CTS3497 / CytosinLab - LARVOL DELTA

A First-in-Human Phase I/II Study Evaluating CTS3497, an MTA-Cooperative PRMT5 Inhibitor, in Advanced or Metastatic MTAP-Deficient Solid Tumors (ESMO 2026) - No abstract available

First-in-human • Metastases • P1/2 data • Oncology • Solid Tumor • MTAP

A first-in-human phase I/II study evaluating CTS3497, an MTA-cooperative PRMT5 inhibitor, in advanced or metastatic MTAP-deficient solid tumors. (ASCO 2026) - P1/2 | "CTS3497 demonstrated a favorable safety profile and promising efficacy in heavily pretreated pts with MTAP-deficient advanced solid tumors, including GI cancers, NSCLC."

First-in-human • Metastases • P1/2 data • Ampulla of Vater Carcinoma • Biliary Cancer • Biliary Tract Cancer • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Gastric Cancer • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • Squamous Cell Carcinoma • Urothelial Cancer • MTAP • PRMT5

The MTA-cooperative PRMT5 inhibitor CTS3497 alone and in synergy with mechanism-based combination targeted therapies for the treatment of MTAP-deleted cancers (AACR 2026) - P1/2 | "In addition, combination of CTS3497 and osimertinib (EGFR-TKI) enhanced anti-tumor efficacy and suppressed acquired resistance to osimertinib in MTAPnullEGFRmut lung cancer xenografts. Furthermore, CTS3497 effectively reversed resistance to adagrasib (KRASG12C) in an adagrasib-resistant MTAPnull model, resulting in profound tumor regression without regrowth even after discontinuation of treatment...CTS3497 represents a promising synthetic-lethal precision medicine for patients with MTAP-deficient cancers either as a single agent or in combination with rational combination partners. Particularly, combination of CTS3497 with CTS2190, a type I PRMT inhibitor, may provide a potential solution for patients post PRMT5 targeted therapy."

Brain Cancer • Glioma • Lung Cancer • Oncology • Pancreatic Cancer • Solid Tumor • BCL2 • CDKN2A • KRAS • MTAP

Targeting arginine methylome in 9p21/MTAP-deleted malignant cancers with a next generation PRMT5-specific inhibitor CTS3497 (AACR 2024) - "Furthermore, a synergistic anti-tumor effect was observed in multiple MTAP-deleted tumors when combining PRMT5 inhibition with CTS2190, an investigational type-I PRMT inhibitor currently in phase I/II clinical trials. Its superior ADME properties and favorable safety profiles observed in preclinical studies mark a breakthrough in the next generation epigenetic therapy. CTS3497 emerges as a promising therapeutic option for patients with MTAP-deleted malignancies."

Brain Cancer • Lung Cancer • Oncology • Solid Tumor • MTAP

First-in-human phase I study of CTS3497, a methylthioadenosine (MTA)-cooperative PRMT5 inhibitor, in patients with advanced/metastatic methylthioadenosine phosphorylase (MTAP)-deficient solid tumors and lymphomas (ESMO 2025) - P1/2 | "Legal entity responsible for the study CytosinLab Therapeutics Co., Ltd. Funding CytosinLab Therapeutics Co., Ltd."

Clinical • First-in-human • Metastases • P1 data • Biliary Cancer • Cholangiocarcinoma • Colorectal Cancer • Hematological Malignancies • Lung Cancer • Lymphoma • Malignant Pleural Mesothelioma • Mesothelioma • Non Small Cell Lung Cancer • Oncology • Pleural Mesothelioma • Solid Tumor • MTAP • PRMT5

A Phase I/II Clinical Study of CTS3497 in Patients With MTAP Deficient Malignacies (clinicaltrials.gov) - P1/2 | N=224 | Recruiting | Sponsor: CytosinLab Therapeutics Co., Ltd.

New P1/2 trial • Brain Cancer • Hematological Malignancies • Lung Cancer • Lymphoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Urothelial Cancer