unparalleled experience in all aspects of anti-fibrotic drug R&D.
Blade’s team has unparalleled experience in all aspects of anti-fibrotic drug R&D including target identification and the discovery and development of small molecule inhibitors, application of preclinical in vivo models of fibrosis, and biomarker discovery/characterization.
BLD-2660 is an optimized small molecule inhibitor of dimeric calpains. Calpains are non-lysosomal calcium dependent proteases. BLD-2660 is a best-in-class calpain inhibitor with robust anti-fibrotic activity in vivo. In biochemical studies, BLD-2660 exhibited potent and selective inhibition of calpains 1,2, and 9. BLD-2660 also proved to be efficacious in multiple animal models of pulmonary, skin, and liver fibrosis. BLD-2660 exhibited high selectivity against related cysteine proteases, high metabolic stability, and a favorable pharmacokinetic profile in preclinical species following oral and intravenous administration.
In July 2018, we initiated the the first-in-human Phase 1, placebo controlled, dose escalation trial that is evaluating the safety and pharmacokinetics (PK) profile of orally administered BLD-2660, a selective small molecule dimeric calpain inhibitor, in healthy volunteers. This study is being conducted in Australia with initial results from healthy volunteers expected by the fourth quarter of 2018.
Our preclinical research has demonstrated:
- Treatment of pulmonary fibrosis and liver fibrosis by applying BLD-2660 in preclinical in vivo prophylactic and therapeutic models
- Evidence of strong potency and selectivity
- Elevated expression of calpain in fibrotic disease has been shown to be commensurate with disease status