Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TABLE 3.3 (

Continued

)

Isoenzyme

Endogenous substrates

Reported

Km

Drug or xenobiotic

substrates

Inducers

Inhibitors

ibuprofen, ketoprofen,mefenamic acid,naproxen (low activityagainst all NSAIDs),bumetanide, furosemide,(dapsone), ethinylestradiol -minor),dobutamine, dopamine,levodopa, carbidopa,entacapone,

R

–oxazepam,

emodin, chrysin,7-hydroxyflavone, galangin,naringenin, quercetincarveol, nopol, citronellol,6-hydroxychrysene

UGT1A10

2-OH-estrone (low),

4-OH estrone (low),dihydrotestosterone,testosterone

Alizarin, anthraflavic acid,

apigenin, Benzo(a)pyrene-t-7,8-dihydrodiol (7

R- and

8 S

-glucuronides, high affinity),

emodin, fisetin, genistein,naringenin, quercetin,quinalizarin, 4-methylumbelliferone,scopoletin, carvacrol, eugenol,mycophenolic acid, 17

b-methyl-

5 b

–androst-4-ene-3

a,17

a-diol

(metabolite of metadienone),nandrolone, 1-methyl-5

a-androst-

1-en-17

b–ol-3-one (metabolite

of metenolone), 5

a-androstane-3

a,

17

b-diol (metabolite of testosterone),

SN-38 (minor), raloxifene(4

0 - b

-glucuronide only)

52