TY - JOUR
T1 - The early preclinical and clinical development of ganaplacide (KAF156), a novel antimalarial compound
AU - Koller, Robin
AU - Mombo-Ngoma, Ghyslain
AU - Grobusch, Martin P.
PY - 2018
Y1 - 2018
N2 - Introduction: Ganaplacide (previously known as KAF156) is a novel antimalarial compound part of the imidazolopiperazine family. Areas covered: At the time of writing, a total of eight studies addressing its preclinical and clinical development have been published on this compound, which is currently in phase 2 of clinical development, alongside lumefantrine in a novel soluble formulation as combination partner. This review provides an overview and interpretation of the published pre-clinical and clinical data of this possible next-generation antimalarial drug. Expert opinion: In the search for a ‘magic bullet’ in malaria therapy and prophylaxis facilitating single encounter radical cure and prophylaxis, ganaplacide demonstrates some promising properties toward this ultimate goal. The available data suggest that ganaplacide exerts multi-stage antimalarial activity, and that its pharmacokinetic profile potentially allows for a simplified dosing regimen compared to that of existing antimalarial drug combinations. The first in-patient results demonstrate promising single-dose antimalarial activity, and no serious in-human safety and tolerability concerns have been reported to date.
AB - Introduction: Ganaplacide (previously known as KAF156) is a novel antimalarial compound part of the imidazolopiperazine family. Areas covered: At the time of writing, a total of eight studies addressing its preclinical and clinical development have been published on this compound, which is currently in phase 2 of clinical development, alongside lumefantrine in a novel soluble formulation as combination partner. This review provides an overview and interpretation of the published pre-clinical and clinical data of this possible next-generation antimalarial drug. Expert opinion: In the search for a ‘magic bullet’ in malaria therapy and prophylaxis facilitating single encounter radical cure and prophylaxis, ganaplacide demonstrates some promising properties toward this ultimate goal. The available data suggest that ganaplacide exerts multi-stage antimalarial activity, and that its pharmacokinetic profile potentially allows for a simplified dosing regimen compared to that of existing antimalarial drug combinations. The first in-patient results demonstrate promising single-dose antimalarial activity, and no serious in-human safety and tolerability concerns have been reported to date.
UR - https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85054436368&origin=inward
UR - https://www.ncbi.nlm.nih.gov/pubmed/30223692
U2 - https://doi.org/10.1080/13543784.2018.1524871
DO - https://doi.org/10.1080/13543784.2018.1524871
M3 - Review article
C2 - 30223692
SN - 1354-3784
VL - 27
SP - 803
EP - 810
JO - Expert opinion on investigational drugs
JF - Expert opinion on investigational drugs
IS - 10
ER -