Tankyrase inhibition for therapy of lung fibrosis
Researchers at Oslo University Hospital (OUH) have developed OM-247, a first-in-class small-molecule drug candidate targeting tankyrase (TNKS) inhibition. This novel therapeutic approach addresses idiopathic pulmonary fibrosis (IPF) by modulating the WNT/YAP signaling pathways, which are central drivers of fibrosis.
Business Opportunity
OM-247 shows potent anti-fibrotic activity in vitro, ex vivo (human precision-cut lung slices), and in validated rodent models. The compound exhibits favorable pharmacological and drug-like properties, positioning it as a promising candidate for clinical development. Currently, there are no TNKS inhibitors in clinical trials for lung fibrosis—an area of high unmet medical need. IPF is a progressive and fatal form of lung fibrosis, with a median survival of only three years after diagnosis. Moreover, patients recovering from severe viral lung infections, including COVID-19, are at increased risk of developing fibrosis, highlighting the urgent need for more effective therapies.
Technology Description
- OM-247 demonstrates favorable ADME properties and oral/inhalation PK profiles.
- Supported by a robust preclinical proof-of-concept dataset, including efficacy in vitro, ex vivo (human lung tissue), and in vivo in mouse and rat models.
- Current IPF therapies (Pirfenidone and Nintedanib) offer only modest efficacy and are associated with significant adverse effects.
- Aberrant WNT/β-catenin and YAP signaling are central to fibrosis progression.
- OM-247 is a highly potent and selective TNKS1/2 inhibitor, directly modulating these pathways.
- No TNKS/WNT/YAP inhibitors are currently in clinical development for fibrotic diseases—providing a clear first-mover advantage.
Fig. 1: Model for TNKS inhibitor anti-fibrotic mechanism of action.
Intellectual Property
WO2019/243822 published 29.12.2019 and WO2022/008896 published 13.01.2022.
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expand_more mode_edit Authors (2)Aina Haugen RengmarkKen Rosendal
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expand_more library_books References (3)
- Brinch SA, Amundsen-Isaksen E, Espada S, et al. (2022 Apr 20), The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models., Cancer Res Commun., 2(4), 233-245
- Leenders RGG, Brinch SA, Sowa ST, et al. (2021), Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II., J Med Chem, 64(24), 17936-17949
- Waaler J, Leenders RGG, Sowa ST, et al. (2020), Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor., J Med Chem, 63(13), 6834-6846
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expand_more cloud_download Supporting documents (1)Product brochureTankyrase inhibition for therapy of lung fibrosis.pdf