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TRIPTORELIN ACETATE |
| 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolylglycinamide; (6-D-Tryptophan)luteinizing hormone-releasing hormone; (D-Trp6)-GnRH; D-Tryptophan-LH-RH; Decapeptyl; Dekapeptil; Diferelin; Diphereline; Triptorelin; Triptorelina; Triptoreline; Triptorelinum; Trelstar; 6-D-Tryptophan-LH-RH; 6-D-Tryptophanluteinizing Hormone-releasing Factor; Detryptoreline; D-TRP-6-LHRH; |
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| PRODUCT IDENTIFICATION |
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CAS RN |
57773-63-4(parent), 140194-24-7 (acetate), 124508-66-3 (pamoate) |
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EINECS RN |
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FORMULA |
C64H82N18O13 |
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MOLE WEIGHT |
1311.45 |
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CHEMICAL FAMILY |
Polypeptide |
| CATEGORIES | LHRH agonist |
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| PHYSICAL AND CHEMICAL PROPERTIES |
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PHYSICAL STATE |
white to slightly yellowish powder |
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MELTING POINT |
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BOILING POINT |
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DENSITY |
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SOLUBILITY IN WATER |
Soluble (Soluble in acetic acid) |
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pH |
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VAPOR DENSITY |
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REFRACTIVE INDEX |
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FLASH POINT |
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| STABILITY AND REACTIVITY | |
| STABILITY | Stable under normal conditions. |
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INCOMPATIBLE MATERIALS |
Strong oxidizing agents. |
| DECOMPOSITION PRODUCTS |
Carbon monoxide, Carbon dioxide, Nitrogen oxides. |
| POLYMERIZATION | Has not been reported |
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NFPA RATINGS |
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| SAFETY |
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HAZARD NOTES |
Toxic, May impair fertility |
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EYE |
May cause eye irritation. |
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SKIN |
May be harmful if absorbed through skin. May cause skin irritation. |
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INGESTION |
May be harmful if swallowed. |
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INHALATION |
May be harmful if inhaled. May cause respiratory tract irritation. |
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CHRONIC |
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| TRANSPORT & REGULATORY INFORMATION |
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UN NO. |
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| HAZARD CLASS |
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| PACKING GROUP |
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| HAZARD SYMBOL |
T |
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RISK PHRASES |
60 |
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SAFETY PHRASES |
53-22-36/37/39-45 |
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| EXTERNAL LINKS & GENERAL INFORMATION | |
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Triptorelin:
A synthetic decapeptide
agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing
greater potency than endogenous LHRH, triptorelin reversibly represses
gonadotropin secretion. After chronic, continuous administration, this agent
effects sustained decreases in LH and FSH production and testicular and ovarian
steroidogenesis. Serum testosterone concentrations may fall to levels typically
observed in surgically castrated men (http://www.cancer.gov/)
Triptorelin is a form of hormone therapy called an LHRH (luteinizing hormonereleasing hormone) agonist. There are two brands of the same drug, which are called Decapeptyl SR and Gonapeptyl Depot. Triptorelin slows down the growth of prostate cancer cells by blocking a message from the brain telling the testicles to produce testosterone. Most prostate cancer cells need testosterone to grow and spread. (http://www.prostate-cancer.org.uk/) Leuprorelin and triptorelin, two Gn-RH analogues, are the first drugs to be licensed in France for preoperative treatment of uterine leiomyoma associated with anaemia, when a reduction in the size of the leiomyoma is necessary to facilitate or modify the surgical technique. A solid-blind placebo-controlled trial of leuprorelin in nearly 300 anaemic women showed no advantage in terms of the need for non autologous transfusion. Three solid-blind placebo-controlled trials have shown that leuprorelin reduces the volume of uterine leiomyomas, but whether or not this facilitates or modifies the surgical technique is not known. An unblinded trial versus lynestrenol in non anaemic women showed a superior effect of leuprorelin on the size of the leiomyoma, but again there were no data on a possible effect on the choice of surgical technique. In the absence of comparative solid-blind trials, the observed effects of triptorelin on the choice of surgical technique are uninterpretable. The adverse effects of leuprorelin are mainly linked to its hormone effect, i.e. flushing, headache, vaginitis and vaginal dryness. There are no recent reviews of the adverse effects of triptorelin in this setting. In practice, for anaemic women with leiomyomas requiring surgery, there is no proof that leuprorelin and triptorelin have any tangible clinical advantages.(http://www.medscape.com/)Triptorelin is a synthetic analogue of gonadorelin (natural GnRH decapeptide) with amino acid (D-tryptophan) substitution in position 6 to inhibit rapid degradation for long activity. Used as triptorelin pamoate or acetate form, triptorelin is used as an antineoplastic in the palliative treatment of prostatic carcinoma, administered intramuscularly. Other analogues with two substituents in position 6 and 10 include Buserelin, Deslorelin. Goserelin, Histrelin, Leuprolide, Nafarelin,
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| SALES SPECIFICATION |
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APPEARANCE |
white to slightly yellowish powder |
| IDENTIFICATION |
pass (HPLC) |
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PURITY |
98.0% min |
| AMINO ACID | ±10% (theoretical Composition) |
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RELATED SUBSTANCES |
2.0% max (total impurity), 1.0% max (Individual impurity) |
| PEPTIDE CONTENT |
80.0%
min (N determination)
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| ACETATE CONTENT |
15.0% max |
| WATER CONTENT | 5.0% max |
| OPTICAL ROTATION | -65.0° ~ -75.0°(c=0.5, 95% HAc) |
| BACTERIAL ENDOTOXINS | 5EU/mg max |
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| PACKING |
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| PRICE INFORMATION |
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