Synonyms: GB-0139 | GB0139 | TD-139 | TD139
Compound class:
Synthetic organic
Comment: Olitigaltin (GB0139) is a galectin-3 inhibitor [3] that is designed for inhalation, and is intended as a therapy for fibrotic lung conditions such as idiopathic pulmonary fibrosis (IPF) [1]. In the fibrotic setting, blocking galectin-3's biological function is predicted to combat the enhanced TGF-β receptor-mediated macrophage differentiation and myofibroblast activation that drives pathological fibrotic changes [2-4].
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References |
1. Hirani N, MacKinnon AC, Nicol L, Ford P, Schambye H, Pedersen A, Nilsson UJ, Leffler H, Sethi T, Tantawi S et al.. (2021)
Target inhibition of galectin-3 by inhaled TD139 in patients with idiopathic pulmonary fibrosis. Eur Respir J, 57 (5). DOI: 10.1183/13993003.02559-2020 [PMID:33214209] |
2. MacKinnon AC, Farnworth SL, Hodkinson PS, Henderson NC, Atkinson KM, Leffler H, Nilsson UJ, Haslett C, Forbes SJ, Sethi T. (2008)
Regulation of alternative macrophage activation by galectin-3. J Immunol, 180 (4): 2650-8. [PMID:18250477] |
3. Mackinnon AC, Gibbons MA, Farnworth SL, Leffler H, Nilsson UJ, Delaine T, Simpson AJ, Forbes SJ, Hirani N, Gauldie J et al.. (2012)
Regulation of transforming growth factor-β1-driven lung fibrosis by galectin-3. Am J Respir Crit Care Med, 185 (5): 537-46. [PMID:22095546] |
4. Partridge EA, Le Roy C, Di Guglielmo GM, Pawling J, Cheung P, Granovsky M, Nabi IR, Wrana JL, Dennis JW. (2004)
Regulation of cytokine receptors by Golgi N-glycan processing and endocytosis. Science, 306 (5693): 120-4. [PMID:15459394] |
5. St-Gelais J, Denavit V, Giguère D. (2020)
Efficient synthesis of a galectin inhibitor clinical candidate (TD139) using a Payne rearrangement/azidation reaction cascade. Org Biomol Chem, 18 (20): 3903-3907. [PMID:32400847] |