Emphasizes the integration of major areas of drug discovery and their importance in candidate evaluation It is believed that selecting the "e;right"e; drug candidate for development is the key to success. In the last decade, pharmaceutical R&D departments have integrated pharmacokinetics and drug metabolism, pharmaceutics, and toxicology into early drug discovery to improve the assessment of potential drug compounds. Now, Evaluation of Drug Candidates for Preclinical Development provides a complete view and understanding of why absorption-distribution-metabolism-excretion-toxicology (ADMET) plays a pivotal role in drug discovery and development. Encompassing the three major interrelated areas in which optimization and evaluation of drug developability is most critical pharmacokinetics and drug metabolism, pharmaceutics, and safety assessment this unique resource encourages integrated thinking in drug discovery. The contributors to this volume: Cover drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, stability, drug formulation, preclinical safety assessment, toxicology, and toxicokinetics Address developability issues that challenge pharma companies, moving beyond isolated experimental results Reveal connections between the key scientific areas that are critical for successful drug discovery and development Inspire forward-thinking strategies and decision-making processes in preclinical evaluation to maximize the potential of drug candidates to progress through development efficiently and meet the increasing demands of the marketplace Evaluation of Drug Candidates for Preclinical Development serves as an introductory reference for those new to the pharmaceutical industry and drug discovery in particular. It is especially well suited for scientists and management teams in small- to mid-sized pharmaceutical companies, as well as academic researchers and graduate students concerned with the practical aspects related to the evaluation of drug developability.

Emphasizes the integration of major areas of drug discovery andtheir importance in candidate evaluationIt is believed that selecting the "right" drug candidate fordevelopment is the key to success. In the last decadepharmaceutical R&D departments have integrated pharmacokineticsand drug metabolism, pharmaceutics, and toxicology into early drugdiscovery to improve the assessment of potential drug compounds.Now, Evaluation of Drug Candidates for Preclinical Developmentprovides a complete view and understanding of whyabsorption-distribution-metabolism-excretion-toxicology (ADMET)plays a pivotal role in drug discovery and development.Encompassing the three major interrelated areas in whichoptimization and evaluation of drug developability is mostcritical--pharmacokinetics and drug metabolism, pharmaceuticsand safety assessment--this unique resource encouragesintegrated thinking in drug discovery. The contributors to thisvolume:* Cover drug transporters, cytochrome P-450 and drug-druginteractions, plasma protein binding, stability, drug formulationpreclinical safety assessment, toxicology, and toxicokinetics* Address developability issues that challenge pharma companiesmoving beyond isolated experimental results* Reveal connections between the key scientific areas that arecritical for successful drug discovery and development* Inspire forward-thinking strategies and decision-makingprocesses in preclinical evaluation to maximize the potential ofdrug candidates to progress through development efficiently andmeet the increasing demands of the marketplaceEvaluation of Drug Candidates for Preclinical Development servesas an introductory reference for those new to the pharmaceuticalindustry and drug discovery in particular. It is especially wellsuited for scientists and management teams in small- to mid-sizedpharmaceutical companies, as well as academic researchers andgraduate students concerned with the practical aspects related tothe evaluation of drug developability.

PREFACE.CONTRIBUTORS.1. INTRODUCTION (Charles B. Davis).2. PHARMACOKINETICS IN PRECLINICAL DRUG DEVELOPMENT: ANOVERVIEW (Dion Brocks).3. THE ROLE OF MEMBRANE TRANSPORTERS IN DRUG DISPOSITION(Fanfan Zhou, Peng Duan, and Guofeng You).4. CYTOCHROME P450: STRUCTURE, FUNCTION, AND APPLICATION INDRUG DISCOVERY AND DEVELOPMENT (Ramesh B. Bambal and StephenE. Clarke).5. THE ROLE OF DRUG METABOLISM AND METABOLITE IDENTIFICATIONIN DRUG DISCOVERY (Xiangming Guan).6. PROTEIN BINDING IN DRUG DISCOVERY AND DEVELOPMENT(Vikram Ramanathan and Nimish Vachharajani).7. PREDICTION OF THE PHARMACOKINETICS IN HUMANS (ChaoHan and Ramesh Bambal).8. PHARMACEUTICS DEVELOPABILITY ASSESSMENT (LianHuang, Jinquan Dong, and Shyam Karki).9. SAFETY ASSESSMENT IN DRUG DISCOVERY (Vito G.Sasseville, William R. Foster, and Bruce D. Car).10. ASSESSMENT OF STRATEGIES UTILIZED TO MINIMIZE THEPOTENTIAL FOR INDUCTION OF ACQUIRED LONG QT SYNDROME AND TORSADE DEPOINTES (Khuram W. Chaudhary and Barry S. Brown).INDEX.