Exam 1 - Lecture 10, Drug Design Flashcards
Stages of Drug Design and Development
ID target disease ID drug target Establish testing procedures Find a lead compound Structure Activity Relationship Identify pharmacophore Drug design - optimizing target interactions Drug design - optimizing pharmacokinetic properties Toxicological and safety test Chemical development and production Patenting and regulatory affairs Clinical trial
Questions to ask new drug
Is the disease widespread?
Dose the disease affect the 1st world?
Are there drugs already on the market?
If so, what are there advantages and disadvantages?
Can 1 ID a market advantage for a new therapy?
Drug targets
Lipids (cell membrane)
Proteins (Receptors, enzymes, carrier proteins, structural proteins like tubulin)
Nucleic Acids (DNA, RNA)
Carbohydrates (Cell surface carbohydrates, Antigens and recognition molecules)
Sources of Lead compounds
Natural world:
Plantlife, Micro-organisms, Animal life, Biochemicals, Marine chemistry
Synthetic world:
Chemical synthesis and combinatorial synthesis
Virtual world:
Computer aided drug design
Opium gave us
Morphine
Cinchona bark gave us
quinine
Yew tree gave us
taxol
Willow tree gave us
salicylic acid
Coca bush gave us
cocaine
Phase 1
carried out on health volunteers
useful in establishing dose levels
useful for studying pharmacokinetics, including drug metabolism
Phase 2
carried out on patients, done as double blind studies
Demonstrates whether drug is therapeutically useful
establish dosing regime, identify side effects
Phase 3
carried out on a larger number of patients
New drug is compared with conventional treatments in terms of therapeutic outcome
Establishes statistical proof for efficacy and safety
Phase 4
Continued after drug reaches market
Studies long term effects when used chronically
ID unusual side effects
Bio-isosteres
replace a functional group with another group which retains the same biological activity
ex. Fluorine for H
