Phase 1/2a Clinical Trial of CPNE7-Derived Peptide for Dentin Hypersensitivity

Objectives: Copine7 (CPNE7) is known to induce odontoblast differentiation and tertiary dentin formation, and thus has potential to be used as dental medicine for dentin hypersensitivity. CPNE7-derived functional peptide (CPNE7-DP, Selcopintide), which replicates functions of CPNE7, has been developed for better stability and manipulation. In this study, randomized, double-blind, dose-escalation, phase 1/2a clinical trial was carried out to assess safety, tolerability, efficacy and pharmacokinetics of Selcopintide in dentin hypersensitivity patients.
Methods: In Part A, 24 subjects of three cohorts of ascending doses (cohort 1, 2.5ug/tooth; cohort 2, 5ug/tooth; cohort 3, 10ug/tooth) were topically applied with Selcopintide at their exposed dentins once, and in Part B, 16 subjects of two cohorts (cohort 1, 5ug/tooth, cohort 2, 10ug/tooth) were applied with Selcopintide multiple times. Each cohort comprised of six subjects in study group and two subjects in placebo group. Safety was evaluated with physical and oral examinations, vital sign, ECG check, clinical laboratory test and adverse event collection. Subjects were also hospitalized for pharmacokinetic blood analysis, and blood samplings were collected before (0h) and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 24h after Selcopintide administration. Primary efficacy was assessed by evaluating change from baseline in cold water measured by visual analogue scale (VAS).
Results: Safety results showed that all adverse events were transient and recovered without occurrence of any serious adverse events. Efficacy results demonstrated that when Selcopintide was applied multiple times in Part B, VAS showed greater reduction in the study group compared to the placebo group. Furthermore, no Selcopintide concentrations were detected at any point of pharmacokinetic blood samplings of all subjects.
Conclusions: Selcopintide up to 10ug/tooth is safe, well tolerated, and when applied multiple times, shows tendency to reduce dentin hypersensitivity. To verify its efficacy, however, larger-scale clinical trial with greater number of subjects will be needed in the future.