TRIPTORELIN

Product Name:TRIPTORELIN

Form:Acetate salt

Purity:95%

Storage:-20^oC

Cas No:57773-63-4

Molar Mass:1311.4

Chemical Formula:C64H82N18O13

Synonyms:Triptoreline; Triptorelina; Arvekap; Triptorelinum; Triptodur; (D-Trp6)-GnRH

IUPAC Name:(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide

SMILES:CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](CC2=CNC3=CC=CC=C32)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CN=CN7)NC(=O)[C@@H]8CCC(=O)N8

InChIKey:VXKHXGOKWPXYNA-PGBVPBMZSA-N

InChI:InChI=1S/C64H82N18O13/c1-34(2)23-46(56(88)75-45(13-7-21-69-64(66)67)63(95)82-22-8-14-52(82)62(94)72-31-53(65)85)76-58(90)48(25-36-28-70-42-11-5-3-9-40(36)42)78-57(89)47(24-35-15-17-39(84)18-16-35)77-61(93)51(32-83)81-59(91)49(26-37-29-71-43-12-6-4-10-41(37)43)79-60(92)50(27-38-30-68-33-73-38)80-55(87)44-19-20-54(86)74-44/h3-6,9-12,15-18,28-30,33-34,44-52,70-71,83-84H,7-8,13-14,19-27,31-32H2,1-2H3,(H2,65,85)(H,68,73)(H,72,94)(H,74,86)(H,75,88)(H,76,90)(H,77,93)(H,78,89)(H,79,92)(H,80,87)(H,81,91)(H4,66,67,69)/t44-,45-,46-,47-,48+,49-,50-,51-,52-/m0/s1

Sequence:XHWSYWLRPG

Target:GnRH

Application:Triptorelin is a potent gonadotropin-releasing hormone (GnRH) agonist used to regulate hormone levels by suppressing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It is widely utilized in the treatment of hormone-sensitive cancers such as prostate cancer, as well as in conditions like endometriosis, uterine fibroids, and central precocious puberty. Triptorelin acts by downregulating GnRH receptors, leading to decreased testosterone and estrogen production. Available in depot formulations, it provides sustained therapeutic effects with minimal dosing frequency. Current research explores its potential in assisted reproductive technologies and other endocrine disorders, broadening its applications in modern medicine.

Current Research:Triptorelin is an established GnRH agonist with a broad spectrum of clinical applications, particularly in hormone-related disorders and oncology. Its ability to suppress gonadal hormone secretion makes it a key therapeutic agent in the management of prostate cancer, breast cancer, and gynecological disorders such as endometriosis and uterine fibroids. Prostate Cancer Treatment Triptorelin is widely used in androgen deprivation therapy (ADT) for advanced prostate cancer. By reducing testosterone levels, it effectively inhibits tumor progression. Current research focuses on optimizing its long-term efficacy and safety, particularly in comparison to other GnRH analogs. Recent studies have also evaluated the impact of intermittent ADT using Triptorelin to reduce side effects such as osteoporosis and cardiovascular risks associated with continuous testosterone suppression. Endometriosis and Gynecological Disorders Triptorelin has demonstrated significant efficacy in treating endometriosis, a condition characterized by ectopic endometrial tissue growth. It induces a hypoestrogenic state, reducing lesion size and alleviating pain. Ongoing trials are investigating combination therapies with estrogen add-back therapy to mitigate hypoestrogenic side effects like osteoporosis and hot flashes. Similar research is being conducted for its role in uterine fibroids, where hormone suppression helps shrink fibroid size and control bleeding. Pediatric Endocrinology: Central Precocious Puberty (CPP) Triptorelin is an approved therapy for CPP, a condition where puberty onset occurs abnormally early. It effectively delays pubertal progression by suppressing gonadotropin secretion. Current studies aim to assess the long-term outcomes on reproductive function and bone health in patients treated with Triptorelin at a young age. Fertility and Assisted Reproductive Technology (ART) Triptorelin is also being explored in controlled ovarian stimulation protocols for in-vitro fertilization (IVF). Its ability to prevent premature luteinizing hormone (LH) surges enhances the success rate of ART procedures. Emerging research is investigating its role in ovarian hyperstimulation syndrome (OHSS) prevention, a common complication in fertility treatments. Emerging Research Areas Beyond its established applications, Triptorelin is being studied for potential roles in hormone-sensitive neurological disorders, transgender hormone therapy, and even as a neuroprotective agent in neurodegenerative diseases like Alzheimer's. As research continues, Triptorelin remains a crucial pharmaceutical agent with expanding therapeutic potential across multiple medical disciplines.

Reference:Wu, G., Zhou, F., Wang, H., Liu, K., Yu, D., Fan, L., ... & Shentu, J. (2024). Effectiveness, pharmacokinetics, and safety of triptorelin acetate microspheres in patients with locally advanced and metastatic prostate cancer. Therapeutic Advances in Medical Oncology, 16, 17588359241307818.