Prodrugs/bioprecursors

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

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

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

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

Hourly volumes*:

CM: 3 p.m.

Tutorial: 5 hours

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

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

2-hour final written exam

• Authorized documents: no
• Non-graphing calculator permitted: yes
• Internet access: no

Inductive (problem-based) and deductive teaching methods. Materials available on the digital workspace (Moodle): Course documents, tutorial documents, past exam papers, and reference publications.

1. Introduction & General Concepts: (2 hours)

- 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 hours)

- Physiology concepts: the digestive system,

- Enzymatic processes related to the degradation of macromolecules,

- Description of epithelial tissue, functional aspects

- Blood and lymphatic systems

1. Biotransformation and conjugation: (2 hours)

- General information on hepatic metabolism

- Main types of reactions

- Impact on the effectiveness of an active ingredient

- Examples.

1. Membrane diffusion & Transport: (3 hours)

- Passive diffusion, Facilitated transport & Active transport,

- Transport systems for biomolecules (sugars, di- and tripeptides, amino acids, etc.)

- Assessment models

5.: Prodrug approaches (6 hours)

- Concept & Definitions, Potentialities

- Molecular vectorization

- Bioprecursors

- Examples

TD (5 hours): Individual work, exercises to be prepared before and during the session.

Case studies (interpretation of data from the literature).

Administrative contact(s):

Master's Program in Chemistry Secretariat

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