Chapter 1 Flashcards
Prelim Notes
a chemical substance of known structure, other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect
Drug
identification of a new chemical entity as a potential therapeutic agent
Discovery phase
compound is tested for safety and efficacy for one or more clinical indications, and in suitable formulations and dosage form
Development phase
The term “drug discovery” is classical and conventional. It should be replaced with the term:
“drug invention”
candidate molecules are chosen on the basis of their pharmacological properties
Drug discovery
non-human studies (e.g. toxicity testing, pharmacokinetic analysis and formulation) are performed
Preclinical development
the selected compound is tested for efficacy, side effects and potential dangers in volunteers and patients
Clinical development
Stages of the New drug synthesis:
Drug discovery, Preclinical development, Clinical development
Drug discovery
Usual time duration?
2-5 years
Drug discovery Usual no. of projects?
100
Drug discovery Components:
- Target selection and validation
- Lead-finding or Lead generation
- Lead optimization
- Pharmacological profiling
is first made that modulation of the activity of a specific protein target will have beneficial therapeutic effects
hypothesis
is a computational docking program in which a specific small molecule of interest is tested against a library of receptor structures
Inverse Docking
derives knowledge from computational analysis of biological data. It includes information stored in genetic code, patient statistics and scientific literature
Bioinformatics
Is done to identify the most useful target among the various identified targets
Target Validation