kisspeptin
Kisspeptins are proteins encoded by the KISS1 gene in humans. Kisspeptins are ligands of the G-protein coupled receptor, GPR54. Kiss1 was originally identified as a human metastasis suppressor gene that has the ability to suppress melanoma and breast cancer metastasis. Kisspeptin-GPR54 signaling has an important role in initiating secretion of gonadotropin-releasing hormone (GnRH) at puberty, the extent of which is an area of ongoing research. Gonadotropin-releasing hormone is released from the hypothalamus to act on the anterior pituitary triggering the release of luteinizing hormone (LH), and follicle stimulating hormone (FSH). These gonadotropic hormones lead to sexual maturation and gametogenesis. Disrupting GPR54 signaling can cause hypogonadotrophic hypogonadism in rodents and humans. The Kiss1 gene is located on chromosome 1. It is transcribed in the brain, adrenal gland, liver, gonads, and pancreas. — Wikipedia
Clinical trial activity
23 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Mar 1, 2009 (NCT00914823)
Timeline
Indications
Studied for
- Amenorrhea · Phase 2
- COVID-19 · Phase 1
- Deficiency Diseases · Phase 1
- Glucose · Phase 1
- Glucose Intolerance · Phase 1
- Gonadal Disorders · Phase 1
- Healthy Volunteers · Phase 3
- Hyperprolactinemia · Phase 2
- Hypogonadism · Phase 2
- Infertility · Phase 3
- Insulin · Phase 1
- Kallmann Syndrome · Phase 1
- Metabolic Diseases · Phase 1
- Neurodegenerative Diseases · Phase 1
- Obesity · Phase 3
- Polycystic Ovary Syndrome · Phase 1
- Pregnancy · Phase 1
- Puberty, Delayed · Phase 1
- Reproductive Health · Phase 1
- Reproductive Physiological Phenomena · Phase 3
- Testosterone · Phase 2
- Women · Phase 1
Mechanism of action
- Metastin receptorAGONIST
KISS1R agonist
Chemistry & pharmacology
SMILES
CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O- Mol. weight
- 1302.46 g/mol
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Multi-specific
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaKisspeptin ↗
- ChEMBLCHEMBL4650403 ↗
- ChEMBLCHEMBL376756 ↗
Also known as
- kisspeptin
- kisspeptin
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07224438 | Phase 2 | Dec 31, 2025 | Harvard University, National Institutes of Health (NIH) |
| NCT07224490 | Phase 1 | Dec 31, 2025 | Harvard University, National Institutes of Health (NIH) |
| NCT05901467 | Phase 1 | Oct 20, 2023 | Harvard University |
| NCT05971849 | Phase 1 | Oct 6, 2023 | Harvard University |
| NCT05896293 | Phase 2 | Feb 3, 2023 | Harvard University |
| NCT05633966 | Phase 1 | Dec 31, 2022 | Harvard University |
| NCT05456854 | Phase 1 | Jun 3, 2022 | Harvard University |
| NCT04975334 | Phase 2 | Mar 31, 2022 | Harvard University |
| NCT04975347 | Phase 1 | Mar 31, 2022 | Harvard University |
| NCT04958109 | Phase 1 | Oct 28, 2021 | Harvard University |
| NCT04648969 | Phase 2 | Jan 20, 2021 | Harvard University |
| NCT04532801 | Phase 1 | Sep 1, 2019 | Harvard University |
| NCT02953834 | Phase 1 | Jun 6, 2017 | Harvard University |
| NCT02956447 | Phase 2 | Mar 1, 2017 | Harvard University |
| NCT03315325 | Phase 3 | Aug 8, 2014 | Quaid-i-Azam University (QAU) |
| NCT03286517 | Phase 3 | Jun 26, 2014 | Quaid-i-Azam University (QAU) |
| NCT02081924 | N/A | Apr 2, 2014 | Imperial College London |
| NCT01952782 | Phase 1 | Jan 1, 2014 | Harvard University |
| NCT03771326 | Phase 3 | Oct 29, 2013 | Quaid-i-Azam University (QAU) |
| NCT01667406 | Phase 2 | Jun 1, 2012 | University of London |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Harvard University | Academic/Hospital | 18 | 18 | 2 | 2009 |
| Quaid-i-Azam University (QAU) | Academic/Hospital | 3 | 3 | 1 | 2013 |
| National Institutes of Health (NIH) | Government | 2 | 0 | 2 | 2025 |
| Imperial College London | Academic/Hospital | 1 | 1 | 1 | 2014 |
| University of London | Academic/Hospital | 1 | 1 | 1 | 2012 |