Oral Formulation Roadmap from Early Drug Discovery to Development

Elizabeth Kwong, PhD, retired from Merck & Co., Inc. in 2011, after 23 years of service. She then established her own company, Kwong Eureka Solutions, as a consultant for small start-up companies and specialty drug products. Dr. Kwong is on the Board of Directors for the Canadian Society of Pharmaceutical Scientists and is also an adjunct professor in the Department of Pharmaceutics at the University of Montreal and Department of Chemistry at Concordia University. More recently, Dr. Kwong also co-founded a start-up company, Giiant Pharma, working on delivering a colon specific PDEIV Inhibitor prodrug for the treatment of ulcerative colitis.

List of Contributors vii

Preface ix

1 Introduction 1
Elizabeth Kwong

2 Lead Identification/Optimization 9
Mei Wong and Mark McAllister

3 Oral Drug Formulation Development in Pharmaceutical Lead Selection Stage 39
Shayne Cox Gad

4 Bridging End of Discovery to Regulatory Filing: Formulations for IND-and Registration-Enabling Nonclinical Studies 89
Evan A. Thackaberry

5 Planning the First Clinical Trials with Clinical Manufacturing Organization (CMO) 115
Elizabeth Kwong and Caroline McGregor

6 Formulation Strategies for High Dose Toxicology Studies: Case Studies 139
Dennis H. Leung, Pierre Daublain, Mengwei Hu and Kung]I Feng

7 Formulation, Analytical, and Regulatory Strategies for First-in-Human Clinical Trials 165
Lorenzo Capretto, Gerard Byrne, Sarah Trenfield, Lee Dowden and Steven Booth

Index 243