ACE-031
Myostatin Inhibitor | Experimental Muscle Growth
ACE-031 is a soluble form of the activin type IIB receptor (ActRIIB) fused to an IgG1 Fc domain. It functions as a decoy receptor, binding and neutralizing myostatin and other TGF-beta superfamily members that normally limit muscle growth. Originally developed by Acceleron Pharma for Duchenne muscular dystrophy (DMD), ACE-031 reached Phase 2 clinical trials before development was halted due to vascular side effects including nosebleeds and telangiectasia. In healthy volunteers, a single dose produced significant increases in lean mass and reductions in fat mass within 29 days.
Moleküler Gösterim
PubChem 2D yapı diyagramı
Referans Flakon
Referans illüstrasyonu — ürün listesi değildir
Etki Mekanizması
ACE-031 acts as a ligand trap for members of the TGF-beta superfamily. By mimicking the extracellular domain of the ActRIIB receptor, it intercepts myostatin (GDF-8), activin A, activin B, and GDF-11 before they can bind cell-surface receptors and activate Smad2/3 signaling. Blocking this pathway removes the natural brake on muscle protein synthesis and satellite cell proliferation, resulting in rapid skeletal muscle hypertrophy. The Fc fusion domain extends circulating half-life through FcRn-mediated recycling and provides bivalent ligand binding.
ACE-031 is a soluble form of the activin type IIB receptor (ActRIIB) fused to an IgG1 Fc domain. It functions as a decoy receptor, binding and neutralizing myostatin and other TGF-beta superfamily members that normally limit muscle growth. Originally developed by Acceleron Pharma for Duchenne muscular dystrophy (DMD), ACE-031 reached Phase 2 clinical trials before development was halted due to vascular side effects including nosebleeds and telangiectasia. In healthy volunteers, a single dose produced significant increases in lean mass and reductions in fat mass within 29 days.
Moleküler Veri
Araştırma Endikasyonları
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Doz Protokolleri
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| Hedef | Doz | Sıklık | Yol |
|---|---|---|---|
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Etkileşimler
Follistatin
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Kaynaklar
- A soluble activin receptor type IIB (ACE-031) increases lean body mass and muscle strength in healthy postmenopausal women — Attie KM, Borgstein NG, Yang Y, Condon CH, Wilson DM, Pearsall AE, Kumar R, Willins DA, Seehra JS, Sherman ML
- A phase 2 trial of ACE-031, a soluble activin receptor type IIB, in boys with Duchenne muscular dystrophy — Campbell C, McMillan HJ, Mah JK, Tarnopolsky M, Selby K, McClure T, Wilson DM, Sherman ML, Bhatt SA, Trachtenberg FL, Kunkel LM, Bhatt RS
- Pharmacokinetic, pharmacodynamic, and safety results from a first-in-human study of ACE-031, a novel activin receptor type IIB/Fc fusion protein — Bhatt RS, Goss A, Wilson DM, Borgstein NG, Sherman ML
- Myostatin inhibition in health and disease — Lee SJ