ATG-042 / Antengene - LARVOL DELTA

Preclinical characterization of ATG-042, a novel MTAP null-selective PRMT5 inhibitor (AACR 2025) - "In summary, ATG-042 is an oral MTAP null-selective PRMT5 inhibitor with potent efficacy against MTAPnull tumor. It also demonstrated good tolerability and brain penetrability."

Preclinical • Bladder Cancer • Genito-urinary Cancer • Hematological Malignancies • Malignant Pleural Mesothelioma • Mesothelioma • Oncology • Pleural Mesothelioma • Solid Tumor • MTAP

Preclinical characterization of ATG-042, a novel MTAPnull-selective PRMT5 inhibitor (PRNewswire) - "ATG-042 showed excellent anti-proliferative activities on multiple endogenous MTAPnull cell lines with IC50 values between 10nM and 100nM. ATG-042 demonstrated high permeability, good metabolic stability, and low risk of drug-drug interaction. In vivo PK study shows that ATG-042 is well absorbed, with a dose-dependent increase in plasma distribution and high oral bioavailability in mice, SD rats and beagle dogs. Furthermore, ATG-042 is brain-penetrable (B/P ratio=51% in mice; KPuubrain=0.73 in rats). ATG-042 showed robust in vivo efficacy in both subcutaneous CDX models (HCT116 -MTAP ko, LU99) and orthotopic CDX model (U87MG-luc) as a single agent....ATG-042 is poised to enter clinical development in the second half of 2025."

New trial • Preclinical • Oncology

ATG-042 (MTAPnull-selective PRMT5 Inhibitor) (PRNewswire) - "Results: ATG-042 showed excellent anti-proliferative activities on multiple endogenous MTAPnull cell lines with IC50 values between 10nM and 100nM. ATG-042 demonstrated high permeability, good metabolic stability, and low risk of drug-drug interaction. In vivo PK study shows that ATG-042 is well absorbed, with a dose-dependent increase in plasma distribution and high oral bioavailability in mice, SD rats and beagle dogs. Furthermore, ATG-042 is brain-penetrable (B/P ratio=51% in mice; KPuubrain=0.73 in rats). ATG-042 showed robust in vivo efficacy in both subcutaneous CDX models (HCT116 -MTAP ko, LU99) and orthotopic CDX model (U87MG-luc) as a single agent. In addition, ATG-042 also exhibited potential synergy in combination with other drugs for antitumor therapy....ATG-042 is poised to enter clinical development in the second half of 2025."

New trial • Preclinical • Oncology

Antengene Announces 2024 Interim Financial Results, Highlights Progress in R&D and Commercialization (PRNewswire) - P1 | N=48 | PERFORM (NCT06028373) | Sponsor: Antengene Biologics Limited | "ATG-031 is the first-in-class humanized anti-CD24 monoclonal antibody to enter clinical trials for cancer in the U.S...In the Phase I PERFORM study, 19 late-stage cancer patients have been treated with early low doses in the dose escalation segment, with no dose-limiting toxicities (DLTs) observed. Observations include stable disease (SD), objective tumor shrinkage, and clinical improvements among enrolled patients. The company targets a Phase I data readout in the first half of 2025....The development of preclinical candidates, including ATG-042, a selective PRMT5 inhibitor targeting MTAP-null tumors, and ATG-201, a CD19 x CD3 T-cell engager, is ongoing."

P1 data • Preclinical • Hematological Malignancies • Oncology • Solid Tumor

Preclinical characterization of ATG-042-198, a novel MTAP null-selective PRMT5 inhibitor (AACR 2024) - "In summary, ATG-042-198 is an oral MTAP null-selective PRMT5 inhibitor with potent efficacy against MTAPnull tumor. It also demonstrated good tolerability and preclinical PK profiles."

Preclinical • Hematological Malignancies • Oncology • MTAP

Antengene Presents Four Preclinical Posters at AACR 2024 (PRNewswire) - "The posters showcased four of Antengene's high-potential emerging programs, including ATG-042, tracking to a H1 2025 IND filing....This preclinical study was designed to test the in vitro/in vivo efficacy, and preclinical pharmacokinetic (PK) properties of ATG-042. According to the results, ATG-042 demonstrated a potent and selective inhibitory effect on the proliferation of MTAP knockout cells, showed high permeability, good metabolic stability, a low risk of drug-drug interaction (DDI), and high oral bioavailability. Importantly, ATG-042 demonstrated good brain penetrability. In CDX models, ATG-042 also potently and selectively inhibited tumor growth without inducing weight loss."

IND • Preclinical • Oncology

Antengene to Present Four Preclinical Abstracts at AACR 2024, Highlighting Focus on Cancer Immunology, Targeted Agents and Novel Technology Platforms (PRNewswire) - "Antengene Corporation Limited...announced that four preclinical abstracts have been selected as poster presentations at the 2024 American Association for Cancer Research Annual Meeting (AACR 2024)....'At the meeting, we will present the first data from our MTAPnull-selective PRMT5 inhibitor program and the first candidate from our companion diagnostic program, a CDx to support our novel Claudin 18.2 ADC, ATG-022. In addition, we are keenly interested in T cell engagers and look forward to presenting results on Antengene's unique AnTenGager platform and one of our first lead programs targeting LILRB4 for Acute Myelogenous Leukemia (AML)'."

Diagnostic • Preclinical • Acute Myelogenous Leukemia • Solid Tumor