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Theranostics with OPS201 and OPS202

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14/10/22 Higher Tumour Uptake and Residence Time …

14/10/19 [⁶⁸Ga]-OPS202 targeting somatostatin receptors …

Theranostics with OPS201 and OPS202

Innovative compounds in clinical development for neuroendocrine tumor management:
Antagonistic Somatostatin Analogs

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.

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].

Theranostic Compounds

The theranostic compounds are based on the antagonistic peptide JR11 which is binding with high affinity to somatos­tatin 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 ⁶⁸Gallium. The therapeutic peptide OPS201 is linked to the chelating agent DOTA and can be labeled with isotopes like ⁹⁰Yttrium or ¹⁷⁷Lutetium.

OPS202

OPS202 is a new ⁶⁸Gallium-labeled 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, 2012].
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.

OPS201

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].

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Neuroendocrine tumors (NETs)

The term neuroendocrine tumors represents a heterogeneous group of neoplasms that arise from endocrine cells of the glands or from endocrine islets in the thyroid, pancreas or the respiratory and gastrointestinal tract. The majority of NETs overexpress somatostatin (sst) receptors. Thus, they can be effectively imaged and treated with radioactive labeled somatostatin analogs with high sensitivity and high selectivity.

OctreoPharm Sciences GmbH

Theranostics: Accelerating the Promises.

The creativity of oncologists, radiochemists and nuclear medicine physicians gave the impulses.

We just make it happen.

A company of IPSEN

The OctreoPharm Sciences GmbH is a company of IPSEN PHARMA SAS, a French pharmaceutical concern.

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