Research ArticleMetabolism, Transport, and Pharmacogenetics
Open Access
Identification and Characterization of ACP-5862, the Major Circulating Active Metabolite of Acalabrutinib: Both Are Potent and Selective Covalent Bruton Tyrosine Kinase Inhibitors
Terry Podoll, Paul G. Pearson, Allard Kaptein, Jerry Evarts, Gerjan de Bruin, Maaike Emmelot-van Hoek, Anouk de Jong, Bart van Lith, Hao Sun, Stephen Byard, Adrian Fretland, Niels Hoogenboom, Tjeerd Barf and J. Greg Slatter
Journal of Pharmacology and Experimental Therapeutics January 2023, 384 (1) 173-186; DOI: https://doi.org/10.1124/jpet.122.001116
Terry Podoll
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Paul G. Pearson
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Allard Kaptein
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Jerry Evarts
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Gerjan de Bruin
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Maaike Emmelot-van Hoek
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Anouk de Jong
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Bart van Lith
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Hao Sun
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Stephen Byard
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Adrian Fretland
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Niels Hoogenboom
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
Tjeerd Barf
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
J. Greg Slatter
Acerta Pharma (a member of the AstraZeneca group), South San Francisco, California (T.P., J.E., A.F., J.G.S.); Acerta Pharma (a member of the AstraZeneca group) Oss, The Netherlands (G.d.B., M.E.-v.H., A.d.J., B.v.L., N.H.); Pearson Pharma Partners, Westlake Village, California (P.G.P.); Covance Laboratories, Madison, Wisconsin (H.S.); Arcinova, Alnwick, United Kingdom (S.B.); and Covalution Holding B.V., Ravenstein, The Netherlands (A.K., T.B.)
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Research ArticleMetabolism, Transport, and Pharmacogenetics
ACP-5862—Major Metabolite of BTK Inhibitor Acalabrutinib
Terry Podoll, Paul G. Pearson, Allard Kaptein, Jerry Evarts, Gerjan de Bruin, Maaike Emmelot-van Hoek, Anouk de Jong, Bart van Lith, Hao Sun, Stephen Byard, Adrian Fretland, Niels Hoogenboom, Tjeerd Barf and J. Greg Slatter
Journal of Pharmacology and Experimental Therapeutics January 1, 2023, 384 (1) 173-186; DOI: https://doi.org/10.1124/jpet.122.001116
Research ArticleMetabolism, Transport, and Pharmacogenetics
ACP-5862—Major Metabolite of BTK Inhibitor Acalabrutinib
Terry Podoll, Paul G. Pearson, Allard Kaptein, Jerry Evarts, Gerjan de Bruin, Maaike Emmelot-van Hoek, Anouk de Jong, Bart van Lith, Hao Sun, Stephen Byard, Adrian Fretland, Niels Hoogenboom, Tjeerd Barf and J. Greg Slatter
Journal of Pharmacology and Experimental Therapeutics January 1, 2023, 384 (1) 173-186; DOI: https://doi.org/10.1124/jpet.122.001116
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