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. It is developed by Galecto Biotech, which is testing the molecule to see if it reduces decompensated cirrhosis and resistance to checkpoint inhibitors (a type of anti-cancer drug).

References

↑ 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.