TFR1 Bicycle

TFR1 Bicycle is a synthetic, small bicyclic peptide developed to bind the human transferrin receptor 1 (TfR1) with high affinity and specificity. These molecules, produced by Bicycle Therapeutics, are ∼2-kDa in size and consist of short, fully synthetic peptide loops constrained by a small-molecule scaffold, forming a stable bicyclic structure. The principal mechanism is targeted delivery: when conjugated to antisense oligonucleotides (ASOs) or siRNAs, TFR1 Bicycles enhance the uptake and potency of these therapeutics in skeletal and cardiac muscle by utilizing TfR1-mediated endocytosis on target tissues. The approach offers several advantages, including high selectivity, non-competitive binding that does not impair TfR1’s natural function, chemical stability, and amenability to diverse molecular payloads. Primary indications under development include neuromuscular and cardiac diseases, with exploration in central nervous system (CNS) disorders and dementia. Bicycle Therapeutics retains rights for non-oligonucleotide applications, and partners (such as Ionis Pharmaceuticals) are pursuing oligonucleotide conjugate therapeutics using this technology[1][2][3][5][6].

Other names

transferrin receptor 1 BicycleTfR1-targeting Bicycle peptideTfR-1-targeting Bicycle peptideTfR 1-targeting Bicycle peptideBCY17901BCY-17901BCY 17901