Probiodrug Provides Update on Clinical Development of P912, its Most Advanced QC-inhibitor for Alzheimer's Disease

HALLE/SAALE, Germany -- 

Probiodrug AG (Probiodrug) today provided an update on PQ912, an inhibitor of glutaminyl cyclase (QC) in clinical development for the treatment of individuals with Alzheimer's disease (AD). QC has been identified as the enzyme responsible for the formation of pyroglutamated (pGlu) toxic Abeta peptides. Numerous studies have elucidated the crucial role of pGlu Abeta peptides in the pathogenesis of AD. Moreover, pGluAbeta species are prominent constituents of plaques associated with AD.

PQ912 is currently being tested in an extended Phase 1 clinical trial, results of which have been reported at the recent Alzheimer's Association International Conference in July 2013 and the International Conference on Alzheimer's & Parkinson's Diseases, which took place in March 2013. In these studies, a total of 140 healthy young and elderly volunteers were administered ascending single doses (from 10 to 1800 mg) and multiple twice-daily (BID) doses (from 20 to 500 mg) of PQ912. PQ912 was safe and well tolerated throughout the dose range tested. For healthy non-elderly and elderly volunteers tested, the maximum tolerated dose was not reached during this study.

PQ912 exposure increased dose proportionally in these individuals. There were no serious adverse events, no apparent dose related AEs, and no clinically relevant laboratory and ECG findings. The exposure of PQ912 in plasma was increased approximately 2-fold in the elderly study participants compared with the non-elderly at the doses tested, suggesting that PQ912 is not metabolized by the liver in the elderly to the same rate that it is in younger individuals. The half-lives in plasma and cerebrospinal fluid (CSF) were essentially the same in the non-elderly and elderly groups. The plasma and CSF drug concentrations were highly correlated. Average QC-inhibition of 70% in CSF was achieved at 400 mg BID in non-elderly and is estimated to be reached at 300 mg BID in elderly.

"PQ912 is the first QC inhibitor ever studied in humans. The total data set generated to date is very promising, leading us to be optimistic about its potential to provide clinical benefit to people with AD," said Dr. Inge Lues, chief development officer of Probiodrug.

Probiodrug expects to advance PQ912 into a Phase 2 clinical study in 2014.

About Probiodrug AG

Probiodrug is a biopharmaceutical company dedicated to the discovery and development of novel therapeutic solutions to treat people with Alzheimer's disease. The Company has medical use and composition of matter patents related to the inhibition of glutaminyl cyclase, providing the Company with a dominant position in this field of research. Probiodrug is backed by institutions such as BB Biotech, Edmond de Rothschild Investment Partners, Goodvent/IBG, HBM, TVM Capital, Life Sciences Partners, Biogen Idec New Ventures, CFH Group, funds managed by Wellington Management and private investors.

Probiodrug's core capabilities are based on its long-standing expertise in the elucidation of the structure and function of enzymes which play a central role in the maturation of hormones. Probiodrug was founded in 1997 by Prof. Dr. Hans-Ulrich Demuth and Dr. Konrad Glund. For more information, please visit