Delving into the Latest Updates on Kisspeptin-10 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Human metastin 45-54, Kisspeptin 112-121, Kisspeptin-10 (human)

Target

KISS1

Action

modulators

Mechanism

KISS1 modulators(KiSS-1 metastasis suppressor modulators)

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic DiseaseUrogenital Diseases+ [2]

Active Indication

Idiopathic Hypogonadotropic HypogonadismReproductive tract disorder NOSsecondary testicular failure+ [3]

Inactive Indication

AgonadismDelayed PubertyInfertility+ [3]

Originator Organization

Mass General Brigham, Inc.

Active Organization

The Schwartz Center for Compassionate HealthcareThe General Hospital Corp.

Inactive Organization

Quaid-i-Azam University

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Sequence Code 2944

Source: *****

The goal of this study is to see whether kisspeptin, a naturally occurring hormone, can stimulate the release of other reproductive hormones in men and women with idiopathic hypogonadotropic hypogonadism (IHH). The investigators are also examining whether kisspeptin can help women release eggs from their ovaries. Kisspeptin will be administered SC for two weeks in a pulsatile fashion. Ultrasound monitoring of ovarian follicular growth (for women) and frequent blood sampling (every 10 minutes for up to 70 minutes) will be performed to assess the physiologic response to kisspeptin over time.
Funding Source: FDA OOPD

Start Date03 Feb 2023

Sponsor / Collaborator

The Schwartz Center for Compassionate Healthcare

100 Clinical Results associated with Kisspeptin-10

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100 Translational Medicine associated with Kisspeptin-10

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100 Patents (Medical) associated with Kisspeptin-10

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136

Literatures (Medical) associated with Kisspeptin-10

01 Feb 2025·Neurological Research

Central administration of p234, kisspeptin antagonist, but not kisspeptin-10, reduces the power of epileptiform activity and slow EEG waves in male rats

Article

Author: Yildirim, Abdulhamit ; Şahin, Zafer ; Kalkan, Ömer Faruk ; Aydin Abidin, Selcen ; Aktaş, Osman ; Abidin, İsmail ; Özyaşar, Ali Faruk ; Uzun, İbrahim

INTRODUCTIONWe aimed to investigate the effects of central kisspeptin-10 and p234 administration on basal brain activity and epilepsy-like conditions induced by 4-aminopyridine (4-AP), as well as their roles in the electrocorticogram (ECoG) power spectrum and EEG waves.METHODSThirty-five male Wistar rats were divided into five groups: sham,4-AP (2.5 mg/kg i.p.), kisspeptin-10 post-treatment (200 pmoli.c.v.), p234 post-treatment (1 nmol i.c.v.), and p234 pre-treatment (1 nmol i.c.v.). We performed 70 minutes of recordings (10 min baseline) for all groups under ketamine/xylazine (90/10 mg/kg) anesthesia. In the post-treatment groups, kisspeptin-10 or p234 injections were administered 20 minutes after epilepsy induction. In the pre-treatment group, p234 was injected after baseline recordings. Following a 20-minute pre-treatment period, 4-AP was administered.RESULTS4-AP alone induced epileptiform activity in all animals, reaching apeak after 30 minutes. Neither kisspeptin-10 nor p234 post-treatment affected 4-AP-induced epileptiform activity (p > 0.05). However, p234 pre-treatment reduced epileptiform activity (p < 0.05). Additionally, kisspeptin-10 did not alter the spectral analysis of the EEG bands or the power of the ECoG (p > 0.05). In contrast, p234 reduced the power of the ECoG and the slow bands (delta and theta) (p < 0.05).CONCLUSIONWe conclude that p234 pre-treatment has an inhibitory effect on neuronal excitability and epileptiform activity in the neocortex.

01 Sep 2024·Biomedical Chromatography

Investigating the detection of the novel doping‐relevant peptide kisspeptin‐10 in urine using liquid chromatography high‐resolution mass spectrometry

Article

Author: Risseeuw, Martijn ; Van Eenoo, Peter ; Colpaert, Thibo ; Deventer, Koen

AbstractKisspeptin‐10 is a peptide hormone capable of increasing circulating follicle‐stimulating hormone, luteinizing hormone and testosterone levels in humans. Clinically, these effects suggest its use as a treatment for infertility. However, its testosterone‐increasing effect indicates potential misuse in sports. As such, it is included in the 2024 World Anti‐Doping Agency Prohibited List. This work describes the successful validation of an initial testing procedure (screening) and a confirmation procedure for kisspeptin‐10 in urine using liquid chromatography–mass spectrometry. Additionally, kisspeptin‐10 was incubated in human serum to mimic endogenous metabolism to improve method sensitivity, as previous research had demonstrated a rapid elimination time of only 30 min after injection (in rats). Four metabolites, corresponding to peptide fragments y9, y8, y7 and y5, were found and added to the ITP in full scan mode. A degradation product discovered during early experimentation was found to probably be caused by oxidation of the tryptophan residue into a kynurenine residue. Further research should elucidate the kinetic parameters of the reaction to improve product stability. Using the validated confirmation procedure, a black‐market vial of kisspeptin‐10 was analysed. The product contained no unexpected impurities, although it appeared to have undergone more degradation than the purchased reference standard.

01 Jul 2024·Cell Reports

Structural basis for hormone recognition and distinctive Gq protein coupling by the kisspeptin receptor

Article

Author: Cao, Yinglong ; Chen, Juanhua ; Li, Shujie ; Shen, Shiyi ; Xu, H Eric ; Liu, Heng ; He, Xinheng ; Duan, Jia ; Wang, Dongxue ; Cheng, Xi

Kisspeptin signaling through its G protein-coupled receptor, KISS1R, plays an indispensable role in regulating reproduction via the hypothalamic-pituitary-gonadal axis. Dysregulation of this pathway underlies severe disorders like infertility and precocious puberty. Here, we present cryo-EM structures of KISS1R bound to the endogenous agonist kisspeptin-10 and a synthetic analog TAK-448. These structures reveal pivotal interactions between peptide ligands and KISS1R extracellular loops for receptor activation. Both peptides exhibit a conserved binding mode, unveiling their common activation mechanism. Intriguingly, KISS1R displays a distinct 40° angular deviation in its intracellular TM6 region compared to other G_q-coupled receptors, enabling distinct interactions with G_q. This study reveals the molecular intricacies governing ligand binding and activation of KISS1R, while highlighting its exceptional ability to couple with G_q. Our findings pave the way for structure-guided design of therapeutics targeting this physiologically indispensable receptor.

100 Deals associated with Kisspeptin-10

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB16210

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Idiopathic Hypogonadotropic Hypogonadism	Phase 2	United States	The Schwartz Center for Compassionate Healthcare	03 Feb 2023
Reproductive tract disorder NOS	Phase 2	United States	The Schwartz Center for Compassionate Healthcare	03 Feb 2023
secondary testicular failure	Phase 2	United States	The Schwartz Center for Compassionate Healthcare	03 Feb 2023
Hyperprolactinemia	Phase 2	United States	The General Hospital Corp.	17 Nov 2017
Hypogonadism	Phase 2	United States	The General Hospital Corp.	17 Nov 2017
Infertility	Phase 1	Pakistan	Quaid-i-Azam University	08 Aug 2014
Agonadism	Phase 1	United States	The General Hospital Corp.	01 Sep 2011
Kallmann Syndrome	Phase 1	United States	The General Hospital Corp.	23 Jun 2009
Malnutrition	Phase 1	United States	The General Hospital Corp.	23 Jun 2009
Polycystic Ovary Syndrome	Phase 1	United States	The General Hospital Corp.	23 Jun 2009

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02956447 (CTgov)	Phase 2	Hypogonadism \| Hyperprolactinemia	36	GnRH+Kisspeptin 112-121 (Intravenous Kisspeptin)	kyoywkpohc(ahriogvphh) = dcknluuvxb cuuyeudevs (wiguqfeuwr, wtmhphokcf - mwadgqhvkx) View more	-	20 Aug 2024
NCT02956447 (CTgov)	Phase 2	Hypogonadism \| Hyperprolactinemia	36	Kisspeptin 112-121 (Subcutaneous Kisspeptin)	yoptsvbzts(ddghkcxwdx) = zazrwwiyit rklmgogpsm (urjcdibhwg, mdqtsrqhcq - xibbtzftqq) View more	-	20 Aug 2024
NCT03315325 (Pubmed \| J Clin Endocrinol Metab)	Phase 3	Infertility	15	Kisspeptin-10	krvnebqizh(mowvtfzljl) = hkhxrpdvgr sggbosqvjr (tdogovdevd ) View more	-	01 Aug 2011

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Biosimilar

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Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

Regulation

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Kisspeptin-10

Overview

Basic Info

Structure/Sequence

Related

External Link

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Biosimilar

Regulation