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Triptorelin Pamoate

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CAT#
10-101-101
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
CAS No.
57773-63-4 (net), 124508-66-3 (pamoate salt)
Sequence
Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2 pamoate salt
M.W/Mr.
1744.96
Molecular Formula
C64H82N18O13
Source
Synthetic
Long-term Storage Conditions
−20°C
Application
Triptorelin 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.
Description
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.
Areas of Interest
Hormonal therapy
  • Background
  • Related Products
  • References

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.

CAS: 25126-32-3 (net)
Sequence: H-Asp-Tyr(SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2 ammonium salt
M.W: 1143.3
Molecular Formula: C49H62N10O16S3
CAS: 38916-34-6 (net), 51110-01-1 (acetate)
Sequence: H-Ala-Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH acetate salt (Disulfide bond)
M.W: 1637.88
Molecular Formula: C76H104N18O19S2
CAS: 75957-60-7 (net), 105184-37-0 (acetate)
Sequence: H-Arg-Lys-Glu-Val-Tyr-OH acetate salt
M.W: 813.89
Molecular Formula: C35H59N9O13
CAS: 103300-74-9
Sequence: (1-methyl-4,5-dihydroorotyl)- His-Pro-NH2
M.W: 477.46
Molecular Formula: C17H23N7O5
CAS: 16960-16-0
Sequence: H-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-OH acetate salt
M.W: 2933.5
Molecular Formula: C136H210N40O31S

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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