Courses

Instructor: Kristen Gilliland 

The impact that modern medicines have had on disease and conditions over the last two centuries has increased life expectancy in situations that gave little hope.  We have seen cancer treatments dramatically improve survival rates and people diagnosed with HIV able to live productive and long lives all due to modern drug discovery.

The Introduction to Drug Discovery and Development course will paint a general overview of what is required to create a successful pharmaceutical drug discovery and development program – from drug inception to market. Students will learn how the success of the program depends upon proper communication and understandings between medicinal chemists, biologists and pharmacologists.  Each student will appreciate the immense difficulties, regulations, laboratory efforts, patience and cost required in producing a successful pharmaceutical drug. A real-world example involving the development of a GlyT1 Inhibitor for the treatment of schizophrenia will illustrate these unique challenges as seen in each stage of the drug discovery and development process.

By the end of this course, you should be able to: 

• Describe the various factors that contribute to the limited success rate of drugs reaching the market, including regulatory challenges, clinical trial outcomes and cost considerations.
• Recognize the regulatory acts that govern drug discovery and development.
• Describe the different stages in drug discovery and development.
• Identify the processes involved and milestones associated with each stage of the drug discovery and development pipeline.
• Describe the critical role of medicinal chemistry, pharmacology and biology in the success of a drug campaign, illustrating how each discipline contributes to the overall process.

Instructor: Colleen Niswender and Olivier Boutaud 

In this course, you will uncover the fundamental principles that drive the development of new therapeutics. This course will start a discussion on proteins and how their structure influences their function, revealing why they are crucial targets for drug development. Next, you will explore enzymes, what they are and examine how their kinetics can be influenced by orthosteric and allosteric modulators. Understanding these dynamics is key to manipulating biochemical pathways for therapeutic purposes. Finally, the focus will turn to receptors and the interactions between receptors and ligands, as we unravel the interconnected concepts like potency, efficacy, and binding.

By the end of this course, you should be able to:

• Explain how enzymes catalyze chemical reactions and classify them based on their catalytic mechanisms.
•  Interpret pharmacological concepts related to protein structure-function relationships, enzyme and receptor roles and druggable targets.
• Differentiate major mechanisms of enzyme inhibition (competitive, noncompetitive, uncompetitive and mixed) and analyze their effects on kinetic parameters (Km, Vmax) using Michaelis–Menten and Lineweaver–Burk plots.
• Apply receptor-occupancy theory to interpret concentration–response curves for orthosteric and allosteric ligands and evaluate mechanisms of receptor regulation.
• Utilize the concepts of receptor expression, ligand affinity and possible multiple binding sites for translational in vivo pharmacology studies.

Instructor: Rachel Crouch

Have you ever wondered what your body does to a drug once ingested? The Introduction to Drug Metabolism and Pharmacokinetics (DMPK) will educate you on how a drug is both metabolized and processed by the body. In addition, you will learn essential DMPK parameters and properties that suggest whether a compound has suitable drug like properties. The discipline of DMPK is essential in determining which compounds in drug discovery process would be suitable candidates for advancement into the drug development process.

By the end of this course, you should be able to:

Describe the processes of absorption, distribution, metabolism and excretion (ADME) and the role that they play in the safety and effectiveness of a drug. 

• Describe the basic pharmacokinetic parameters that are governed by ADME, how they are determined from a plasma concentration versus time curve and their role in drug discovery and development.
• Explain the concept of drug metabolism as it relates to drug discovery and development, including a description of important enzymes, reactions and experimental approaches to study drug metabolism.
• Explain the clinical relevance of pharmacokinetic drug-drug interactions (DDI), how they occur and in vitro methods to evaluate the DDI liability of a drug.
• Describe preclinical in vivo and in vitro experimental methods to predict the human pharmacokinetics of a drug.
• Explain how the evaluation of drug metabolism and pharmacokinetic (DMPK) properties informs drug optimization efforts and selection of drug candidates.

Instructor: Aaron Bender 

When a drug target is identified and validated, how does a medicinal chemist prepare a potential clinical development candidate for that target?  Introduction to Medicinal Chemistry will take you on that journey – from hit-to-lead activities to essential synthetic organic transformations to structure activity relationships (SAR). For application purposes, case studies are presented to emphasize both the challenges and successes that exist along the path of every novel pharmaceutical drug campaign.   

By the end of this course, you will be able to: 

• Identify common structural features in pharmaceutical drugs and understand how these features help define potency, absorption, distribution, metabolism and excretion of that particular drug in the body.
• Differentiate and describe the various synthetic organic reactions used frequently in medicinal chemistry and their purpose of use. 
• Analyze and address common medicinal chemistry challenges associated with drug discovery and development.

Instructor: Craig Lindsley

You've taken your courses, you've studied the material, passed your exams, but what does all this look like in real time in the lab? What would a career in drug discovery and development look like? This course will focus on a decade worth of work on the metabotropic glutamate receptor subtype 5 negative allosteric modulator project for Parkinson's Disease. We will use this course to show you how pharmacology, drug metabolism, pharmacokinetics and medicinal chemistry come together to work towards the goal of finding novel therapeutics for real-life patients.

By the end of this course, you will be able to: 

• Describe the initial hypothesis driving the research and understand the basic science to begin a drug discovery program.

• Identify and analyze key parameters need to monitor while in the lead optimization process.

• Describe synthetic chemistry routes and discuss the structure-activity relationships.

• Explain the overall process and discuss results for in vivo pharmacodynamic studies and PET receptor occupancy.

• Describe the purpose and design of IND-enabling studies, including toxicology, formulation and GMP-scale synthesis requirements, and summarize the data expectations for advancing a compound from pre-clinical development into clinical trials.

* This course can only be taken as part of the complete AD3 Bundle.