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Triptorelin Pamoate

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.

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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

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Specification Technical Data Publications Customer reviews and Q&A
M.F/FormulaC64H82N18O13
M.W/Mr.1744.96
SequencePyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2
Labeling TargetGonadotropin-releasing hormone (GNRH) Receptor
ApplicationTriptorelin pamoate is classified as a gonadotropin releasing hormone (GnRH) agonist. In adult men with advanced prostate cancer, triptorelin pamoate can be used to help lower testosterone levels, which can be beneficial in stopping or slowing the growth of abnormal prostate tissue.
ActivityAgonist
Biological ActivityTriptorelin, a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts.
Areas of InterestCancer Research
Pituitary & Hypothalamic Hormones
Veterinary Medicine
FunctionsPeptide binding
TargetGonadotropin-releasing hormone (GnRH)
Source#Synthetic
Solubility−20°C
OrganismHuman
References

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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