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DRUG CLASS:

Galectin inhibitor

4ms
Davanat-Mimetic Galactomannan and Its Sulfated Derivative: Structure and Antitumor Effects against Melanoma. (PubMed, Biomacromolecules)
Although in vitro lymphocyte proliferation was not observed, CD3+ cells increased in the metastatic lungs. These results suggest GGH and GGHS as immunostimulatory agents, with GGH as potential melanoma adjuvant therapy.
Journal
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LGALS1 (Galectin 1)
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Davanat (galactomannan)
6ms
The Immunomodulatory Role of Galectin-1 in the Tumour Microenvironment and Strategies for Therapeutic Applications. (PubMed, Cancers (Basel))
Approaches such as OTX008, anti-Gal1 monoclonal antibodies, and Gal1-targeted vaccines have demonstrated the ability to downregulate tumour progression by inhibiting Gal1 activity. These findings highlight the therapeutic promise of Gal1 not only as a novel target for cancer therapy but also as a potential prognostic biomarker, offering opportunities for the development of more effective and less toxic treatment strategies.
Review • Journal
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FASLG (Fas ligand) • LGALS1 (Galectin 1)
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OTX-008
7ms
Galectin-1: An important regulator in myeloid differentiation and acute myeloid leukemia as well as a promising prognostic indicator and therapeutic target. (PubMed, Int Immunopharmacol)
Treatment with OTX008, an LGALS1 inhibitor, markedly diminished the viability of primary malignant bone marrow cells from AML patients. Notably, LGALS1 expression was significantly reduced exclusively in AML-M5 patients after treatment, which may be due to its higher expression in AML-M5 subtype compared to other FAB subtypes. In summary, our findings indicate that LGALS1 could serve as an independent prognostic risk factor and a promising therapeutic target in AML, providing novel insights into AML pathogenesis and laying the foundation for the development of new therapeutic strategies.
Journal
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LGALS1 (Galectin 1)
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OTX-008
over1year
Nematode Galectin Inhibits Basophilic Leukaemia RBL-2H3 Cells Apoptosis in IgE-Mediated Activation. (PubMed, Int J Mol Sci)
Tci-gal-1 modulates apoptosis, degranulation, and production of cytokines by activated RBL-2H3 cells without detectable influence on gene transcription. This parasite protein is crucial for modulation of the protective immune response and the inhibition of chronic inflammation driven by mast cell activity.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • FASLG (Fas ligand) • IL2 (Interleukin 2) • LGALS1 (Galectin 1) • IL10 (Interleukin 10) • IL13 (Interleukin 13)
over1year
A Quantitative Human Red Blood Cell Agglutination Assay for Characterisation of Galectin Inhibitors. (PubMed, Int J Mol Sci)
Quantification of hemagglutination was shown to be optimal using U-bottom plates imaged and analysed with FIJI ImageJ rather than flat-bottom plates read for absorbance on an optical density plate reader. Galectin-3-induced red blood cell agglutination efficacy increased significantly from blood group O to A to B. However, for both the galectin-1 monomer and concatemer, a more comparable effect was observed between blood group B and O, but with more potent effects than in blood group A. Inhibition assays for both galectin-3 and galectin-1 induced-hemagglutination were able to demonstrate clear concentration responses and expected selectivity profiles for a set of small-molecule glycomimetics, confirming the historical profiles obtained in biochemical binding and functional cellular assays.
Journal
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LGALS1 (Galectin 1)
over2years
Enrollment change • Trial withdrawal • Metastases
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CD8 (cluster of differentiation 8) • IL2RA (Interleukin 2 receptor, alpha) • CCR7 (Chemokine (C-C motif) receptor 7) • CD27 (CD27 Molecule) • LGALS3 (Galectin 3) • FAS (Fas cell surface death receptor) • FOXP3 (Forkhead Box P3) • ISG20 (Interferon Stimulated Exonuclease Gene 20)
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Keytruda (pembrolizumab) • belapectin (GR-MD-02)
over2years
GR-MD-02 Plus Pembrolizumab in Melanoma, Non-small Cell Lung Cancer, and Squamous Cell Head and Neck Cancer Patients (clinicaltrials.gov)
P1, N=36, Completed, Providence Health & Services | Active, not recruiting --> Completed | N=22 --> 36 | Trial completion date: May 2025 --> Oct 2022
Trial completion • Enrollment change • Trial completion date • Metastases
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BRAF (B-raf proto-oncogene) • CD4 (CD4 Molecule)
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Keytruda (pembrolizumab) • belapectin (GR-MD-02)
over2years
GR-MD-02 + Pembrolizumab Versus Pembrolizumab Monotherapy in Melanoma and Squamous Cell Head and Neck Cancer Patients (clinicaltrials.gov)
P2, N=92, Suspended, Providence Health & Services | Trial completion date: Mar 2031 --> Jul 2031 | Trial primary completion date: Mar 2027 --> Jul 2027
Trial completion date • Trial primary completion date • Metastases
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CD8 (cluster of differentiation 8) • IL2RA (Interleukin 2 receptor, alpha) • CCR7 (Chemokine (C-C motif) receptor 7) • CD27 (CD27 Molecule) • LGALS3 (Galectin 3) • FAS (Fas cell surface death receptor) • FOXP3 (Forkhead Box P3) • ISG20 (Interferon Stimulated Exonuclease Gene 20)
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Keytruda (pembrolizumab) • belapectin (GR-MD-02)
almost3years
Galectin-9 and PD-L1 antibody blockade combination therapy inhibits tumour progression in pancreatic cancer. (PubMed, Immunotherapy)
Furthermore, in a murine model of PDAC, combined anti-galectin-9 and anti-PD-L1 treatment was associated with a greater decrease in tumor growth compared with treatment with either antibody therapy alone. Anti-PD-L1 antibody treatment for PDAC patients may be enhanced by inhibiting galectin-9.
Journal • Combination therapy • PD(L)-1 Biomarker • IO biomarker
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LGALS9 (Galectin 9)