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RKER-206 is a novel, modified activin receptor type IIB (ActRIIB) ligand trap being developed by Keros Therapeutics. It is designed to selectively bind and inhibit specific transforming growth factor-beta (TGF-β) superfamily ligands, including activin A, growth and differentiation factor 8 (GDF8, or myostatin), and GDF11, which are key negative regulators of bone and muscle remodeling. By trapping these ligands, RKER-206 prevents their downstream SMAD2/3 signaling, thereby promoting bone formation and reversing bone loss. In preclinical studies, RKER-206 has demonstrated the ability to reverse bone loss and improve trabecular bone microarchitecture in mouse models of estrogen-deficient osteoporosis, highlighting its therapeutic potential for postmenopausal osteoporosis.
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