Preclinical studies for repurposing of Aloxistatin

Infection with SARS-CoV-2 can lead to severe courses of COVID-19. Effective therapies that limit mortality from this disease and thereby also help maintain a well-functioning healthcare system continue to be in high demand. Aloxistatin (E64D) is a cysteine protease inhibitor that has been known for many decades and was originally developed for treating neurodegenerative diseases and muscular dystrophy. In addition, Aloxistatin has shown efficient inhibition of SARS-CoV-2 replication in in-vitro experiments, making this drug, which has already undergone clinical testing, a candidate for drug repurposing for COVID-19 treatment.

Under the BMBF funding call "Investigation of COVID-19 following the outbreak of SARS-CoV-2", inhalation toxicology studies under GLP conditions were performed at Fraunhofer ITEM to prepare for regulatory approval of the cysteine protease inhibitor Aloxistatin.  The studies included safety pharmacological and histopathological endpoints as well as blood tests. Given the successful toxicological characterization of Aloxistatin, a phase-I inhalation trial with Aloxistatin in healthy volunteers has now been initiated at the University Medical Center Freiburg im Breisgau, Germany.