1. 6-d-tryptophan-luteinizing Hormone-releasing Factor (pig)
2. Ay 25650
3. Ay-25650
4. Ay25650
5. Cl 118532
6. Cl-118532
7. Cl118532
8. D-trp-6-lh-rh
9. Decapeptyl
10. Decapeptyl Depot
11. Decapeptyl Lp
12. Decapeptyl Trimestral
13. Embonate, Triptorelin
14. Gnrh, Trp(6)-
15. Lhrh, Trp(6)-
16. Lhrh, Tryptophyl(6)-
17. Pamoate, Triptorelin
18. Trelstar
19. Trimestral, Decapeptyl
20. Triptorelin Embonate
21. Triptorelin Pamoate
22. Wy 42462
23. Wy-42462
24. Wy42462
1. 57773-63-4
2. Triptoreline
3. Arvekap
4. (d-trp6)-gnrh
5. Decapeptyl
6. Triptorelina
7. Triptorelinum
8. Trelstar
9. Triptodur
10. Diphereline
11. (6-d-tryptophan)luteinizing Hormone-releasing Hormone
12. Cl 118532
13. Cl-118532
14. Pglu-his-trp-ser-tyr-d-trp-leu-arg-pro-gly-nh2
15. Ay-25650
16. Luteinizing Hormone-releasing Factor (pig), 6-d-tryptophan
17. Cl 118,532
18. Chebi:63633
19. Wy 42462
20. Ay 25650
21. Pamorelin
22. Salvacyl
23. Trelstar Depot
24. 5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-tryptophyl-l-leucyl-l-arginyl-l-prolylglycinamide
25. Trelstar La
26. Luteinizing Hormone-releasing Factor (swine), 6-d-tryptophan-
27. Bim 21003
28. Wy 42422
29. Tryptorelin
30. Diferelin
31. D-tryptophan-lh-rh
32. Triptoreline [inn-french]
33. Triptorelinum [inn-latin]
34. Triptorelina [inn-spanish]
35. Trellasar
36. Moapar
37. Triptorelin [usan:inn:ban]
38. Decapeptyl Sr
39. Pamorelin La
40. Unii-9081y98w2v
41. Triptorelin (swine)
42. Wy-42462
43. D-trp6-lhrh
44. Debio-8206
45. Triptorelin (usan/inn)
46. (d-trp6)-lh-rh
47. Gtpl1177
48. Schembl5079698
49. Chembl1201334
50. Dtxsid2048375
51. Schembl22289009
52. Hms2090c17
53. Ex-a3857
54. Bim-21003
55. Akos030213249
56. 9081y98w2v
57. Cs-5745
58. Db06825
59. Ncgc00167301-01
60. Ncgc00167301-02
61. As-71149
62. Bn-52014
63. Hy-12551
64. 73t634
65. C75704
66. D06247
67. [d-trp6]-lh-rh, >=97% (hplc), Powder
68. Ab01275488-01
69. A936467
70. Pglu-his-trp-ser-tyr-d-trp-leu-arg-pro-glynh2
71. Q1992452
72. (s)-1-((3s,6s,9s,12s,15r,18s,21s)-3-((1h-imidazol-5-yl)methyl)-6,15-bis((1h-indol-3-yl)methyl)-21-(3-guanidinopropyl)-12-(4-hydroxybenzyl)-9-(hydroxymethyl)-18-isobutyl-1,4,7,10,13,16,19-heptaoxo-1-((s)-5-oxopyrrolidin-2-yl)-2,5,8,11,14,17,20-heptaazadocosan-22-oyl)-n-(2-amino-2-oxoethyl)pyrrolidine-2-carboxamide
73. Glycinamide, 5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-tryptophyl-l-leucyl-l-arginyl-l-prolyl-
| Molecular Weight | 1311.4 g/mol |
|---|---|
| Molecular Formula | C64H82N18O13 |
| XLogP3 | -0.3 |
| Hydrogen Bond Donor Count | 17 |
| Hydrogen Bond Acceptor Count | 15 |
| Rotatable Bond Count | 33 |
| Exact Mass | 1310.63087474 g/mol |
| Monoisotopic Mass | 1310.63087474 g/mol |
| Topological Polar Surface Area | 490 Ų |
| Heavy Atom Count | 95 |
| Formal Charge | 0 |
| Complexity | 2710 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 9 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
| 1 of 2 | |
|---|---|
| Drug Name | Trelstar |
| PubMed Health | Triptorelin (Injection) |
| Drug Classes | Antineoplastic Agent, Endocrine-Metabolic Agent |
| Drug Label | TRELSTAR is a white to slightly yellow lyophilized cake. When reconstituted, TRELSTAR has a milky appearance. It contains a pamoate salt of triptorelin, a synthetic decapeptide agonist analog of gonadotropin releasing hormone (GnRH). The chemical... |
| Active Ingredient | Triptorelin pamoate |
| Dosage Form | Injectable |
| Route | Intramuscular |
| Strength | eq 11.25mg base/vial; eq 3.75mg base/vial; eq 22.5mg base/vial |
| Market Status | Prescription |
| Company | Watson Labs |
| 2 of 2 | |
|---|---|
| Drug Name | Trelstar |
| PubMed Health | Triptorelin (Injection) |
| Drug Classes | Antineoplastic Agent, Endocrine-Metabolic Agent |
| Drug Label | TRELSTAR is a white to slightly yellow lyophilized cake. When reconstituted, TRELSTAR has a milky appearance. It contains a pamoate salt of triptorelin, a synthetic decapeptide agonist analog of gonadotropin releasing hormone (GnRH). The chemical... |
| Active Ingredient | Triptorelin pamoate |
| Dosage Form | Injectable |
| Route | Intramuscular |
| Strength | eq 11.25mg base/vial; eq 3.75mg base/vial; eq 22.5mg base/vial |
| Market Status | Prescription |
| Company | Watson Labs |
Triptorelin is indicated for the palliative treatment of advanced prostate cancer.
FDA Label
For the synchronisation of ovulation in weaned sows to enable a single fixed-time artificial insemination.
The first administration of triptorelin is followed by a transient surge of follicle stimulating hormone (FSH), luteinizing hormone (LH), estradiol,and testosterone. The time, peak and decline of testosterone in the body varies depending on the dose administered. This initial surge is often responsible for worsening of prostate cancer symptoms such as urethral or bladder outlet obstruction, bone pain, spinal cord injury and hematuria in the early stages. A sustained decrease in FSH and LH, and significant reduction of testicular steroidogenesis is usually seen 2-4 weeks post-initiation of therapy. This result is a reduction of serum testosterone to levels which are typically seen in surgically castrated men. Ultimately, tissues and functions that require these hormones become inactive. The effects of triptorelin can usually be reversed once the drug is discontinued.
Antineoplastic Agents, Hormonal
Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079) (See all compounds classified as Antineoplastic Agents, Hormonal.)
Luteolytic Agents
Chemical compounds that cause LUTEOLYSIS or degeneration of the CORPUS LUTEUM. (See all compounds classified as Luteolytic Agents.)
QH01CA97
L - Antineoplastic and immunomodulating agents
L02 - Endocrine therapy
L02A - Hormones and related agents
L02AE - Gonadotropin releasing hormone analogues
L02AE04 - Triptorelin
Absorption
Following IV administration of triptorelin, triptorelin is completely absorbed.
Route of Elimination
Elimination of triptorelin involves both the kidneys and the liver.
Volume of Distribution
After a single IV dose of 0.5mg, the volume of distribution of triptorelin peptide in healthy males was 30 - 33L.
Clearance
In healthy male volunteers, total clearance of triptorelin was 211.9 mL/min.
The metabolism of triptorelin in humans is not well understood; however, metabolism likely does not involve hepatic enzymes such as cytochrome P450. Whether or not triptorelin affects, or how it affects other metabolizing enzymes is also poorly understood. Triptorelin has no identified metabolites.
The pharmacokinetics of triptorelin follows a 3 compartment model. The half lives are estimated to be 6 minutes, 45 minutes, and 3 hours respectively.
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.
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