Probiodrug to
present at 255th ACS National Meeting & Exposition
The Inhibition of Glutaminyl Cyclase as a New Concept for
the Treatment of Alzheimer's Disease: PQ912, the First-In-Class
QC-Inhibitor in Clinical Development for AD
HALLE (SAALE),
Germany, 16 March 2018 - Probiodrug AG (Euronext Amsterdam:
PBD), a biopharmaceutical company developing novel therapeutic
solutions to treat Alzheimer's disease (AD), announced today that
an oral presentation will be held at the 255th
National Meeting & Exposition of the American Chemical Society
(ACS). The conference will take place in New Orleans, USA from 18
to 22 March 2018.
Dr Ulrich Heiser,
Director Medicinal Chemistry/CMC will give a presentation
entitled "Inhibition of glutaminyl cyclase as a
new concept for the treatment of Alzheimer's disease: PQ912, the
first-in-class QC-inhibitor in clinical development for AD" on
Sunday, 18 March 2018, at 2:45 pm CST in La Nouvelle Orleans
Ballrooms A/B - Ernest N. Morial Convention Center. The
presentation will be part of the Division of Medicinal
Chemistry.
N-terminally pyroglutamylated
forms of the Abeta peptide (pEAbeta) have been identified to seed
and sustain the formation of highly neuro-/synaptotoxic oligomers.
Therefore, they are assumed to be an early key pathological culprit
in AD pathology. With the identification of the zinc-dependent
enzyme Glutaminyl Cyclase (QC) as the responsible enzyme of pEAbeta
formation, the application of QC inhibitors emerged as a new
disease modifying treatment concept for AD.
The course towards the
identification of the QC-inhibitor PQ912 will be presented.
Starting out from one of the first potent representatives PBD150,
an attractive candidate molecule for development was obtained. With
molecular features rendering the starting PBD150 unsuitable, the
comprehensive SAR study into main areas of the molecule, namely the
metal-binding group and the central scaffold, led to the
identification of a new class of inhibitors. Thereby challenges due
to the specific requirements when addressing the zinc-dependent
target QC in the CNS were mastered: besides the enablement of a
sufficient blood brain barrier passage, the important selectivity
against metal-dependent off-targets as well as a sufficient and
pH-independent inhibitory potency had to be maintained. The talk
will also include core results from pre-clinical and clinical
development.
Dr Inge Lues,
Chief Development Officer of Probiodrug, commented:
"Our first in class small molecule QC-I PQ912, selected for
development due to a good drug-like profile and a comprehensive
preclinical proof of concept data package, shows an excellent dose-
dependent brain penetration and target engagement in man and an
attractive therapeutic window. The first 3-month trial in early AD
patients provided a set of positive pharmacodynamic and efficacy
results which all support the underlying concept of QC-Inhibition
reducing the seeding of highly synaptotoxic oligomers and providing
guidance for the outline of the next Phase 2b study, which is in
the planning process."
###
For more information, please
contact:
Probiodrug
Dr Konrad Glund, CEO
Email: contact@probiodrug.de
Optimum Strategic
Communications
Mary Clark, Supriya Mathur, Hollie Vile
Tel: +44 (0) 203 714 1787
Email: probiodrug@optimumcomms.com
The Trout Group
Tricia Truehart, Kelly Mueller
Tel: +1 (646) 378-2953
Email: ttruehart@troutgroup.com
MC Services AG
Anne Hennecke, Caroline Bergmann
Tel: +49 (0) 211 529 252 20
Email: probiodrug@mc-services.eu
Notes to Editors:
About Probiodrug AG
Headquartered in Halle (Saale), Germany, Probiodrug AG (Euronext
Amsterdam: PBD) is a biopharmaceutical company focused on the
development of new therapeutic products for the treatment of
Alzheimer's disease (AD). Probiodrug has identified a new
therapeutic concept linked to disease initiation and progression.
The development approaches are targeting a key neuro-/synaptotoxic
component of the pathology, pyroglutamate-Abeta (pGlu-Abeta) as a
therapeutic strategy. Its lead product, PQ912, has successfully
completed a Phase 2a (SAPHIR) study. The company's pipeline also
includes PBD-C06, an anti-pGlu-Abeta-specific monoclonal antibody,
in preclinical development. Probiodrug has medical use and
composition of matter patents related to the inhibition of QC and
anti-pGlu-Abeta-specific monoclonal antibodies, and has, in the
Company's view, a leading position in this field of research.
Founded in 1997 by Hans-Ulrich
Demuth and Konrad Glund, the company successfully developed a novel
therapeutic concept for diabetes - the DP4 inhibitors - which
provided the basis for a novel class of antidiabetics - the
gliptins. Today, Probiodrug aims to become a leading company in the
development of AD treatments and to thereby provide a better life
for Alzheimer's disease patients.
About
PQ912
Probiodrug's lead product candidate, PQ912, is a highly specific
and potent inhibitor of Glutaminyl Cyclase (QC), the enzyme
catalyzing the formation of synaptotoxic pGlu-Abeta. PQ912 has
shown therapeutic effects in AD animal models. A Phase-1 study in
healthy young and elderly volunteers revealed a dose dependent
exposure and showed good safety and tolerability up to the
highest dose with >90% target occupancy in the spinal
fluid. In June 2017, Probiodrug announced top-line data of the
Phase-2a SAPHIR trial of PQ912 and presented the study results at
CTAD 2017. The positive effects seen on secondary exploratory
efficacy markers strongly support (a) the hypothesis of pGlu-Abeta
being synaptotoxic and (b) the therapeutic concept pursued by
Probiodrug. The study revealed a positive benefit risk ratio of
PQ912 and provides important guidance how to move forward in the
development of PQ912 as a disease-modifying drug for AD.
Altogether, the results make the program highly attractive for
further development; the company has initiated the preparation of a
Phase 2b core program.
www.probiodrug.de
About Alzheimer's
disease
Alzheimer's disease is a neurological disorder, which is the most
common form of dementia, and ultimately leads to death. Today, 47
million people live with dementia worldwide, and this number is
projected to treble to more than 131 million by 2050, as the global
population ages. Dementia also has a huge economic impact.
Alzheimer's has an estimated, global societal cost of US$ 818
billion, and it will become a trillion dollar disease by 2018.
(World Alzheimer Report 2016).
Forward Looking Statements
Information set forth in this press release
contains forward-looking statements, which involve a number of
risks and uncertainties. The forward-looking statements contained
herein represent the judgment of Probiodrug AG as of the date of
this press release. Such forward-looking statements are neither
promises nor guarantees, but are subject to a variety of risks and
uncertainties, many of which are beyond our control, and which
could cause actual results to differ materially from those
contemplated in these forward-looking statements. We expressly
disclaim any obligation or undertaking to release publicly any
updates or revisions to any such statements to reflect any change
in our expectations or any change in events, conditions or
circumstances on which any such statement is based.