GB3226 / Galecto, Bridge Medicines - LARVOL DELTA

GB3226, a novel, orally active, first-in-class small molecule inhibitor of ENL-yeats and FLT3 kinase for the treatment of Relapsed/Refractory Acute Myeloid Leukemia (ASH 2025) - "In cell-based assays, GB3226potently inhibited proliferation of both MV4; 11 (IC50=18 nM) and MOLM13 (IC50=32 nM) cell lines andwas additive/synergistic when combined with standard-of-care agents, including venetoclax, gilteritinib,and revumenib. We have developed GB3226, a novel, oral, first-in-class, dual inhibitor of ENL-YEATS and FLT3for the treatment of AML. Preclinical studies demonstrate that GB3226 exhibits potent anti-leukemicactivity and has the potential for combination use with multiple therapeutic agents across diverse AMLgenotypes. GB3226 has shown robust in vitro and in vivo efficacy, along with a favorable preclinical safetyprofile."

Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • FLT3 • HOXA9 • KIT • MEIS1 • MELK • NTRK3 • TET2

A phase 1/2 study of GB3226, a novel dual inhibitor of ENL-yeats and FLT3, in patients with relapsed/refractory Acute Myeloid Leukemia (ASH 2025) - P1/2 | "Phase 2 of the study aims at assessing the efficacy of GB3226, measured by the rate of completeremission (CR) and CR with partial hematologic recovery (CRh).Additionally, the study will explore pharmacodynamic (PD) markers in peripheral blood and bone marrowto elucidate GB3226's biological effects and identify potential biomarkers predictive of clinical response. This open-label, multicenter, seamless Phase 1/2 study will enrol adult patients (aged ≥18years) with R/R AML, who have failed at least one prior line of therapy (e.g., chemotherapy, venetoclax-based regimens). Phase 1 employs a dose-escalation design across three cohorts to assess the impact of CYP3A4 inhibitorson GB3226 PK and safety and define the maximal tolerated dose (MTD).Cohort A: No CYP3A4 modifiersCohort B: Coadministration with strong CYP3A4 inhibitors (e.g., voriconazole, and posaconazole)Cohort C: coadministration with moderate CYP3A4 inhibitors (e.g., isavuconazole)GB3226 is administered..."

Clinical • P1/2 data • Acute Myelogenous Leukemia • Hematological Disorders • Hematological Malignancies • Leukemia • CD14 • FLT3 • HEY1 • HOXA9 • ITGAM • MEIS1

Galecto Reports Third Quarter 2025 Operating...Results (GlobeNewswire) - "...'During the quarter, we received constructive regulatory guidance from the FDA on our pre-IND submission for GB3226, a novel small molecule dual inhibitor of ENL-YEATS and FLT3 with potential to address a broad portion of patients with acute myeloid leukemia (AML), including those with high-risk genetic mutations....This regulatory feedback...aligns with our plan to submit an IND in the first quarter of 2026 and initiate a Phase 1 trial in AML'."

FDA event • IND • Acute Myelogenous Leukemia

Galecto Reports Second Quarter 2025 Operating and Financial Results (GlobeNewswire) - "...'We remain focused on advancing our lead program, GB3226, a dual ENL-YEATS and FLT3 inhibitor for multiple genetic subsets of AML....Our goal is to submit an Investigational New Drug (IND) application to the FDA in Q1 2026, and we are actively advancing key IND-enabling activities across pharmacology, toxicology, and CMC to support a smooth transition into the clinic'. Preclinical data to date support the therapeutic potential of GB3226 both as a monotherapy and in combination to address the menin-resistant population within AML....The Company anticipates that its cash and cash equivalents will be sufficient to fund operating expenses and capital requirements into 2026, including the submission of an investigational new drug application for GB3226 to the FDA."

Commercial • IND • Preclinical • Acute Myelogenous Leukemia

An Open-label, Dose-Escalation and Dose-Expansion Study of GB3226 in Patients With Relapsed/Refractory Acute Myeloid Leukemia (clinicaltrials.gov) - P1/2 | N=184 | Not yet recruiting | Sponsor: Galecto Biotech AB

New P1/2 trial • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology

Galecto Reports First Quarter 2025 Operating and Financial Results (GlobeNewswire) - "...'During the first quarter, we continued to advance GB3226, our dual ENL-YEATS and FLT3 inhibitor for multiple genetic subsets of AML'....'We continued preclinical studies to support our planned IND submission, which remains on track for Q1 2026. To date, preclinical data have shown significant improvement in efficacy compared to current FLT3 and menin inhibitors, with activity across a broad spectrum of patient genotypes'."

IND • Preclinical • Acute Myelogenous Leukemia

Galecto Reports Full-Year 2024 Financial Results (GlobeNewswire) - "Acquired global rights to Bridge Medicines’ BRM-1420 program, now GB3226, a novel dual ENL-YEATS and FLT3 inhibitor for multiple genetic subsets of acute myeloid leukemia (AML). GB3226 is a potent and selective inhibitor designed to disrupt key oncogenic pathway signaling. Preclinical data showed GB3226’s superior efficacy to both FLT3 and menin inhibitors in animal models, as well as additive or synergistic activity in combination with standard-of-care treatments....GB3226 on track for IND submission in Q1 2026."

IND • Preclinical • Acute Myelogenous Leukemia

Galecto Reports Third Quarter 2024 Financial Results (GlobeNewswire) - "Galecto plans to submit an investigational new drug application (IND) for BRM-1420 in the US in late 2025 or early 2026 and initiate clinical studies in patients with AML thereafter."

IND • New trial • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology

Galecto Completes Strategic Review to Focus on Oncology and Liver Disease and Acquires Acute Myeloid Leukemia Preclinical Asset from Bridge Medicines (GlobeNewswire) - "Galecto, Inc...announced that, following an intensive strategic review process, Galecto has determined to focus on cancer and liver disease, leveraging its existing clinical stage asset GB1211, which has shown positive results in non-small cell lung cancer (NSCLC) and decompensated cirrhosis clinical studies. Galecto further announced that it has bolstered its pipeline with the acquisition of the global rights to BRM-1420, a novel, first-in-class asset developed by Bridge Medicines, a company co-founded by Takeda...As consideration for the acquisition of the global rights of BRM-1420, Galecto issued 62,594 shares of common stock to Bridge Medicines...As part of the strategic alternative review process, Galecto has determined not to further advance GB2064, its LOXL-2 inhibitor candidate, at this time....Galecto plans to file an IND for BRM-1420 in the US in late 2025 or early 2026 and initiate clinical studies in patients with AML thereafter."

Commercial • Discontinued • IND • Pipeline update • Acute Myelogenous Leukemia • Myelofibrosis • Non Small Cell Lung Cancer