OTX-008 / Merck (MSD) 
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  • ||||||||||  paclitaxel / Generic mfg.
    Journal:  Targeting Galectin-1 Overcomes Paclitaxel Resistance in Esophageal Squamous Cell Carcinoma. (Pubmed Central) -  Nov 16, 2024   
    Combining OTX008 with clinical taxane formulations effectively reversed paclitaxel resistance in vitro and in vivo. Elevated galectin-1 levels thus serve as an indicator of response to paclitaxel therapy in ESCC, offering a therapeutic intervention strategy to overcome drug resistance.
  • ||||||||||  Jakafi (ruxolitinib) / Incyte, OTX-008 / Merck (MSD), resatorvid (TAK-242) / Takeda, Akaza Bioscience
    Monocyte-Driven Aberrant Inflammation in Myeloproliferative Neoplasms Is Regulated By Galectin-1 (Seaport Ballroom EFGH (Manchester Grand Hyatt San Diego)) -  Nov 6, 2024 - Abstract #ASH2024ASH_2251;    
    Additionally, Gal-1 expression was induced by MPLW515L and JAK2V617F and inhibited by ruxolitinib, a JAK inhibitor, in Ba/F3 cells...Pharmacologic inhibition of Gal-1 by OTX008 suppressed the expression and secretion of inflammatory cytokines in MPN monocytes and monocytic cell lines...Notably, targeting TLR4 via both neutralizing antibody and pharmacologic inhibition (TAK-242) abrogated the proinflammatory effects of Gal-1 on monocytes...We further evaluated therapeutic effects of targeting global glycosylation in MPN via 2-Deoxy-D-glucose (2-DG), a global glycosylation inhibitor, which decreased splenomegaly and reduced elevated platelets and hematocrit in JAK2V617F knock-in mice...We further demonstrate that Gal-1 fuels monocyte inflammation by interacting with TLR4 and activation of OXPHOS and PI3K-AKT-mTOR signaling pathways. Our results uncover a novel therapeutic avenue for targeting aberrant Gal-1 and global glycosylation in MPNs.
  • ||||||||||  Jakafi (ruxolitinib) / Novartis, Incyte, OTX-008 / Merck (MSD)
    Galectin-1 Fuels Monocyte-Driven Hyperinflammation and Represents a Novel Therapeutic Target in Myeloproliferative Neoplasms (SDCC - Halls G-H) -  Nov 3, 2023 - Abstract #ASH2023ASH_5962;    
    Additionally, galectin-1 expression was induced by MPL W515L and JAK2 V617F and inhibited by ruxolitinib in Ba/F3 cells...Furthermore, OTX008, a galectin-1 inhibitor, inhibited the transcription and secretion of inflammatory cytokines in MPN patient CD14+ monocytes and monocytic cell lines...We further demonstrate that galectin-1 fuels inflammation potentially via metabolic reprogramming of monocytes and activation of PI3K-AKT-mTOR signaling. Our data also suggest galectin-1 as a putative therapeutic target in MPNs.
  • ||||||||||  Tagrisso (osimertinib) / AstraZeneca, OTX-008 / Merck (MSD)
    A Osimertinib And Otx008 Impair Survival Of Glioblastoma Cells By Inhibiting Ras (Grote Zaal Foyer) -  Sep 28, 2023 - Abstract #EANO2023EANO_307;    
    The EGFR-inhibitor Osimertinib and the selective Galectin-1 inhibitor OTX008 showed antiproliferative effect in immortalized glioblastoma cell line U87 and were also able to inhibit activation of Ras. Future experiments should focus on the downstream signalling of the pathways, especially in EGFR mutated glioblastoma stem cells.
  • ||||||||||  OTX-008 / Merck (MSD)
    The role of galectin-1 in SCLC: Prognostic significance and therapeutic implications () -  Jul 27, 2023 - Abstract #ESMO2023ESMO_3458;    
    Conclusions Our findings suggest that high levels of Gal-1 and PLR are associated with poorer OS in SCLC patients and can be useful as clinical prognostic biomarkers. Moreover, our in vivo model suggests that the inhibition of Gal-1 could be a novel potential therapy with a significant impact in combination with platinum-based therapy.
  • ||||||||||  OTX-008 / Merck (MSD)
    Journal:  Galectin-1, a novel promising target for outcome prediction and treatment in SCLC. (Pubmed Central) -  Nov 23, 2022   
    in this study, high levels of Gal-1 and PLR were associated with poorer OS in SCLC patients, supporting their utility as clinical prognostic biomarkers. Moreover, the in vivo model suggests the inhibition of Gal-1 as a novel potential therapy for this disease with very poor prognosis.
  • ||||||||||  OTX-008 / Merck (MSD)
    The LMP1/Lgals1-NF-Kb-IRF1-PDL1 Axis Promotes Immune Escape in Nasopharyngeal Carcinoma (Henry B. Gonzalez Convention Center, Exhibit Hall 1) -  Aug 1, 2022 - Abstract #ASTRO2022ASTRO_1085;    
    Our study demonstrates the therapeutic benefit of MSCs on age-related olfactory dysfunction and suggests Gal1 as a key mediator of the anti-inflammatory action of MSCs. Our findings reveal a regulatory axis for programmed death ligand 1 (PD-L1) expression in NPC cells, and targeting one component in this axis, Lgals1, is effective in boosting the immunogenicity of NPCs, providing a therapeutic avenue for treating NPC in clinic.
  • ||||||||||  OTX-008 / Merck (MSD)
    Journal:  Transcriptional control of brain tumor stem cells by a carbohydrate binding protein. (Pubmed Central) -  Feb 15, 2022   
    Importantly, we establish that galectin1 forms a complex with the transcription factor HOXA5 to reprogram the BTSC transcriptional landscape. Our data unravel an oncogenic signaling pathway by which the galectin1/HOXA5 complex maintains BTSCs and promotes glioblastoma.
  • ||||||||||  OTX-008 / Merck (MSD)
    Journal:  New Treatment Strategy Targeting Galectin-1 against Thyroid Cancer. (Pubmed Central) -  Jun 3, 2021   
    Finally, the sensitive 8505c line was xenografted in nude mice, and 3 weeks of OTX008 treatment (5 mg/kg/day) demonstrated a significant reduction in tumor and lung metastasize sizes without side effects. Overall, OXT008 showed significant anti-cancer effects both in vitro and in vivo in thyroid cancer lines expressing Gal-1, supporting further investigation of the molecular mechanisms of the drug and future clinical trials in patients with anaplastic thyroid cancer.
  • ||||||||||  OTX-008 / Merck (MSD)
    Clinical, Journal, IO biomarker:  Immunomodulatory effects of galectin-1 in patients with chronic lymphocytic leukemia. (Pubmed Central) -  Apr 27, 2021   
    OTX008 caused a reduction in IL-10 production as well as IL-2, but no significant alteration in the expression of DC maturation markers or T regulatory cell (Treg) frequency was observed. The results of our study suggest that Gal-1 from CLL serum give rise to a specific IL-10 CD4 T cell phenotype, other than Treg, that could mediate immunodeficiency development in CLL patients.
  • ||||||||||  OTX-008 / Merck (MSD)
    Journal:  Galectin-1 studies in proliferative diabetic retinopathy. (Pubmed Central) -  Nov 21, 2020   
    The results of our study suggest that Gal-1 from CLL serum give rise to a specific IL-10 CD4 T cell phenotype, other than Treg, that could mediate immunodeficiency development in CLL patients. These results suggest that galectin-1is involved in the pathogenesis of PDR.
  • ||||||||||  OTX-008 / Merck (MSD)
    [VIRTUAL] Galectin-1 studies in proliferative diabetic retinopath (Abstract Channel) -  Sep 28, 2020 - Abstract #EURETINA2020EURETINA_811;    
    These results suggest that galectin-1is involved in the pathogenesis of PDR. These results suggest that galectin-1 is involved in the pathogenesis of PDR.
  • ||||||||||  OTX-008 / Merck (MSD)
    Galectin-1 Inhibition Sensitizes Radiation Treatment in a Pre-clinical model of Glioblastoma (Ballroom Lawn) -  Oct 29, 2019 - Abstract #SNO2019SNO_449;    
    OTX008 treatment plus radiation was associated with downregulation of Gal1 and Ki67 in treated tumors, as well as decreased microvessel density and VEGFR2 expression. Finally, combination studies showed OTX008 synergy with radiation therapies, principally when OTX008 was administered first.  This study provides insights of Gal-1inhibitory effects of OTX008 and its enhancement of the efficacy of radiotherapy in mouse models of GB suggest that further studies are warranted.
  • ||||||||||  OTX-008 / Merck (MSD)
    Journal:  Galectin-1 is a new fibrosis protein in type 1 and type 2 diabetes. (Pubmed Central) -  Jul 11, 2019   
    In summary, Gal-1 is highly expressed in kidneys of type 1 and 2 diabetic mice, and AP4 is a major transcription factor that activates Gal-1 under hyperglycemia. Inhibition of Gal-1 by OTX-008 blocks activation of Akt and prevents accumulation of Gal-1, suggesting a novel role of Gal-1 inhibitor as a possible therapeutic target to treat renal fibrosis in diabetes.-Al-Obaidi, N., Mohan, S., Liang, S., Zhao, Z., Nayak, B. K., Li, B., Sriramarao, P., Habib, S. L. Galectin-1 is a new fibrosis protein in type 1 and type 2 diabetes.