Small molecules as kinetoplastid specific proteasome inhibitors for leishmaniasis: a patent review from 1998 to 2021.
Mohd ImranShah Alam KhanAbida KhanAhmed Subeh AlshrariMahmoud Mudawi Eltahir MudawiMohammed Kanan AlshammariAishah Ali HarshanNoufah Aqeel AlshammariPublished in: Expert opinion on therapeutic patents (2022)
A little amount of work has been done on KSPIs, but the study results are quite encouraging. LXE408 and GSK3494245 are two KSPIs in different phases of clinical trials. Some other small molecules have also shown KSP inhibitory potential, but they are not in clinical trials. The KSPIs are promising next-generation orally active patient compliant drugs against kinetoplastid diseases, including leishmaniasis. However, the main challenge to discover the KSPIs will be the resistance development and their selectivity against the proteasome of eukaryotic cells.