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Its oral bioavailability is achieved by incorporating the absorption enhancer SNAC (Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate), which works through two mechanisms: (1) temporarily raising the local pH in the stomach to reduce pepsin-induced degradation of the peptide drug, and (2) forming hydrophobic ion pairs (HIP) with the peptide drug, improving its membrane permeability
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Reddiar SB, De Veer M, Paterson BM, Sepehrizadeh T, Wai DCC, Csoti A et al (2023) A biodistribution study of the radiolabeled K V 1.3-blocking peptide DOTA-HsTX1[R14A] demonstrates brain uptake in a mouse model of neuroinflammation