Identification of Three Novel Ring Expansion Metabolites of KAE609, a New Spiroindolone Agent for the Treatment of Malaria, in Rats, Dogs, and Humans

No abstract is available for this paper.

• Publication year

  2016

• Venue

  Drug Metabolism And Disposition

• Publication date

  2016-05-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/dmd.115.069112PMID 26921386
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• 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

  2016cited by this paper
• Artemisinin resistance-associated polymorphisms at the K13-propeller locus are absent in Plasmodium falciparum isolates from Haiti.

  2015cited by this paper
• Artemisinin-Resistant Plasmodium falciparum Parasites Exhibit Altered Patterns of Development in Infected Erythrocytes

  2015cited by this paper
• A First-in-Human Randomized, Double-Blind, Placebo-Controlled, Single- and Multiple-Ascending Oral Dose Study of Novel Antimalarial Spiroindolone KAE609 (Cipargamin) To Assess Its Safety, Tolerability, and Pharmacokinetics in Healthy Adult Volunteers

  2014cited by this paper
• Spiroindolone KAE609 for falciparum and vivax malaria.

  2014cited by this paper
• Antimalarial drug resistance in Bangladesh, 1996-2012.

  2013cited by this paper
• Na+ Regulation in the Malaria Parasite Plasmodiumfalciparum Involves the Cation ATPase PfATP4 and Is a Target of the Spiroindolone Antimalarials

  2013cited by this paper
• Emerging artemisinin resistance in the border areas of Thailand

  2013cited by this paper
• Reduced Artemisinin Susceptibility of Plasmodium falciparum Ring Stages in Western Cambodia

  2012cited by this paper
• Why do metabolites circulate?

  2012cited by this paper
• Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery

  2011cited by this paper
• Spirotetrahydro β-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria

  2010cited by this paper
• Spiroindolones, a Potent Compound Class for the Treatment of Malaria

  2010cited by this paper
• Assessment of three human in vitro systems in the generation of major human excretory and circulating metabolites.

  2009cited by this paper
• Metabolites in safety testing (MIST): considerations of mechanisms of toxicity with dose, abundance, and duration of treatment.

  2009cited by this paper
• Predicting circulating human metabolites: how good are we?

  2009cited by this paper
• Metabolism and toxicity of drugs. Two decades of progress in industrial drug metabolism.

  2008cited by this paper
• Oxidative and nonoxidative decarboxylation of N-Alkyl-N-phenylglycines by horseradish peroxidase. Mechanistic switching by varying hydrogen peroxide, oxygen, and solvent deuterium.

  2004cited by this paper
• Antimalarial drug resistance.

  2004cited by this paper
• Drug metabolites in safety testing.

  2003cited by this paper
• Drug metabolites in safety testing.

  2002cited by this paper
• Non-oxidative decarboxylation of glycine derivatives by a peroxidase.

  2002cited by this paper

• CYP3A-Mediated Carbon–Carbon Bond Cleavages in Drug Metabolism

  2024cites this paper
• Recent developments in antimalarial drug discovery.

  2023cites this paper
• Metabolite Bioanalysis in Drug Development: Recommendations from the IQ Consortium Metabolite Bioanalysis Working Group

  2023cites this paper
• The early preclinical and clinical development of cipargamin (KAE609), a novel antimalarial compound.

  2020cites this paper
• Flow-cell radionuclide analysis

  2020cites this paper
• Pharmacokinetics and Metabolite Profiling of Trepibutone in Rats Using Ultra-High Performance Liquid Chromatography Combined With Hybrid Quadrupole-Orbitrap and Triple Quadrupole Mass Spectrometers

  2019cites this paper
• The development process for discovery and clinical advancement of modern antimalarials.

  2019cites this paper
• 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

  2016influential citation