Drug Metabolism in Drug Design and Development Basic Concepts and Practice

Etoposide

PSC-833(Valspodar)



Decrease in total

clearance (



41%),

renal clearance (



32%)

and nonrenalclearance (



48%)

P-gp, CYP3A4

Boote et al. (1996)

Erythromycin



Rifampin Increase in erythromycin

breath test (ERMBT value):(median ERMBT iv:twofold, oral: unchanged)

P-gp, CYP3A4

Paine et al. (2002)

Fexofenadine

Erythromycin



Increase in AUC

(2.09-fold) andC

max

(1.82-fold)

P-gp

Davit et al. (1999)

Fexofenadine

Erythromycin



Increase in AUC

(+109%)

P-gp

Simpson and Jarvis (2000)

Fexofenadine

Azithromycin



Increase in AUC

(+67%)

P-gp

Gupta et al. (2001)

Fexofenadine



Rifampin Increase in oral

clearance (1.9-fold)and

C

max

(0.59-fold),

no change in renalclearance and

t1/2

P-gp

Hamman et al. (2001)

Fexofenadine

Azithromycin



Increase in

AUC (+67%)

P-gp

Gupta et al. (2001)

Fexofenadine



St. John’s

wort

Decrease in AUC

(

14%), after long-term

administration

P-gp

Wang et al. (2002)

Fexofenadine

Ketoconazole



Increase in AUC

(2.64-fold) andC

max

(2.35-fold)

P-gp

Davit et al. (1999)

(continued

)

165