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OSU-03012 (AR-12) 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, while also having antifungal activity via disruption of phosphoinositide-dependent kinase-1 activity. When combined with PDE5 inhibitors such as sildenafil or tadalafil, OSU-03012 was found to show enhanced anti-tumour, antibiotic and antiviral activity against a wide variety of organisms, with this activity thought to be mediated via inhibition of the chaperone protein BiP.
Orphan drug designation
The European Commission has designated AR-12 as an orphan drug for use in combination with other drugs for treatment of two infections diseases, cryptococcosis and tularaemia. AR-12 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.
