Drug discovery; pharmacological persepctive

Question 1

In vitro assays:

Answer 1

Target based

Phenotypic

Question 2

Hit identification:

Answer 2

once you have validated target synthesis compounds which work.
molecules have affinity for target

Question 3

in viro pharmacology assays:

Answer 3

enzyme inhibitors
receptor agonist/antagonist
antibact drugs

Question 4

efficacy

Answer 4

dose of drug needed to make a specific effect

Question 5

what is efficacy depended on

Answer 5

receptor density
affinity
potency

Question 6

what is affinity

Answer 6

strength of chemical interactions responsible for drug-target interaction

Question 7

what is potency

Answer 7

degree of functional change imparted to receptor upon binding of drug

Question 8

what is lead identification

Answer 8

validation hits are tested to determine factors such as
drug-like properties
metabolic properties

Question 9

what is lead optimisation

Answer 9

improve physiochem and drug like properties

Question 10

3r’s

Answer 10

reduce
refine
replace

Question 11

ICH guidelines

Answer 11

QUALITY
SAFETY
EFFICACY
MULTI DISCIPLINAY

Question 12

before entering clinical trails what needs to occur

Answer 12

• efficacy studies in whole body systems

- drug safety

Question 13

what does candidate selection test for

Answer 13

potency
selectivity
bioavailability
IP position

Question 14

phase 1 clinical trials:

checks for what

Answer 14

safety
tolerability
bioavailability
rather than efficacy

Question 15

phase 2 clinical trails:

checks for what

Answer 15

determines efficacy of drug i

Question 16

phase 2 clinical trials:

large numbers of …………..

Answer 16

patients

Question 17

phase 3 clinical trial:

………..versions of previous trials

Answer 17

larger

Question 18

phase 4:

have what studies

Answer 18

post -marketing studies

Question 19

why is pharmacovigilence important

Answer 19

• information on safety collected during drug development is incomplete
• animal test no enough to prove human safety