OAT-4828 / Molecure - LARVOL DELTA

Structure-Guided Discovery of OAT-4828 as Potent, Selective, and Orally Bioavailable USP7 Inhibitor with In Vivo Antileukemic Activity. (PubMed, J Med Chem) - "Its pharmacokinetic profile in mice and preliminary safety assessments of the molecule encouraged us to use OAT-4828 as a tool compound for in vivo investigations. OAT-4828 was well-tolerated in mice, demonstrating significant antileukemic activity in a syngeneic model of B-cell derived non-Hodgkin lymphoma."

Journal • Preclinical • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Targeted Protein Degradation • USP7

Therapeutic inhibition of USP7 promotes antitumor immune responses. (PubMed, J Immunother Cancer) - "Overall, OAT-4828 demonstrates significant anticancer efficacy in melanoma and colon cancer models by activating the immune system, suggesting that USP7 may function as a checkpoint contributing to immunosuppression in cancer."

Journal • Colon Cancer • Colorectal Cancer • Melanoma • Oncology • Solid Tumor • Targeted Protein Degradation • PD-L1 • USP7

The development of a USP7 inhibitor for cancer immunotherapy (EACR 2025) - "Material and The activity and selectivity of OAT- 4828, an inhibitor we designed, was assessed in enzymatic assays... We conclude that USP7-MDM2-p53 is implicated in the antitumor function of immune cells and shapes the tumor microenvironment. Altogether, we confirm USP7 as an attractive target for cancer immunotherapy and present a strong rationale for the development of USP7 inhibitors for clinical use."

Chronic Lymphocytic Leukemia • Colon Cancer • Colorectal Cancer • Hematological Malignancies • Immunology • Leukemia • Lymphoma • Melanoma • Oncology • Solid Tumor • Targeted Protein Degradation • CD69 • GZMB • IFNG • IL2RA • MDM2 • USP7