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Research ArticleArticle

Bioavailability, Biotransformation, and Excretion of the Covalent BTK Inhibitor Acalabrutinib in Rats, Dogs, and Humans

Terry Podoll, Paul G. Pearson, Jerry Evarts, Tim Ingallinera, Elena Bibikova, Hao Sun, Mark Gohdes, Kristen Cardinal, Mitesh Sanghvi and J. Greg Slatter
Drug Metabolism and Disposition November 15, 2018, dmd.118.084459; DOI: https://doi.org/10.1124/dmd.118.084459
Terry Podoll
1 Acerta Pharma, South San Francisco, CA;
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  • For correspondence: terry.podoll@iv-po.com
Paul G. Pearson
2 Pearson Pharma Partners, Westlake Village, CA;
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Jerry Evarts
1 Acerta Pharma, South San Francisco, CA;
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Tim Ingallinera
1 Acerta Pharma, South San Francisco, CA;
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Elena Bibikova
1 Acerta Pharma, South San Francisco, CA;
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Hao Sun
3 Covance, Madison, WI;
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Mark Gohdes
3 Covance, Madison, WI;
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Kristen Cardinal
3 Covance, Madison, WI;
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Mitesh Sanghvi
4 Xceleron, Germantown, MD
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J. Greg Slatter
1 Acerta Pharma, South San Francisco, CA;
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Data Supplement

  • Supplemental Data -

    Supplemental Table 1 - Pharmacokinetic parameters for [14C]acalabrutinib and metabolites in pooled plasma samples after a single oral dose of [14C]acalabrutinib to rats (100 mg/kg)

    Supplemental Figure 1 - Reconstructed ion chromatogram and radiochromatogram from analysis of a 1-hour pooled plasma sample obtained from male rats after a single oral administration of [14C]ACP-196 (Group 1, 100 mg/kg)

    Supplemental Table 2 - Pharmacokinetic parameters for [14C]acalabrutinib and metabolites in pooled plasma samples after a single oral dose of [14C]acalabrutinib to dogs (30 mg/kg)

    Supplemental Figure 2 - Reconstructed ion chromatogram and radiochromatogram from analysis of a 2-hour pooled plasma sample obtained from male dogs after a single oral administration of [14C]ACP-196 (Group 1, 30 mg/kg)

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