Drug Metabolism in Drug Design and Development Basic Concepts and Practice

Bile acids:

hyodexycholic acid

Estrogens:

Estriol, estradiol

(17

b-hydroxy), 4-hydroxy estrone

(high) 2- hydroxy estrone,2- hydroxy estriol

Pregnanes:

3 a

-hydroxy pregnanes,

Androgens:

3 a

-, 16

a-, 17

b-androgens,

Others:

5 a

• and

5 b

-dihydroaldosterone,

trans-retinoic acid,

Carboxylic acid-containing drugs:

benoxaprofen, ciprofibrate, clofibricacid, diflunisal, dimethylxanthenone-4-acetic acid (DMXAA), fenoprofen,ibuprofen, indomethacin, ketoprofen,naproxen, pitavastatin, simvastatinacid, tiaprofenic acid,valproic acid, zaltoprofen, zomepirac.

Opioids:

morphine 3OH

>

6OH,

buprenorphine, nalorphine,naltrexone, codeine (low)and naloxone.

UGT2B8UGT2B9 C18, C19, C20 steroids,

fatty acids (C6–C12)

Morphine

UGT2B10 No known substratesUGT2B11 No known substratesUGT2B12UGT2B13

17

b-Estradiol

(low)

4-Hydroxy biphenyl

4-Hydroxy

biphenyl(competitive)

UGT2B14

Estriol

UGT2B15

Testosterone

,

dihydrotestosterone

S-oxazepam:

30

mM (Court, 2002)

UGT2B16UGT2B17

Testosterone

, androsterone

UGT2B18UGT2B19UGT2B20UGT2B21

55