Drugs/bioprecursors

Knowledge of the limitations associated with the administration of an active ingredient (solubility, bioavailability, etc.).

General description of the enzymatic systems involved in the biotransformation of nutrients and exogenous compounds.

Description of the main modes of membrane passage and transport systems of fundamental biomolecules (sugars, amino acids, nucleosides...).

Examples of prodrug(s) and bioprecursor(s) design.

Hourly volumes* :

CM : 15 H

TD : 5 H

Understand and be able to analyze the problems associated with the administration of an active ingredient

Be able to propose a prodrug(s) and/or bioprecursor(s) strategy for a biomolecule.

Final written exam of 2 hours

• Authorized documents: no
• Non-graphic calculator allowed: yes
• Internet allowed : no

Inductive (problematic) and deductive pedagogy, Support(s) available on the ENT (Moodle): Course documents, TD documents, exam annals and reference publications.

1. Introduction & General Concepts: (2 H)

- Definitions and Basic Concepts (ADME)

- Limiting factors between the site of administration and the site of action of a biomolecule

- Main routes of administration (advantages & disadvantages)

1. Nutrient absorption (2 H)

- Notions of physiology: the digestive system,

- Enzymatic processes related to the degradation of macromolecules,

- Description of the epithelial tissue, functional aspects

- Blood and lymphatic pathways

1. Biotransformation and conjugation: (2 H)

- General information on hepatic metabolism

- Main types of reactions

- Impact on the effectiveness of an active ingredient

- Examples.

1. Membrane Diffusion & Transport: (3 H)

- Passive Diffusion, Facilitated Transport & Active Transport,

- Biomolecule transport systems (sugars, di and tri-peptides, amino acids, ...)

- Evaluation models

5: Prodrug approaches (6 H)

- Concept & Definitions, Potentialities

- Molecular Vectorization

- Bioprecursors

- Examples

TD (5 H): Individual work, exercises to prepare before and during the session.

Case studies (interpretation of data from the literature).

Administrative contact(s):

Secretariat Master Chemistry

https://master-chimie.edu.umontpellier.fr/