Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TABLE 17.1 CYP isoform-specific inducers and substrates used in

in vitro

models.

CYP

Preferred inducer (

m

M)

Acceptable inducer (

m

M)

Substrate

References

1A2

3-Methylcholanthrene (2)

Lansoprazole (10)

7-Ethoxyresorufin

Curi-Pedrosa et al., (1994)

Omeprazole (25–100)

LeCluyse et al., (2000)

b-Naphthoflavone (33–50)

Meunier et al., (2000)

2A6

Dexamethasone (50)

Pyrazole (1000)

Coumarin

Meunier et al., (2000)

2B6

Phenobarbital (500–1000)

Phenytoin (50)

S-Mephenytoin

LeCluyse et al., (2000)

2C8

Rifampin (10)

Phenobarbital (500)

Paclitaxel

LeCluyse et al., (2000)Gerbal-Chaloin et al., (2001)

2C9

Rifampin (10)

Phenobarbital (100)

S-Warfarin

Gerbal-Chaloin et al., (2001)

2C19

Rifampin (10)

S-Mephenytoin

Gerbal-Chaloin et al., (2001)

3A4

Rifampin (10)

Phenobarbital (100–2000)

Testosterone

Goodwin et al., (1999)

Dexamethasone (33–250)

Midazolam

LeCluyse et al., (2000)

Phenytoin (50)

Luo et al., (2002)

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