Drug Discovery and Lead Optimization

Davidson College via edX Professional Certificate

Overview

Embark on a journey through the fascinating world of pharmaceutical research with this comprehensive six-course program. The Professional Certificate in Drug Discovery and Lead Optimization provides you with a complete view of how potential new medicines are discovered and advanced into clinical trials. This program stands at the intersection of science, business, and regulation—equipping you with the multidisciplinary knowledge that defines successful pharmaceutical professionals.

Whether you're looking to enter the pharmaceutical industry, enhance your current role, or deepen your understanding of drug development, this certificate program delivers critical insights into the complex process of bringing new treatments to patients. Through real-world case studies and practical applications, you'll develop a sophisticated understanding of how scientific innovation translates into life-changing therapies.

No prior experience is required to begin this transformative learning journey, making it accessible to career-changers and industry professionals alike. The program's modular approach allows you to build your expertise systematically, from foundational concepts to advanced techniques in lead optimization.

Syllabus

Courses under this program:
Course 1: Innovate & Regulate: Drug Research, Costs, Clinical Trials & Approval

At some point in their life, essentially everyone needs to use medication for some type of disease treatment or cure. While medications offer great benefits, the cost of drugs, especially new drugs, and the lack of treatment for some diseases can raise questions about business activity behind the creation of new drugs. Better understanding of how drugs are discovered and developed as well as the legal and regulatory factors that affect the industry can help one better recognize both the shortcomings and opportunities faced by the drug industry at large.

Course 2: Measuring Pharmacodynamics: From Ligand Binding to Clinical Outcomes

Drugs are biologically active compounds. Drug discovery and drug development rely on methods for measuring biological activity. The term “activity” is quite general. In practice, a substance’s biological activity can refer to how a substance affects a biological pathway, cell-level responses, safety risks, how long a substance resides within in a system, as well as a substance’s effects in an organism (called pharmacodynamics). The design of methods for measuring activity is a critical aspect of drug discovery. The design of robust and informative methods can accelerate the drug discovery and development process.

Course 3: Introduction to Pharmacokinetics: From ADME to PK/PD

A critical aspect of a drug involves how a drug is dosed and circulates throughout the body of a patient. These qualities are aspects of a drug’s pharmacokinetics or PK. Pharmacokinetics encompasses how a drug is absorbed and flows through a patient until it is ultimately eliminated. While pharmacokinetics covers drug behavior in a living organism, PK properties can often be predicted through laboratory tests for a compound’s ADME properties. ADME stands for absorption, distribution, metabolism, and excretion. The PK and ADME properties of potential drug are closely monitored throughout the discovery and early development stages of a drug campaign.

Course 4: Preclinical Safety: From In Vitro Assays to Human Dose Predictions

Drugs are approved based on their “safety and efficacy”. Determining the safety of a drug occurs through studies that are largely completely separate from efficacy studies. The safety studies fall under the umbrella of preclinical safety. While a drug’s therapeutic benefit is typically narrow and well-defined, the potential safety risks of a compound can be very broad. Preclinical studies therefore search broadly in order to reveal any possible safety issues in a compound. Safety studies ultimately determine dosing limits for clinical trials as well as the final approved drug product.

Course 5: Lead Discovery & Optimization for Efficacy, PK, & Safety

Understanding the efficacy, potency, pharmacokinetics, and safety of compounds is important, but compounds almost always require improvement in their properties in order to become drugs. The process of improvement is called lead optimization and requires a thorough understanding of how a molecule’s structure affects its function, whether efficacy, PK, or toxicity. Unraveling a compound’s structure-function relationship enables lead optimization and hopefully results in the discovery of a compound that can be advanced into clinical trials.

Course 6: Literature Case Studies in Drug Discovery

Once a person understands the ideas of drug efficacy, potency, pharmacokinetics, and safety, original research articles can be readily understood. The Journal of Medicinal Chemistry of the American Chemical Society regularly publishes a series of articles called Drug Annotations. These articles summaries a drug discovery program from a pharmaceutical company. The article covers everything from the indication of the drug, key pathways and promising drug targets within the pathways, library screening, lead selection, lead optimization, and both preclinical safety and PK/ADME studies. The articles are excellent articles for students who are testing their knowledge of drug discovery.

Courses

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5 weeks, 5-7 hours a week, 5-7 hours a week
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In this course about the business of the pharmaceutical industry, students will learn how the economic, legal, and regulatory landscape affect the scientific research that leads to the discovery and development of new drugs. The three-week course starts with a general overview of drug regulation, recognition of patient needs, and listing the distinct stages of a drug campaign. The second week covers clinical trials, research costs, and the effect of patents and intellectual property. In the final week, students will learn about biological drugs, drug approval, drug research outside of large pharma, and the makeup of research pipelines in large drug firms.

No previous experience or knowledge is required to enroll. Students only need to have an interest in better understanding the various factors that affect the research of new drugs. The course is designed in modules. Each module opens with a short video on a selected topic. The module continues with a short reading or exercise with an assessment activity. Each module will require approximately 1 hour to complete, and the course includes 15 modules. Two approaches to the course are recommended. One, a student might spend an hour per day on the course and complete all 15 modules in approximately three weeks. Two, a student with additional available time may be able to work through the entire course in just a single week or over an extended weekend.

Students signed up for the Audit Track have access to the instructional video materials. Students enrolled through the Verified Track have access to the instructional videos, the readings and activities, the assessments, as well as selected additional videos related to the primary instructional videos.
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3 weeks, 5-10 hours a week, 5-10 hours a week
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In this course about measuring biological activity, students will learn different methods of activity measurement encountered at different stages of a drug program. The three-week course starts with an introduction to drug targets, which are biological molecules affected by drugs. The second week emphasizes biochemical, cellular, and computational methods for determining the extent to which a drug can affect the action of its target and associated signal pathways. In the final week, students will transition to in vivo studies and the interpretation of dose-response curves.

Students in the course should understand the concepts of proteins and biological pathways. Students should also be comfortable with algebraic expressions, including logarithmic functions. The course is designed in modules. Each module opens with a short video on a selected topic. The module continues with a short reading or exercise with an assessment activity. Each module will require approximately 1 hour to complete, and the course includes 15 modules. Two approaches to the course are recommended. One, a student might spend an hour per day on the course and complete all 15 modules in approximately three weeks. Two, a student with additional available time may be able to work through the entire course in just a single week or over an extended weekend.

Students signed up for the Audit Track have access to the instructional video materials. Students enrolled through the Verified Track have access to the instructional videos, the readings and activities, the assessments, as well as selected additional videos related to the primary instructional videos.
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3 weeks, 5-10 hours a week, 5-10 hours a week
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In this course about ADME and PK, students will learn how the PK properties of drug candidate are analyzed to guide decisions by the entire drug discovery team. The three-week course starts with the use of drug concentration-time data points to determine the key pharmacokinetic parameters of a compound. The second week focuses on the types of laboratory and animal studies that assist in the prediction of the human PK properties of a compound. In the final week, students will learn how the PK properties are used with efficacy data to predict the human efficacious dose and assist in drug formulation.

Students in the course should understand human anatomy and cell structure. Students should also be comfortable with algebraic expressions, including logarithmic and exponential functions. A fundamental understanding of the structure of organic molecules and their functional groups will also be helpful. The course is designed in modules. Each module opens with a short video on a selected topic. The module continues with a short reading or exercise with an assessment activity. Each module will require approximately 1 hour to complete, and the course includes 15 modules. Two approaches to the course are recommended. One, a student might spend an hour per day on the course and complete all 15 modules in approximately three weeks. Two, a student with additional available time may be able to work through the entire course in just a single week or over an extended weekend.

Students signed up for the Audit Track have access to the instructional video materials. Students enrolled through the Verified Track have access to the instructional videos, the readings and activities, the assessments, as well as selected additional videos related to the primary instructional videos.
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3 weeks, 5-10 hours a week, 5-10 hours a week
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In this course about preclinical safety, students will learn methods for quantifying the safety of a potential drug. The three-week course starts with the origins of preclinical safety programs as well as preliminary safety testing for promising compounds in a drug program. The second week emphasizes in vivo safety studies in representative rodent and non-rodent preclinical animal species. In the final week, students will learn how the PK properties are used with efficacy data to predict the human efficacious dose and assist in drug formulation.

Students in the course should understand human anatomy. An understanding of both pharmacodynamics and pharmacokinetics will also be helpful. The course is designed in modules. Each module opens with a short video on a selected topic. The module continues with a short reading or exercise with an assessment activity. Each module will require approximately 1 hour to complete, and the course includes 15 modules. Two approaches to the course are recommended. One, a student might spend an hour per day on the course and complete all 15 modules in approximately three weeks. Two, a student with additional available time may be able to work through the entire course in just a single week or over an extended weekend.

Students signed up for the Audit Track have access to the instructional video materials. Students enrolled through the Verified Track have access to the instructional videos, the readings and activities, the assessments, as well as selected additional videos related to the primary instructional videos.
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3 weeks, 5-10 hours a week, 5-10 hours a week
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In this course about lead selection and lead optimization, students will learn methods for discovering and optimizing leads with the end goal of advancing a compound into the clinic. The three-week course starts with the processes for finding molecules with promising activity for initiation of a drug program. The second week covers the criteria used to select the best molecules as new leads for the optimization stage. In the final week, students will learn different methods for identifying structural changes that will optimize a lead’s efficacy and PK properties as well as reduce toxicity.

Students in the course should understand pharmacodynamics, drug activity, pharmacokinetics, and preclinical safety. Students should also be comfortable with algebraic expressions, including logarithmic and exponential functions. A fundamental understanding of the structure of organic molecules and their functional groups is also required. The course is designed in modules. Each module opens with a short video on a selected topic. The module continues with a short reading or exercise with an assessment activity. Each module will require approximately 1 hour to complete, and the course includes 15 modules. Two approaches to the course are recommended. One, a student might spend an hour per day on the course and complete all 15 modules in approximately three weeks. Two, a student with additional available time may be able to work through the entire course in just a single week or over an extended weekend.

Students signed up for the Audit Track have access to the instructional video materials. Students enrolled through the Verified Track have access to the instructional videos, the readings and activities, the assessments, as well as selected additional videos related to the primary instructional videos.
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3 weeks, 5-10 hours a week, 5-10 hours a week
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In this course about drug discovery case studies, students will read five different Drug Annotations articles. Each article will require approximately two hours to read thoroughly and fully process. Including assessment questions based on the articles, the full course should require no more than 15 hours of effort.

Students in the course should understand lead selection, lead optimization, pharmacodynamics, drug activity, pharmacokinetics, and preclinical safety. A fundamental understanding of the structure of organic molecules and their functional groups is also required. The course has no structure beyond having a module for each case study article. A handful of 10-15-minute videos with discussions of other Drug Annotation articles are provided for reference. Each module provides a link to the open access article on the Journal of Medicinal Chemistry website.

Students signed up for the Audit Track have access to the links to the case studies and the sample Drug Annotation article videos. Students enrolled through the Verified Track also have access to assessment questions.