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ActRIIB inhibitor

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  • Project profile
    Project name: ActRIIB inhibitor
    Indications: Cancer cachexia
    Research phase: Pre-clinical
    Cooperation demands: License-out or co-development
  • Highlights

    1. MoA:


    When tumor cachexia occurs, the TGF-β family ligands in the blood activate ActRIIB (activin II receptor B) on the skeletal muscle cell membrane, activate various forms of protein degradation, and inhibit protein synthesis;


    ActRIIB inhibitors can significantly inhibit ActRIIB activity, effectively block the MSTN/ActRIIB signaling pathway, reduce muscle atrophy and improve grip, thus alleviate symptoms of tumor cachexia.


    Excellent preclinical results


    Highlight:


    1. Great ActRIIB kinase inhibition ability (nM level);


    2. Effectively alleviate atrophy of C2C12 myotubes induced by culture supernatant of C26 and LLC tumor cells;


    3. Effectively alleviate atrophy of C2C12 myotubes induced by TGF-β family ligands MSTN (GDF-8) and TGF-β1;


    4. PK test indicates good oral absorption;


    5. Effectively alleviate weight loss and muscle atrophy in C26 tumor bearing mice with cachexia, restore muscle strength in mice, and improve symptoms of cachexia.


  • Project Introduction

    1. Asset type: ActRIIB inhibitor

    2. Indication: Cancer cachexia

    3. Modality:Small molecule

    4. Research:Pre-clinical

    5. Demands: License-out or co-development

    Highlight:

    1. Great ActRIIB kinase inhibition ability (nM level);

    2. Effectively alleviate atrophy of C2C12 myotubes induced by culture supernatant of C26 and LLC tumor cells;

    3. Effectively alleviate atrophy of C2C12 myotubes induced by TGF-β family ligands MSTN (GDF-8) and TGF-β1;

    4. PK test indicates good oral absorption;

    5. Effectively alleviate weight loss and muscle atrophy in C26 tumor bearing mice with cachexia, restore muscle strength in mice, and improve symptoms of cachexia.

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