Ateneo - UPO

Medicinal Chemistry: Absorption. Metabolism. Bonds involved in the interaction with the target site. Role of stereochemistry in target site interaction. Potential drug targets. Receptors as drug targets. Enzymes as drug targets. Miscellaneous. Drug discovery. Hit and lead compounds. Identification of hit and lead compounds. Identification of drug-like molecules. Drug optimization. Optimizing interaction with the target. Optimizing access to the target. Pharmacology: General principles of pharmacokinetics and pharmacodynamics. General principles of neurotransmission and drugs acting at the synaptic and junctional level. General principles of membrane receptor functioning and the associated intracellular signaling pathways. Biopharmaceutics and Preformulation: An in-depth overview of the fundamental principles governing drug design and development. The main objective is to provide students with the necessary skills to understand how the physicochemical characteristics of an active pharmaceutical ingredient, together with excipients, influence pharmaceutical formulation, bioavailability, and drug behavior in the body. The course begins with the classification of pharmaceutical dosage forms based on their physical structure, route of administration, and release mode. It then explores preformulation aspects in detail—a critical phase in which stability, solubility, and key properties of the active ingredient are studied. Drug diffusion and dissolution are analyzed, with particular focus on the Noyes–Whitney equation, which describes the dissolution rate. A significant part of the course is devoted to biopharmaceutics and pharmacokinetics, especially the LADME system, which outlines the fate of the drug in the body (Liberation, Absorption, Distribution, Metabolism, and Elimination). The concepts of bioavailability and bioequivalence are also discussed, as they are essential to understanding therapeutic efficacy and the interchangeability of medicines. Finally, the course addresses drug release mechanisms from both conventional and advanced solid dosage forms—such as reservoir, matrix, and osmotic systems—providing a comprehensive understanding of the challenges and opportunities in drug design and development.

G. Costantino, G. Sbardella, Chimica Farmaceutica, EdiSES A. Gasco, F. Gualtieri, C. Melchiorre Chimica Farmaceutica Casa Editrice Ambrosiana; W. Foye, Principi di Chimica Farmaceutica, Piccin; E. Stevens, Medicinal Chemistry: The Modern Drug Discovery Process, Pearson. Farmacologia. Taglialatela, Cantarella Leone, Mattioli Moretti- IV edizione SORBONA; Le basi della farmacologia. Karen Whalen zanichelli Paolo Caliceti, Tecnologia farmaceutica, 2025, CEA Casa Editrice Ambrosiana. Aulton ME, Taylor K.M.G. Tecnologie farmaceutiche, 2015 EDRA LSWR. Ansel, HC et al. Principi di calcolo farmaceutico. Quindicesima edizione. 2017 Ed. Edra. Farmacopea Ufficiale Italiana edizione vigente. Farmacopea Europea edizione vigente. Lachman L, Lieberman H, Kanig J. The theory and practice of industrial pharmacy. Ed. Lea & Febiger, USA. Fabris L, Rigamonti S. La fabbricazione industriale dei medicinali. Ed. Esculapio, Bologna.

Medicinal Chemistry: Knowledge and understanding. At the end of the course, students will have acquired a solid understanding of the basic concepts of medicinal chemistry, in particular the journey of a drug through the body—from the pharmaceutical phase to the pharmacodynamic phase. Students will also be introduced to the strategies behind drug discovery, drug design, and drug development. Ability to apply knowledge and understanding. For both the specific drugs covered and structurally related compounds, students will be able to apply their knowledge and understanding to recognize chemical structures, discuss their chemical and physicochemical properties, mechanisms of action, structure–activity relationships, and metabolic properties, and propose potential synthetic routes for their production. Knowledge management and judgment skills. Students will develop the ability to make informed judgments on structure–activity relationships, metabolism and related toxicity, drug production, and drug–drug interactions. They will also be equipped with the tools needed to critically assess pharmaceutical chemistry literature and scientific articles. Communication skills. Students will be able to clearly and, when appropriate, creatively explain topics discussed in class and respond effectively to questions, feedback, and suggestions. Learning skills. The course will help students develop the ability to manage their own body of knowledge on drug chemistry in a dynamic and increasingly independent way. Pharmacology: The course aims to achieve the following objectives: Provide students with fundamental knowledge of pharmacology.Build a framework that allows the integration of future professional knowledge about drugs into their academic foundation. Foster critical thinking skills for the study of specific drugs. Provide essential knowledge on the general aspects of drugs (pharmacokinetics and pharmacodynamics), as well as the mechanisms of action, with a view to potential pharmacotherapeutic applications. Equip students with critical tools for understanding experimental approaches in drug identification and characterization. Biopharmaceutics and Preformulation: Knowledge and understanding. By the end of the course, students will have acquired a solid understanding of the fundamental concepts of biopharmaceutics and preformulation. They will be able to clearly distinguish between a drug, a medicinal product, and an excipient, and classify the main pharmaceutical forms based on their structure, route of administration, and release mechanism. They will understand the theoretical foundations of drug design and development, with particular emphasis on the preformulation and stability phases, and will be familiar with diffusion, solubility, and dissolution processes, including applications of the Noyes–Whitney equation. Ability to apply knowledge and understanding. Students will be able to apply their knowledge to correlate the physicochemical properties of an active pharmaceutical ingredient with the most appropriate dosage form. They will be capable of analyzing how formulation and technological factors affect drug release from conventional solid forms and explaining the release mechanisms of advanced systems such as reservoir, matrix, and osmotic dosage forms. Independent judgment. The course fosters the development of independent critical thinking in evaluating processes involved in pharmaceutical form design and optimization. Students will be able to formulate reasoned judgments on the efficacy and safety of a medicinal product, considering its biopharmaceutical properties and technological implications. Communication skills. Students will be able to clearly express the key concepts learned, using appropriate scientific terminology. This includes the ability to describe the LADME process and to explain concepts such as bioavailability, bioequivalence, and the Biopharmaceutical Classification System (BCS) in both academic and professional contexts. Learning skills. The course will provide a strong foundation for engaging with more advanced topics in drug formulation and development. Students will cultivate a proactive attitude toward research and continuous learning, recognizing the importance of the interplay between scientific knowledge and industrial application.

Passing all first-year exams is a prerequisite for all third-year exams. Knowledge of biochemistry, physiology, and pathology is essential for a full understanding of the course.

Medicinal Chemistry: The course consists of lectures supported by slides, which are provided to students at the beginning of the course. Both general and specific topics will be presented, offering essential knowledge for understanding the subject matter. Class discussions will be encouraged to develop transferable skills—across different drug classes—such as predicting the chemical and physicochemical properties of drugs based on their structure, identifying key structural elements relevant to the mechanism of action, and recognizing structural alerts that may lead to toxic effects. At the end of each module, blackboard exercises will be carried out to support exam preparation. Pharmacology: The course content will be delivered through oral presentations supported by video projections that explain the topics covered. Active student participation will be encouraged by recalling concepts already addressed in other courses that relate to various aspects of drug science. Biopharmaceutics and Preformulation: The course will mainly be delivered through lectures. Some seminars will be held by professionals working in the pharmaceutical industry to illustrate the practical application of the theoretical concepts covered. On certain occasions, students will be invited to answer questions collaboratively on topics previously addressed and to retrieve supplementary learning materials from the AIFA, EMA, and FDA websites.

Students with disabilities, Specific Learning Disorders (SLD), or Special Educational Needs (SEN) can request dedicated services and tools by contacting the Staff for Career Development and Student Services and by visiting the dedicated page on the University website: https://uniupo.it/it/servizi/servizi-studenti-disabili-e-dsa Once they have contacted the University Staff, students with disabilities, SLD, or SEN may also reach out to the course instructor to discuss exam arrangements and teaching-related matters.

The exam consists of a written and/or oral test with theoretical questions covering the course content from a knowledge-based perspective. Some questions focus on a drug molecule for which the chemical structure, pharmacokinetic parameters, and pharmaceutical form are provided by the instructor. Students will be required to identify or comment on acidic, basic, and stereogenic centers, intermolecular interactions, possible metabolic reactions, compliance with Lipinski’s rule, pharmacokinetic characteristics, formulation aspects, and more. To pass the exam, students must correctly answer more than half of the questions. These assessments will verify that the student has achieved the intended learning objectives: knowledge and understanding of the content, the ability to explain it clearly and accurately, and the ability to apply acquired knowledge and skills to specific problems related to the chemical and pharmaceutical aspects of the drug classes covered. The final grade, expressed on a scale of thirty, will be based on the following criteria: Theoretical and applied knowledge and understanding of the topics covered; Independent judgment and ability to make connections between topics; Communication skills and appropriate use of technical language; Learning ability.

Medicinal Chemistry: Definition of medicinal chemistry. Absorption and absorption mechanisms. Passive transport. Partition coefficient. Fick’s law. Ion pair transport. Carrier-mediated transport. Vesicular transport. Paracellular transport. Oral absorption and first-pass metabolism. Distribution and plasma protein binding. Phase I and Phase II metabolism. Effects of metabolism. Soft and hard drugs. Types of bonds involved in drug–target interaction: Covalent bond, ionic bond, dipole–dipole and ion–dipole interactions, hydrogen bonds, halogen bonds, charge transfer, van der Waals forces, hydrophobic interactions, π–π interactions. Role of stereochemistry in drug–target interaction: Three-point interaction model, Pfeiffer’s rule, eutomer, distomer, eudismic ratio, chiral switch, and methods to obtain enantiomerically pure drugs. Possible drug targets: Structurally specific and nonspecific drugs. Receptors as drug targets. Enzymes as drug targets: active site inhibitors, reversible competitive, non-competitive, irreversible inhibitors, transition state analogs, suicide inhibitors. Miscellaneous targets: Transport proteins, structural proteins, protein–protein interaction inhibitors, lipid-targeting drugs. Drug discovery: Hit and lead compounds. Selection of disease, target, and bioassay. High-throughput screening, NMR screening, virtual screening. Parallel and combinatorial synthesis. Lead identification: Natural products, serendipity, modification of natural ligands, me-too drugs, SOSA approach, compound library screening, de novo drug design, fragment-based drug design. Drug-likeness: Lipinski’s and Veber’s rules. Drug optimization: Optimizing target interaction: structure–activity relationships, isosterism and bioisosterism (classical and non-classical), pharmacophore identification, and multiple drug design strategies (structure extension, chain extension/contraction, homology, vinylogy, benzology, ring expansion/contraction, ring variation, ring fusion, structure simplification, rigidification, conformational blockers, twin drugs, and hybrids). Optimizing target access: modifying hydrophobic/hydrophilic properties, improving resistance to chemical/enzymatic degradation, prodrugs and mutual prodrugs. Practical exercises on the blackboard with examples of drug molecules (functional group identification, acidic/basic/stereogenic centers, possible intermolecular interactions, possible metabolic reactions, etc.). Pharmacology: Definition of pharmacology. Drug classification and nomenclature. Chemical, natural, biotechnological drugs, and advanced therapies. Routes of drug administration. Pharmacokinetics: absorption, distribution, metabolism, elimination, drug interactions, pharmacogenetics, main pharmacokinetic parameters. Examples from pharmacology, pharmacognosy, and toxicology illustrating pharmacokinetic processes. Pharmacodynamics: dose–response curves, therapeutic indices, ligand–receptor interactions, and occupancy theory (including binding methods and analysis). Pharmacological modulation of response: agonists, antagonists, blockers, inhibitors, partial agonists, inverse agonists. Main neurotransmitters and their systems. Overview of preclinical and clinical drug testing. Individual variability in drug response. Case studies: cholinergic system, adrenergic system, GABA receptor, local anesthetics Biopharmaceutics and Preformulation: Drugs, medicinal products, excipients, and pharmaceutical forms. Classification criteria for dosage forms: physical form, route of administration, and release mechanism. Drug design and development: formulation, preformulation, and stability. General principles of diffusion, solubility, and dissolution; dissolution rate and the Noyes–Whitney equation. Biopharmaceutics and pharmacokinetics: the LADME system (Liberation, Absorption, Distribution, Metabolism, Elimination); bioavailability and bioequivalence; Biopharmaceutical Classification System (BCS). Drug release from conventional solid dosage forms: impact of formulation and technological factors. Drug release mechanisms from non-conventional solid dosage forms: reservoir, matrix, and osmotic systems

Medicinal Chemistry: Students will acquire the fundamental principles of medicinal chemistry, including pharmacokinetic and pharmacodynamic concepts, which will be further explored in subsequent courses. They will be able to apply this knowledge to analyze drug molecules, assessing their chemical, metabolic, and drug-likeness properties. They will also understand the role of medicinal chemistry in drug discovery and design, as well as strategies to optimize drug properties. Pharmacology: At the basic level, students must understand ADME mechanisms, drug molecular targets, and key efficacy and toxicity parameters. They should be able to apply theoretical knowledge to therapeutic contexts and communicate concepts using proper terminology. At the advanced level, students will compare active compounds, choose suitable routes of administration based on drug profiles, and explain pharmacokinetic and pharmacodynamic interactions and their therapeutic implications. Biopharmaceutics and Preformulation: By the end of the course, students will understand the main pharmaceutical dosage forms, classification criteria, and the fundamentals of preformulation and formulation. They will be able to relate the physicochemical properties of active ingredients to appropriate dosage forms and assess drug release mechanisms, including those of advanced systems. The course fosters critical thinking in evaluating drug efficacy and safety, strengthens scientific communication skills, and encourages a proactive, research-oriented mindset in pharmaceutical development.