Peptide with low content of d-CYS 38 epimer
A solid-phase peptide synthesis method controls epimerization to produce Kv1.3 inhibitors with high purity and specificity, addressing the challenge of peptide synthesis and ensuring effective clinical trial candidates.
Patent Information
- Application Number
- PCT/EP2025/081740
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-11-04
- Filing Date
- 2025-11-04
- Publication Date
- 2026-05-07
AI Technical Summary
The synthesis of peptides, particularly those inhibiting the Kv1.3 channel, is challenging due to epimerization during solid-phase peptide synthesis, which affects the conformation and bioactivity, making it difficult to achieve high purity and specificity for clinical trials.
A method for preparing Kv1.3 channel inhibitors with high purity using solid-phase peptide synthesis (SPPS) by controlling the epimerization of Cys38, ensuring at least 95% purity of the L-cysteine-containing compound A and minimal D-cysteine-containing compound B, through specific resin and deprotection conditions.
The method enables the production of highly potent and selective Kv1.3 inhibitors with consistent pharmacokinetic properties and improved safety profiles, meeting regulatory standards for clinical trials.