Enrupatinib

Product Description

EI-1071 is a small-molecule drug that inhibits the tyrosine kinase activity of the Colony Stimulating Factor-1 Receptor (CSF-1R). EI-1071 has a potentially best-in-class therapeutic index or potency-versus-toxicity profile, shows efficient blood-brain-barrier penetration and causes robust reduction of brain microglia in pre-clinical models. EI-1071 also reduces tumor-associated macrophage numbers and improves tumor control in cancer models. Some pre-clinical data with EI-1071 was presented at the American Association for Cancer Research 2019 Annual Meeting, the abstract for which can be found here and the poster here. EI-1071 is a promising therapeutic candidate for Alzheimer's disease and other neurodegenerative diseases where microglia-mediated neuro-inflammation is implicated in disease progression. A first-in-human phase 1 clinical trial to evaluate safety of EI-1071 in healthy volunteers was recently completed, in which EI-1071 proved to be relatively safe. This phase 1 clinical trial and a new phase 2 trial in Alzheimer's disease patients, to evaluate the ability of EI-1071 to reduce neuro-inflammation as judged by imaging and other biomarkers (in preparation), were both funded in part thanks to the Alzheimer's Association Part the Cloud program. EI-1071 is also being developed for the treatment of recurrent and/or diffuse Tenosynovial Giant Cell Tumors (TGCT), a debilitating disease of the joints driven by over-expression of CSF-1, for which a phase 2 trial is being planned to start in 2023. (Sourced from: https://www.elixiron.com/)

Mechanisms of Action: CSF-1R Inhibitor

Novel Mechanism: No

Modality: Small Molecule

Route of Administration: Oral

FDA Designation: Orphan Drug - Idiopathic Pulmonary Fibrosis|Pulmonary Fibrosis *

Approval Status: Not Approved

Approved Countries: None

Approved Indications: None

Company: Elixiron Immunotherapeutics (Hong Kong) Ltd.
Company Location:
Company Founding Year: None
Additional Commercial Interests: None