Triptorelin pamoate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
CAT No: 10-101-101
CAS No:57773-63-4 (net), 124508-66-3 (pamoate salt)
Synonyms/Alias:5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolylglycine amide, 4,4'-methylenebis(3-hydroxy-2-naphthoate) (salt); Decapeptyl; Diphereline; Gonapeptyl; Luteinizing hormone-releasing factor (swine), 6-D-tryptophan-, 4,4'-methylenebis(3-hydroxy-2-naphthalenecarboxylate) (salt); Pamorelin; Trelstar; Trelstar depot; Trelstar LA; Triptorelin embonate; UNII-08AN7WA2G0
Triptorelin Pamoate is a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH), formulated as a pamoate salt to enable sustained-release properties. Characterized by its high receptor affinity and prolonged activity profile, this compound is widely utilized in research settings where modulation of the hypothalamic-pituitary-gonadal axis is required. Its unique formulation allows for controlled and extended peptide release, offering significant advantages in experimental protocols that demand stable and predictable hormonal suppression. Triptorelin Pamoate's structural stability and solubility also make it a preferred choice for in vivo studies, ensuring consistent pharmacodynamic responses over extended periods. Researchers value its ability to provide reproducible results in endocrine investigations, facilitating the exploration of complex physiological pathways with minimal variability.
Reproductive Endocrinology Research: In the realm of reproductive biology, Triptorelin Pamoate serves as a powerful tool for investigating the regulation of gonadotropin secretion. By acting as a potent GnRH agonist, it initially stimulates and then downregulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) through receptor desensitization. This property enables researchers to model and study the physiological consequences of suppressed gonadotropin levels, such as alterations in gonadal steroidogenesis, gametogenesis, and feedback mechanisms within the hypothalamic-pituitary-gonadal axis. The sustained-release formulation is particularly advantageous for long-term studies, eliminating the need for frequent dosing and minimizing animal handling stress, thereby improving data quality and experimental reproducibility.
Oncology Research: Triptorelin Pamoate is extensively deployed in preclinical oncology models to elucidate the role of hormonal regulation in hormone-sensitive tumors. Its ability to induce profound and sustained suppression of gonadotropins provides a reliable means to study tumor responses to hormonal deprivation, particularly in prostate and breast cancer models. Through this mechanism, researchers can dissect the molecular and cellular pathways influenced by androgen or estrogen deprivation, evaluate the efficacy of novel anti-tumor agents in combination with endocrine therapy, and investigate resistance mechanisms to hormonal manipulation. The extended release offered by the pamoate formulation supports chronic dosing regimens, aligning with the timeframes required for tumor progression studies.
Neuroendocrinology Studies: In investigations focused on the central regulation of hormonal axes, Triptorelin Pamoate is utilized to probe the neuroendocrine controls governing reproductive and metabolic functions. Its capacity to modulate GnRH receptor activity allows for precise manipulation of downstream hormonal cascades, facilitating studies into the neurobiological basis of puberty, sexual differentiation, and stress responses. Scientists leverage its predictable pharmacokinetics to conduct longitudinal studies on the impact of altered GnRH signaling on brain structure, neuroplasticity, and behavior. The stable and prolonged action of this peptide analogue is essential for dissecting the temporal dynamics of neuroendocrine feedback loops.
Animal Model Development: Researchers employ Triptorelin Pamoate in the creation and maintenance of animal models that require sustained suppression of reproductive hormones. These models are instrumental in studying the effects of gonadal hormone deprivation on systemic physiology, including bone density, cardiovascular health, and metabolic regulation. The extended-release nature of the pamoate salt ensures steady-state hormone suppression, which is critical for modeling chronic conditions or evaluating interventions over several weeks or months. This approach reduces variability associated with fluctuating hormone levels and enhances the reliability of experimental outcomes.
Endocrine Disruption Assessment: The compound is also a valuable asset in toxicological and environmental research, where it facilitates the assessment of endocrine-disrupting chemicals. By establishing a baseline of suppressed gonadotropin activity, Triptorelin Pamoate allows scientists to evaluate how test substances interfere with hormonal feedback mechanisms or restore endocrine function. This application is crucial for understanding the potential risks posed by environmental contaminants and for developing strategies to mitigate their impact on reproductive health and development. The reproducible and sustained suppression achieved with this formulation enables robust comparative analyses across diverse experimental conditions.
Peptide Mechanism Elucidation: Beyond its established roles, Triptorelin Pamoate is increasingly employed in basic research to unravel the mechanistic aspects of peptide-receptor interactions and downstream signaling events. Its well-characterized action as a GnRH analogue provides a model system for studying receptor desensitization, internalization, and the modulation of intracellular signaling pathways. Researchers utilize it to dissect the temporal patterns of gene expression, protein phosphorylation, and cellular adaptation in response to chronic peptide exposure. These insights contribute to a deeper understanding of peptide therapeutics and the design of next-generation analogues with improved pharmacological profiles.
Gonadotropin-releasing hormone agonists are widely used as androgen deprivation therapy in many men with locally advanced or metastatic prostate cancer. Gonadotropin-releasing hormone agonists are delivered by intramuscular injection every 1, 3 or 6 months, but in some patients subcutaneous injection may be more appropriate. This study assessed the efficacy and safety profile of the gonadotropin-releasing hormone agonist, triptorelin pamoate, when administered by the subcutaneous route.
Lebret, T., Rouanne, M., Hublarov, O., Jinga, V., Petkova, L., Kotsev, R., ... & Dutailly, P. (2015). Efficacy of triptorelin pamoate 11.25 mg administered subcutaneously for achieving medical castration levels of testosterone in patients with locally advanced or metastatic prostate cancer. Therapeutic advances in urology, 7(3), 125-134.
To compare the efficacy of monthly administrations of the luteinizing hormone-releasing hormone agonists triptorelin pamoate and leuprolide acetate to induce and maintain castrate levels of serum testosterone in men with advanced prostate cancer. Triptorelin reduced testosterone concentrations less rapidly, but maintained castration as effectively as leuprolide. There was no evidence that the slower onset of castration caused deleterious effects.
Heyns, C. F., Simonin, M. P., Grosgurin, P., Schall, R., & Porchet, H. C. (2003). Comparative efficacy of triptorelin pamoate and leuprolide acetate in men with advanced prostate cancer. BJU international, 92(3), 226-231.
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