Fusion Pharmaceuticals Announces FDA IND Approval for FPI-2059, an Investigational Small Molecule Radiopharmaceutical Targeting NTSR1 Expressing Solid Tumors

HAMILTON, ON and BOSTON, June 23, 2022 /CNW/ – Fusion Pharmaceuticals Inc. (Nasdaq: FUSN), a clinical-stage oncology company focused on developing next-generation radiopharmaceuticals as precision medicines, today announced that the Food and Drug Administration (FDA) of the United States has authorized the New Drug Applications (IND) for [225Ac]-FPI-2059 (FPI-2059) and the corresponding imaging analog [111In]-FPI-2058 (FPI-2058). FPI-2059 is a targeted alpha therapy (TAT) designed to use a small molecule to target and deliver actinium-225 to tumor sites expressing neurotensin receptor 1 (NTSR1), a protein that is overexpressed in several types of tumors solids, including colorectal, pancreatic, gastric, differentiated neuroendocrine prostate, squamous cell carcinoma of the head and neck, and Ewing’s sarcoma.

“The FPI-2059 program showcases Fusion’s ability to use our platform technology and R&D expertise to efficiently convert different classes of targeting molecules into TATs against novel targets designed to treat cancers with high unmet need. “, said John ValiantPh.D. “With FPI-2059, we believe there is a significant opportunity to treat several types of solid tumors, including neuroendocrine differentiated prostate cancer where PSMA expression is typically low and, therefore, patients are not adequately treated with existing radioligands. We look forward to advancing FPI-2059, Fusion’s first small molecule-based TAT and third clinical program, into a Phase 1 study.”

Merger acquired [177Lu]- IPN-1087 (IPN-1087), a lutetium-based beta-emitting radiopharmaceutical, from Ipsen in April 2021and converts the compound to an alpha emitter [225Ac]-FPI-2059. In clinical studies, IPN-1087 has shown promising early safety data and good absorption in several tumor types. In a direct in vivo comparison of therapeutic efficacy in a murine xenograft model of colorectal cancer between FPI-2059 and IPN-1087, results show that tumor regression with FPI-2059 is achieved at doses approximately 1500 times lower than IPN-1087.

Fusion plans to initiate a Phase 1, non-randomized, open-label clinical trial in patients with NTSR1-expressing solid tumors to study safety, tolerability and pharmacokinetics and to establish the recommended Phase 2 dose. will prioritize six solid tumor indications, including squamous cell carcinoma of the head and neck, pancreas, neuroendocrine prostate, colorectal, gastric and Ewing’s sarcoma. The study uses a 3+3 dose escalation design to evaluate multiple escalating doses of FPI-2059. As part of the screening process, patients will receive an imaging analog of FPI-2059, FPI-2058, and only those who meet predefined criteria for tumor uptake and safety will receive FPI-2059.

Radiopharmaceuticals are precision medicine in that therapeutic alpha can be converted into a corresponding imaging analog with a different radionuclide (in this case, indium), used to screen for a biomarker in patients with tumors that express the cancer target, increasing the likelihood of response to therapy. Fusion plans to provide additional guidance on FPI-2059 program timelines following initial patient screening experience to better predict patient enrollment cadence.

About REIT-2059

[225Ac]-FPI-2059 (FPI-2059) is a targeted alpha therapy combining actinium-225 with a small molecule designed to target neurotensin receptor 1 (NTSR1), in development as a potential treatment for various solid tumors. NTSR1 is a promising target for cancer therapy that is overexpressed in multiple solid tumors, including colorectal, pancreatic, gastric, differentiated neuroendocrine prostate, head and neck cancers, and Ewing’s sarcoma. FPI-2059 is currently being evaluated in a phase 1 study.

About Fusion

Fusion Pharmaceuticals is a clinical-stage oncology company focused on the development of next-generation radiopharmaceuticals as precision medicines. Utilizing proprietary Fast-Clear™ bonding technology and leveraging the company’s expertise in actinium sourcing and manufacturing, Fusion connects alpha particle-emitting isotopes to various targeting molecules to seamlessly deliver selectively alpha-emitting payloads to tumors. Fusion’s lead program, FPI-1434 targeting insulin-like growth factor-1 receptor, is currently in a Phase 1 clinical trial. The pipeline includes FPI-1966 targeting insulin-like growth factor-3 receptor growth inhibitors (FGFR3) and FPI-2059, a small molecule acquired from Ipsen, targeting the neurotensin receptor 1 (NTSR1). In addition to a robust proprietary pipeline, Fusion is collaborating with AstraZeneca to co-develop up to three novel targeted alpha therapies (TATs), the first of which is currently in IND studies, and is exploring up to five combination programs between Fusion TATs and DNA Damage Repair Inhibitors (DDRis) and immuno-oncology agents from AstraZeneca. Fusion also recently entered into a collaboration with Merck to evaluate FPI-1434 in combination with Merck’s KEYTRUDA® (pembrolizumab) in patients with IGF-1R-expressing solid tumors.

Forward-looking statements

This press release contains “forward-looking statements” for purposes of the safe harbor provisions of the Private Securities Litigation Reform Act of 1995, including, but not limited to, statements regarding the future business of Fusion Pharmaceuticals Inc. (the “Company”) and financial performance. For this purpose, all statements contained herein that are not statements of historical fact may be deemed to be forward-looking statements. Without limiting the foregoing, the words “expect”, “plan”, “anticipate”, “intend”, “will” and similar expressions are also intended to identify forward-looking statements, as are statements expressed or implied regarding the Company’s potential drug candidates, including any express or implied statements regarding the successful development of product candidate FPI-2059. Actual results may differ materially from those indicated by these forward-looking statements due to risks and uncertainties, including, but not limited to, the following: there can be no assurance that the Company will advance any product clinical candidate or other component of its potential pipeline to the clinical, regulatory process or commercialization; management’s expectations could be affected by unforeseen delays in patient recruitment or regulatory actions or delays; uncertainties related to clinical trials or unsuccessful results thereof, including additional data relating to ongoing clinical trials evaluating its product candidates; the Company’s ability to obtain additional financing required to conduct its research, development and commercialization activities; changes to the Company’s business plan or objectives; the Company’s ability to attract and retain qualified personnel; competition in general; and the Company’s ability to obtain, maintain and enforce patent and other intellectual property protections for its product candidates and discoveries. These forward-looking statements involve known and unknown risks, uncertainties and other factors that may cause actual results to differ materially from any future results, performance or achievements expressed or implied by such statements. These and other risks that may impact management’s expectations are further described under the heading “Risk Factors” in the Company’s Quarterly Report on Form 10-Q for the three months ended March 31. 2022, as filed with the SEC and in any subsequent periodic or subsequent filings. current report that the Company files with the SEC. All forward-looking statements reflect the Company’s estimates only as of the date of this release (unless another date is indicated) and should not be taken to reflect the opinions, expectations or beliefs of the Company as of any date subsequent to the date of this press release. Although Fusion may elect to update these forward-looking statements at some time in the future, it expressly disclaims any obligation to do so, even if the Company’s estimates change.

Investors and others should note that Fusion communicates with its investors and the public using Fusion’s website, www.fusionpharma.com, including, but not limited to, corporate disclosures, investor presentations, SEC filings, and press releases. The information that Fusion publishes on this website could be considered material information. Accordingly, Fusion encourages investors, the media and other interested persons to regularly review the information Fusion posts there.

Amanda Cray
Senior Director of Investor Relations and Corporate Communications
[email protected]

SOURCE Fusion Pharmaceuticals Inc.

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