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
studies.
Course
Schedule Typical drug Discovery Processes: Classical routes for successful drug discovery.
- Key
Milestones and decision points.
- Scientific
Skills Base Required ( Medicinal Chemistry, Biology, ADMET, Informatics)
- Small
Molecule v. Biologic Drugs
- Target
Product Profile.
- Scientific activities and their phasing
Project
Initiation:
Matching the project to the organisation's needs.
- Best
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.
- Drug
action at the cellular level.
- Target
tractability.
- Translational
research.
- Target
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.
- Scientific
activities and their phasing.
- Key
Scientific Tools in Drug Discovery:
- Genomics, Proteomics, Chemogenomics, Stem cell biology.
- Low Throughput screening, High Throughput Screening, High Content Screening, Biostructural Analysis (X-Ray).
- Potency
and selectivity analysis - key
Constants and Parameters.
- In vitro ADMET methodologies and
their application:
- Cellular permeability - adsorption at the gut and blood brain barrier.
- Cyp 450 / P-glycoprotein / glucuronidation / metabolic stability.
- Protein binding.
Medicinal Chemistry:
- Chemical and physical properties of
drug-like compounds.
- Structure activity relationships (SAR).
- The company compound library and
its use.
- Cheminformatics.
- Virtual compound screening.
- Efficacy in animal models of
disease:
- 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.
- Essential
attributes of a clinical candidate.
- Manufacture.
- Formulation.
- Pharmacokinetics
(PK) and Pharmacodynamics (PD).
- Toxicology
Assays.
- hERG.
Course Ends