GRPR

SYDNEY, Oct. 3, 2023 /PRNewswire/ -- Clarity Pharmaceuticals (ASX: CU6) ("Clarity"), a clinical-stage radiopharmaceutical company with a mission to develop next-generation products that improve treatment outcomes for children and adults with cancer, is pleased to announce the dosing of the first patient in its theranostic 64Cu/67Cu SAR-Bombesin Phase I/II trial in metastatic castrate resistant prostate cancer (mCRPC). No issues were observed during the administration of 6GBq of 67Cu SAR-Bombesin and the participant continues to be followed for further safety and efficacy assessments as per protocol. COMBAT, which derives from "Copper-67 SAR-Bombesin in metastatic castrate resistant prostate cancer (NCT05633160)1 is a dose escalation and cohort expansion trial for up to 38 participants. 64Cu SAR-Bombesin is used to visualise gastrin-releasing peptide receptor (GRPr)-expressing lesions and select candidates for subsequent 67Cu SAR-Bombesin therapy. The aim for the trial is to determine the safety and efficacy of 67Cu SAR-Bombesin in participants with GRPr expressing mCRPC who are ineligible for therapy with 177Lu PSMA-617. These patients are unlikely to benefit from prostate-specific membrane antigen (PSMA)-targeted agents and represent a significant unmet need for both imaging and therapy. Doses of up to 14GBq of 67Cu SAR-Bombesin, in up to four cycles, are planned to be investigated in this trial (pending safety reviews). Clarity's Executive Chairperson, Dr Alan Taylor, commented, "SAR-Bombesin has already resulted in improvements to the management of prostate cancer for patients with PSMA-negative or low PSMA expressing lesions through diagnostic trials and we hope to confirm its safety and efficacy in this theranostic trial. We look forward to progressing the COMBAT trial and building on the compelling data from our preclinical and clinical studies to date. Combined with the logistical and manufacturing benefits of Targeted Copper Theranostics and with commercial quantities of the 67Cu radioisotope now being routinely produced domestically in the US, we see a clear path to bringing SAR-Bombesin and SAR-bisPSMA to the prostate cancer patient population in need of novel treatments." About SAR-Bombesin SAR-Bombesin is a highly targeted pan-cancer radiopharmaceutical with broad cancer application. It targets the gastrin-releasing peptide receptor (GRPr) present on cells of a range of cancers, including but not limited to prostate, breast and ovarian cancers. GRPr is found in up to 100% of prostate cancers, including prostate cancers that don't express PSMA (PSMA-negative)2-6. The product utilises Clarity's proprietary sarcophagine (SAR) technology that securely holds copper isotopes inside a cage-like structure, called a chelator. Unlike other commercially available chelators, the SAR technology prevents copper leakage into the body. SAR-Bombesin is a Targeted Copper Theranostic (TCT) that can be used with isotopes of copper-64 (Cu-64 or 64Cu) for imaging and copper-67 (Cu-67 or 67Cu) for therapy. 64Cu SAR-Bombesin and 67Cu SAR-Bombesin are unregistered products. Individual results may not represent the overall safety and efficacy of the products. The data outlined in this announcement has not been assessed by health authorities such as the US Food and Drug Administration (FDA). A clinical development program is currently underway to assess the efficacy and safety of these products. There is no guarantee that these products will become commercially available. About Prostate Cancer Prostate cancer is the second most common cancer diagnosed in men globally and the fifth leading cause of cancer death worldwide7. The American Cancer Institute estimates in 2023 there will be 288,300 new cases of prostate cancer in the US and around 34,700 deaths from the disease8. Approximately 25% of mCRPC patients have low or no uptake of a PSMA-targeting tracer.9 These patients are therefore unlikely to respond to therapeutic PSMA-targeted products and currently have few treatment options available to them. Given the prostate cancer indication is one of the largest in oncology, there is a significant unmet medical need in this segment. The SAR-Bombesin product could offer valuable imaging and therapeutic options for not only PSMA-negative patients, but also the large number of patients that have the target receptor on their cancers. About Clarity Pharmaceuticals Clarity is a clinical stage radiopharmaceutical company focused on the treatment of serious disease. The Company is a leader in innovative radiopharmaceuticals, developing targeted copper theranostics based on its SAR Technology Platform for the treatment of cancer in children and adults. References 1. ClinicalTrials.gov NCT05633160, 2. Markwalder R, Reubi JC. Gastrin-releasing peptide receptors in the human prostate: relation to neoplastic transformation. Cancer research. 1999;59(5):1152-1159. 3. Fleischmann A, Waser B, Reubi JC. High expression of gastrin-releasing peptide receptors in the vascular bed of urinary tract cancers: promising candidates for vascular targeting applications. Endocrine-related cancer. 2009;16(2):623-633. 4. Ananias HJ, van den Heuvel MC, Helfrich W, de Jong IJ. Expression of the gastrin-releasing peptide receptor, the prostate stem cell antigen and the prostate-specific membrane antigen in lymph node and bone metastases of prostate cancer. The Prostate. 2009;69(10):1101-1108. 5. Reubi JC, Wenger S, Schmuckli-Maurer J, Schaer JC, Gugger M. Bombesin receptor subtypes in human cancers: detection with the universal radioligand (125)I-[D-TYR(6), beta-ALA(11), PHE(13), NLE(14)] bombesin(6-14). Clin Cancer Res. 2002;8(4):1139-1146. 6. Sun B, Halmos G, Schally AV, Wang X, Martinez M. Presence of receptors for bombesin/gastrin-releasing peptide and mRNA for three receptor subtypes in human prostate cancers. The Prostate. 2000;42(4):295-303. 7. Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries <> 8. American Cancer Society, Cancer Statistics Center, 9. Vlachostergios PJ, Niaz MJ, Sun M, et al. Prostate-Specific Membrane Antigen Uptake and Survival in Metastatic Castration-Resistant Prostate Cancer. Frontiers in oncology. 2021;11. This announcement has been authorised for release by the Executive Chairperson. SOURCE Clarity Pharmaceuticals

New name reflects the company's pipeline of paired fluorine-18 PET diagnostics and radioligand therapies to find and treat cancer, led by a GRPR-targeting program for prostate cancer THE WOODLANDS, Texas--(BUSINESS WIRE)-- Fuzionaire Diagnostics, Inc. announced today that it has changed its name to Fuzionaire Theranostics, Inc. (“Fuzionaire Tx”). Originally directed to make diagnostic radiopharmaceuticals for PET scans, the company's HetSiFA® library has become a powerful theranostics platform that can also make radioligand therapies. HetSiFAs, or heteroaromatic silicon-fluoride acceptors, are modular radiolabeling moieties that enable rapid prototyping of peptide-based theranostics and the rapid manufacturing of fluorine-18 (18F) PET companions at large scale. HetSiFA-based radioligand therapies use leading alpha- and beta-emitting radionuclides. The HetSiFA® platform creates chemically identical diagnostic and therapeutic companions, a feature that enables a personalized therapeutic dose for each cancer patient. The name change marks a milestone in the company's growth plan and reflects a developing theranostic pipeline in oncology. Preclinical Oncology Pipeline Beginning With GRPR-Positive Prostate Cancer The company's first theranostic development program aims to improve the care of patients with metastatic prostate cancer by targeting the gastrin-releasing peptide receptor (GRPR) with a chemically identical and scalable 18F/ lutetium-177 (177Lu) theranostic pair. GRPR has emerged as a promising and validated target for prostate cancer to complement the widely utilized target prostate-specific membrane antigen (PSMA). In recent years, several PSMA-targeting radiopharmaceuticals have become available to patients worldwide. Novartis's PSMA-targeting radioligand therapy Pluvicto®, Lantheus's 18F PET imaging agent Pylarify®, Blue Earth Diagnostics' 18F PET imaging agent Posluma®, and ABX's PET imaging agent 18F-PSMA-1007 have been approved by regulatory agencies. Like Pylarify, Posluma, and 18F-PSMA-1007, Fuzionaire Tx's HetSiFA-based PET diagnostics use the nuclide 18F, which offers superior availability, production scalability, and image resolution as compared to gallium-68 (68Ga), often used in theranostics. Like Posluma, Fuzionaire Tx's HetSiFA-based radiopharmaceuticals are enabled by silicon. Posluma is the first drug approved by the FDA with a silicon-fluoride acceptor (SiFA) moiety. Fuzionaire Tx's patented HetSiFAs share the manufacturing advantages of SiFAs but with additional features, including an ability to create a more comprehensive array of theranostic candidates with different physicochemical and labeling properties. HetSiFAs are protected by a portfolio of issued and pending patents covering HetSiFAs and HetSiFA-containing candidates and the underlying silicon chemistry. In the context of the growth of PSMA radiopharmaceuticals and recent evidence that not all patients can benefit from them, GRPR has emerged as the most promising target to complement PSMA. The success of 18F/177Lu theranostics targeting PSMA underscores the need for an 18F/177Lu theranostic targeting GRPR. In this context, Fuzionaire Tx’s lead program targeting GRPR could occupy a key space in the portfolio of radiopharmaceuticals for prostate cancer. Additional Programs and Possibilities With origins in Robert Grubbs' lab at Caltech and the Crump Institute for Molecular Imaging at UCLA, the company's programs are advancing through a multi-party collaboration with McGill University, McMaster University, and Montreal-based contract research organization Paraza Pharma. The company is also advancing its programs in consultation with Prof. Mathias Schreckenberger, Director of the Nuclear Medicine Department at the University Medical Center Mainz in Germany, and the radiopharmaceutical contract development and manufacturing organization AtomVie Global Radiopharma Inc. The company's pipeline can expand further. The modularity of the HetSiFA platform enables the company to expand its pipeline rapidly with existing collaborators and new partners. In addition to the GRPR program, the company has discovery-stage programs for lung cancer and PSMA/GRPR-positive prostate cancer. Initial preclinical data from the GRPR program will be presented by Alexey Kostikov, PhD, Associate Professor at McGill University, at the American Chemical Society Fall Conference in August 2023. “We are motivated to continue to innovate in how we collaborate with new partners to expand the use of HetSiFAs and the ecosystem supporting these important new labeling moieties, and to advance our GRPR and other programs through clinical trials,” said Nick Slavin, CEO of Fuzionaire Tx. “By doing so, we can create new ways to treat cancer and make new theranostic medicines more accessible.” About Fuzionaire Theranostics Fuzionaire Theranostics is a radiopharmaceutical company on a mission to make theranostic treatments more accessible to people with cancer. With origins in Nobel laureate Robert Grubbs' lab at Caltech, the company's patented HetSiFA® platform offers manufacturing advantages in a clinical setting and enables a personalized therapeutic dose for each cancer patient. Current development plans address pressing clinical needs in prostate and lung cancer. For more, visit us at:

SYDNEY, July 24, 2023 /PRNewswire/ -- Clarity Pharmaceuticals (ASX: CU6) ("Clarity", "the Company"), a clinical stage radiopharmaceutical company with a mission to develop next-generation products that improve treatment outcomes for children and adults with cancer, is pleased to announce the Phase II US-based diagnostic 64Cu SAR-Bombesin trial (SABRE NCT05407311)1 for patients with prostate cancer has reached its fifty percent recruitment milestone, with 25 out of 50 participants enrolled and imaged. SABRE (Copper-64 SAR-Bombesin in Biochemical Recurrence of prostate cancer) is a Phase II Positron Emission Tomography (PET) imaging trial of participants with PSMA-negative biochemical recurrence (BCR) of prostate cancer following definitive therapy. It is a multi-centre, single arm, non-randomised, open-label trial of 64Cu-labelled SAR-Bombesin in 50 participants. The primary objectives of the trial are to investigate safety and tolerability of the product as well as its ability to correctly detect recurrence of prostate cancer. Andrei Iagaru, MD, the Lead Principal Investigator for the trial, commented, "We have been working on Bombesin for many years now and I am very excited with the progress of the SABRE trial and the continued exploration and validation of the clinical benefits associated with the SAR-Bombesin agent. It gives hope to clinicians and patients who have no other suitable diagnostic options available due to their cancers having low or no PSMA expression. Being able to visualise the disease can change the entire treatment paradigm for these patients. Once we can see the cancer, clinicians can then find the most suitable therapeutic regiment to maximise treatment outcomes. Based on the promising preclinical and clinical data to date, SAR-Bombesin is an exciting new product for better managing these patients that have few options at present in the face of a devastating diagnosis. We look forward to recruiting the remaining 25 patients in the trial and further analysing the trial data." Clarity's Executive Chairman, Dr Alan Taylor, commented, "We continue to build significant positive data on our SAR-Bombesin product. In addition to the SABRE trial, we are actively recruiting participants to our theranostic trial, COMBAT, and have recently finished recruitment into an investigator initiated Phase II diagnostic trial, BOP, with this product. Subject to the outcome of the SABRE trial, Clarity is planning to launch a pivotal Phase III diagnostic trial for first product approval in the US. "SAR-Bombesin has already resulted in improvements to the management of prostate cancer for patients that are PSMA-negative or have low PSMA expressing tumours and we hope to confirm its safety and efficacy in our clinical programs. We look forward to progressing the development of SAR-Bombesin and potentially providing a large patient population with accurate and precise detection and treatment of their prostate cancer." About SAR-Bombesin SAR-Bombesin is a highly targeted pan-cancer radiopharmaceutical with broad cancer application. It targets the gastrin-releasing peptide receptor (GRPr) present on cells of a range of cancers, including but not limited to prostate, breast and ovarian cancers. GRPr is found in approximately 75-100% of prostate cancers, including prostate cancers that don't express PSMA (PSMA-negative)2-6. The product utilises Clarity's proprietary sarcophagine (SAR) technology that securely holds copper isotopes inside a cage-like structure, called a chelator. Unlike other commercially available chelators, the SAR technology prevents copper leakage into the body. SAR-Bombesin is a Targeted Copper Theranostic (TCT) that can be used with isotopes of copper-64 (Cu-64 or 64Cu) for imaging and copper-67 (Cu-67 or 67Cu) for therapy. About Prostate Cancer Prostate cancer is the second most common cancer diagnosed in men globally and the fifth leading cause of cancer death worldwide7. The American Cancer Institute estimates in 2023 there will be 288,300 new cases of PC in the US and around 34,700 deaths from the disease8. Approximately 20% of prostate cancers with BCR are PSMA-PET negative9-12. These patients are therefore unlikely to respond to therapeutic PSMA-targeted products and currently have few treatment options available to them. Given the prostate cancer indication is one of the largest in oncology, there is a significant unmet medical need in this segment. The SAR-Bombesin product could offer valuable imaging and therapeutic options for not only PSMA-negative patients, but also the large number of patients that have the target receptor on their cancers. About Clarity Pharmaceuticals Clarity is a clinical stage radiopharmaceutical company focused on the treatment of serious disease. The Company is a leader in innovative radiopharmaceuticals, developing TCTs based on its SAR technology platform for the treatment of children and adults with cancer. References 1. ClinicalTrials.gov Identifier: NCT05407311, 2. Markwalder R, Reubi JC. Gastrin-releasing peptide receptors in the human prostate: relation to neoplastic transformation. Cancer research. 1999;59(5):1152-1159. 3. Fleischmann A, Waser B, Reubi JC. High expression of gastrin-releasing peptide receptors in the vascular bed of urinary tract cancers: promising candidates for vascular targeting applications. Endocrine-related cancer. 2009;16(2):623-633. 4. Ananias HJ, van den Heuvel MC, Helfrich W, de Jong IJ. Expression of the gastrin-releasing peptide receptor, the prostate stem cell antigen and the prostate-specific membrane antigen in lymph node and bone metastases of prostate cancer. The Prostate. 2009;69(10):1101-1108. 5. Reubi JC, Wenger S, Schmuckli-Maurer J, Schaer JC, Gugger M. Bombesin receptor subtypes in human cancers: detection with the universal radioligand (125)I-[D-TYR(6), beta-ALA(11), PHE(13), NLE(14)] bombesin(6-14). Clin Cancer Res. 2002;8(4):1139-1146. 6. Sun B, Halmos G, Schally AV, Wang X, Martinez M. Presence of receptors for bombesin/gastrin-releasing peptide and mRNA for three receptor subtypes in human prostate cancers. The Prostate. 2000;42(4):295-303. 7. Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries, 8. American Cancer Society: Key Statistics for Prostate Cancer, 9. Afshar-Oromieh A, Holland-Letz T, Giesel FL, et al. Diagnostic performance of 68Ga-PSMA-11 (HBED-CC) PET/CT in patients with recurrent prostate cancer: evaluation in 1007 patients. Eur J Nucl Med Mol Imaging. 2017 Aug;44(8):1258-1268. 10. Ferraro DA, Rüschoff JH, Muehlematter UJ, et al. Immunohistochemical PSMA expression patterns of primary prostate cancer tissue are associated with the detection rate of biochemical recurrence with 68Ga-PSMA-11-PET. Theranostics. 2020;10(14):6082-6094. 11. Baratto L, Song H, Duan H, et al. PSMA- and GRPR-Targeted PET: Results from 50 Patients with Biochemically Recurrent Prostate Cancer. J Nucl Med. 2021;62(11):1545-1549. 12. Mapelli P, Ghezzo S, Samanes Gajate AM, et al. 68Ga-PSMA and 68Ga-DOTA-RM2 PET/MRI in Recurrent Prostate Cancer: Diagnostic Performance and Association with Clinical and Histopathological Data. Cancers (Basel). 2022;14(2):334. For more information, please contact: This announcement has been authorised for release by the Executive Chairman. Company Codes: Australia:CU6