Lecture 2 Lead Optimization

Question 1

What are the goals for lead optimization? (Questions to ask to optimize LEAD)

Answer 1

Slide 3

Question 2

What are some key criteria for the lead series?

Answer 2

Slide 4

Question 3

What is the iterative process of lead optimization?

Answer 3

Slide 5

Question 4

How do you infer the function of the drug?

Answer 4

Slide 6

Question 5

How do you optimize the drug + eg?

Answer 5

Slide 7, 8, 9

Question 6

What are some criteria for absorption of drug?

Answer 6

Slide 11

Question 7

What are some considerations regarding oral administration?

Answer 7

Slide 12

Question 8

What other considerations for absorption and how is it tested?

Answer 8

Slide 13

Question 9

Using an example, demonstrate how a drug is tested to be suitable for method of administration/absorption?

Answer 9

Slide 15, 16, 17

Question 10

How do you calculate bioavailability?

Answer 10

Slide 18

Question 11

What is distribution?

Answer 11

Slide 19

Question 12

What is clearance?

Answer 12

Slide 20, 21, 22

Question 13

Why is it important to learn about metabolism of a drug + 2 Eg?

Answer 13

Slide 23, 24, 25

Question 14

What assay to test for metabolism? and purpose?

Answer 14

Slide 26

Question 15

What assay to test for permeability?

Answer 15

Slide 27

Question 16

What secondary assays to select the best lead drug?

Answer 16

Slide 28 (2D) and Slide 29 (3D)

Question 17

Why should in vivo testing be done?

Answer 17

Slide 30

Question 18

How is in vivo studies done?

Answer 18

Slide 31, 32

Question 19

Why do we use human chimeric mice instead of control mice?

Answer 19

Slide 32

Question 20

What are some evaluation techniques/assays to evaluate drug?

Answer 20

Slide 33

Question 21

What are the key considerations for optimizing ADME?

Answer 21

• Summary of the content for considerations for ADME