Triptorelin Pamoate

Triptorelin Pamoate (also called Triptorelin Embonate) is a potent LHRH (GnRH) agonist. Triptorelin Pamoate is a salt form of triptorelin suitable for obtaining controlled release formulations. After a transient increase, continuous administration of triptorelin results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.

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.