Research ArticleArticle
Identification of Three Novel Ring Expansion Metabolites of KAE609, a New Spiroindolone Agent for the Treatment of Malaria, in Rats, Dogs, and Humans
Su-Er W. Huskey, Chun-qi Zhu, Melissa M. Lin, Ry R. Forseth, Helen Gu, Oliver Simon, Fabian K. Eggimann, Matthias Kittelmann, Alexandre Luneau, Alexandra Vargas, Hongmei Li, Lai Wang, Heidi J. Einolf, Jin Zhang, Sarah Favara, Handan He and James B. Mangold
Drug Metabolism and Disposition May 2016, 44 (5) 653-664; DOI: https://doi.org/10.1124/dmd.115.069112
Su-Er W. Huskey
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Chun-qi Zhu
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Melissa M. Lin
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Ry R. Forseth
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Helen Gu
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Oliver Simon
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Fabian K. Eggimann
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Matthias Kittelmann
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Alexandre Luneau
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Alexandra Vargas
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Hongmei Li
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Lai Wang
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Heidi J. Einolf
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Jin Zhang
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Sarah Favara
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
Handan He
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
James B. Mangold
Drug Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, East Hanover, New Jersey (S.-E.W.H., C.Z., R.R.F., H.G., H.L., L.W., H.J.E., J.Z., S.F., H.H., J.B.M.); Technical Research and Development, Novartis Pharma, East Hanover, NJ (M.M.L.); Novartis Institute for Tropical Diseases, Singapore (O.S.); and Global Discovery Chemistry, Bioreactions Group, Novartis Institutes for BioMedical Research, Basel, Switzerland (F.K.E., M.K., A.L., A.V.)
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In this issue
Research ArticleArticle
Ring Expansion Metabolites of KAE609 (a Spiroindolone)
Su-Er W. Huskey, Chun-qi Zhu, Melissa M. Lin, Ry R. Forseth, Helen Gu, Oliver Simon, Fabian K. Eggimann, Matthias Kittelmann, Alexandre Luneau, Alexandra Vargas, Hongmei Li, Lai Wang, Heidi J. Einolf, Jin Zhang, Sarah Favara, Handan He and James B. Mangold
Drug Metabolism and Disposition May 1, 2016, 44 (5) 653-664; DOI: https://doi.org/10.1124/dmd.115.069112
Research ArticleArticle
Ring Expansion Metabolites of KAE609 (a Spiroindolone)
Su-Er W. Huskey, Chun-qi Zhu, Melissa M. Lin, Ry R. Forseth, Helen Gu, Oliver Simon, Fabian K. Eggimann, Matthias Kittelmann, Alexandre Luneau, Alexandra Vargas, Hongmei Li, Lai Wang, Heidi J. Einolf, Jin Zhang, Sarah Favara, Handan He and James B. Mangold
Drug Metabolism and Disposition May 1, 2016, 44 (5) 653-664; DOI: https://doi.org/10.1124/dmd.115.069112
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