Monopar Therapeutics Inc. announced promising preclinical imaging and therapeutic efficacy data for its MNPR-101 radiopharmaceutical program. This novel first-in-class radiopharma program targets cancers expressing the urokinase plasminogen activator receptor (uPAR), which include a majority of all triple-negative breast, colorectal, and pancreatic cancers. MNPR-101 Conjugated to Imaging Radioisotope: Maximizing the dose delivered to the tumor relative to normal tissue is of paramount importance in radiopharmaceutical therapy.

Monopar?s in-house radiopharmaceutical development team was able to significantly increase tumor uptake of MNPR-101-Zr while minimizing uptake in healthy tissue, as shown in this preclinical positron emission tomography (PET) sequential imaging time-series. The high specificity and durable tumor uptake are evident in the After Optimization panel below. MNPR-101 Conjugated to Therapeutic Radioisotopes: Preclinical data to date demonstrate compelling and durable anti-tumor benefits with MNPR-101 conjugated to therapeutic radioisotopes.

Figure 2 below shows preclinical efficacy data in a triple negative breast cancer as well as a pancreatic cancer human tumor xenograft mouse model utilizing two different therapeutic radioisotopes conjugated to MNPR-101; one of these radioisotopes has already been disclosed as being actinium-225 (Ac-225). The results in both show near complete elimination of the tumor after a single injection of the radiopharmaceutical agent. These studies demonstrate the potential of a MNPR-101 based radiopharmaceutical to provide a very meaningful clinical benefit to patients.