[Golan] = Golan, David E., Armen H. Tashjian, and Ehrin J. Armstrong, eds. Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. Lippincott Williams & Wilkins, 2011. ISBN: 9781608312702. [Preview with Google Books]
[C&D] = Klaassen, Curtis. Casarett & Doull’s Toxicology: The Basic Science of Poisons. 8th ed. McGraw-Hill Professional, 2013. ISBN: 9780071769235.
| SES # | TOPICS | READINGS | |
|---|---|---|---|
| Overview of the Drug Discovery Process; Fundamental Principles | |||
| L1 | Introduction and Fundamentals | [Golan] Chapter 1 | |
| L2 | Overview of Drug Development 1 | [Golan] Chapter 49 | |
| L3 | Overview of Drug Development 2 | [Golan] Chapter 49 | |
| R1 | Fundamentals | [Golan] Chapters 1 and 2 | |
| L4 | Biochemistry Review Exercise | No readings for this session. | |
| L5 | Uptake and Distribution |
[Golan] Chapters 2 and 3 [C&D] Chapter 5 |
|
| L6 | Dr. Keith Hoffmaster, Novartis: Drug Transporters 1 |
[Golan] Chapter 4 [C&D] Chapter 7 Giacomini, Kathleen M., Shiew-Mei Huang, et al. “Membrane Transporters in Drug Development.” Nature Reviews Drug Discovery 9, no. 3 (2010): 215–36. Brouwer, Kim L. R., Dietrich Keppler, et al. “In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development.” Clinical Pharmacology & Therapeutics 94, no. 1 (2013): 95–112. |
|
| L7 | Dr. Keith Hoffmaster, Novartis: Drug Transporters 2 |
[Golan] Chapter 4 [C&D] Chapter 7 |
|
| R2 | Drug Metabolism 1 |
[Golan] Chapter 4 |
|
| L8 | Drug Metabolism 2 |
[Golan] Chapter 4 |
|
| L9 | Drug Toxicity 1 |
[Golan] Chapters 5 and 41 Guidance for Industry: Drug-Induced Liver Injury: Premarketing Clinical Evaluation. (PDF) U.S. Department of Health and Human Services; Food and Drug Administration; Center for Drug Evaluation and Research (CDER); Center for Biologics Evaluation and Research (CBER). July 2009. Giacomini, Kathleen M., Shiew-Mei Huang, et al. “Membrane Transporters in Drug Development.” Nature Reviews Drug Discovery 9, no. 3 (2010): 215–36. |
|
| R3 | Lecture Review Session | No readings for this session. | |
| L10 | Drug Toxicity 2 |
[Golan] Chapters 5 and 41 |
|
| L11 | Pharmacokinetics |
[Golan] Chapters 2 and 3 [C&D] Chapter 5 |
|
| R4 | Quiz Review | No readings for this session. | |
| Case Studies and Literature Discussions; Case Study Project | |||
| L12 | Case Study: Omeprazole Pharmacogenetics |
Chang, M., G. Tybring, et al. “Interphenotype Differences in Disposition and Effect on Gastrin Levels of Omeprazole—Suitability of Omeprazole as a Probe for CYP2C19.” British Journal of Clinical Pharmacology 39, no. 5 (1995): 511–18. Furuta, Takahisa, Mitsushige Sugimoto, et al. “CYP2C19 Pharmacogenomics Associated with Therapy of Helicobacter Pylori Infection and Gastro-Esophageal Reflux Diseases with a pPoton Pump Inhibitor.” Pharmacogenomics 8, no. 9 (2007): 1199–210. Lindberg, Per, Peter Nordberg, et al. “The Mechanism of Action of the Antisecretory Agent Omeprazole.” Journal of Medicinal Chemistry 29, no. 8 (1986): 1327–29. Court, Michael H. “A Pharmacogenomics Primer.” The Journal of Clinical Pharmacology 47, no. 9 (2007): 1087–103. [Golan] Chapter 6 and 46 |
|
| R5 | Overview of Drug Development 3 | [Golan] Chapter 49 | |
| L13 | Case Study | No readings for this session. | |
| L14 | Case Study: Antibiotics |
[Golan] Chapters 32, 33, and 34 Antibiotic Resistance Threats in the United States, 2013 (PDF - 4.0MB) Centers for Disease Control and Prevention. Dwyer, Daniel J., Michael A. Kohanski, et al. “Role of Reactive Oxygen Species in Antibiotic Action and Resistance.” Current Opinion in Microbiology 12, no. 5 (2009): 482–9. |
|
| R6 | Project Help Session | No readings for this session. | |
| L15 | Case Study | No readings for this session. | |
| L16 | Dr. Alex Wood, MIT Senior Lecturer/Novartis: Case Study: Oncology Drugs | Hanahan, Douglas, and Robert A. Weinberg. “Hallmarks of Cancer: The Next Generation.” Cell 144, no. 5 (2011): 646–74. | |
| R7 | Project Help Session | No readings for this session. | |
| L17 | Case Study: Statins |
[Golan] Chapter 19 Press Release: “Rate of Kidney Damage in Crestor Patients Is 75 Times Higher Than in Patients Taking Other Cholesterol Drugs.” October 29, 2004. |
|
| R8 | Project Help Session | No readings for this session. | |
| L18 | Case Study: GWAS and Statin Toxicity |
Niemi, M. “Transporter Pharmacogenetics and Statin Toxicity.” Clinical Pharmacology & Therapeutics 87, no. 1 (2010): 130–3. Link, E., S. Parish, et al. “SLCO1B1 Variants and Statin-Induced Myopathy—A Genomewide Study.” The New England Journal of Medicine 359, no. 8 (2008): 789. |
|
| L19 | Dr. Bernard Fermini, Pfizer: Case Study: Cardiotoxicity | No readings for this session. | |
| R9 | Project Help Session | No readings for this session. | |
| L20 | Dr. Teresa Wright, Shire Pharmaceuticals: Preclinical Drug Development | [Golan] Chapter 49 | |
| R10 | Project Help Session | No readings for this session. | |
| L21 | Dr. Keith Hoffmaster: Case Study: PK / PD | No readings for this session. | |
| L22 | Case Study: Sarilumab Phase III Clinical Result |
Carroll, John. “Regeneron, Sanofi Hit a Trio of Goals in First PhIII Test of Rheumatoid Arthritis Drug.” Fierce Biotech, November 22, 2013. Huet, Natalie (rep.) and Elizabeth Piper (ed.). “Sanofi, Regeneron Arthritis Drug Meets Goals in Phase 3 Trial.” Reuters, November 22, 2013. Bennett, Simeon. “Sanofi Rheumatoid Arthritis Drug Cuts Pain, Damage in Study.” Bloomberg, November 22, 2013. |
|
| R11 | Prof. Doug Lauffenburger: Systems Pharmacology | No readings for this session. | |
| L23 | Dr. Tess Schmalbach, Schmalbach LLC: The Clinical Size of Drug Development | [Golan] Chapters 50 and 51 | |
