Up284 / Up Therap - LARVOL DELTA

Evaluation of Up284 as a selective proteasome inhibitor for prostate cancer therapy (AACR 2024) - "Furthermore, Up284 has been found to induce apoptosis in PC3 cells, surpassing the efficacy of bortezomib...It is well-tolerated in mice and holds promise for oral administration, demonstrating a proteasome-dependent reporter protein stabilization effect superior to ixazomib. Importantly, Up284 has induced tumor regression and improved survival rates in various cancer models, including ovarian and breast cancers.In conclusion, Up284 emerges as a lead candidate for targeted prostate cancer therapy due to its high specificity, substantial therapeutic index, and potent anti-cancer activity both in vitro and in vivo. Further development and clinical investigation of Up284 are warranted to fully explore its therapeutic potential."

Breast Cancer • Genito-urinary Cancer • Oncology • Ovarian Cancer • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

ADRM1 inhibitor, Up284 induces replication stress and suppresses cell proliferation in triple-negative breast cancer (AACR 2025) - "Together, our results indicate that ADRM1 is a promising target for TNBC therapy and suggest that this ADRM1 inhibitor, Up284, has the potential for clinical application in the treatment of TNBC. Our analysis will unravel the novel mechanistic insight into the therapeutic potential of this compound and provide preclinical evidence to develop further combination therapy."

Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • ADRM1 • BRCA • CHEK1 • ER • HER-2 • PGR • UCHL5

Development and anticancer properties of Up284, a spirocyclic candidate ADRM1/RPN13 inhibitor. (PubMed, PLoS One) - "Cell lines derived from diverse cancer types (ovarian, triple negative breast, colon, cervical and prostate cancers, multiple myeloma and glioblastoma) were sensitive to Up284, including several lines resistant to bortezomib or cisplatin. Up284 cleared from plasma in a few hours and accumulated in major organs by 24 h. A single dose of Up284, when administered to mice intra peritoneally or orally, inhibited proteasome function in both muscle and tumor for >48 h. Up284 was well tolerated by mice in repeat dose studies. Up284 demonstrated therapeutic activity in xenograft, syngeneic and genetically-engineered murine models of ovarian cancer."

Journal • Brain Cancer • Cervical Cancer • CNS Tumor • Genito-urinary Cancer • Glioblastoma • Hematological Disorders • Hematological Malignancies • Metabolic Disorders • Multiple Myeloma • Oncology • Ovarian Cancer • Pain • Prostate Cancer • Solid Tumor • Targeted Protein Degradation • Thrombocytopenia • Triple Negative Breast Cancer