First-in-Class, myofibroblast-targeted DR5 agonist for fibrosis
Mechanism of Action
Engineered, trimeric rhTRAIL
- · Fibrosis Represents an Unmet Medical Need
- - Can occur in any organ, leads to excessive scar tissue accumulation and organ damage
- - Poor medical outcomes, lack of effective treatments
- - Potential in orphan diseases and larger indication
TLY012 selectively blocks normal fibroblasts activation and induces apoptosis in myofibroblasts in fibrotic tissues.
- · MFBs (a.k.a. activated fibroblasts/stellate cells) cause activation of multiple pathways that lead to scar tissue formation
- · Current investigational drugs target only single downstream pathways not the MFBs, the originator of fibrosis
- · TLY012, a PEGylated recombinant human TRAIL protein, binds upregulated Death Receptor 5 (DR5) on MFBs and effectively shuts down fibrotic pathways and inactivates MFBs.
- · TLY012 is a potential first in class treatment for various fibrotic diseases
- - TLY012 selectively blocks and/or eradicates myofibroblasts (activated fibroblasts/stellate cells) in fibrotic regions
- - TLY012 reverses existing fibrosis - validated in various animal models with liver, skin, and pancreatic fibrosis
- · Nature Communications, volume 10, Article number: 1128 (2019)
- · Hepatology, Volume64, Issue 1, 209-223