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Pharmaceutical Peptides

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Name: Triptorelin

English synonyms: pglu-his-trp-ser-Tyr-d-trp-leu-arg-pro-gly-NH2; PYROGLU-HIS-TRP-SER-TYR-D-TRP-LEU-ARG-PRO-GLYNH2

CAS no. : 57773-63-4

Molecular formula: C64H82N18O13

Molecular weight: 1311.47

EINECS no. : 637-328-4

Triptorelin, 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. By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. Triptorelin is marketed under the brand names Decapeptyl (Ipsen) and Diphereline and Gonapeptyl (Ferring Pharmaceuticals).

Triptorelin is a synthetic agonist analog of gonadotropin releasing hormone (GnRH). Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone.

Triptorelin is a man-made form of a hormone that regulates many processes in the body. The Trelstar brand of triptorelin is used in men to treat the symptoms of prostate cancer. Trelstar treats only the symptoms of prostate cancer and does not treat the cancer itself.

Clinically, it is mainly used for the treatment of endometriosis, hormone-dependent prostate cancer, breast cancer, children's true precocious puberty, and can also be used for assisted fertility technology. The main adverse reactions of triprorelin are as follows: urinary disorders, breast swelling and pain, bone pain, etc., may also occur in the early treatment of men, hot flashes, hypolibido and impotence. Atrophy of breasts and testicles in rare male female and sleep disorder. A small amount of vaginal bleeding may occur in girls during the first week of treatment and may be corrected by short-term additional therapy. Hot flashes, bleeding or bleeding spots, vaginal dryness, headache and weakness may occur during treatment in women, and abdominal and/or pelvic pain may occur when gonadotropins are used in combination. Slight loss of trabecular matrix may occur as estrogen concentration decreases to postmenopausal levels. It usually returns to normal six to nine months after treatment stops. Patients with endometriosis may have irreversible amenorrhea after medication.

Single Impurity (HPLC) 1.0%max
Amino Acid Composition ±10% of theoretical
Peptide Content (N%) ≥80.0%
Water Content(Karl Fischer) ≤6.0%
Acetate Content (HPIC) ≤15.0%
MS(ESI) Consistent
Mass Balance 95.0~105.0%
Specific Rotation (20/D) -65.0~-75.0°(c=0.5 1%HAc)

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