Refining the in vitro and in vivo critical parameters for p-glycoprotein, [I]/IC50 and [I2]/IC50, that allow for the exclusion of drug candidates from clinical digoxin interaction studies

Molecular Pharmaceutics

Volumn 7, Issue 2, 2010, Pages 398-411

  Cook, Jack A ^a,b   Feng, Bo ^b   Fenner, Katherine S ^b   Kempshall, Sarah ^b   Liu, Ray ^b   Rotter, Charles ^b   Smith, Dennis A ^b   Troutman, Matthew D ^b   Ullah, Mohammed ^b   Lee, Caroline A ^b  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b Department of Dynamics and Metabolism ^*

Author keywords

I2 IC50; I IC 50; Calcein AM; Digoxin; IC50; In vitro in vivo correlation; P glycoprotein (P gp); Pharmacokinetics; Receiver operating characteristic (ROC)

Indexed keywords

AMIODARONE; ATORVASTATIN; AVASIMIBE; CAPTOPRIL; CARVEDILOL; CONIVAPTAN; DIGOXIN; DILTIAZEM; DOFETILIDE; EPLERENONE; FELODIPINE; GLYCOPROTEIN P; ISRADIPINE; LANOXICAP; LASOFOXIFENE; MILAMELINE; NICARDIPINE; NIFEDIPINE; NITRENDIPINE; PRAMIPEXOLE; QUINIDINE; RANOLAZINE; SERTRALINE; TELMISARTAN; TORCETRAPIB; TROGLITAZONE; UK 369003; UNCLASSIFIED DRUG; UNINDEXED DRUG; VARENICLINE; VERAPAMIL; VORICONAZOLE;

AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG POTENCY; FALSE NEGATIVE RESULT; FALSE POSITIVE RESULT; HUMAN; HUMAN CELL; IC 50; MAXIMUM PLASMA CONCENTRATION; MEASUREMENT ERROR; PREDICTION; PRIORITY JOURNAL; RELIABILITY; STEADY STATE;

CLINICAL TRIALS AS TOPIC; DIGOXIN; DRUG INTERACTIONS; HUMANS; INHIBITORY CONCENTRATION 50; P-GLYCOPROTEIN; PHARMACEUTICAL PREPARATIONS;

EID: 77950571874     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp900174z     Document Type: Article

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