Theranostics with OPS201 and OPS202

design: spreepunkt.de. 3D illustration: Guido Alfs.
Theranostics with OPS201 and OPS202
The OctreoPharm Sciences GmbH (OPS) is a privately
held clinical development biopharmaceutical company
focusing on radiopharmaceuticals for the diagnosis
and therapeutic control of tumors. The company,
founded in 2010, is located at the Biomedical Research
Campus in Berlin-Buch (Germany) and in Würzburg
(Germany).
OctreoPharm Sciences GmbH
Campus Berlin-Buch
Robert-Roessle-Strasse 10
13125 Berlin | GERMANY
Phone +49 (0)30 94893360
Fax +49 (0)30 94893364
Email info@octreopharm.com
www.octreopharmsciences.com
The first Antagonistic Somatostatin Analogs
in Clinical Development
Theranostic
Compounds
Ga-OPS202
68
Antagonistic Peptid
JR11=OPS200
Y-OPS201
90
Therapeutic
177
OPS202 is a new
Chelator DOTA
r2
sst
Radiolabeled somatostatin receptor antagonists were shown to
be preferable to agonists for in vivo peptide receptor targeting of
tumors. OctreoPharm Sciences introduced a theranostic couple
of new antagonistic peptides for the diagnosis and treatment of
neuroendocrine tumors into clinical development.
Chelator NODAGA
sstr2
Antagonistic Somatostatin Analogs
ss
tr2
Diagnostic
The theranostic compounds are based
on the antagonistic peptide JR11 which
is binding with high affinity to somatos­
tatin receptor subtype 2, predominantly
expressed on neuroendocrine tumors.
The diagnostic compound OPS202 is
coupled to the chelator NODAGA and
can be labeled with the radionuclide
68
Gallium. The therapeutic peptide
OPS201 is linked to the chelating agent
DOTA and can be labeled with isotopes
like 90Yttrium or 177Lutetium.
Innovative compounds in clinical development
for neuroendocrine tumor management
Lu-OPS201
Galliumlabeled somatostatin receptor antagonist in clinical development for positron
emission tomography (PET, PET/CT).
Preclinical data on OSP202 indicate
the potential to detect even smallest
lesions of NETs [Fani, Braun et al. J Nucl Med,
GTP
DP
2012].
GTP
DP
G
G
GDP
GDP
GTP
GTP
GT
P
P
GT
GT
P
Activated state
Resting state
68
OctreoPharm Sciencesʹs continuing
development of a labeling technology
using a specific chelator and buffer
system allows labeling at room temperature in just a couple of minutes. A
phase I/II clinical trial is currently being
conducted.
P
GT
OPS201 is aimed for tumor
cell-selective internal peptide receptor
radionuclide therapy (PRRT) with 90Y
or 177Lu on neuroendocrine tumors. In
a pilot study under compassionate use
the PRRT treatment with 177Lu-OPS201
showed very good clinical results
[Wild, Fani et al. J Nucl Med, 2014].
Superior binding behavior of Antagonistic Somatostatin Analogs
The new class of antagonistic peptides is independent of the
somatostatin receptor activation state (G-protein phosphorylation).
Therefore, they utilize many more binding sites on the tumor cell
surface, while agonistic peptides only target activated receptors
[Ginj, Zhang et al. PNAS, 2006].
A
B
Examplary PET/CT scans with 68Ga-OPS202 from
ongoing clinical trials
A: 68Ga-OPS202 PET/CT scan of a 45-year-old,
female patient suffering from a neuroendocrine
carcinoma with multiple liver metastases
[phase I/II trial, EudraCT No 2014-001881-88; Courtesy of
Prof. Damian Wild, University Hospital Basel].
B: 68Ga-OPS202 PET/CT scan of a 53-year-old,
male patient suffering from a well-differentiated,
functional neuroendocrine neoplasm (VIPoma) of
the pancreas body with multiple liver metastases
[investigator-initiated study; Courtesy of Prof. Richard Baum,
Zentralklinik Bad Berka].