BMP: Drug discovery 5 Flashcards
What are the main stages in drug discovery
- Targey Discovery
- Lead Discovery
- Lead Optimisation
- Preclinical development
- Clinical Trial P1
- CT P2
- CT P3
- Launch
What is involved in Target discovery
- Biochemistry
- Animal/ clinical disease modelling
- Target identification
- Target validation
- Microarry profiling
- Assay development
What is involved in lead Discovery?
- High throughput screening (HTS)
- screening collections
- Fragment based screening
- Focused libaries
What is involved in lead optimisation?
- structured based drug design
- Medicinal chemsitry
- Selectivity screens
- ADEMT screens
- PK
- cellular/ animal disease modesl
What is involved in preclinical development?
- Toxocology
- In vivo safety pharmacology
- formulation
- Dose prediction
What is involved in CT P1
- Toleratability
- PK
What is involved in CT P2?
- Efficacy
What is involved in CT P3
Safety and efficay
What is involved in launch?
Indication discovery and expansion
What methods are used during the early stages of drug discovery?
One or more of the following:
- Combinitorial screeing
- Phenotypic screening
- Virtual screening
- Rational drug design
What is combinatorial screening?
- Step 1: Synthesis of building blocks containing groups X and Y
- Step 2: Generation of combinatorial libaries by independent screening and purification
- Step 3: Lead investigation through HTS screening
What is a phenotype?
what is screening
- Biochemical or physiologica lcharacteristics of an individual
- Screening means testing extracts against cell lines dervide from a diverse array of human tumours
What is phenotypic screening
Phenotypic screening is a type of screening used in biological research and drug discovery to identify substances such as small molecules, peptides, or RNAi that alter the phenotype of a cell or an organism in a desired manner.
What is virtual screening
Computer based docking of a diverse familes of small molwcules with homology models of the biological target
Virtual screening (VS) is a computational technique used in drug discovery to search libraries of small molecules in order to identify those structures which are most likely to bind to a drug target, typically a protein receptor or enzyme.
What is involved in drug rationale desgin?
- •Druggability and target validation
- 1.Target involved in biomedical cascade of disease
- 2.Target responsive to small molecule treatment
- •Rational drug design (general procedure)
•
Identify natural ligand
See how the ligand binds to the target
Substitute structural features of the natural ligand to create agonist/antagonist
