Drug intelligence / Profile preview

RAP-1332

Development stage
Preclinical
Lead developer
Merck
Modality
Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes
Administration
Subcutaneous
01

Overview

RAP-1332 is a preclinical-stage homodimeric recombinant fusion protein (ligand trap) developed by Acceleron Pharma (now Merck & Co.) that selectively binds and neutralizes transforming growth factor beta 1 (TGF-β1) and transforming growth factor beta 3 (TGF-β3). It serves as a murine surrogate/orthologue of the human therapeutic candidate ACE-1332. Structurally, RAP-1332 consists of the extracellular domain of murine TGF-beta receptor type II (TGFβRII) fused to a murine IgG2a Fc domain. By sequestering TGF-β1 and TGF-β3, RAP-1332 prevents ligand-receptor engagement and downstream SMAD2/3 signaling, thereby blocking epithelial-to-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT). It has been evaluated in preclinical mouse models of chronic biliary injury, primary sclerosing cholangitis (PSC)-like biliary injury, liver fibrosis, myelofibrosis, and systemic sclerosis-associated interstitial lung disease (SSc-ILD).

Other names
murine TGF-beta trap RAP-1332murine TGFβRII-Fc
02

Targets

TGFB1 (Transforming growth factor Beta-1 proprotein)TGFB3 (Transforming growth factor beta 3)

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