Selvigaltin

Selvigaltin
Clinical data
Other names	GB1211
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name (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	122443488;
IUPHAR/BPS	11202;
ChemSpider	115010772;
UNII	94EN2E6BLW;
KEGG	D12763;
ChEMBL	ChEMBL5182222;
Chemical and physical data
Formula	C19H16BrF3N4O4S
Molar mass	533.32 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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]

References[edit]

^ 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.
^ "New Agent Shows Promise in Decompensated Cirrhosis". www.gastroendonews.com. Retrieved 3 December 2023.
^ 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.
^ 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.

[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.

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