LXE408

LXE408 is a first-in-class, orally active small molecule that acts as a selective inhibitor of the kinetoplastid proteasome. It was discovered by Novartis with support from Wellcome and is being co-developed with the Drugs for Neglected Diseases initiative (DNDi). LXE408 demonstrates potent anti-parasitic activity against all kinetoplastid parasites tested to date—including Leishmania species responsible for visceral and cutaneous leishmaniasis (such as L. donovani, L. infantum, L. major, and L. braziliensis), Trypanosoma cruzi (Chagas disease), and Trypanosoma brucei (human African trypanosomiasis). The drug exhibits high selectivity for the parasite proteasome over mammalian counterparts due to its noncompetitive binding mode revealed by cryo-EM studies. As of early 2025, it is in Phase II clinical trials for both visceral leishmaniasis in India and Ethiopia and cutaneous leishmaniasis in the Americas[1][2][4][6].

Other names

1799330-15-6CHEMBL4748352CHEMBL-4748352CHEMBL 4748352