PEPTIDE-BASED DRUGS
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- Versione italiana
- Academic year
- 2016/2017
- Teacher
- DELIA PRETI
- Credits
- 6
- Didactic period
- Secondo Semestre
- SSD
- CHIM/08
Training objectives
- Biologically active peptides have attracted a growing interest in the pharmaceutical industry, resulting in the recent marketing of a number of peptide/protein drugs. In addition, an increasing series of peptide/protein drugs is currently being evaluated in advanced clinical trials. The main objective of the course is to provide students with the KNOWLEDGE of the theoretical basis needed to understand the chemistry, the pharmacodynamics/pharmacokinetic features and the growing application potential of peptide/protein medicines divided into therapeutic classes. Of particular relevance for the professional practice, the course will stimulate the acquirement of SKILLS in the recognition and description, with appropriate language, of the structural and pharmacodynamic aspects of the different drug classes and their therapeutic uses.
Prerequisites
- Basic notions from the courses of general chemistry, organic chemistry, chemistry of natural substances, molecular biology, animal biology and anatomy. In particular, the ability to recognize a functional group and the relative chemical reactivity is recommended. In addition, knowledge of: the concept of chirality, the structural parameters affecting the solubility of a molecule, the chemico-physical parameters governing the interaction between atoms and functional groups. Finally, notions concerning the structure and physiology of animal cells, the anatomical location of cells and tissues, the processes of transcription and translation of DNA in gene expression.
Course programme
- The course includes 48 hours of classroom lessons during which the following topics will be covered.
PEPTIDES AND PROTEIN (12 hours): critical analysis of the recent market expansion of peptide/protein drugs. Structure and general properties of amino acids and peptides. Basic notions about peptide synthesis: protecting groups in peptide synthesis; methods of activation for peptide coupling; liquid synthesis; solid phase synthesis. Peptide drugs vs. "traditional medicines": strengths, weaknesses, perspectives. Pharmacokinetic (absorption, distribution and elimination) of peptide drugs.
PEPTIDOMIMETIC (12 hours): definition; concept of bioactive conformation; concept of conformational restriction; conformational analysis in peptide systems. Design of a peptidomimetic: non-natural amino acids, cyclic peptides, peptide bond isosteres. General overview of the main therapeutic indications of peptide drugs currently in the market or in advanced clinical trials.
PEPTIDE/PEPTIDOMIMETIC drugs currently in therapy for the following indications (12 hours):
Cancer: Zoladex (goserelin) Velcade (bortezomib), Lupron / ENANTONE / Eligard (leuprorelin), Somatuline (lanreotide) Sandostatin (octreotide);
Cardiovascular disorders: Angiomax (bivalirudin), Integrilin (eptifibatide);
Disorders of the central nervous system: Copaxone (glatiramer);
Metabolic disorders: Victoza (liraglutide); Byetta (exenatide); Lyxumia (lixisenatide); Eperzan / Tanzeum (albiglutide)
Infectious diseases: Incivek (telaprevir) Victrelis (boceprevir);
Hematologic disorders: Firazyr (icatibant) Kalbitor (ecallantide);
Gastrointestinal disorders: GATTEX (teduglutide), Linzess (linaclotide).
PROTEIN THERAPEUTICS OBTAINED BY BIOTECHNOLOGY PROCESSING (12 hours):
Hormones (insulin, somatropin);
Blood factors (antithrombin);
Hematopoietic growth factors (erythropoietin, growth factor KGF);
Cytokine (interleukin-2);
Interferons;
Enzymes;
Vaccines;
Monoclonal antibodies: clinical use in anticancer therapy (rituximab, trastuzumab), rejection prophylaxis (basiliximab, daclizumab), in the treatment of rheumatoid arthritis (infliximab, certolizumab), psoriasis (efalizumab), asthma (Omalizumab) and viral infections (palivizumab) . Didactic methods
- Oral classroom lectures for a total of 48 hours during which all the topics of the program will be faced.
Learning assessment procedures
- A final oral examination will assess the achievement of the proposed educational objectives above described. The examination of about 20 minutes will consist of three questions, one for each main section of the detailed program that can be downloaded from the web page of the course:
PART 1: General topics (basic principles of the chemistry of amino acids and peptides, basic principles on the synthesis of peptides, the concept of “peptidomimetic”, pharmacokinetic aspects of peptide drugs and peptidomimetics)
PART 2A: PEPTIDE DRUGS AND PEPTIDOMIMETICS
PART 2B: PROTEINS AS BIOTECH DRUGS
The aim of the questions is to evaluate the study level and the comprehension of the analysed topics. Each questions will be evaluated with a maximum of 10 points. Reference texts
- Didactic material provided by the teacher (articles and slides).
Specific topics can be explored on the following texts / websites:
1. V. Santagada, G. Caliendo. Peptidi e Peptidomimetici. PICCIN
2. Wilson and Gisvold’s Textbook of organic medicinal and pharmaceutical chemistry. XII edizione.
3. PRONTUARIO TERAPEUTICO REGIONALE al seguente sito:
http://salute.regione.emilia-romagna.it/documentazione/ptr
