Drug development Flashcards
What are the current models of drug development?
- lead compound identification
- pre-clinical research
- filing for regulatory status
- clinical trials on humans
- marketing the drug
What is druggability?
the ability of a protein target to bind small molecules with high affinity (sometimes called ligandability)
Name different sources of drugs
- Medicines from plants
- Inorganic elements
- Organic molecules
- Bacteria/fungi/moulds
- Stereoisomers
- Immunotherapy antibodies
- Medicines from animals
- Gene therapy
Name medicine from a plant
Digitalis plant used for dropsy (heart failure) – digoxin
Name medicine from inorganic elements
- Platinum (Pt) based anti cancer agents
- Bismuth (Bi) – antacids (Pepto-Bismol)
- Gold (Ag) - arthritis
Name medicine from organic molecules
- Chloroform
- Phenol
Name medicine from bacteria/fungi/moulds
Antibiotics
Name medicine from immunotherapy antibodies
Vaccinations for hep B, influenza, tetanus, mumps
Name medicine from animals
- Endocrine Hormones such as
- Insulin
- Thyroxine
- Steroids
What are some pharmacokinetic issues for immunotherapy?
- Immunoglobulin: (IgG MW 150kD) – not filtered by kidney
- FcRn Receptor: systemic receptors which absorb IgG into cells protecting them from metabolism
- Mouse antibodies: not substrates for human FcRn receptor – result shorter half-life in man than human antibodies
Which recombinant proteins are used clinically today?
- Insulin
- Erythropoetin
- Growth hormone
- Interleukin 2
- Gamma interferon
- Interleukin 1 receptor antagonist
What is gene therapy?
Gene therapy consists of a recombinant nucleic acid used in or administered to a human being with a view to regulating, replacing, adding or deleting a genetic sequence
What is rational drug design?
The process of finding new medications based on the knowledge of a biological target
Describe rational drug design
- The drug is most commonly an organic small molecule that activates or inhibits the function of a biomolecule
- Involves the design of molecules that are complementary in shape and charge to the bio-molecular target with which they interact and therefore will bind to it
What does rational drug design rely on?
- Relies on computer modeling techniques (computer-aided drug design)
- Relies on the knowledge of the three-dimensional structure of the bio-molecular target is known as structure-based drug design
