PK/PD in Drug Research & Development

Description of the Course:

The primary objective of PK/PD modeling is the prediction of the time course of the drug effect and its relation to dose and exposure. PK/PD modeling has become a key success factor in drug R&D. PK/PD represents and extremely useful tool for the selection of drug candidates, their optimization, and for maximal exploitation of early clinical studies for an optimal design of pivotal Phase 3 trials. PK/PD relies on prior in vitro bioassays, animal, and early clinical studies. PK/PD modeling is part of pharmacometrics and can be based also on the patho-physiological mechanisms and progression of the disease to predict therapeutic effects.

This comprehensive and detailed two-day course describes the PK/PD studies from an industrial perspective to achieve a successful regulatory submission. The course is intended for those that have a previous background in PK/PD but also for those who wish to get an in-depth training in PK/PD whilst not being specialists in the field.

The course will provide a review of the PK processes and of PD studies from a pharmacological perspective. Preclinical PK/PD studies including the role of radiolabelled studies and the evaluation of pharmacologically active and/or toxic metabolites and toxicokinetics will be described.

The dose-exposure-effects will be explained through physiologically- and mechanism-based PK/PD modelling to design first-in human and later clinical trials. Clockwise and counterclockwise hysteresis as common forms of PK/PD correlations will be covered as well as the use of biomarkers to assess target occupancy and their difference from surrogate endpoints. The application of MRSD and MABEL approaches and microdosing as regulatory requirements and tools for a correct design and conduction of early clinical trials, will be explained.

Biological and advanced therapies are becoming more important, and the course will provide an overview of PK/PD studies for these new agents. The scientific background, study design, and data interpretation for population pharmacokinetics will be covered. Finally, the course will describe how the potential for a NCE to exert drug-drug interaction is assessed in pre- and clinical development.

Attendance will provide an overview of the above topics including temporal placement throughout the drug R&D program. This will be done without excessive use of mathematics. The course will provide trouble-shooting strategies for all the main studies and will focus on the critical aspect for a smooth conduction, interpretation, and use of PK/PD for the successful selection and registration of New Chemical and Biological Entities.

Learning objectives

By the end of this two-day intensive course, you will get:

• An understanding the PK/PD studies in drug R&D from an industrial perspective.
• A deeper insight into the optimal strategies to design and interpret the relevant PK/PD studies.
• An appreciation of the role of biomarkers in drug R&D and their optimal use for study design and outcome evaluation.
• An overview of the crucial aspects of the first in human study design, conduction, and interpretation.
• Answers to your questions on the differences between small molecules and biological and advanced therapies as far as PK/PD are concerned.
• A coverage of how drug interaction occurs and how to predict them during drug R&D.

This course is right for you if:

• You want to understand the values of PK/PD studies in drug R&D from an industrial perspective.
• ‍You want to explore the optimal strategies to select, design, conduct and interpret the relevant preclinical and clinical PK/PD studies.
• You want to assess the role of biomarkers in drug R&D and their optimal use for study design and outcome evaluation.
• You want to understand the crucial aspects of the first in human study design, conduction, and interpretation including regulatory authorization.
• You want to avoid failure of PK/PD studies conducted either in-house or contracted externally.
• You want to understand the differences between small molecules and biological and advanced therapies as far as PK/PD are concerned.
• You want to understand drug interaction and how to predict them early to avoid R&D programs delays.

Who Should Attend?

This course has been specifically designed to address the needs of those working in the following areas:

• Regulatory
• Medical Affairs
• Licensing
• Project Management
• Outsourcing
• Pre-clinical Discovery and Development
• Clinical Research and Development
• Medical Writing

‍Draft Schedule:

DAY 1:

Session 1. Fundamentals of Pharmacokinetics

• An understanding the PK/PD studies in drug R&D from an industrial perspective.
• ‍Absorption, Distribution, Metabolism and Excretion.
• Critical aspects in relation to PK/PD, tissue distribution and plasma protein binding.
• PK after oral/intravenous dosing.
• PK after single/repeated doses. Accumulation and superposition principles.
• Absolute and relative bioavailability, and PK linearity.
• Study design, PK models, results interpretation, and relevance for PK/PD.

Coffee break 15:15-15:30

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