Curated reading path
Follow the real development paths of Enlicitide and ICOTYDE from screening hits and structural optimization to oral exposure and clinical translation.
11 published articles in recommended order
Peptide 1185 is already stable and highly engineered, so why continue to modify a small number of residues? This article uses real patent SAR to distinguish experimental results from structural interpretation.
icotrokinra still has difficulty crossing the intestinal epithelium, but its gastrointestinal stability, 200 mg dose, and picomolar-level potency allow even limited absorption to generate effective systemic exposure.
From first-in-human exposure to FRONTIER and ICONIC, icotrokinra ultimately demonstrated that an oral cyclic peptide of nearly 1900 Da can translate limited absorption into clinical efficacy for patients and become an FDA-approved drug.
Compare the targets, discovery technologies, molecular optimization, and oral delivery strategies of the two oral cyclic peptide drugs Icotrokinra and Enlicitide to understand how they are turning the drug space between traditional small molecules and antibodies into an actively developable direction.
Starting from the approval of two oral cyclic peptides, this article analyzes R&D opportunities for cyclic peptide therapeutics in antibody replacement, targeted radiopharmaceuticals, chronic diseases, intracellular protein–protein interactions, and targeted protein degradation.