SELECTED TOPICS OF MEDICINAL CHEMISTRY - BIOTECHNOLOGICAL DRUGS
Learning outcomes of the course unit
SUPPLEMENT TO PHARMACEUTICAL CHEMISTRY:
The course aims at providing the necessary methodological tools for understanding the molecular basis of drug action, with particular reference to the drugs included in the program.
Knowledge and understanding: the relationships between chemical structure and pharmaceutical, pharmacodynamic and pharmacokinetic properties,the study of the chemical and physico-chemical properties of the drugs, the mechanism of action, the most important biotransformations and metabolic considerations, the classification of the drugs and the nomenclature.
Applying knowledge and understanding: through the frequency of the course the student will be able to apply his knowledge to the interpretation of the mechanism of action and the pharmacological profile of the drugs and their metabolic characteristics, the discussion of the structure-activity relationships, the definition of a correct nomenclature according to international rules, the ability to communicate with people in different areas such as pharmacology, pharmaceutical technology, biotechnology.
Communication skilles: being treated the acquisition of a formally correct language, is stimulated the ability to express the contents in a clear way.
BIOTECHNOLOGICAL DRUGS: The main goal of the course is to provide basic information to know and understand the properties, application and problems related to the production, characterization and use of drugs of biotechnological origin.
The comprehensive introduction on methodologies for production, characterization and purification of protein therapeutics, and the description of their pharmacodynamic and pharmacokinetic properties, toxicity and immunogenicity will allow the student to apply his/her knowledge to the identification and evaluation of the relevant properties and issues related to each biotech drug.
Basic concepts of medicinal chemistry, biochemistry, organic chemistry, pharmacology and phisiology. The part of Biotechnological Drugs also requires knowledge of immunology.
Course contents summary
- Drugs used in the treatment of hyperlipoproteinemia and antithrombotic. Drugs of endocrine and metabolic system, FANS.
- Biotech methodologies.
Important classes of biotech drugs in different therapeutic areas, such as hormones, enzymes, cytokines, monoclonal antibodies.
Supplement to Pharmaceutical Chemistry:
Antilipoproteinemic drugs and inhibitors of cholesterol synthesis: Bile acid sequestrants, HMG-CoA reductase inhibitors, cholesterol absorption inhibitors, fibrates, nicotinic acid.
Insulin and medications used to treat diabetes.
Corticosteroids: Biosynthesis of corticosteroids. Development of corticosteroid drugs. SAR.
Thyroid function and thyroid medications.
Calcium homeostasis: pharmacological therapies for osteoporosis, for hyperparathyroidism, for hypoparathyroidism, for hypercalcaemia.
Female sex hormones: estrogenic and progestinic substances.
Male sex hormones: androgenic substances.
Non-steroidal anti-inflammatory drugs: Antipyretic analgesics. Anti-inflammatory analgesics. COX-2 inhibitors. Drugs for the treatment of arthritis. Antithrombotic drugs: anticoagulants, antiaggregants and fibrinolytics.
Introduction to biotechnology.
Basic elements of molecular biotechnology.
Production of biotech compounds: cultivation and downstream processing.
Biophysical and biochemical analyses of recombinant proteins.
Chemical and physicochemical properties and reactivity of recombinant proteins; stability of proteins and mechanisms of degradation.
Pegylation of therapeutic proteins
Fusion proteins and soluble receptors.
Hormones: insulin, glucagon, growth hormone, follicle-stimulating hormone, luteinizing hormone, parathyroid hormone.
Cytokines: interleukines (IL-1, IL-2); interferons; hematopoietic growth factors (G-SCF, erythropoietin).
Blood proteins: tissue-type plasminogen activator, clotting factors (VII, VIII, IX).
Enzymes: human deoxyribonuclease, beta-glucocerebrosidase, alpha-galactisodase.
Recombinant vaccines: genetically improved live vaccines, live vectors, genetically improved subunit vaccines
Monoclonal antibodies, immunoconjugates and radioimmunoconjugates: rituximab, ofatumumab, ibritumomab tiuxetan, gemtuzumab ozogamicin, muromonab, catumaxomab, daclizumab, basiliximab, infliximab, adalimumab, certolizumab pegol, cetuximab, bevacizumab, ranibizumab.
Soluble receptors: etanercept, abatacept.
W.O. FOYE: “Principi di Chimica Farmaceutica”, Piccin.
G.L. PATRICK: "Introduzione alla Chimica Farmaceutica", EdiSES.
WILSON & GISVOLD: "Chimica Farmaceutica", casa Editrice Ambrosiana.
Maria Luisa Calabrò, Compendio di Biotecnologie Farmaceutiche, EdiSES, Napoli, 2008.
Daan J.A. Crommelin, Robert D. Sindelar, Biotecnologie Farmaceutiche, Zanichelli, Bologna.
Thomas L. Lemke, David A. Williams, Victoria F. Roche, S. William Zito, Foye’s Principi di Chimica Farmaceutica, sesta edizione italiana, Piccin, Padova, 2013. (per il capitolo dedicato)
Daan J.A. Crommelin, Robert D. Sindelar, Bernd Meibohm, Pharmaceutical Biotechnology, Fourth Edition, Springer, 2013.
Through oral lessons with slides will be presented and discussed matters relating to the course content.
Assessment methods and criteria
The achievement of the objectives of the course is checked by oral examination. The markes obtained in the two modules will be mediated.
For Supplement to Pharmaceutical Chemistry, through questions regarding the course topics will be determined knowledge and understanding of the student.
Through questions about the connections between different topics, the interpretation of the action and the pharmacological profile of drugs, the structure-activity relationships and structure-pharmacokinetic properties will be cheked the skills of the student. This is the minimum threshold for the exam to be sufficient.
For Biotechnological Drugs, questions related to all the topics treated during the course, will be used to assess the knowledge and comprehension of the contents of the course achieved by the student. The ability of the student to apply the acquired knowledge will be also evaluated through connections among topics.
Preparation is be considered sufficient if the student proves knowledge and understanding of the basic aspects of each topic and is able to apply this knowledge to the discussion.
During the examination use of an appropriate terminology will also be assessed.
Lectures are conducted with the aid of slides whose contents are available to students. The teaching material available online is not a replacement but a supplementary of reference texts, and a guide to a better understanding of the topics to be studied.