Ozarelix
From PeptidePlaza, the free peptide reference · Entry #1190 · Anti-Aging · Sources fetched 2026-09-11 · Editorial standards
Ozarelix (also known as ozarelixum, LHRH antagonist SPI-153, SPI-153, Ozarelix [INN]) is a anti-aging research peptide. Ozarelix is a synthetic peptide and a gonadotropin-releasing hormone (GnRH) receptor antagonist.
Ozarelix functions as a gonadotropin-releasing hormone receptor antagonist, meaning it blocks the action of GnRH. It has been investigated for its potential use in conditions such as prostatic hyperplasia and castration-resistant prostatic neoplasms, reaching Phase 2 clinical trials for both indications. The compound has been the subject of several studies, including research into its aggregation behavior and the impact of polyelectrolyte structure on nanoassemblies with cationic peptides. Ozarelix is currently in Phase 3 of clinical development.
1 Mechanism of action
Gonadotropin-releasing hormone receptor antagonist (antagonist)
Primary targets: Gonadotropin-releasing hormone receptor
2 Reported effects
Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.
2.1 Indicated / studied for
- Prostatic Hyperplasia
- Prostatic Neoplasms, Castration-Resistant
3 Chemical and physical properties
| CAS number | 295350-45-7 |
|---|---|
| Molar mass | 1459.1 g/mol |
| Purity (typical) | Not independently verified |
| Storage | −20 °C, lyophilised powder, desiccated |
| Solubility | Sterile water / bacteriostatic water |
| Receptors / targets | Gonadotropin-releasing hormone receptor |
4 Research studies (7)
- Aggregation Behavior of Structurally Similar Therapeutic Peptides Investigated by (1)H NMR and All-Atom Molecular Dynamics Simulations
Molecular pharmaceutics (2022) - Gateways to clinical trials
Methods and findings in experimental and clinical pharmacology (2007) - Nanofibers resulting from cooperative electrostatic and hydrophobic interactions between peptides and polyelectrolytes of opposite charge
Langmuir : the ACS journal of surfaces and colloids (2011) - The impact of polyelectrolyte structure on the shape of nanoassemblies with cationic peptides
Journal of pharmaceutical sciences (2013) - Gateways to clinical trials
Methods and findings in experimental and clinical pharmacology (2007) - Fluorescence spectroscopic determination of the critical aggregation concentration of the GnRH antagonists Cetrorelix, Teverelix and Ozarelix
Journal of fluorescence (2010) - Ozarelix, a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors
The Prostate (2010)
5 Safety and risk profile
5.1 Regulatory status
Ozarelix is currently classified as Phase 3 clinical trials. It has no approved human indication in the United States; availability elsewhere does not imply demonstrated safety or efficacy.
6 Frequently asked questions
- What is Ozarelix?
- Ozarelix is a synthetic peptide that acts as a gonadotropin-releasing hormone (GnRH) receptor antagonist. This means it works by blocking the effects of GnRH in the body.
- How does Ozarelix work?
- Ozarelix functions as a gonadotropin-releasing hormone receptor antagonist. By binding to and blocking the GnRH receptor, it prevents the natural hormone from exerting its effects.
- What is Ozarelix studied for?
- Ozarelix has been studied for its potential use in treating prostatic hyperplasia and castration-resistant prostatic neoplasms. It has advanced to Phase 2 clinical trials for these conditions.
- What is the regulatory status of Ozarelix?
- Ozarelix is currently in Phase 3 of clinical development, indicating it is undergoing advanced testing to evaluate its efficacy and safety.
7 References
- Ozarelix — compound summary PubChem. View source
- Ozarelix — molecule record ChEMBL. View source
- Ozarelix — published literature (7 records) PubMed. View source
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