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

• Main Authors: Leong, F.J, Li, R, Jain, J.P, Lefèvre, G, Magnusson, B, Diagana, T.T, Partel, P
• Other Authors: MICROBIOLOGY AND IMMUNOLOGY
• Format: Article
• Published: American Society for Microbiology 2020
• Subjects: alanine aminotransferase; amylase; aspartate aminotransferase; bilirubin; cipargamin; creatine kinase; fat; lactate dehydrogenase; liver enzyme; paracetamol; placebo; triacylglycerol lipase; antimalarial agent; indole derivative; spiro compound; abdominal discomfort; adult; alanine aminotransferase blood level; amylase blood level; area under the curve; Article; aspartate aminotransferase blood level; bilirubin blood level; cohort analysis; controlled study; diarrhea; dizziness; double blind procedure; drug absorption; drug blood level; drug clearance; drug distribution; drug efficacy; drug elimination; drug exposure; drug half life; drug induced headache; drug safety; drug tolerability; enzyme blood level; female; follow up; food intake; gastrointestinal symptom; hematoma; human; human experiment; lactate dehydrogenase blood level; lipid diet; male; maximum plasma concentration; nausea; pharmacological parameters; randomized controlled trial; semen abnormality; side effect; single drug dose; time to maximum plasma concentration; triacylglycerol lipase blood level; urinalysis; dose response; drug administration; normal human; Antimalarials; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Healthy Volunteers; Humans; Indoles; Spiro Compounds
• Online Access: https://scholarbank.nus.edu.sg/handle/10635/180137
• Institution: National University of Singapore

10.1128/AAC.03393-14