Ozarelix
Also known as: D63153, Ozarelix acetate, SPI-153
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Summary
Ozarelix is a third-generation GnRH antagonist peptide investigated primarily for the treatment of prostate cancer and benign prostatic hyperplasia (BPH). Unlike GnRH agonists, it produces immediate androgen suppression without an initial hormonal flare, making it potentially advantageous in patients with advanced prostate cancer at risk of clinical exacerbation.
Mechanism of Action
Competitive antagonist of gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland, leading to immediate suppression of LH and FSH secretion without an initial testosterone surge (flare), resulting in rapid castrate levels of testosterone.
Routes of Administration
Goals & Uses
- Prostate cancer androgen deprivationOncologyModerate
- Reduction of lower urinary tract symptoms (LUTS)UrologyLow
- Testosterone suppression without flareEndocrinologyModerate
- Benign prostatic hyperplasia (BPH) symptom reliefUrologyModerate
Contraindications
- Severe hepatic impairmentOrganModerateLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Hypersensitivity to GnRH analoguesAllergy/ImmunologyHigh
Adverse Effects
- QT interval prolongationCardiacUncommon
- Injection site reactionsLocalCommon
- Hot flashesEndocrine / VasomotorCommon
- FatigueGeneralCommonLow energy or tiredness
- Erectile dysfunctionSexual/ReproductiveCommon
- Bone mineral density reductionMusculoskeletalUncommon
Drug Interactions
- Anticoagulants (e.g., warfarin)Low
- QT-prolonging agents (e.g., antiarrhythmics, antipsychotics)Moderate
Population Constraints
- Pediatric patientsAgeAbsolute
- Females of reproductive potentialReproductiveRelative
- Patients with osteoporosisMusculoskeletalRelative
- Patients with pre-existing cardiovascular diseaseCardiovascularRelative
Regulatory Status
- European UnionInvestigationalNo EMA marketing authorization; evaluated in European clinical trials for prostate cancer and BPH.
- United StatesInvestigationalStudied in Phase II clinical trials; no FDA approval obtained. Development appears stalled.
- United KingdomInvestigationalNo MHRA approval; remains an investigational compound.
Ozarelix has not received FDA, EMA, or other major regulatory approval. It was studied in Phase II clinical trials for prostate cancer and BPH but development has not progressed to Phase III or approval as of available data.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Ozarelix?
Ozarelix is a third-generation GnRH antagonist peptide investigated primarily for the treatment of prostate cancer and benign prostatic hyperplasia (BPH). Unlike GnRH agonists, it produces immediate androgen suppression without an initial hormonal flare, making it potentially advantageous in patients with advanced prostate cancer at risk of clinical exacerbation.
What is Ozarelix used for?
Ozarelix is educationally associated with: Prostate cancer androgen deprivation, Reduction of lower urinary tract symptoms (LUTS), Testosterone suppression without flare, Benign prostatic hyperplasia (BPH) symptom relief. Educational only — not medical advice.
How is Ozarelix administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Ozarelix?
Reported adverse effects include: QT interval prolongation, Injection site reactions, Hot flashes, Fatigue, Erectile dysfunction, Bone mineral density reduction. This list is not exhaustive — consult a qualified clinician.
Who should avoid Ozarelix?
Recorded contraindications: Severe hepatic impairment, Pregnancy, Hypersensitivity to GnRH analogues. Consult a qualified clinician before use.