Chao Han & Charles B. Davis 
Evaluation of Drug Candidates for Preclinical Development [PDF ebook] 
Pharmacokinetics, Metabolism, Pharmaceutics, and Toxicology

Emphasizes the integration of major areas of drug discovery and
their importance in candidate evaluation

It is believed that selecting the ‘right’ 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.

Tabella dei contenuti

PREFACE.

CONTRIBUTORS.

1. INTRODUCTION (Charles B. Davis).

2. PHARMACOKINETICS IN PRECLINICAL DRUG DEVELOPMENT: AN
OVERVIEW (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 IN
DRUG DISCOVERY AND DEVELOPMENT (Ramesh B. Bambal and Stephen
E. Clarke).

5. THE ROLE OF DRUG METABOLISM AND METABOLITE IDENTIFICATION
IN DRUG DISCOVERY (Xiangming Guan).

6. PROTEIN BINDING IN DRUG DISCOVERY AND DEVELOPMENT
(Vikram Ramanathan and Nimish Vachharajani).

7. PREDICTION OF THE PHARMACOKINETICS IN HUMANS (Chao
Han and Ramesh Bambal).

8. PHARMACEUTICS DEVELOPABILITY ASSESSMENT (Lian
Huang, 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 THE
POTENTIAL FOR INDUCTION OF ACQUIRED LONG QT SYNDROME AND TORSADE DE
POINTES (Khuram W. Chaudhary and Barry S. Brown).

INDEX.

Circa l’autore

Chao Han, PHD, is Associate Director of Pharmacokinetics,
Modeling and Simulation, Clinical Pharmacology Sciences, Centocor
R&D. He has been working in drug discovery and early
development for more than ten years, published over thirty research
articles in peer-reviewed journals, and written three book
chapters.

Charles B. Davis, PHD, heads Drug Metabolism and
Pharmacokinetics for the cancer Metabolism Drug Discovery Unit
within Cancer Research at Glaxo Smith Kline. He has more than twenty
years experience in preclinical and clinical development and has
served on the leadership teams of three of GSK’s Centers of
Excellence in Drug Discovery.

Binghe Want, PHD, is Professor and Georgia research
Alliance Eminent Scholar in Drug Discovery in the Department of
Chemistry, Georgia State University and Georgia cancer Coalition
Distinguished Scientist. He also serves as editor in chief of
Medicinal research Reviews and is lead editor of Drug Delivery:
Principles and Applications (Wiley).