Auspex Pharmaceuticals, Inc, a late clinical stage biopharmaceutical company focussed on developing and commercialising novel medicines for the treatment of orphan diseases, has received US patent for composition of matter and method of treatment covering its deuterium-containing form of pirfenidone (SD-560) drug candidate being developed for the potential treatment of idiopathic pulmonary fibrosis (IPF) and other fibrotic conditions:
US Patent No. 8,680,123 covers the method of treatment, prevention or amelioration of, among other things, fibrotic conditions such as IPF with SD-560;US Patent No. 8,383,823 is a composition of matter patent covering SD-560; and European Patent No. 2170828B covers deuterium-containing form of pirfenidone, including SD-560, pharmaceutical composition and method of treatment using such deuterated pirfenidone for the treatment, prevention or amelioration of IPF and other fibrotic conditions.
"Our pioneering efforts in the field of selective deuterium modifications for improving the metabolic stability and pharmacokinetic profile of oral small molecules are continuing to be validated through the issuance of additional composition of matter and method of treatment claims worldwide," said Pratik Shah, president and chief executive officer of Auspex. "The expansion of our intellectual property estate and, in particular, these new patents significantly enhance the value proposition for our SD-560 programme."
SD-560 is a novel investigational drug in late pre-clinical development for the potential treatment of orphan indications such as IPF and other fibrotic conditions. SD-560 is on track to initiate Phase 1 clinical trials with data expected to be reported in 2015. Using our proprietary capabilities in deuterium chemistry, we have made chemical modifications within the pirfenidone molecule to create the novel drug candidate SD-560. Deuterium is a non-toxic, naturally occurring form of hydrogen. The substitution of deuterium (2H) for hydrogen (1H) at specific positions improves the stability of pirfenidone and attenuates the breakdown of the drug's active metabolite resulting in a differentiated pharmacokinetic profile compared to pirfenidone. This profile should enable less frequent dosing, improved tolerability, reduced interpatient variability in drug metabolism, as well as reduced drug interactions and potentially improved efficacy. Pirfenidone is known to reduce the proliferation of fibroblasts and inhibits the production of fibrogenic and inflammatory mediators such as TGF-beta, TNF-alpha and IL-1beta. Pirfenidone has been approved in Europe, Japan, Canada, India and other countries for the treatment of IPF, but has limited efficacy, significant side effects and must be taken three to four times daily. Auspex believes that SD-560 can potentially have significant benefits over pirfenidone in efficacy as well as safety and tolerability.