Page data last changed: . Registry refreshes and identity assessments are separate from scientific content review.
A clinical-stage GnRH antagonist studied as an alternative to established agents.
Also known as: teverelix TFA · GnRH antagonist
Part of the Foundational & therapeutic peptides cluster
Overview
Teverelix is a synthetic decapeptide GnRH antagonist that binds competitively and reversibly to pituitary GnRH receptors, suppressing luteinizing hormone and follicle-stimulating hormone. It is an investigational compound studied in prostate disorders and is not authorized by Health Canada. This page is educational and is not medical advice.
Source & context
Biological / chemical source: Synthetic decapeptide analog of GnRH
Primary research or clinical context: Investigational GnRH antagonist studied for prostate cancer and benign prostatic conditions; not authorized by Health Canada
Where it sits in the class
Teverelix belongs to the same peptide-antagonist family as cetrorelix, ganirelix, abarelix, and degarelix. Research interest centers on formulation and pharmacokinetics that could offer practical advantages, but its status remains investigational.
Mechanism
By competitively blocking the GnRH receptor, teverelix suppresses gonadotropins without the initial hormone flare characteristic of agonists. Reported clinical studies have evaluated its pharmacokinetics, safety, and hormone-suppressing effects.
Sequence of the selected reference form
Sequence backbone for the reference form: Teverelix parent free peptide. Termini, stereochemistry and modifications are described below.
XXXSYXLXPA
X1=Ac-D-2Nal; X2=D-4-chlorophenylalanine; X3=D-3-pyridylalanine; X6=D-homocitrulline; X8=N6-isopropyl-L-lysine; A10=D-alaninamide.. X marks a noncanonical residue; see the expanded sequence and reference chemistry below.
Analyze sequences in the playground →Structure & chemistry
Molecular identity & reference confidence
Source-supported reference
The selected parent has D-homocitrulline6 and N6-isopropyl-Lys8. PubChem’s full stereochemical key matches NIH GSRS and the expanded sequence agrees with an original study. The old CID is incomplete/conflicting; TFA and acetate salts have separate masses.
- Molecular form
- Teverelix parent free peptide
- Species
- Synthetic GnRH antagonist; no natural source species applies
- Termini (N / C)
- N-acetyl-D-2-naphthylalanyl / D-alaninamide
Average reference mass · Molecular identity assessment: 2026-10-05
Reference policy updated: 2026-10-05
- PubChem PUG REST selected parent properties · 2026-10-05
- PubChem selected-parent biologic notation · 2026-10-05
- PubChem selected-parent identifiers with depositor attribution · 2026-10-05
- NIH GSRS independently selected parent record · 2026-10-05
- Original teverelix self-assembly study, materials chemical definition · 2026-10-05
Ac-D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Tyr-D-hCit-Leu-Lys(iPr)-Pro-D-Ala-NH2
- Molecular formula
- C74H100ClN15O14
- Average reference mass
- ≈ 1,459.1
- Backbone
- Teverelix parent free peptide
- C-terminus
- D-alaninamide
- PubChem CID: 16135076
- CAS RN: 151272-78-5
- UNII: D19V7048JK
Chemistry values: curated profile, PubChem.
Clinical development snapshot
ClinicalTrials.gov lists 4 registered studies with “Teverelix” as an intervention (snapshot 2026-09-06). A registry footprint is not evidence of efficacy or approval.
| NCT | Title | Phase | Status | Updated |
|---|---|---|---|---|
| NCT07733934 | Study of Teverelix DP on Prostate Volume, Urinary Function and Clinical Outcomes Following Acute Urinary Reten | Phase 2 | not yet recruiting | 2026-07-29 |
| NCT07457164 | A Study Investigating the Pharmacokinetics, Pharmacodynamics, Efficacy and Safety of Teverelix DP, a Gonadotro | Phase 2 | not yet recruiting | 2026-03-12 |
| NCT04693507 | Teverelix Evaluated in Advanced Prostate Cancer | Phase 2 | completed | 2024-07-23 |
| NCT03781947 | A Study of Parenterally-administered Teverelix TFA in Healthy Male Volunteers | Phase 1 | completed | 2020-03-17 |
Teverelix — reconstitution calculator
Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.
Reference form: Teverelix parent free peptideAverage reference mass: 1,459.1 Da
Enter an amount to see the volume it corresponds to.
Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.
FAQ about Teverelix
What is Teverelix?+
Teverelix is a synthetic decapeptide GnRH antagonist that binds competitively and reversibly to pituitary GnRH receptors, suppressing luteinizing hormone and follicle-stimulating hormone. It is an investigational compound studied in prostate disorders and is not authorized by Health Canada. This page is educational and is not medical advice.
What Canadian product status is recorded for Teverelix?+
Canadian product status for Teverelix has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.
What is the length of the selected reference form for Teverelix?+
The selected reference form (Teverelix parent free peptide) has 10 residues or residue-derived units in its backbone. Other forms in this family may have a different length.
Related peptides
References & further reading
- 1.Ulys et al. (2024). Efficacy, tolerability, and safety of teverelix DP in patients with advanced prostate cancer: A multicenter, open-label, phase 2 trial. Prostate
- 2.MacLean et al. (2022). Pharmacokinetic, Safety, and Pharmacodynamic Properties of Teverelix Trifluoroacetate, a Novel Gonadotropin-Releasing Hormone Antagonist, in Healthy Adult Subjects. Clin Pharmacol Drug Dev
- 3.MacLean et al. (2023). Safety, Pharmacokinetic and Pharmacodynamic Evaluation of Teverelix for the Treatment of Hormone-Sensitive Advanced Prostate Cancer: Phase 2 Loading-Dose-Finding Studies. Medicina (Kaunas)
- 4.Erb et al. (2000). Pituitary and gonadal endocrine effects and pharmacokinetics of the novel luteinizing hormone-releasing hormone antagonist teverelix in healthy men--a first-dose-in-humans study. Clin Pharmacol Ther
- 5.Sannala et al. (2024). A Model-Informed Drug Development Approach to Design a Phase 3 Trial of Teverelix Drug Product in Advanced Prostate Cancer Patients with Increased Cardiovascular Risk. Clin Pharmacol Drug Dev
- 6.Ulys et al. (2025). Teverelix is a potential treatment option for the prevention of acute urinary retention recurrence in men suffering from benign prostatic hyperplasia. Int Urol Nephrol
- 7.Li et al. (2026). Mechanism of Self-Assembly of the Gonadropin Releasing Hormone Antagonist Teverelix into Amyloid Fibrils. Mol Pharm
- 8.Mallardé et al. (2003). PLGA-PEG microspheres of teverelix: influence of polymer type on microsphere characteristics and on teverelix in vitro release. Int J Pharm
- 9.PubChem — compound summary for Teverelix (CID 16135076)