Overview

Pharmacokinetics (PK) and pharmacodynamics (PD) play a key role in drug development, and a good understanding of the implications of PK/PD data is crucial when designing clinical trials or preparing a drug submission dossier. As a professional working with PK/PD data on a regular basis, you must have a solid understanding of the topic to communicate effectively with the development teams – a daunting and challenging task, due to the breadth and complexity of the topic area.

This course assumes no prior PK knowledge and aims to give you a broad understanding of this fascinating subject, using multiple case studies and relevant examples. You will learn what pharmacokinetics involves, what data is collected, and its impact on the drug development process. By learning these skills, you will be able to understand, communicate, and challenge the data presented to you.

Why Should You Attend

To get a better understanding of the different aspects that contribute to the pharmacokinetic profile of a new chemical entity. PK studies asses drug exposure to facilitate drug development. PK studies offer great support to learn and confirm the key characteristics of new molecular entities in a quantitative manner. This provides evidences for optimizing drug development plans and enabling critical decision-making. Drug development without PK is considered at a higher risk of failure.

Key Learning Objectives

The course reviews the general concepts and basic elements of pharmacokinetics. The course will describe the processes that a drug undergoes after administration such as the absorption (when not administered intravenously), the distribution, including plasma protein binding, the metabolism (the biotransformation of the drug into its metabolites) and the excretion (via the bile in faces and via the kidney in urine). The use of PK during drug development will also be described. PK studies can facilitate knowledge management and decision making to streamline drug discovery and development and to reduce the attrition rate. The following topics will be discussed in details:

  • Absorption
  • Distribution
  • Metabolism
  • Excretion
  • Volume of distribution
  • Plasma protein binding
  • Clearance
  •  Elimination half-life

Agenda

THE ROLE OF PK IN DRUG DEVELOPMENT

  • What is PK?
  • Pharmacology, pharmacodynamics, and pharmacokinetics
  • Definitions

UNDERSTAND THE PK/PD MODEL OF THERAPEUTICS

  • Dose, concentration, biophase, effect, clinical endpoints

 THE IMPORTANCE OF PK THROUGHOUT DRUG R&D

  • The Increasing Importance of PK In the Go/No Go Decision
  • Inter disciplinary Interaction in The Pharmaceutical Industry – Let’s all Speak the Same Language
  • PK and the Regulatory Authorities
  • PK As a Strategy Tool
  • How PK Knowledge Is Used to Reduce Time and Cost

WHAT DO WE MEASURE AND HOW DO WE MEASURE IT?

Fundamentals of Pharmacokinetics:

ABSORPTION

  • Administration routes: oral, intravenous, parenteral, local
  • Site of absorption
  • Factors affecting the absorption
  • Molecular weight
  • Solubility
  • Permeability
  • Ionization
  • Bioavailability: rate and extent
  • Drug transporters: how do they affect drug absorption?

DISTRIBUTION

  • Physiology of distribution processes
  • Physiological values of distribution volumes
  • Plasma protein binding why do we measure it?
  • Drug transporters: how do they affect drug distribution?
  • Volume of distribution of small molecule vs biological products

METABOLISM

  • Physiology of metabolic processes
  • Phase 1 and Phase 2 metabolism
  • Metabolic enzymes
  • Liver first pass effect
  • Metabolite identification: always possible?
  • Pharmacologically active metabolites
  • Toxic metabolites
  • Drug transporters: how do they affect drug metabolism?
  • What the Regulatory Authorities require?

ELIMINATION

  • Physiology of elimination processes
  • Biliary elimination
  • Enterohepatic cycling
  • Urinary excretion, active secretion, and reabsorption
  • Physiological values describing the elimination processes
  • Drug transporters: how do they affect elimination?
  • Is elimination always necessary?

MAIN PHARMACOKINETIC PARAMETERS

  • Basic Terminology Such as Half-Life, Clearance, and Volume of Distribution
  • Physiological relevance and interrelationship between clearance, volume of distribution, and half-life
  • Total plasma clearance, hepatic clearance, renal clearance

Who Will Benefit

Clinical research associates, medicinal chemists, pharmacologists, toxicologists, project managers, business development managers, medical writers.

FDA Faculty Dr. Stefano Persiani

Faculty Dr. Stefano Persiani 

Internal & External Innovation, Director Translational Sciences and Pharmacokinetics at Rottapharm Biotech

Italy

Dr. Stefano Persiani is currently Director of Translational Sciences and Pharmacokinetics at Rottapharm Biotech, Italy. He graduated in Pharmacy at the University of Milan, Italy and completed a Post-Doctoral fellowship in the Department of Pathology of the University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA, and later as a Research Associate in the Department of Pharmaceutics of the University of Southern California, School of Pharmacy in Los Angeles, California, USA. After these academic positions, he entered the pharmaceutical industry at Farmitalia Carlo Erba, Pharmacia, Upjohn, and Zambon Group and in the CRO sector as Scientific Director for Clinical Pharmacology

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