Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| A single-center, randomized, double-blind, active, and placebo-controlled study of KAI-1678, a novel PKC-epsilon inhibitor, in the treatment of acute postoperative orthopedic pain. | 2013-06 |
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| The safety and efficacy of KAI-1678- an inhibitor of epsilon protein kinase C (εPKC)-versus lidocaine and placebo for the treatment of postherpetic neuralgia: a crossover study design. | 2013-04 |
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| PKC delta and epsilon in drug targeting and therapeutics. | 2009 |
| Substance Class |
Protein
Created
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| Protein Sub Type | |
| Sequence Type | COMPLETE |
| Record UNII |
32P8I5VL5A
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| Record Status |
Validated (UNII)
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| Record Version |
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| Name | Type | Language | ||
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Preferred Name | English | ||
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Common Name | English | ||
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Systematic Name | English |
| Code System | Code | Type | Description | ||
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124037376
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1253964-58-7
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admin on Mon Mar 31 23:05:57 GMT 2025 , Edited by admin on Mon Mar 31 23:05:57 GMT 2025
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NO STRUCTURE GIVEN | |||
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KAI-1678
Created by
admin on Mon Mar 31 23:05:57 GMT 2025 , Edited by admin on Mon Mar 31 23:05:57 GMT 2025
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PRIMARY | Official Title: A Double-Blind, Randomized, Placebo- and Active-Comparator-Controlled, Single-Dose Study to Assess the Efficacy of KAI-1678 Administered by Subcutaneous Infusion in Subjects With Postherpetic Neuralgia, Purpose: The purpose of this study is to determine whether KAI-1678 is effective in the treatment of postherpetic neuralgia pain, Primary Outcome Measures: The effect of KAI-1678 on mean change from baseline in pain intensity at 6 hours (PID 6). (Time Frame: Day 1) (Designated as safety issue: No) Measurements are made using a qualified pain scale and the change from basline is calculated at 6 hours. | ||
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1041004-14-1
Created by
admin on Mon Mar 31 23:05:57 GMT 2025 , Edited by admin on Mon Mar 31 23:05:57 GMT 2025
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PRIMARY | |||
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32P8I5VL5A
Created by
admin on Mon Mar 31 23:05:57 GMT 2025 , Edited by admin on Mon Mar 31 23:05:57 GMT 2025
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
Originator: KAI Pharmaceuticals; Developer: Amgen; Class: Anti-inflammatory,Non-opioid analgesic, Peptide, Small molecule; Mechanism of Action: Protein kinase C epsilon inhibitor; Highest Development Phase: Discontinued for Neuropathic pain, Postoperative pain; Most Recent Events: 05 Jul 2012 KAI Pharmaceuticals has been acquired by Amgen, 22 Apr 2010 KAI Pharmaceuticals completes a phase IIa trial (NCT01106716) in Neuropathic pain in Australia, 21 Oct 2009 Pharmacodynamics data from a preclinical study in Neuropathic pain presented at the 39th Annual Meeting of the Society for Neuroscience (SfN-2009)
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ACTIVE MOIETY |
KAI-1678, First-in-Class Compound, Enters Phase 2a Clinical Testing for the Treatment of Pain: KAI-1678 is an isozyme-selective, small peptide inhibitor of the epsilon protein kinase C pathway. Epsilon PKC is a well-validated target for both inflammatory and neuropathic pain in the preclinical, peer-reviewed scientific literature. KAIs approach is the first to enable the specificity of action required to make epsilon PKC inhibition a viable clinical approach.
KAI-1678 has been shown to be highly effective at reversing pain in preclinical models of both neuropathic and inflammatory pain.
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ACTIVE MOIETY |
Synonym: KAI-1678, CAS Registry Number: 1253964-58-7, System Generated Number: 1253964587
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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID REPLACEMENT | [1_21] | ARGININE |
Amount:
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ARGININAMIDE, L- | 29626ZE0WY | |
| AMINO ACID REPLACEMENT | [1_1] | GLUTAMIC ACID |
Amount:
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ACETYL GLUTAMIC ACID | MA61H539YZ |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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