Conjugated bisphosphonates for the diagnosis and therapy of bone diseases

Bone metastases are very common in advanced solid tumors of various origin in many malignancies: breast, lung, prostate and many others. Bone metastases are incurable, causing severe pain, pathological fractures, nerve compression and hypercalcemia. Impair quality of life. The patent is on ⁶⁸Ga- and ¹⁷⁷Lu-labelled bisphosphonates, mainly ZOLEDRONATE. Aim: Diagnose bone metastases and achieve palliative or curative treatment. Most potent theranostic compound. Patient studies very successful.

Inventors: F. Rösch, M. Meckel
Applicant: SCV
Priority Day: 17.10.2014
Registration: DE 10 2014 115 154.2
IP for countries: DE + PCT
Owner: SCV
Exclusive license: SCV to ITM MUNICH. Plans for clinical trial.

Method and device for isolating a chemically and radiochemically cleaned ⁶⁸Ga-radionuclide and for marking a marking precursor with the ⁶⁸Ga-radionuclide

Use of a ⁶⁸Ga/⁶⁸Ga radionuclide generator in medical application. The invention adds a cation exchanger cartridge online to the eluent. Achieves purification of ⁶⁸Ga, mainly from ⁶⁸Ge parent activity, but also stable zinc. Platform for many important ⁶⁸Ga-PET tracers in routine production Worlwide. SCV distributed generator and post-processing module. 2009, SCV gave an exclusive license to EZAG, Germany. EZAG implemented the technology into their automated modules and generators.

Inventors: F. Rösch/ D. Filosofov / KP Zhernosekov  / M. Jennewein 
Applicant: University of Mainz
Priority Day: 21.04.2005
Registration: DE102004057225.9
IP for countries: DE, AT, BE, CH, DK, EP, ES, FR, GB, IT, NL, SE, US
Owner: SCV
Exclusive license: SCV to EZAG

Compound made of a metal ion and a labeling precursor with one or more targeting vectors and use of this compound

Usually radiopharmaceuticals utilize only one targeting vector for a given disease.
Some cancer cells offer more than one molecular target. The invention: combine two different targeting vectors in one and the same molecule, e.g. a PSMA inhibitor and a bisphosphonate, simultaneously accumulating on bone metastases of prostate cancer and substantially increase the radiation dose delivered by e.g. a ¹⁷⁷Lu-labelled theranostic.
Aim: Better treatment of patients of late stage PCa.

Inventors: F. Rösch, P. Riss, C. Burchhardt 
Applicant: University of Mainz
Priority Day: 04.09.2008
Registration: DE102008045937.2
IP for countries: DE, AT, CH, LI, FR, GB
Owner: SCV

Smart-drug-delivery-system
and pharmaceutic kit for dual nuclear medicine-cytotoxic theranostic

Cytostatic drugs accumulate in all cells, not only in tumor cells. Chemotherapy causes severe side-effects; ineffective in more than 50% of patients. The invention: selective delivery of a cytostatic drug to an individual tumor using a tumor-specific transporter molecule. Small molecular drug delivery will selectively enhance the concentration of the cytostatic drug in the tumor and minimize whole body uptake.

Option: Use ⁶⁸Ga to monitor in vivo the pharmacology of the delivery system via PET/CT for patient-individual selection of subsequent treatment.

Inventors: F. Rösch, T. Grus, H. Lahnif 
Applicant: University of Mainz
Priority Day: 20.12.2019
Registration: DE 10 2019 135 564.8
IP for countries: DE

Labelling precursors with sqquaric acid

Most epithelial tumors (lung, breast, colon, etc.) have tumor microenvironment for supply chains. 

Tumor stroma composed of CAF: Cancer Associated Fibroblasts FAP (Fibroblast Activation Protein) are the main consituent.
Small molecule inhibititors turned into radio-theranostics for PET/CT diagnosis and therapy with ⁹⁰Y-, ¹⁷⁷Lu-, ²²⁵Ac- FAPi analogs. Expected to be the next block buster in nuclear medicine. 

Inventors: F. Rösch, L. Greidenstein, Grus, R. Bergmann
Applicant: University of Mainz
Priority Day: 24.10.2018
Registration: DE 10 2018 126 558.1
Owner: University of Mainz
IP for countries: DE, PCT