatocytes was used to test the absorption and first‐pass metabolism of two drugs: phenacetin and omeprazole. The metabolism of these drugs by CYP1A2, CYP2C19 and CYP3A4 was evaluated by the calculation of bioavailabilities and of intrinsic clearances using a pharmacokinetic (PK) model. To demonstrate the usefulness of the device and of the PK model, predictions were compared with in vitro and in vivo results from the literature. Based on t...
Source: Biopharmaceutics and Drug Disposition - April 1, 2015 Category: Drugs & Pharmacology Authors: Thibault Bricks, Jérémy Hamon, Marie José Fleury, Rachid Jellali, Franck Merlier, Yves Edouard Herpe, Alexandre Seyer, Jean‐Marc Regimbeau, Frédéric Bois, Eric Leclerc Tags: Original Paper Source Type: research

Complex patients ‐ complex DDI: is there a straight way forward?
(Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 12, 2015 Category: Drugs & Pharmacology Authors: Amin Rostami‐Hodjegan Tags: Editorial Commentary Source Type: research

Involvement of microsomal NADPH‐cytochrome P450 reductase in metabolic reduction of drug ketones
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 12, 2015 Category: Drugs & Pharmacology Authors: Matthias Lehr, Jörg Fabian, Walburga Hanekamp Tags: Short Communication Source Type: research

Plasma vs. heart tissue concentration in humans – literature data analysis of drugs distribution
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 12, 2015 Category: Drugs & Pharmacology Authors: Zofia Tylutki, Sebastian Polak Tags: Invited Review Source Type: research

Identification and characterization of in vitro and in vivo metabolites of steroidal alkaloid veratramine
In conclusion, CYP2D6 and SULT2A1 mediated hydroxylation and sulfation were identified as the major biotransformation for veratramine. This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 12, 2015 Category: Drugs & Pharmacology Authors: Chunming Lyu, Wenbin Zhou, Yufeng Zhang, Shen Zhang, Fang Kou, Hai Wei, Ning Zhang, Zhong Zuo Tags: Original Paper Source Type: research