balomenib (ZE63-0302) / Eilean Therap - LARVOL DELTA

Study to Assess Safety, Tolerability, PK, and PD of Multiple Doses of ZE63-0302 Administrated Orally in T2DM Patients. (clinicaltrials.gov) - P1 | N=60 | Recruiting | Sponsor: Eilean Therapeutics | Not yet recruiting ➔ Recruiting

Enrollment open • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Сlinical Study Aiming to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Ascending Doses of ZE63-0302 in Healthy Volunteers (clinicaltrials.gov) - P1 | N=82 | Completed | Sponsor: Eilean Therapeutics | Recruiting ➔ Completed | Trial completion date: Jun 2025 ➔ Nov 2025

First-in-human • Trial completion • Trial completion date

A randomized placebo-controlled Phase 1 trial in healthy volunteers investigating safety, pharmacokinetics and pharmacodynamics of a novel menin inhibitor, balomenib (ZE63-0302): Interim analysis. (ASH 2025) - "This interim analysis focuses on the 7 SADcohorts (20, 100, 300 mg, 600 mg, 300 mg with food, 300 mg with food in high BMI participants, and 600with itraconazole) and the 3 MAD cohorts (600 mg QD, 300 mg BID, and 300/600 mg BID for 7 days).Results...The most frequent TEAE was nausea(Grade 1 or Grade 2, controllable with ondansetron)...Dose-proportional systemic exposure wasobserved, and target engagement was established. The safety of balomenib in both pre-clinical andclinical studies thus far suggest it will be an exceptional therapeutic to combine with other agents inKMT2A/MEN1 dependent malignancies."

Clinical • P1 data • PK/PD data • KMT2A • MEIS1 • NPM1

Study to Assess Safety, Tolerability, PK, and PD of Multiple Doses of ZE63-0302 Administrated Orally in T2DM Patients. (clinicaltrials.gov) - P1 | N=60 | Not yet recruiting | Sponsor: Eilean Therapeutics

New P1 trial • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Сlinical Study Aiming to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Ascending Doses of ZE63-0302 in Healthy Volunteers (clinicaltrials.gov) - P1 | N=88 | Recruiting | Sponsor: Eilean Therapeutics

New P1 trial

An Exploratory Randomised, Double-Blind, Placebo-Controlled, First-in-Human Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Ascending Doses of ZE63-0302 in Healthy Volunteers (ANZCTR) - P1 | N=88 | Recruiting | Sponsor: Eilean Therapeutics AU Pty Ltd (A subsidiary of Eilean Therapeutics LLC) | N=40 ➔ 88

Enrollment change • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology

An Exploratory Randomised, Double-Blind, Placebo-Controlled, First-in-Human Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Ascending Doses of ZE63-0302 in Healthy Volunteers (ANZCTR) - P1 | N=40 | Recruiting | Sponsor: Eilean Therapeutics AU Pty Ltd (A subsidiary of Eilean Therapeutics LLC) | Not yet recruiting ➔ Recruiting | Initiation date: Apr 2024

Enrollment open • Trial initiation date • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology

THE NOVEL MENIN INHIBITOR ZE63-0302 HAS AN IMPRESSIVE SAFETY PROFILE AND UNIQUE CHEMISTRY THAT SUGGESTS IMPROVED EFFICACY AGAINST RESISTANCE MUTATIONS. (EHA 2024) - "ZE63-0302 is a novel menin inhibitor with comparable in vitro and in vivo activity compared to SNDX-5613, butwith a more favorable safety profile. The unique binding modality is expected to decrease the emergence ofresistance mutations that have occurred with SYDX-5613 and other menin inhibitors. The promising singleagent and combination studies with multiple validated targeted therapies in AML support clinical developmentof ZE63-0302 which are being initiated at this time"

Clinical • IO biomarker • Cardiovascular • FLT3 • KMT2A • MEN1 • NPM1

Expert Systems Celebrates a Milestone with Eilean Therapeutics: Initiation of First-in-Patient Trial of Balamenib, a Selective Best-in-Class Menin Inhibitor (PRNewswire) - "Expert Systems...proudly announces a significant milestone in partnership with Eilean Therapeutics LLC: the start of Phase 1 trial of balamenib (ZE63-0302), a highly selective inhibitor of the menin–KMT2A binding interaction, under the Clinical Trial Notification (CTN) scheme of the Australian Therapeutics Goods Administration (TGA)."

Trial status • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology

An Exploratory Randomised, Double-Blind, Placebo-Controlled, First-in-Human Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Ascending Doses of ZE63-0302 in Healthy Volunteers (ANZCTR) - P1 | N=40 | Not yet recruiting | Sponsor: Eilean Therapeutics AU Pty Ltd (A subsidiary of Eilean Therapeutics LLC)

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

EILEAN THERAPEUTICS APPROVED TO INITIATE FIRST PATIENT TRIAL WITH BALAMENIB (ZE63-0302), A SELECTIVE BEST-IN-CLASS MENIN INHIBITOR (PRNewswire) - "Eilean Therapeutics LLC...announced that Eilean Therapeutics Australia Pty, Ltd, received clearance from the Human Research Ethics Committee in Australia to begin a Phase 1 trial of balamenib (ZE63-0302) under the Clinical Trial Notification (CTN) scheme of the Australian Therapeutics Goods Administration (TGA). The Phase 1 program includes a single ascending dose trial in healthy volunteers to evaluate the safety, pharmacokinetics and target engagement profile of balamenib, a highly selective inhibitor of the menin–KMT2A binding interaction."

Trial status • Acute Myelogenous Leukemia • Oncology