Triptorelin (trifluoroacetate salt)

Triptorelin is a synthetic gonadotropin-releasing hormone (GnRH) peptide agonist that binds to the GnRH receptor (GnRHR; K_i = 0.3 nM in CHO cells expressing the human receptor).¹ It inhibits the growth of DU145, LNCaP, and PC3 prostate and OVCAR-3 ovarian cancer cells (IC₅₀s = 62.1, 73.4, 98.1, and 67.7 μM, respectively).² Triptorelin also inhibits the growth of the triple-negative breast cancer (TNBC) cell lines HCC1806 and MDA-MB-231 (EC₅₀s = 58.29 and 31.59 μM, respectively).³ It stimulates follicle stimulating hormone (FSH) and luteinizing hormone (LH) release from primary rat pituitary cells when used at a concentration of 50 nM.² It also decreases tumor volume of Dunning R3327H prostate tumor flank implants and reduces prostate and testis weight in rats when administered at a dose of 1 mg/kg per day.⁴ Formulations containing triptorelin have been used in the palliative treatment of advanced prostate cancer.

1.Nederpelt, I., Georgi, V., Schiele, F., et al.Characterization of 12 GnRH peptide agonists - a kinetic perspectiveBr. J. Pharmacol.173(1)128-141(2016) 2.Varamini, P., Rafiee, A., Giddam, A.K., et al.Development of new gonadotropin-releasing hormone-modified dendrimer platforms with direct antiproliferative and gonadotropin releasing activityJ. Med. Chem.60(20)8309-8320(2017) 3.Kwok, C.W., Treeck, O., Buchholz, S., et al.Receptors for luteinizing hormone-releasing hormone (GnRH) as therapeutic targets in triple negative breast cancers (TNBC)Target Oncol.10(3)365-373(2015) 4.Princivalle, M., Broqua, P., White, R., et al.Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonistJ. Pharmacol. Exp. Ther.320(3)1113-1118(2007)