18 September 2018 - - German radiopharmaceutical group Isotopen Technologien München AG has signed a Research Evaluation and Option Agreement for a worldwide exclusive license with German pharmaceutical company Merck KGaA, Darmstadt, Germany, the company said.

Merck KGaA is in the development and manufacturing of active pharmaceutical ingredients with particular expertise related to reduced folates.

This partnership with Merck KGaA will allow for a broader application of ITM´s Theranostics platform to include diagnosis and therapy of patients with folate receptor-positive cancers.

The partnership covers the evaluation of Merck KGaA first-in-class folate derivatives as radiolabeled diagnostic and therapeutic agents for the treatment of serious oncological folate receptor-positive diseases.

Under the agreement ITM receives an option for a worldwide exclusive license for clinical development and commercialisation of radiolabeled folate derivatives, while Merck KGaA will supply folate precursors for radiolabeling.

Folate receptors are known to be overexpressed by several cancer types, such as ovarian, lung, breast and other types of cancers.

The restricted expression of folate receptors to only a few sites in normal tissues makes them an attractive diagnostic and therapeutic target.

Folate is a B vitamin that is critical to DNA synthesis as well as other essential cell processes. Folate derivatives retain their receptor binding properties when conjugated to pharmaceuticals.

They have been proven to be promising compounds for cancer treatment for quite some time and therefore represent an outstanding addition to ITM´s Targeted Radionuclide Therapy pipeline.

In folate receptor targeting, the folate moiety of the folate-based radiopharmaceutical acts as targeting molecule for both diagnosis and therapy. The radiopharmaceutical is injected into the patient´s body, where it binds to the corresponding receptors on the tumor tissue.

The radio-conjugate is then absorbed by the tumor cells. For diagnostic application, medical radioisotopes with short half-lives, like Gallium-68, are combined with the targeting molecule.

With highly sensitive molecular imaging technologies like PET (Positron Emission Tomography), whole-body diagnostic images are created.

For targeted treatment, folate derivatives are complexed with medical radioisotopes with longer half-lives, like ITM´s highly pure no-carrier-added Lutetium-177.

The availability of folate receptor-targeted radiopharmaceuticals for both diagnosis and therapy opens up the way for radiotheranostic applications in various indications.