RGX-019-MMAE / Inspirna, Rockefeller University - LARVOL DELTA

Targeting myeloid epithelial tyrosine kinase (MERTK) receptor in acute myeloid leukemia using a novel antibody-drug conjugate, RGX-019-MMAE (AACR 2024) - "High MERTK expression in monocytic AML suggested that MERTK is a promising therapeutic target in this subtype. RGX-019-MMAE significantly induced AML cell death and produced a synergistic anti-leukemic effect in combination with chemotherapeutic agents and targeted therapy in vitro, suggesting its potential for targeting patients with high-risk AML."

ADC • IO biomarker • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • AXL • MERTK • PTPN11

RGX-019-MMAE inhibits leukemia progression by targeting MER proto-oncogene tyrosine kinase (MERTK) in acute myeloid leukemia. (PubMed, J Exp Clin Cancer Res) - No abstract available

Journal • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • MERTK

A MERTK-Targeting Antibody-Drug Conjugate Selectively Depletes M2 Tumor-Associated Macrophages and MERTK-Expressing Cancer Cells. (PubMed, Cancer Res) - "Furthermore, unlike other MERTK-targeting small molecules or antibodies, no retinal toxicity of RGX-019-MMAE was observed in vivo. These findings reveal that combined therapeutic targeting of MERTK in cancer cells and M2 macrophages offers enhanced opportunities for anti-tumor efficacy in a wide range of MERTK-expressing tumors."

IO biomarker • Journal • Oncology • MERTK

Targeting Myeloid Epithelial Tyrosine Kinase (MERTK) Receptor in Acute Myeloid Leukemia Using a Novel Antibody Drug Conjugate, Rgx-019-MMAE (ASH 2023) - "Finally, we investigated the synergistic effect of RGX-019-MMAE with Venetoclax (BCL2 inhibitor) or 5-Azacytidine in vitro. RGX-019-MMAE significantly induced cell death in AML cell lines and primary AML patient samples. RGX-019-MMAE, combined with chemotherapeutic agents and targeted therapy, produces a synergistic anti-leukemic effect. Our data indicates that MERTK is a potential therapeutic target in AML patients with monocytic subtypes of leukemia."

IO biomarker • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • Solid Tumor • AXL • MERTK • PTPN11

RGX-019-MMAE, a novel MERTK-targeting antibody-drug conjugate (ADC) with robust anti-tumor efficacy in both solid and liquid tumors. (ASCO 2023) - "Collectively, RGX-019-MMAE’s robust anti-tumor efficacy in multiple aggressive tumors, and MERTK’s expression profile on cancer cells and normal tissue support further advancement of RGX-019-MMAE as a drug candidate for development in solid and liquid cancers."

Clinical • Acute Myelogenous Leukemia • Hematological Disorders • Hematological Malignancies • Oncology • Ophthalmology • Solid Tumor • Triple Negative Breast Cancer • MERTK • PTPN11

[VIRTUAL] In vivo efficacy and safety of RGX-019, a MerTK targeting monoclonal antibody (AACR-II 2020) - "Additionally, no clinical hematologic toxicities were observed. Pro-inflammatory macrophage-related cytokines were detected in the plasma after RGX-019 dosing, confirming target engagement in vivo.The MOA and safety profile of RGX-019, along with its high selectivity, affinity, in vivo efficacy, and immunologic activity, support further advancement of RGX-019 as a clinical candidate for development in solid and liquid cancers."

Late-breaking abstract • Breast Cancer • Leukemia • Lung Cancer • Melanoma • Multiple Myeloma • Non Small Cell Lung Cancer • Oncology • Thoracic Cancer • AXL • GAS6 • MERTK • PROS1

RGENIX Presents Results from Preclinical Safety and Efficacy Studies of RGX-019 at the 2020 AACR Annual Meeting (Businesswire) - "...RGX-019 demonstrated a favorable safety profile in a 28-day dose-range finding toxicology study in monkeys. Of note, retinal toxicity - a finding associated with other MerTK targeting approaches - was not observed at any dose of RGX-019. The results overall demonstrate that RGX-019 can potently target MerTK signaling on both cancer cells and immune-suppressive M2 macrophages with a novel mechanism, resulting in anti-tumor activity with a wide therapeutic window."

Preclinical • Oncology • Solid Tumor

Characterization of the anti-cancer and immunologic activity of RGX-019, a novel pre-clinical stage humanized monoclonal antibody targeting the MERTK receptor (AACR 2019) - "This activity results in robust repression of cancer cell growth both in vitro and in vivo. Overall, these data support further development of RGX-019 as a cancer therapeutic."

Late-breaking abstract

"#Rgenix To Present Abstract on #RGX-019 at #AACR19 https://t.co/gWFKrvMFoT" (,@1stOncology)

Rgenix presents pre-clinical data on RGX-019 at the 2019 AACR Annual Meeting (Businesswire) - “Rgenix, Inc….announced today it is presenting pre-clinical data from ongoing research of RGX-019...for the treatment of advanced cancer. In a presentation of a late-breaking abstract, 'Characterization of the anti-cancer and immunologic activity of RGX-019, a novel pre-clinical stage humanized monoclonal antibody targeting the MERTK receptor,' which was accepted for the 2019 American Association of Cancer Research Annual Meeting, Isabel Kurth Ph.D., Rgenix VP of Research, discussed data showing RGX-019 to be a potent and selective inhibitor of MERTK signaling, resulting in suppression of cancer growth and activation of the innate immune response.”

Late-breaking abstract • Preclinical

Newly added product (Businesswire) - Preclinical, Triple Negative Breast Cancer

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