DMPK and PK/PD in Drug Discovery: Principles, Strategy, and Translation -

About Course

DMPK and PK/PD in Drug Discovery: Principles, Strategy, and Translation is a comprehensive, self-paced course designed to build a practical understanding of how drug disposition, systemic and tissue exposure, pharmacological response, and biomarkers influence drug discovery and development decisions.

Designed for PhD students, postdoctoral researchers, pharmacologists, biologists, preclinical scientists, and professionals interested in pharmaceutical and biotechnology drug discovery, this course connects fundamental DMPK and PK/PD principles with real-world preclinical and translational applications.

Through six structured modules, you will explore:

The role of DMPK and pharmacokinetics in drug discovery
ADME, drug disposition, metabolism, distribution, and clearance
Preclinical PK study design and interpretation
Pharmacodynamics, target engagement, and biomarker strategies
PK/PD integration and exposure–response relationships
Translational DMPK, dose selection, and development decision-making

Real-world examples, published research, representative datasets, scientific case studies, quizzes, and curated learning materials are integrated throughout the course.

By the end of the course, you will be able to understand and interpret key DMPK, PK, PD, biomarker, and exposure–response concepts and recognize how these data are integrated to support drug discovery, candidate selection, and translational development.

Course Content

Foundations of DMPK and Pharmacokinetics in Drug Discovery
This module establishes the fundamental principles of DMPK and pharmacokinetics and their roles within a drug discovery program. Learners will understand how drug exposure is generated, described, and used to answer fundamental questions about the behavior of a therapeutic candidate in vivo.

Role of DMPK and Pharmacokinetics in Drug Discovery
Absorption, Distribution, Metabolism, and Excretion (ADME)
Fundamental Pharmacokinetic Parameters and Concentration–Time Profiles
Route of Administration, Bioavailability, and Drug Exposure

Drug Disposition: Molecular Properties, Distribution, Metabolism, and Clearance
This module examines the biological and physicochemical factors that determine observed drug exposure. Learners move beyond describing a PK curve to understanding why a compound behaves the way it does in vivo.

Preclinical Pharmacokinetic Study Design and Data Interpretation
This module translates pharmacokinetic principles into experimental strategy. Learners will understand how preclinical PK studies are designed, how samples and concentration–time data are generated, and how study-design decisions influence the reliability and interpretation of PK results.

Pharmacodynamics, Target Engagement, and Biomarker Strategy
This module connects drug exposure with biological activity. Learners will understand the distinction between administering a dose, achieving exposure, engaging a therapeutic target, producing a pharmacodynamic response, and ultimately generating a therapeutic effect.

PK/PD Integration and Exposure–Response Relationships
This module integrates pharmacokinetics and pharmacodynamics to determine whether sufficient drug exposure produces the intended biological and therapeutic response. Learners will begin using PK/PD evidence to interpret efficacy and understand why a compound succeeds or fails in a pharmacology study.

Translational DMPK and PK/PD in Drug Development
This module integrates the course concepts and introduces how preclinical DMPK and PK/PD evidence contributes to candidate selection, dose strategy, safety margins, and translation toward human development.

DMPK and PK/PD in Drug Discovery: Principles, Strategy, and Translation

About Course

Through six structured modules, you will explore:

Course Content

Role of DMPK and Pharmacokinetics in Drug Discovery

Absorption, Distribution, Metabolism, and Excretion (ADME)

Fundamental Pharmacokinetic Parameters and Concentration–Time Profiles

Route of Administration, Bioavailability, and Drug Exposure

Drug Disposition: Molecular Properties, Distribution, Metabolism, and Clearance
This module examines the biological and physicochemical factors that determine observed drug exposure. Learners move beyond describing a PK curve to understanding why a compound behaves the way it does in vivo.

Physicochemical Properties, Solubility, and Permeability

Plasma Protein Binding and Tissue Distribution

Drug Metabolism, Metabolic Stability, and Species Differences

Clearance, Elimination, and Their Impact on Drug Exposure

Objectives and Design of Preclinical PK Studies

Sampling Strategy and Generation of Concentration–Time Profiles

Dose–Exposure Relationships, Dose Proportionality, and Accumulation

Bioanalysis, Data Quality, and Fundamentals of PK Analysis

Fundamentals of Pharmacodynamics and Drug Response

Target Engagement and Mechanism-Based Pharmacology

Biomarkers in Preclinical and Translational Drug Discovery

Temporal Relationships Between Exposure and Pharmacological Response

Principles of PK/PD Integration

Exposure–Response and Exposure–Efficacy Relationships

Design of Integrated PK/PD Studies

Interpretation of PK/PD Data for Drug Discovery Decisions

Translational DMPK and PK/PD in Drug Development
This module integrates the course concepts and introduces how preclinical DMPK and PK/PD evidence contributes to candidate selection, dose strategy, safety margins, and translation toward human development.

Species Differences and Translation of Preclinical Pharmacokinetics

Efficacious Exposure, Therapeutic Window, and Dose Selection

Preclinical-to-Human Translation and Human PK Prediction

Integrated DMPK and PK/PD Case Study: From Compound Evaluation to Development Decision

About Course

Through six structured modules, you will explore:

Course Content

Role of DMPK and Pharmacokinetics in Drug Discovery

Absorption, Distribution, Metabolism, and Excretion (ADME)

Fundamental Pharmacokinetic Parameters and Concentration–Time Profiles

Route of Administration, Bioavailability, and Drug Exposure

Drug Disposition: Molecular Properties, Distribution, Metabolism, and Clearance This module examines the biological and physicochemical factors that determine observed drug exposure. Learners move beyond describing a PK curve to understanding why a compound behaves the way it does in vivo.

Physicochemical Properties, Solubility, and Permeability

Plasma Protein Binding and Tissue Distribution

Drug Metabolism, Metabolic Stability, and Species Differences

Clearance, Elimination, and Their Impact on Drug Exposure

Objectives and Design of Preclinical PK Studies

Sampling Strategy and Generation of Concentration–Time Profiles

Dose–Exposure Relationships, Dose Proportionality, and Accumulation

Bioanalysis, Data Quality, and Fundamentals of PK Analysis

Fundamentals of Pharmacodynamics and Drug Response

Target Engagement and Mechanism-Based Pharmacology

Biomarkers in Preclinical and Translational Drug Discovery

Temporal Relationships Between Exposure and Pharmacological Response

Principles of PK/PD Integration

Exposure–Response and Exposure–Efficacy Relationships

Design of Integrated PK/PD Studies

Interpretation of PK/PD Data for Drug Discovery Decisions

Translational DMPK and PK/PD in Drug Development This module integrates the course concepts and introduces how preclinical DMPK and PK/PD evidence contributes to candidate selection, dose strategy, safety margins, and translation toward human development.

Species Differences and Translation of Preclinical Pharmacokinetics

Efficacious Exposure, Therapeutic Window, and Dose Selection

Preclinical-to-Human Translation and Human PK Prediction

Integrated DMPK and PK/PD Case Study: From Compound Evaluation to Development Decision

Start Your Scientific Excellence Journey

Drug Disposition: Molecular Properties, Distribution, Metabolism, and Clearance
This module examines the biological and physicochemical factors that determine observed drug exposure. Learners move beyond describing a PK curve to understanding why a compound behaves the way it does in vivo.

Translational DMPK and PK/PD in Drug Development
This module integrates the course concepts and introduces how preclinical DMPK and PK/PD evidence contributes to candidate selection, dose strategy, safety margins, and translation toward human development.