Phase IIa proof-of-concept trial meets primary and secondary endpoints

Marburg, Germany, 21 February 2014

  • Significant improvement in lung function in both early and late phase asthmatic response

  • Outstanding safety profile confirmed

sterna biologicals GmbH & Co. KG (“sterna biologicals”) announced today top-line results of its recently completed phase IIa proof-ofconcept trial of SB010, an inhaled first-in-class GATA-3 antagonist for the treatment of Th2- driven asthma. The study – a randomised, double-blind, parallel group, multi-centre clinical trial – was designed to establish efficacy of SB010 in improving lung function (FEV1) as measured by the area under the FEV1 curve (AUC) in the late phase asthmatic response after specific allergen challenge compared to placebo treatment.

43 mild asthmatic patients were randomised to obtain 39 evaluable patients (N=21 in SB010 group and N=18 in placebo group) with respect to the primary endpoint. Participants were exposed to the same concentration of their respective specific allergen pre and post 28 day dosing. At screening, patients had to demonstrate a biphasic lung function reaction to specific allergen provocation defined as a decline of ≥20% in the early phase asthmatic response (EAR) and ≥15% in the late phase asthmatic response (LAR) as well as presence of eosinophils in sputum.

Compared to placebo, SB010 significantly improved lung function in both the early and late phase asthmatic response. SB010 attenuated the decline in mean LAR AUC by 34% (decline in median LAR AUC attenuated by 48%) compared to a 1% worsening in mean lung function in the placebo group (p=0.02). SB010 also attenuated the decline in mean EAR AUC by 11% (decline in median EAR AUC attenuated by 15%) compared to a 10% worsening in mean lung function in the placebo group (p=0.03).

SB010 was also safe and well tolerated. No serious treatment emergent adverse events occurred in both treatment groups. The total number of patients with treatment emergent adverse events was small (N=14), of which N=8 were in the placebo group and N=6 in the SB010 group. None of the events was likely SB010-related according to the investigators.

Professor Norbert Krug, principal investigator of the trial, commented: “For many years, GATA-3 has been a highly promising but previously elusive target for novel asthma therapies. This clinical trial demonstrates that treatment with a GATA-3-specific DNAzyme results in significantly improved lung function. Further clinical studies are clearly warranted.”

Jonas Renz, Managing Director, added: “We are extremely excited by the strong efficacy data and solid safety profile of SB010. SB010 is one of the very few drug candidates to have shown significant clinical effects in both EAR and LAR. This confirms the advantage of our highly differentiated approach to comprehensive and specific Th2 pathway downregulation and underscores the disruptive potential of SB010 in the asthma landscape.”

sterna biologicals intends to publish the full results in an academic journal and present at upcoming scientific conferences.

Professor Jens Hohlfeld, principal investigator of the Phase Ib study in asthmatic patients, will focus on safety data obtained in patients and Dr Holger Garn will give an overview of the entire Phase I programme.

About SB010
sterna biologicals’ drug candidate SB010 is an inhaled DNAzyme-based GATA-3 antagonist. GATA-3 is the master transcription factor in regulating Th2-driven inflammatory diseases such as asthma. It is generally accepted that GATA-3 is necessary and sufficient for the production of key cytokines interleukin (IL)-4, IL- 5, and IL-13, which cause inflammation. In pre-clinical development, SB010 significantly reduced expression of these cytokines and was safe and well-tolerated in toxicological studies with negligible side-effects. DNAzymes are single-stranded DNA molecules comprising a catalytic domain flanked by two binding domains. The binding domains attach to a specific sequence of targeted mRNA (antisense), in case of SB010 GATA-3 mRNA. After binding to the target, the catalytic domain then cleaves the mRNA, thereby inhibiting relevant cytokine expression.

About asthma
Asthma is a major chronic inflammatory disease of the airways affecting an estimated 300 million people worldwide. In OECD countries, prevalence is around 10% and increasing, with greater than average prevalence amongst women, children, and the elderly.