Acoramidis (AG10) is a potent and selective kinetic stabilizer and ligand of transthyretin (TTR) ligand with apparent binding constant (Kapp) of 193 nM for WT-TTR.
AG10 binds TTR with negative cooperativity (Kd1 = 4.8 nM, Kd2 = 314 nM),  V122I-TTR with Kd1 of 6.2 ± 2.0 nM and a Kd2 of 139 ± 80 nM.
AG10 is a highly effective and selective stabilizer of WT and V122I-TTR.
AG10 also prevents the dissociation of V122I-TTR in serum obtained from patients with FAC and protects human cardiomyocytes from TTR amyloid toxicity very effectively.
AG10 binds V122I-TTR with high affinity and to kinetically stabilize the tetramer, G10 is significantly better than tafamidis in inhibiting the amyloidogenesis of WT and V122I-TTR.
AG10 prevents dissociation of V122I-TTR in serum samples obtained from patients with familial amyloid cardiomyopathy.
AG10 stabilizes V122I- and WT-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum.