KAE609 (Cipargamin), a New Spiroindolone Agent for the Treatment of Malaria: Evaluation of the Absorption, Distribution, Metabolism, and Excretion of a Single Oral 300-mg Dose of [14C]KAE609 in Healthy Male Subjects

• Published in: Drug metabolism and disposition Vol. 44; no. 5; pp. 672 - 682
• Main Authors: Huskey, Su-Er W., Zhu, Chun-qi, Fredenhagen, Andreas, Kühnöl, Jürgen, Luneau, Alexandre, Jian, Zhigang, Yang, Ziping, Miao, Zhuang, Yang, Fan, Jain, Jay P., Sunkara, Gangadhar, Mangold, James B., Stein, Daniel S.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.05.2016
• Subjects: Administration, Oral; Adult; Body Fluids - metabolism; Carbon Radioisotopes - metabolism; Feces - chemistry; Healthy Volunteers; Humans; Hydroxylation - drug effects; Indoles - pharmacology; Malaria - drug therapy; Male; Metabolic Networks and Pathways - drug effects; Middle Aged; Oxidation-Reduction; Spiro Compounds - pharmacology; DPM; LLOQ; ADME; MS; AUC; LC-MS/MS; SFC; NMR; QC; Vz/F; t1/2; UPLC; m/z; ICRP; P450; PK; PRA; HPLC; CL/F; KAE609

KAE609 [(1′R,3′S)-5,7′-dichloro-6′-fluoro-3′-methyl-2′,3′,4′,9′-tetrahydrospiro[indoline-3,1′-pyridol[3,4-b]indol]-2-one] is a potent, fast-acting, schizonticidal agent in clinical development for the treatment of malaria. This study investigated the absorption, distribution, metabolism, and excreti...