Prodrugs/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 membrane passageways and transport systems for fundamental biomolecules (sugars, amino acids, nucleosides, etc.).

Examples of prodrug and bioprecursor design.

Hourly volumes* :

CM: 15 H

TD: 5 H

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

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

2-hour final written exam

• 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, tutorial documents, exam annals and reference publications.

1. Introduction & General Concepts: (2 H)

- Definitions and Basics (ADME)

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

- Main routes of administration (advantages and disadvantages)

1. Nutrient absorption (2 H)

- Notions of physiology: the digestive system,

- Enzymatic processes related to the degradation of macromolecules,

- Description of epithelial tissue, functional aspects

- Blood and lymphatic tract

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, etc.)

- Evaluation models

5.: Pro-Drug Approaches (6 H)

- Concept & Definitions, Potentialities

- Molecular vectorization

- Bioprecursors

-Examples

Tutorials (5 hours): Individual work, exercises to be prepared 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/