A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers

• Main Authors: Leong, F.J, Zhao, R, Zeng, S, Magnusson, B, Diagana, T.T, Pertel, P
• Other Authors: MICROBIOLOGY AND IMMUNOLOGY
• Format: Article
• Published: American Society for Microbiology 2020
• Subjects: alanine aminotransferase; alkaline phosphatase; antimalarial agent; imidazolopiperazine; placebo; unclassified drug; imidazole derivative; KAF156; piperazine derivative; abdominal pain; adult; alanine aminotransferase blood level; alkaline phosphatase blood level; application site excoriation; area under the curve; Article; blood chemistry; controlled study; contusion; diarrhea; diet restriction; dizziness; dose calculation; double blind procedure; drug absorption; drug blood level; drug clearance; drug half life; drug induced headache; drug safety; drug tolerability; drug withdrawal; elimination half-life; eye injury; female; first in human study; follow up; food intake; gastritis; gastrointestinal disease; hematology; hematuria; human; joint injury; kidney clearance; laceration; limb pain; major clinical study; malaria; male; maximum plasma concentration; nausea; neuralgia; neurologic disease; oropharynx pain; peripheral edema; presyncope; randomized controlled trial; repeated drug dose; rhinitis; risk assessment; side effect; single drug dose; systemic circulation; time to maximum plasma concentration; upper respiratory tract infection; urinalysis; urinary excretion; volume of distribution; vomiting; adolescent; dose response; drug administration; drug effects; drug resistance; intestine absorption; middle aged; normal human; oral drug administration; parasitology; physiology; Plasmodium falciparum; Plasmodium vivax; young adult; Administration, Oral; Adolescent; Adult; Antimalarials; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Drug Resistance; Female; Healthy Volunteers; Humans; Imidazoles; Intestinal Absorption; Malaria; Male; Middle Aged; Piperazines; Placebos; Young Adult
• Online Access: https://scholarbank.nus.edu.sg/handle/10635/180135
• Institution: National University of Singapore

10.1128/AAC.03478-14