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KAI 1678 is a first-in-class, isoenzyme selective, a small peptide inhibitor of protein kinase C epsilon. It was in development for the treatment of neuropathic and postoperative pain. However, KAI-1678 treatment results were negative.

Approval Year

PubMed

PubMed

TitleDatePubMed
PKC delta and epsilon in drug targeting and therapeutics.
2009
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 Apr
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 Jun
Substance Class Protein
Created
by admin
on Sat Dec 16 10:10:58 GMT 2023
Edited
by admin
on Sat Dec 16 10:10:58 GMT 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
32P8I5VL5A
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
KAI-1678
Common Name English
KP-1678
Code English
L-ARGININAMIDE, N-ACETYL-L-.ALPHA.-GLUTAMYL-L-ALANYL-L-VALYL-L-SERYL-L-LEUCYL-L-LYSYL-L-PROLYL-L-THREONYLGLYCYLGLYCYL-L-TYROSYLGLYCYL-L-ARGINYL-L-LYSYL-L-LYSYL-L-ARGINYL-L-ARGINYL-L-GLUTAMINYL-L-ARGINYL-L-ARGINYL-
Systematic Name English
Code System Code Type Description
PUBCHEM
124037376
Created by admin on Sat Dec 16 10:10:58 GMT 2023 , Edited by admin on Sat Dec 16 10:10:58 GMT 2023
PRIMARY
CAS
1253964-58-7
Created by admin on Sat Dec 16 10:10:58 GMT 2023 , Edited by admin on Sat Dec 16 10:10:58 GMT 2023
NO STRUCTURE GIVEN
CLINICAL_TRIALS.GOV
KAI-1678
Created by admin on Sat Dec 16 10:10:58 GMT 2023 , Edited by admin on Sat Dec 16 10:10:58 GMT 2023
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.
CAS
1041004-14-1
Created by admin on Sat Dec 16 10:10:58 GMT 2023 , Edited by admin on Sat Dec 16 10:10:58 GMT 2023
PRIMARY
FDA UNII
32P8I5VL5A
Created by admin on Sat Dec 16 10:10:58 GMT 2023 , Edited by admin on Sat Dec 16 10:10:58 GMT 2023
PRIMARY
Related Record Type Details
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)
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.
ACTIVE MOIETY
Synonym: KAI-1678, CAS Registry Number: 1253964-58-7, System Generated Number: 1253964587
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL