CTS2190 / CytosinLab - LARVOL DELTA

Efficacy and safety results of a first-in-class PRMT1 inhibitor CTS2190 in patients (pts) with immune checkpoint inhibitor (ICI) insensitive advanced solid tumors (ESMO 2026) - No abstract available

Checkpoint inhibition • Clinical • Metastases • Oncology • Solid Tumor

Efficacy and safety results of a first-in-class PRMT1 inhibitor CTS2190 in patients (pts) with immune checkpoint inhibitor (ICI)–insensitive advanced solid tumors. (ASCO 2026) - P1/2 | "CTS2190 has shown superior safety and promising efficacy in heavily pretreated pts with advanced solid tumors to achieve the clinical proof-of-concept. More patients are being enrolled at RP2Ds in current phase IIa cohort expansion study in NSCLC, mCRPC, TNBC, PDAC and other indications of interest. Studies to combine CTS2190 with SoCs in solid tumors are being planned."

Checkpoint inhibition • Clinical • IO biomarker • Metastases • Castration-Resistant Prostate Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Solid Tumor • Triple Negative Breast Cancer • MTAP • PRMT1

CTS2190, a first-in-class PRMT1 inhibitor in phase I/II clinical development, demonstrates robust and broad monotherapy efficacy and provides a rationale for novel combinations based on translational findings (AACR 2026) - P1/2 | "Furthermore, the combinatorial potential of CTS2190 was investigated with targeted therapies (Enzalutamide, Osimertinib, Gilteritinib), a radioligand therapy (Lu177-PSMA), and an anti-PD-1 antibody across relevant in vivo models. The compelling single-agent activity of CTS2190 in preclinical models corroborates its ongoing clinical investigation. The broad and potent synergy observed with targeted, radioligand, and immunotherapeutic agents provides a strong mechanistic rationale for the imminent clinical development of novel CTS2190-based combination regimens, positioning it as a versatile therapeutic strategy for multiple cancers."

Clinical • Monotherapy • P1/2 data • Oncology • Solid Tumor

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

The pharmacological intervention of protein arginine methyltransferase 1 (PRMT1) leads to metastatic castration-resistant prostate cancer (mCRPC) repression through unique and significant androgen receptor (AR) downregulation and epigenetic modulation (AACR 2025) - "CTS2190 not only decreases AR and asymmetric dimethylarginine (ADMA) levels, but also expression of prostate-specific antigen (PSA), MYC, and many downstream genes in AR signaling pathway in 22RV1 model, more effectively than docetaxel, enzalutamide, or even PROTAC targeting AR degradation. Taken together, our findings highlight CTS2190 as a therapeutic agent, either alone or in combination, for a broader range of patients with ARPI-resistant mCRPC. CTS2190 is currently under evaluation in a phase I/II clinical trial, with an expansion cohort including mCRPC patients."

Metastases • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AR • PRMT1 • TOP1

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

Mouse clinical trials (MCT) and other comprehensive pharmacology approaches highlight protein arginine methyltransferase 1 (PRMT1) targeting in various solid tumors with promising efficacy and combined mode-of-actions (MoAs) beyond epigenetic regulation (AACR 2025) - P1/2 | "CTS2190 not only demonstrates synthetic lethality with epigenetic instability, DDR, or RNA splicing (RS) dysregulation, but also as an ideal partner for a wide range of cancer therapies, including combinations with PRMT5i, a type-II PRMT member in both MTAPnull and wild-type genetic context. Ongoing clinical and translational studies for CTS2190 will pioneer the breakthrough and pave the way for developing more next-generation epigenetic therapies in solid tumors."

Preclinical • Breast Cancer • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Gastric Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor • Squamous Cell Carcinoma • Triple Negative Breast Cancer • MTAP • PRMT1

Preliminary efficacy and safety results from an ongoing Phase I/II trial of CTS2190, a PRMT1 inhibitor, in patients with advanced/metastatic solid tumors [WITHDRAWN] (ESMO 2025) - No abstract available

Clinical • Metastases • P1/2 data • Oncology • Solid Tumor

Preliminary efficacy results from an ongoing phase I/II trial of CTS2190, a PRMT1 inhibitor, in patients with advanced/metastatic solid tumors. (ASCO 2025) - P1/2 | "CTS2190 demonstrated a favorable safety profile and promising efficacy in heavily pretreated pts with advanced solid tumors, particularly in immunologically cold mCRPC and PD-(L)1 primarily resistant NSCLC. These results position CTS2190 as a promising therapeutic option to fulfil unmet medical needs following ICIs therapies. PFS of pts with PD-(L)1 primary resistance."

Clinical • IO biomarker • Metastases • P1/2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Immunology • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Solid Tumor • AR • PRMT1

First results from phase I/II study of CTS2190, a novel small-molecule inhibitor of type I PRMTs, in patients with advanced solid tumors (ESMO 2024) - P1/2 | "CTS2190 was well tolerated and showed encouraging antitumor activities in advanced and/or metastatic solid tumors, including NSCLC, TNBC, HNSCC and ESCC. Further investigation of CTS2190 in larger pts population is ongoing including biomarker exploration."

Clinical • Metastases • P1/2 data • Breast Cancer • Colorectal Cancer • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Gastrointestinal Cancer • Head and Neck Cancer • Hematological Malignancies • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer

CTS2190 Phase I /II Clinical Study in Patients (clinicaltrials.gov) - P1/2 | N=224 | Recruiting | Sponsor: CytosinLab Therapeutics Co., Ltd. | N=120 ➔ 224

Enrollment change • Breast Cancer • Gastrointestinal Cancer • Hepatology • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Solid Tumor • Triple Negative Breast Cancer

CTS2190, a next-generation epigenetic inhibitor for targeting type I PRMT deregulated human tumors (AACR 2023) - "The anti-tumor activity was dose-dependent and correlated with the inhibition of type I PRMT activity as measured by decrease in ADMA and increase in MMA. In summary, CTS2190 is a promising type I PRMT inhibitor and clinical trial is underway to explore the proof-of-concept anti-tumor benefit for patients."

Oncology • Solid Tumor • PRMT1