First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity
ABSTRACT Dentin hypersensitivity is characterized by transient, sharp pain resulting from dentin exposure due to enamel or cementum loss. Current treatments, which primarily focus on superficial tubule occlusion or nerve desensitization, provide only temporary relief. Copine7 (CPNE7) induces odontob...
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| Format: | Article |
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Wiley
2025-08-01
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| Series: | Clinical and Translational Science |
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| Online Access: | https://doi.org/10.1111/cts.70326 |
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| author | Myung Jin Lee Yoon Seon Lee Joo‐Cheol Park Hyun Chul Kim So Hyun Park Howard Lee Won Jun Shon |
| author_facet | Myung Jin Lee Yoon Seon Lee Joo‐Cheol Park Hyun Chul Kim So Hyun Park Howard Lee Won Jun Shon |
| author_sort | Myung Jin Lee |
| collection | DOAJ |
| description | ABSTRACT Dentin hypersensitivity is characterized by transient, sharp pain resulting from dentin exposure due to enamel or cementum loss. Current treatments, which primarily focus on superficial tubule occlusion or nerve desensitization, provide only temporary relief. Copine7 (CPNE7) induces odontoblast differentiation and physiologic dentin regeneration, enabling biological dentin sealing and presenting a novel therapeutic approach. This study reports the first‐in‐human results of a randomized, double‐blind, dose‐escalation phase 1/2a clinical trial evaluating the safety, tolerability, preliminary efficacy, and pharmacokinetics of the CPNE7‐derived functional peptide (selcopintide) in patients with dentin hypersensitivity. In Part A (Single Ascending Dose, SAD), 24 participants received a single topical application of selcopintide at ascending doses (2.5, 5, and 10 μg/tooth) in a 6:2 randomization ratio (treatment: placebo). In Part B (Multiple Ascending Dose, MAD), 16 participants received three topical applications (5 and 10 μg/tooth) over 15 days (day 1, 8, and 15; visits 2–4) with the same randomization ratio. Efficacy endpoints were assessed by changes in cold water, evaporative air, and tactile sensitivity. In Part B, the 10 μg selcopintide group demonstrated statistically significant reductions from the baseline across all three measures (p < 0.05), with a mean decrease of −23.2 ± 19.4 mm in VAS, the primary efficacy endpoint. All doses were well tolerated, with no serious adverse events and no detectable systemic absorption of selcopintide. These findings support the safety, tolerability, and preliminary efficacy of selcopintide as a novel therapeutic candidate for the treatment of dentin hypersensitivity. |
| format | Article |
| id | doaj-art-8348d4fe4c684275a627e434f7fd873c |
| institution | Kabale University |
| issn | 1752-8054 1752-8062 |
| language | English |
| publishDate | 2025-08-01 |
| publisher | Wiley |
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| series | Clinical and Translational Science |
| spelling | doaj-art-8348d4fe4c684275a627e434f7fd873c2025-08-23T17:10:43ZengWileyClinical and Translational Science1752-80541752-80622025-08-01188n/an/a10.1111/cts.70326First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin HypersensitivityMyung Jin Lee0Yoon Seon Lee1Joo‐Cheol Park2Hyun Chul Kim3So Hyun Park4Howard Lee5Won Jun Shon6Department of Conservative Dentistry, School of Dentistry and Institute of Oral Bioscience Jeonbuk National University Jeonju Republic of KoreaDepartment of Conservative Dentistry, Dental Research Institute and School of Dentistry Seoul National University Seoul South KoreaDepartment of Oral Histology–Developmental Biology, Dental Research Institute and School of Dentistry Seoul National University Seoul South KoreaDepartment of Clinical Pharmacology and Therapeutics Seoul National University Hospital Seoul Republic of KoreaDepartment of Conservative Dentistry, Dental Research Institute and School of Dentistry Seoul National University Seoul South KoreaDepartment of Clinical Pharmacology and Therapeutics Seoul National University Hospital Seoul Republic of KoreaDepartment of Conservative Dentistry, Dental Research Institute and School of Dentistry Seoul National University Seoul South KoreaABSTRACT Dentin hypersensitivity is characterized by transient, sharp pain resulting from dentin exposure due to enamel or cementum loss. Current treatments, which primarily focus on superficial tubule occlusion or nerve desensitization, provide only temporary relief. Copine7 (CPNE7) induces odontoblast differentiation and physiologic dentin regeneration, enabling biological dentin sealing and presenting a novel therapeutic approach. This study reports the first‐in‐human results of a randomized, double‐blind, dose‐escalation phase 1/2a clinical trial evaluating the safety, tolerability, preliminary efficacy, and pharmacokinetics of the CPNE7‐derived functional peptide (selcopintide) in patients with dentin hypersensitivity. In Part A (Single Ascending Dose, SAD), 24 participants received a single topical application of selcopintide at ascending doses (2.5, 5, and 10 μg/tooth) in a 6:2 randomization ratio (treatment: placebo). In Part B (Multiple Ascending Dose, MAD), 16 participants received three topical applications (5 and 10 μg/tooth) over 15 days (day 1, 8, and 15; visits 2–4) with the same randomization ratio. Efficacy endpoints were assessed by changes in cold water, evaporative air, and tactile sensitivity. In Part B, the 10 μg selcopintide group demonstrated statistically significant reductions from the baseline across all three measures (p < 0.05), with a mean decrease of −23.2 ± 19.4 mm in VAS, the primary efficacy endpoint. All doses were well tolerated, with no serious adverse events and no detectable systemic absorption of selcopintide. These findings support the safety, tolerability, and preliminary efficacy of selcopintide as a novel therapeutic candidate for the treatment of dentin hypersensitivity.https://doi.org/10.1111/cts.70326clinical trialsefficacypharmacokineticssafetytolerance |
| spellingShingle | Myung Jin Lee Yoon Seon Lee Joo‐Cheol Park Hyun Chul Kim So Hyun Park Howard Lee Won Jun Shon First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity Clinical and Translational Science clinical trials efficacy pharmacokinetics safety tolerance |
| title | First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity |
| title_full | First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity |
| title_fullStr | First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity |
| title_full_unstemmed | First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity |
| title_short | First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity |
| title_sort | first in human study of safety tolerability efficacy and pharmacokinetics of cpne7 derived peptide selcopintide for dentin hypersensitivity |
| topic | clinical trials efficacy pharmacokinetics safety tolerance |
| url | https://doi.org/10.1111/cts.70326 |
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