Selvigaltin

Last updated
Selvigaltin
Selvigaltin.svg
Clinical data
Other namesGB1211
Legal status
Legal status
  • Investigational
Identifiers
  • (2R,3R,4S,5R,6R)-2-(5-Bromopyridin-3-yl)sulfanyl-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxane-3,5-diol
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C19H16BrF3N4O4S
Molar mass 533.32 g·mol−1
3D model (JSmol)
  • C1=C(C=C(C(=C1F)F)F)C2=CN(N=N2)[C@H]3[C@H]([C@H](O[C@@H]([C@@H]3O)SC4=CC(=CN=C4)Br)CO)O
  • InChI=1S/C19H16BrF3N4O4S/c20-9-3-10(5-24-4-9)32-19-18(30)16(17(29)14(7-28)31-19)27-6-13(25-26-27)8-1-11(21)15(23)12(22)2-8/h1-6,14,16-19,28-30H,7H2/t14-,16+,17+,18-,19-/m1/s1
  • Key:FNCLKJPMEFPXOR-QFACEVIFSA-N

Selvigaltin (GB1211) is the first small-molecule, orally delivered galectin-3 inhibitor to be discovered. [1] It is developed by Galecto Biotech, which is testing the molecule to see if it reduces decompensated cirrhosis [2] and resistance to checkpoint inhibitors (a type of anti-cancer drug). [3] [4]

Related Research Articles

<span class="mw-page-title-main">Cancer immunotherapy</span> Artificial stimulation of the immune system to treat cancer

Cancer immunotherapy (immuno-oncotherapy) is the stimulation of the immune system to treat cancer, improving on the immune system's natural ability to fight the disease. It is an application of the fundamental research of cancer immunology and a growing subspecialty of oncology.

<span class="mw-page-title-main">Tremelimumab</span> Monoclonal antibody

Tremelimumab, sold under the brand name Imjudo, is a fully human monoclonal antibody used for the treatment of hepatocellular carcinoma. Tremelimumab is designed to attach to and block CTLA-4, a protein that controls the activity of T cells, which are part of the immune system.

<span class="mw-page-title-main">Cediranib</span> Chemical compound

Cediranib is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.

<span class="mw-page-title-main">PDCD1LG2</span> Protein-coding gene in the species Homo sapiens

Programmed cell death 1 ligand 2 is a protein that in humans is encoded by the PDCD1LG2 gene. PDCD1LG2 has also been designated as CD273. PDCD1LG2 is an immune checkpoint receptor ligand which plays a role in negative regulation of the adaptive immune response. PD-L2 is one of two known ligands for Programmed cell death protein 1 (PD-1).

Treatment of lung cancer refers to the use of medical therapies, such as surgery, radiation, chemotherapy, immunotherapy, percutaneous ablation, and palliative care, alone or in combination, in an attempt to cure or lessen the adverse impact of malignant neoplasms originating in lung tissue.

<span class="mw-page-title-main">BI 811283</span> Chemical compound

BI 811283 is a small molecule inhibitor of the Aurora B kinase protein being developed by Boehringer Ingelheim for use as an anti-cancer agent. BI 811283 is currently in the early stages of clinical development and is undergoing first in human trials in patients with solid tumors and acute myeloid leukemia.

<span class="mw-page-title-main">TIGIT</span> Protein-coding gene in the species Homo sapiens

TIGIT is an immune receptor present on some T cells and natural killer cells (NK). It is also identified as WUCAM and Vstm3. TIGIT could bind to CD155 (PVR) on dendritic cells (DCs), macrophages, etc. with high affinity, and also to CD112 (PVRL2) with lower affinity.

Galecto Biotech is a biotechnology company that develops small molecules for the treatment of severe diseases, including fibrosis, cancer and inflammation. The company was founded in 2011 by leading galectin scientists and biotech executives from Sweden, United Kingdom, and Denmark. The company today is incorporated in the U.S., and has its operating headquarters in Copenhagen, Denmark.

<span class="mw-page-title-main">Atezolizumab</span> Monoclonal anti-PD-L1 antibody

Atezolizumab, sold under the brand name Tecentriq, is a monoclonal antibody medication used to treat urothelial carcinoma, non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), hepatocellular carcinoma and alveolar soft part sarcoma, but discontinued for use in triple-negative breast cancer (TNBC). It is a fully humanized, engineered monoclonal antibody of IgG1 isotype against the protein programmed cell death-ligand 1 (PD-L1).

<span class="mw-page-title-main">PD-1 and PD-L1 inhibitors</span> Class of anticancer drugs

PD-1 inhibitors and PD-L1 inhibitors are a group of checkpoint inhibitor anticancer drugs that block the activity of PD-1 and PDL1 immune checkpoint proteins present on the surface of cells. Immune checkpoint inhibitors are emerging as a front-line treatment for several types of cancer.

<span class="mw-page-title-main">VISTA (protein)</span> Protein-coding gene in the species Homo sapiens

V-domain Ig suppressor of T cell activation (VISTA) is a type I transmembrane protein that functions as an immune checkpoint and is encoded by the C10orf54 gene.

Checkpoint inhibitor therapy is a form of cancer immunotherapy. The therapy targets immune checkpoints, key regulators of the immune system that when stimulated can dampen the immune response to an immunologic stimulus. Some cancers can protect themselves from attack by stimulating immune checkpoint targets. Checkpoint therapy can block inhibitory checkpoints, restoring immune system function. The first anti-cancer drug targeting an immune checkpoint was ipilimumab, a CTLA4 blocker approved in the United States in 2011.

EPI-7386 is an N-terminal domain antiandrogen, or antagonist of the N-terminal domain (NTD) of the androgen receptor (AR), which is under development for the treatment of prostate cancer. The compound was developed as a successor of previous drugs in the EPI series such as EPI-001, ralaniten (EPI-002), and ralaniten acetate (EPI-506). EPI-7386 shows 20-fold higher antiandrogenic potency than ralaniten in vitro (IC50 = 535 nM vs. 9,580 nM, respectively), as well as greater stability in human hepatocytes. It is planned to enter phase I clinical trials in 2020.

Roy S. Herbst is an American oncologist who is the Ensign Professor of Medicine, Professor of Pharmacology, Chief of Medical Oncology, and Associate Director for Translational Research at Yale Cancer Center and Yale School of Medicine in New Haven, Connecticut.

Belvarafenib is a small molecule RAF dimer inhibitor which shows anti-tumor clinical activity in cancer patients with BRAFV600E- and NRAS- mutations.

Julie Renee Brahmer is an American thoracic oncologist. She is the co-director of the Upper Aerodigestive Department within the Bloomberg~Kimmel Institute for Cancer Immunotherapy at Johns Hopkins University and the Marilyn Meyerhoff Professor in Thoracic Oncology.

<span class="mw-page-title-main">Resigratinib</span> Chemical compound

Resigratinib (KIN-3248) is an experimental anticancer medication which acts as a fibroblast growth factor receptor inhibitor (FGFRi) and is in early stage human clinical trials.

Favezelimab/pembrolizumab is a fixed-dose combination of two monoclonal antibodies developed by Merck to treat various cancers.

Favezelimab (MK-4280) is an experimental anti-cancer monoclonal antibody developed by Merck. It is being tested by itself and in a fixed-dose combination with pembrolizumab.

<span class="mw-page-title-main">Opnurasib</span> Chemical compound

Opnurasib (JDQ-443) is a small-molecule covalent KRASG12C inhibitor developed for non-small-cell lung cancer.

References

  1. Aslanis, Vassilios; Slack, Robert J.; MacKinnon, Alison C.; McClinton, Catherine; Tantawi, Susan; Gravelle, Lise; Nilsson, Ulf J.; Leffler, Hakon; Brooks, Ashley; Khindri, Sanjeev K.; Marshall, Richard P.; Pedersen, Anders; Schambye, Hans; Zetterberg, Fredrik (March 2023). "Safety and pharmacokinetics of GB1211, an oral galectin-3 inhibitor: a single- and multiple-dose first-in-human study in healthy participants". Cancer Chemotherapy and Pharmacology. 91 (3): 267–280. doi: 10.1007/s00280-023-04513-y . ISSN   1432-0843. PMC   10010643 . PMID   36914828.
  2. "New Agent Shows Promise in Decompensated Cirrhosis". www.gastroendonews.com. Retrieved 3 December 2023.
  3. Ghiringhelli, François; Doucet, Ludovic; Barre, Patricia; Pichon, Eric; Ponce Aix, Santiago; Juan-Vidal, Oscar; Carcereny, Enric; Sethi, Tariq; Lindmark, Bertil; MacKinnon, Alison; Aslanis, Vassilios; Rajiwate, Zahir; Basse, Linda (1 June 2022). "GALLANT-1: Galectin-3 (Gal-3) inhibitor GB1211 plus atezolizumab (atezo) in patients with non–small cell lung cancer (NSCLC)—A randomized, double-blind trial". Journal of Clinical Oncology. 40 (16_suppl): TPS9152. doi:10.1200/JCO.2022.40.16_suppl.TPS9152. S2CID   249450443.
  4. Mabbitt, Joseph; Roper, James A.; Slack, Robert John (1 June 2022). "Resistance to anti-PD-1/anti-PD-L1: GB1211 reverses galectin-3 induced blockade of pembrolizumab and atezolizumab binding to PD-1/PD-L1". Journal of Clinical Oncology. 40 (16_suppl): 2607. doi:10.1200/JCO.2022.40.16_suppl.2607.