Acalabrutinib (ACP-196): A covalent Bruton tyrosine kinase inhibitor with a differentiated selectivity and in vivo potency profile

Journal of Pharmacology and Experimental Therapeutics

Volumn 363, Issue 2, 2017, Pages 240-252

  Barf, Tjeerd ^a   Covey, Todd ^a   Izumi, Raquel ^a   Van De Kar, Bas ^a   Gulrajani, Michael ^a   Van Lith, Bart ^a   Van Hoek, Maaike ^a   De Zwart, Edwin ^a   Mittag, Diana ^a   Demont, Dennis ^a   Verkaik, Saskia ^a   Krantz, Fanny ^a   Pearson, Paul G ^a   Ulrich, Roger ^a   Kaptein, Allard ^a  

^a Acerta Pharma BV   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

ACALABRUTINIB; EPIDERMAL GROWTH FACTOR RECEPTOR; IBRUTINIB; INTERLEUKIN 2; SPEBRUTINIB; AGAMMAGLOBULINAEMIA TYROSINE KINASE; BENZAMIDE DERIVATIVE; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PYRAZINE DERIVATIVE;

ADULT; ANIMAL EXPERIMENT; ARTICLE; AUC (0-24 H); CONTROLLED STUDY; COVALENT BOND; DRUG BINDING; DRUG CLEARANCE; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INHIBITION; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; ENZYME INHIBITION; HUMAN; HUMAN CELL; HUMAN EXPERIMENT; IN VIVO STUDY; MAXIMUM CONCENTRATION; MOUSE; NONHUMAN; NORMAL HUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PRIORITY JOURNAL; PROTEIN EXPRESSION; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUME OF DISTRIBUTION; ANIMAL; ANTAGONISTS AND INHIBITORS; BAGG ALBINO MOUSE; BLOOD; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; ENZYMOLOGY; JURKAT CELL LINE; METABOLISM; MONONUCLEAR CELL;

ANIMALS; BENZAMIDES; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; JURKAT CELLS; LEUKOCYTES, MONONUCLEAR; MICE; MICE, INBRED BALB C; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRAZINES;

EID: 85032433762     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.117.242909     Document Type: Article

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