OSU-03012


OSU-03012 is a celecoxib derivative with anticancer and anti-microbial activity. Unlike celecoxib, OSU-03012 does not inhibit COX, but inhibits several other important enzymes instead which may be useful in the treatment of some forms of cancer. When combined with PDE5 inhibitors such as sildenafil or tadalafil, OSU-03012 was found to show enhanced anti-tumour effects in cell culture. OSU-03012 has been shown to inhibit completely vaccinia virus in cell based assay.

Antimicrobial agent

Antimicrobial activity is often not against the microbe directly, but rather host-directed activity that works on the cellular host to disrupt the pathogen within the cell. Since the median lethal dose, in vitro, against macrophages is ~7 μM and near its effective concentration formulation of the compound has been shown to enhances its activity. For example, encapsulation of OSU-03012 into biodegradable polymeric micro/nanoparticles significantly reduces cytotoxicity, increases drug concentration per a cell, reduces toxicity in vivo, and facilitates needle-free delivery in vivo.

Orphan drug designation

The European Commission has designated OSU-03012 as an orphan drug for use in combination with other drugs for treatment of two infections diseases, cryptococcosis and tularaemia. OSU-03012 received an orphan drug designation in combination with the antifungal drug fluconazole for cryptococcosis of the brain. It also received this designation for tularaemia in combination with the antibacterial drug gentamicin.