FPI-2265 / AstraZeneca - LARVOL DELTA

AlphaBreak: FPI-2265 (225Ac-PSMA-I&T) for Patients With PSMA-Positive Metastatic Castration-Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov) - P2/3 | N=100 | Recruiting | Sponsor: Fusion Pharmaceuticals Inc. | N=60 ➔ 100

Enrollment change • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

FPI-2265 (225Ac-PSMA-I&T) and Olaparib for Patients With Metastatic Castration-Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov) - P2 | N=85 | Recruiting | Sponsor: Fusion Pharmaceuticals Inc.

New P2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Targeted Alpha Therapy with 225Actinium-Prostate Specific Membrane Antigen (PSMA)-I&T of Castration-resISTant Prostate Cancer (TATCIST). (clinicaltrials.gov) - P2 | N=115 | Active, not recruiting | Sponsor: Fusion Pharmaceuticals Inc. | Recruiting ➔ Active, not recruiting | Trial completion date: Dec 2025 ➔ Jul 2025 | Trial primary completion date: Dec 2024 ➔ Apr 2025

Enrollment closed • Trial completion date • Trial primary completion date • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor • BRCA • MSI

FPI-2265: Data from P2/3 AlphaBreak trial (NCT06402331) for mCRPC H2 2025 (AstraZeneca) - Q4 & FY2024 Results

P2/3 data • Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer

FPI-2265: Data from P2/3 AlphaBreak trial (NCT06402331) for mCRPC post 2025 (AstraZeneca) - Q2 2024 Results

P2/3 data • Metastatic Castration-Resistant Prostate Cancer • Oncology

Fusion Pharmaceuticals Announces Clinical Program and Manufacturing Updates (PRNewswire) - "The Company announced today that it has aligned with the FDA on its submitted Phase 2/3 protocol for FPI-2265, a targeted alpha therapy (TAT) targeting prostate specific membrane antigen (PSMA) for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC) with progressive disease. The updated development plan includes a Phase 2 dose optimization lead-in, expected to complete enrollment by the end of 2024, and a Phase 3 registrational trial expected to begin in 2025...The Phase 2 portion of the protocol is designed to evaluate the safety and efficacy of FPI-2265 across three dosing regimens in approximately 60 patients with mCRPC...The Phase 2 trial is expected to initiate in the second quarter of 2024 with enrollment completed by year-end. The Company will seek to hold an End of Phase 2 meeting with the FDA to determine the recommended Phase 3 dosing regimen based on analysis of the Phase 2 data..."

Clinical protocol • New P2/3 trial • New trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Combinatorial effect of the PSMA targeted alpha therapeutic, [225Ac]-FPI-2265, and olaparib in a pre-clinical prostate cancer tumor model (SNMMI 2024) - "[177Lu]-FPI-2263 exhibited elevated uptake in PSMA-expressing xenografts while demonstrating minimal uptake in PSMA-negative normal tissues. Additionally, [225Ac]-FPI-2265 safely demonstrated therapeutic effectiveness as a monotherapy, with enhanced efficacy observed in combination with olaparib. These results suggest that the combination of [225Ac]-FPI-2265 and olaparib may offer increased therapeutic benefits in patients with prostate cancer and provide support for future clinical investigation."

Preclinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Acquisition of Fusion Pharmaceuticals Completed (PRNewswire) - "Fusion Pharmaceuticals...announced the successful completion of the acquisition of all of the issued and outstanding shares of Fusion by a wholly-owned subsidiary of AstraZeneca AB by way of a statutory plan of arrangement under section 192 of the Canada Business Corporations Act, referred to as the Arrangement....The Arrangement complements AstraZeneca's leading oncology portfolio with the addition of the Fusion pipeline of RCs, including their most advanced program, FPI-2265, a potential new treatment for patients with metastatic castration-resistant prostate cancer (mCRPC), and brings new expertise and pioneering R&D, manufacturing and supply chain capabilities in actinium-based RCs to AstraZeneca....As a result of the Arrangement, Fusion has become a wholly owned subsidiary of AstraZeneca, with operations continuing in Canada and the US."

M&A • Metastatic Castration-Resistant Prostate Cancer

Fusion Pharmaceuticals Shareholders Approve Acquisition by AstraZeneca (PRNewswire) - "Fusion Pharmaceuticals...announced that at a special meeting of its shareholders (the 'Shareholders'), held virtually earlier today, the Shareholders voted in favour of the resolution to approve the previously announced plan of arrangement with a wholly-owned subsidiary of AstraZeneca under the Canada Business Corporations Act pursuant to which AstraZeneca will acquire all of the issued and outstanding shares of Fusion (the 'Arrangement')....The arrangement is subject to court approval, as well as other customary closing conditions. Subject to the satisfaction of such conditions, the transaction is expected to be completed in the second quarter of 2024....Fusion's clinical-stage development portfolio includes lead program, FPI-2265, targeting PSMA for mCRPC and novel RCs targeting solid tumors."

M&A • Metastatic Castration-Resistant Prostate Cancer

Fusion Pharmaceuticals Announces First Patient Dosed in the Phase 2 Portion of the AlphaBreak Trial Evaluating FPI-2265 in Metastatic Castration-Resistant Prostate Cancer (PRNewswire) - "Fusion Pharmaceuticals...announced that the first patient has been dosed in the Phase 2 portion of the AlphaBreak trial evaluating FPI-2265 (225Ac-PSMA I&T) in patients with metastatic castration-resistant prostate cancer (mCRPC)....The AlphaBreak trial is a Phase 2/3, randomized, open-label, multicenter study to evaluate the safety and efficacy of FPI-2265 in patients with mCRPC previously treated with 177Lu-PSMA radiotherapy....The Phase 2 portion of the AlphaBreak trial is expected to complete enrollment of approximately 60 patients by the end of 2024....The Phase 3 global registration portion of the AlphaBreak trial will enroll approximately 550 patients and is expected to begin in 2025."

Trial status • Metastatic Castration-Resistant Prostate Cancer

AlphaBreak: FPI-2265 (225Ac-PSMA-I&T) for Patients With PSMA-Positive Metastatic Castration-Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov) - P2/3 | N=60 | Recruiting | Sponsor: Fusion Pharmaceuticals Inc.

Metastases • New P2/3 trial • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Fusion Pharmaceuticals Reports First Quarter 2024 Financial Results and Announces Clinical Program Updates (Canada Newswire) - "Patient enrollment and dosing is ongoing in the Phase 1, multi-center, open-label clinical trial designed to investigate the safety, tolerability, dosimetry, biodistribution, and pharmacokinetics of FPI-2059 as well as preliminary anti-tumor activity in participants with NTSR1 expressing advanced metastatic solid tumors....R&D Expenses: Research and development expenses for the first quarter of 2024 were $21.3 million, compared to $15.9 million for the same period in 2023. The increase was primarily due to an increase in FPI-2265 program-related costs for our Phase 2 clinical trial of FPI-2265 in patients with mCRPC, and an increase in manufacturing-related costs."

Commercial • Trial status • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Preliminary efficacy and safety results from the (TATCIST) trial: A PSMA-directed targeted alpha therapy with FPI-2265 (225Ac-PSMA-I&T) for the treatment of metastatic castration-resistant prostate cancer (mCRPC) (AACR 2024) - P2 | "Preliminary efficacy and safety data as of 30Jan24 suggest that FPI-2265 is active in heavily pretreated pts with progressive mCRPC, including pts who received prior Lu therapy. Higher PSMA SUVmean was associated with improved PSA responses, Safety and tolerability were consistent with other published studies of 225Ac-PSMA-RLTs. These initial results support further investigation of FPI-2265 and a new phase 2/3 trial will begin enrolling soon."

Clinical • Metastases • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Fusion Pharmaceuticals Announces Presentation of Interim Data from the Phase 2 TATCIST Clinical Trial Evaluating FPI-2265 at the AACR Annual Meeting 2024 (PRNewswire) - P2 | N=115 | TATCIST (NCT05219500) | Sponsor: Fusion Pharmaceuticals Inc. | "The results are being presented at the AACR 2024 Annual Meeting....As of the March 1, 2024 data cutoff, 35 patients received at least one dose of FPI-2265, with 25 patients having at least 12 weeks of follow-up....From the efficacy-evaluable patient population, PSA50 (≥50% decline in prostate-specific antigen by 12 weeks after first treatment) response was achieved in 10 out of 20 patients (50%) regardless of prior lutetium treatment. PSA50 was achieved in 61% of lutetium-naïve participants and 42% of lutetium-treated participants....FPI-2265 demonstrated meaningful improvement in secondary endpoints which include maximum % PSA decline, and independent reviewer-assessed response rates....Fusion is advancing a Phase 2/3 trial for FPI-2265 in patients with mCRPC....The Phase 2 portion is expected to be initiated in the second quarter of 2024. A Phase 3 global registrational trial is expected..."

New P2/3 trial • New P3 trial • P2 data • Metastatic Castration-Resistant Prostate Cancer

Fusion Pharmaceuticals Reports Fourth Quarter and Full Year 2023 Financial Results and Announces Clinical Program Updates (PRNewswire) - "FPI-2265:...Following analysis of the Phase 2 data and an end of Phase 2 meeting to determine the recommended Phase 3 dosing regimen with the FDA, a Phase 3 global registrational trial in approximately 550 patients is expected to begin in 2025.....The Company is also pursuing the opportunity to potentially move this therapeutic candidate into earlier lines of treatment with combinations of FPI-2265 and olaparib. Fusion expects to initiate a combination trial in the first half of this year."

New P3 trial • New trial • Metastatic Castration-Resistant Prostate Cancer

Fusion Pharmaceuticals to be Acquired by AstraZeneca, Accelerating Development of Next-Generation Radioconjugates to Treat Cancer (PRNewswire) - "Fusion Pharmaceuticals...announced the Company has entered into a definitive agreement to be acquired by AstraZeneca. The acquisition marks a major step forward in AstraZeneca delivering on its ambition to transform cancer treatment and outcomes for patients by replacing traditional regimens like chemotherapy and radiotherapy with more targeted treatments....This acquisition complements AstraZeneca's leading oncology portfolio with the addition of the Fusion pipeline of RCs, including the Company's most advanced program, FPI-2265, a potential new treatment for patients with metastatic castration-resistant prostate cancer (mCRPC)."

M&A • Metastatic Castration-Resistant Prostate Cancer

Fusion Pharmaceuticals to Present Interim Data from the Phase 2 TATCIST Clinical Trial Evaluating FPI-2265 at the 2024 AACR Annual Meeting (PRNewswire) - "Fusion Pharmaceuticals...announced that interim efficacy and safety data from the Phase 2 TATCIST clinical trial evaluating FPI-2265 in patients with metastatic castration-resistant prostate cancer (mCRPC) has been selected for a clinical trial poster presentation at the American Association for Cancer Research (AACR) Annual Meeting 2024..."

P2 data • Metastatic Castration-Resistant Prostate Cancer

Fusion Pharmaceuticals Enters into Exclusive Worldwide License Agreement with Heidelberg University and Euratom for Actinium-Based PSMA Targeted Radiotherapy (PRNewswire) - "Fusion Pharmaceuticals Inc...today announced that it has entered into an exclusive worldwide license agreement with Heidelberg University and Euratom represented by the European Commission, Joint Research Centre (together, the 'Licensors'). The license agreement grants Fusion exclusive worldwide rights to utilize, develop, manufacture and commercialize compounds covered by the patent, which includes ²²⁵Ac-PSMA I&T ('FPI-2265') for the treatment of prostate specific membrane antigen (PSMA)-expressing cancers. In addition, Fusion and the Licensors have signed an agreement to settle the parties' dispute related to an inter partes review ('IPR') of a U.S. patent owned by the Licensors which was instituted in August 2023 by the United States Patent and Trademark Board....Under the terms of the license agreement, Fusion will pay the Licensors an aggregate upfront fee of €1.0 million..."

Licensing / partnership • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Targeted Alpha Therapy With 225Actinium-Prostate Specific Membrane Antigen (PSMA)-I&T of Castration-resISTant Prostate Cancer (TATCIST). (clinicaltrials.gov) - P2 | N=115 | Recruiting | Sponsor: Fusion Pharmaceuticals Inc. | Trial completion date: Dec 2024 ➔ Dec 2025 | Trial primary completion date: Dec 2023 ➔ Dec 2024

Metastases • Trial completion date • Trial primary completion date • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor • BRCA • MSI

Fusion Pharmaceuticals Announces Clinical Program and Manufacturing Updates (PRNewswire) - "The TATCIST trial was designed to evaluate patients with mCRPC with progressive disease, including patients who are naïve to PSMA-targeted radiopharmaceuticals and those who have been pre-treated with 177Lu-based PSMA radiopharmaceutical therapy. Fusion intends to report data from approximately 25 to 30 patients in April 2024 and then prioritize enrollment in the new Phase 2/3 trial....Doses produced out of Fusion's manufacturing facility are expected to support FPI-2265 manufacturing and are expected to be expanded to include Fusion's other proprietary and partnered programs."

Commercial • P2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Metastatic Castration-Resistant Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Fusion Pharmaceuticals Announces Third Quarter 2023 Financial Results and Clinical Program Updates (PRNewswire) - "The Phase 1, multi-center, open-label clinical trial is designed to investigate the safety, tolerability, and pharmacokinetics of FPI-1434 in patients with solid tumors expressing IGF-1R....Fusion is currently enrolling Cohort 2 in the cold/hot dosing regimen at 25 kBq/kg. The Company expects to report data from this cohort around year-end 2023....R&D Expenses: Research and development expenses for the third quarter of 2023 were $14.6 million, compared to $16.6 million for the same period in 2022. The decrease was primarily due to a decrease in FPI-1966 program-related activities as a result of the Company ceasing clinical development for the program and a decrease in manufacturing-related costs for our Phase 1 clinical trial of FPI-1434, partially offset by program expenses for our Phase 2 clinical trial of FPI-2265."

Commercial • Enrollment status • P1 data • Breast Cancer • Cervical Cancer • Endometrial Cancer • Gynecologic Cancers • Head and Neck Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • Squamous Cell Carcinoma of Head and Neck

Fusion Pharmaceuticals Announces Fourth Quarter 2022 Financial Results and Clinical Program Updates (PRNewswire) - "FPI-2265...Fusion plans to expand the Phase 2 program to additional sites and expects to report data on approximately 20 to 30 patients in the first quarter of 2024....FPI-1434...The Company anticipates reporting safety, pharmacokinetics, and imaging data, including any evidence of anti-tumor activity, from the Phase 1 trial in the second quarter of 2023. Fusion continues to anticipate the initiation of a Phase 1 combination trial with FPI-1434 and KEYTRUDA^® (pembrolizumab) to occur six to nine months following determination of the recommended Phase 2 dose of FPI-1434 monotherapy."

P1 data • P2 data • Trial status • Breast Cancer • Cervical Cancer • Endometrial Cancer • Eye Cancer • Genito-urinary Cancer • Gynecologic Cancers • Head and Neck Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Melanoma • Ocular Melanoma • Oncology • Ovarian Cancer • Prostate Cancer • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer • Uveal Melanoma

Targeted Alpha Therapy With 225Actinium-PSMA-I&T of Castration-resISTant Prostate Cancer (TATCIST). (clinicaltrials.gov) - P2 | N=100 | Recruiting | Sponsor: Excel Diagnostics and Nuclear Oncology Center | Trial primary completion date: Dec 2022 ➔ Dec 2023

Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • BRCA • MSI

Fusion Pharmaceuticals to Acquire Phase 2 Program for 225Ac-PSMA I&T, a Radiopharmaceutical Targeting Metastatic Castrate Resistant Prostate Cancer (PRNewswire) - "Fusion Pharmaceuticals Inc...announced the acquisition from RadioMedix, Inc. ('RadioMedix') of the investigational new drug application ('IND') for an ongoing Phase 2 clinical trial (the 'TATCIST' trial) evaluating 225Ac-PSMA I&T, a small molecule targeting prostate specific membrane antigen ('PSMA') expressed on prostate cancers. Following the closing, the alpha-emitting radiopharmaceutical being evaluated in the TATCIST trial will be known as FPI-2265....Fusion plans to expand the Phase 2 program to additional sites and expects to report data on 20 to 30 patients in the first quarter of 2024."

P2 data • Trial status • Genito-urinary Cancer • Oncology • Prostate Cancer