Drug Metabolism in Drug Design and Development Basic Concepts and Practice

SLC10A2

ASBT

Intestine, kidney

Bile salts, such as taurocholate

All major bile salts,

BQ-123, CsA

SLC15A1

PEPT1

Intestine, Kidney

Dipeptides, tripeptides, and

peptidomimetic drugs suchas glycylsarcrosine,valacyclovir,and

b

-lactam antibiotics

(cephalexin, ceftibuten)

Glycylsarcrosine,

protonophore, suchas carbonyl cyanide4-trifluoromethoxy-phenylhydrazone(FCCP) and inhibitorsof the Na+/H+exchanger, such asamiloride

H

+

dependent

SLC15A2

PEPT2

Kidney

SLC21A8/

SLCO1B3

OATP-8,

OATP1B3

Liver

Digoxin, bile acids, BQ123,

E17

bG, DHEAS,

estrone sulfate

Digoxin

SLC21A3/

SLCO1A2

OATP-A,

OATP,OATP1A2

Brain, liver, intestine,

testis, prostate

Relative bulky and

hydrophobic organicanions (including bile acid,bilirubin, prostaglandin E

, 2

tetraiodothyronine, andtriiodothyronine), neutralcompound ouabain, andorganic cations such asN

-methyl quinidine and

rocuronium.

CsA, verapamil, rifampin,

ketoconazole, HIVinhibitors, Quinidine,indocyanine green

ND

SLC21A6/

SLCO1B1

OATP-C,

LST-1,OATP2,OATP1B1

Liver

Estrone Sulfate, E17

bG,

DHEAS, bromsulfophtalein(BSP), fexofenadine, DNP-

s-

glutathione, LTC

, pravastatin, 4

rifampicin

(continued

)

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