The one day 'Introduction to Drug Discovery' course:
(A 200+ figure manual plus reference list is provided and four individual/team exercises are also included).
Step-by-step from project initiation through lead compound/biologic identification to selection of candidate for clinical trials.
- Selection of a target human protein whose
modulation results in the desired therapeutic effect.
- Obtaining a compound/biologic capable of carrying this out in vitro and in animal disease models.
- Prediction of the
compound/biologic’s safety in humans via in vitro and animal model
Schedule Typical drug Discovery Processes: Classical routes for successful drug discovery.
Milestones and decision points.
Skills Base Required ( Medicinal Chemistry, Biology, ADMET, Informatics)
Molecule v. Biologic Drugs
- Scientific activities and their phasing
Matching the project to the organisation's needs.
Practice in Project Initiation:
- Use of a Target Product Profile (TPP).
Target Protein Selection:
Identifying the right protein drug target for the disease.
How to select the right protein drug target for the disease.
action at the cellular level.
proteins for existing small molecule drugs. (GPCR, Ion
Channels, Nuclear Receptors, Kinases).
Lead / Lead Series Identification:
The path to obtaining a lead compound with the quality to become a Clinical Candidate.
activities and their phasing.
Scientific Tools in Drug Discovery:
- Genomics, Proteomics, Chemogenomics, Stem cell biology.
- Low Throughput screening, High Throughput Screening, High Content Screening, Biostructural Analysis (X-Ray).
and selectivity analysis - key
Constants and Parameters.
- In vitro ADMET methodologies and
- Cellular permeability - adsorption at the gut and blood brain barrier.
- Cyp 450 / P-glycoprotein / glucuronidation / metabolic stability.
- Protein binding.
- Chemical and physical properties of
- Structure activity relationships (SAR).
- The company compound library and
- Virtual compound screening.
- Efficacy in animal models of
- Animal models in: Inflammation, Cancer, HIV-AIDS.
- Essential attributes of a Lead Compound.
Clinical Candidate Identification:
Final ‘polishing’ of the lead compound with a view to its further Development.
attributes of a clinical candidate.
(PK) and Pharmacodynamics (PD).