Brain accumulation of the EML4-ALK inhibitor ceritinib is restricted by P-glycoprotein (P-GP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2)

Pharmacological Research

Volumn 102, Issue , 2015, Pages 200-207

  Kort, Anita ^a   Sparidans, Rolf W ^b   Wagenaar, Els ^a   Beijnen, Jos H ^a,b   Schinkel, Alfred H ^a  

^a NETHERLANDS CANCER INSTITUTE   (Netherlands)

^b UTRECHT UNIVERSITY   (Netherlands)

Author keywords

ABCB1; ABCG2; ALK inhibitor; Blood brain barrier; Ceritinib; Oral availability

Indexed keywords

1,2,3,4,6,7,12,12A OCTAHYDRO 6 ISOBUTYL 9 METHOXY 1,4 DIOXOPYRAZINO[1',2':1,6]PYRIDO[3,4 B]INDOLE 3 PROPANOIC ACID TERT BUTYL ESTER; BREAST CANCER RESISTANCE PROTEIN; CERITINIB; MULTIDRUG RESISTANCE PROTEIN; MULTIDRUG RESISTANCE PROTEIN 1; ABC TRANSPORTER; ABCG2 PROTEIN, MOUSE; ANAPLASTIC LYMPHOMA KINASE; CRIZOTINIB; MICROTUBULE ASSOCIATED PROTEIN; ONCOPROTEIN; ORGANIC ANION TRANSPORTER; PROTEIN TYROSINE KINASE; PYRAZOLE DERIVATIVE; PYRIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; SULFONE; TUMOR PROTEIN;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; DRUG ABSORPTION; DRUG ACCUMULATION; DRUG BIOAVAILABILITY; DRUG BRAIN LEVEL; DRUG DISPOSITION; IN VITRO STUDY; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOAVAILABILITY; BRAIN; DRUG EFFECTS; KNOCKOUT MOUSE; METABOLISM; PHYSIOLOGY; TISSUE DISTRIBUTION; TRANSPORT AT THE CELLULAR LEVEL;

ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT; BLOOD-BRAIN BARRIER; BRAIN; MALE; MICE; MICE, KNOCKOUT; MICROTUBULE-ASSOCIATED PROTEINS; NEOPLASM PROTEINS; ONCOGENE PROTEINS, FUSION; ORGANIC ANION TRANSPORTERS; P-GLYCOPROTEINS; PYRAZOLES; PYRIDINES; PYRIMIDINES; RECEPTOR PROTEIN-TYROSINE KINASES; SULFONES; TISSUE DISTRIBUTION;

EID: 84946832481     PISSN: 10436618     EISSN: 10961186     Source Type: Journal    
DOI: 10.1016/j.phrs.2015.09.003     Document Type: Article

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