TNIK
Rentosertib:
Treating Fibrotic diseases
Treating Fibrotic diseases
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Current Stage:
Phase IIa Completed -
Wholly-owned and Available for Licensing
Indication
Idiopathic pulmonary fibrosis (IPF) is a type of chronic scarring lung disease characterized by a progressive and irreversible decline in lung function affecting around 5 million people globally. IPF carries a poor prognosis with a median survival of 3 to 4 years and represents a significant unmet medical need. Nintedanib and Pirfenidone are two drugs approved for treatment. However, their efficacy is moderate, and they do not halt or reverse the disease. Moreover, the side effects are frequent and include nausea, diarrhea, and liver damage risk leading to high discontinuation rate.
About Rentosertib
Rentosertib is a potentially first-in-class small molecule developed utilizing generative AI. By inhibiting TNIK, Rentosertib aims to halt or reverse fibrotic processes, offering a disease-modifying treatment for patients with IPF.
Encouraging clinical data showed that patients receiving 60 mg QD Rentosertib experienced the greatest mean improvement in lung function, as measured by forced vital capacity (FVC), with a mean change of +98.4 mL, compared to a mean decline of -20.3 mL in the placebo group.
Encouraging clinical data showed that patients receiving 60 mg QD Rentosertib experienced the greatest mean improvement in lung function, as measured by forced vital capacity (FVC), with a mean change of +98.4 mL, compared to a mean decline of -20.3 mL in the placebo group.
TNIK+Rentosertib Mechanism of Action
Rentosertib: Small-molecule drug candidate designed to treat fibrosis-related indications by inhibiting the TRAF2- and NCK-interacting kinase (TNIK), a newly identified anti-fibrotic target discovered through Insilico Medicine’s Pharma.AI platform. Targeting TNIK, INS018_055 Inhibits:
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TGF-β dependent fibrogenesis, and EMT (epithelial mesenchymal transition) /FMT (fibroblast-to-myofibroblast transition).
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NF-kB signal pathway leading to anti-inflammation.
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Downstream genes/interacting partners of YAP/TAZ, which are reported to promote fibrosis.
Assays Completed
Enzymatic
Toxicology studies
In vitro cell-based
Developability/CMC
In vitro ADMET studies
In vivo efficacy studies
In vivo PK studies
In vivo PK-PD
In vivo efficacy studies with single agent
Bleomycin and combo study with Nintedanib & Pirfenidone
Phase 1 Clinical Stage Development
Phase 1 Clinical Stage Development
