GB0139
inhaled galectin-3 inhibitor Ph. II for IPF + Ph. Ib/IIa for COVID-19 pneumonitis synthetic galactoside derivative medRxiv, January 10, 2022 Galecto, Inc., Copenhagen, DE
Other molecules you may be interested in
tenapanor
Context. Tenapanor (Ardelyx) is an oral, first-in-class Na + /H + exchanger isoform 3 (NHE3) inhibitor approved by the FDA for irritable bowel syndrome with constipation (IBS-C) in adults. NHE3 is expressed predominantly in the gut and kidney and its role as a key mediator of sodium and water homeostasis makes the protein an ideal target for [...]
resmetirom
On Mar. 14th, 2024, resmetirom (REZDIFFRA™) became the first and only medicine approved by the FDA for the treatment of NASH (non-alcoholic steatohepatitis, aka MASH). Resmetirom, an oral, liver-targeting, once-daily THR-β-selective agonist originally discovered at Roche Nutley, was first highlighted as a Molecule of the Month in Dec. 2022. Now, with the FDA’s accelerated approval, this 2023 Molecule of the Year nominee reflects a historic milestone for liver drug discovery. This article reviews how the molecule works, how it was discovered, and why it’s a big deal.
TAK-906
The Altos Therapeutics /Takeda D2/D3 receptor antagonist, TAK-906 , is a peripherally-restricted, non-BBB penetrant molecule, targeting the stomach and vomiting center in the area postrema to treat gastroparesis. Gastroparesis is a chronic condition characterized by delayed gastric emptying, resulting in nausea, vomiting, pain, and anorexia [...]
difamilast
PDE4 inhibitors have shown promise in a range of pulmonary, dermatological and neurological diseases, but have been hampered by side effects including emesis and diarrhea . Difamilast , originated by Otsuka , recently approved for the treatment of atopic dermatitis [...]
ziritaxestat
Ziretaxestat, an oral autotaxin (ATX) inhibitor originated by Galapagos, once garnered excitement as the first molecule to complete a Ph. III clinical program in idiopathic pulmonary fibrosis since the approvals of nintedanib and pirfenidone. Following the disappointing clinical data and discontinuation of the molecule, this annotation revisits ziritaxestat in the context of other inhibitors, recaps the therapeutic hypothesis and how it was discovered, summarizes notable molecular properties for drug discovery scientists, and discusses what happened and what’s next.
