In May, 2005, a single stranded LNA oligonucleotide (SPC2996) entered a multi-center Phase I/II clinical study in patients with Chronic Lymphocytic Leukaemia (CLL). This study is conducted by the Copenhagen-based company Santaris Pharma which holds world-wide rights to commercialize LNA therapeutics. This antisense LNA molecule targets Bcl-2 mRNA, and is of the so-called gapmer constitution with two LNA flanks around a central DNA segment enabling efficient RNA binding and RNAase H mediated cleavage of target RNA.
Enzon Pharmaceuticals, who has entered into close collaboration with Santaris Pharma, plans to initiate clinical trails with a second LNA antisense molecule during first quarter 2007. Also this LNA antisense molecule that targets HIF-1α mRNA is designed as an oncology product.
See http://www.santaris.com for further information.