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Triptorelin/GnRH 2mg/vial Is Used To Treat Hormone-dependent Diseases. CAS: 57773-63-4

Triptorelin/GnRH 2mg/vial Is Used To Treat Hormone-dependent Diseases. CAS: 57773-63-4

Triptorelin is a synthetic gonadotropin-releasing hormone (GnRH) decapeptide analog. Its molecular structure incorporates substitutions at the 6th and 10th amino acids of natural GnRH, significantly enhancing its affinity for receptors and greatly increasing its resistance to enzymatic degradation. Clinically, triptorelin exhibits a unique "bidirectional regulatory" mechanism: in the initial administration phase, it briefly stimulates the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH); however, with continued administration, it leads to desensitization and downregulation of pituitary GnRH receptors, thereby strongly inhibiting gonadotropin secretion and ultimately reducing testosterone or estradiol levels to a castration state.

Product Introduction

Methods of Administration (Key Points)

Route: Daily aqueous injection → subcutaneous injection in the abdomen/thigh; sustained-release microspheres/suspension → deep intramuscular injection in the buttock (Trelstar limited to IM, do not mix IV/SC).

Prostate Cancer (Androgen Deprivation): 3.75 mg IM/SC every 4 weeks; or 11.25 mg/12 weeks; or 22.5 mg/24 weeks. Anti-androgens (bicalutamide/cyproterone acetate) can be used to cover the flare-up 2–4 weeks before the first dose to prevent worsening of bone pain, urinary tract obstruction, and spinal cord compression.

Endometriosis/Uterine Fibroids: Starting from day 1–5 of the menstrual cycle, 3.75 mg every 4 weeks for 3–6 months (a second course is not recommended); add-back estrogen and progesterone can be used to alleviate hypoestria symptoms.

Central precocious puberty (CPP): 50 μg/kg body weight every 4 weeks (or 11.25 mg/12 weeks, 22.5 mg/24 weeks), discontinue when bone age is ≥12 years for girls and ≥13 years for boys.

Assisted reproduction (pituitary downregulation): Dapoxetine 0.1 mg SC daily, or mid-luteal long-acting gonadotropin 1.875–3.75 mg once daily, until estrogen levels reach target levels, then initiate gonadotropin.

Monitoring: Testosterone/estradiol ratio, LH/FSH ratio, bone mineral density (mandatory for >6 months of treatment), prostate symptoms, blood glucose, and blood lipids; women should use non-hormonal contraception for the first month of treatment, and start medication after ruling out pregnancy.

Contraindications: Pregnancy (Category X), hypersensitivity to GnRH analogs, non-hormone-dependent prostate cancer, castrated (surgical/medical) prostate cancer, active osteoporosis, progressive brain tumors (children).

 

Application Scenarios:
1. FDA-Approved Indications:
Advanced Prostate Cancer: Triptorelin is a first-line option for androgen deprivation therapy (ADT), inhibiting the proliferation and metastasis of androgen-dependent prostate cancer cells by lowering serum testosterone to castration levels.

2. Widespread Clinical Applications (Off-label/Global Registration):
Central Precocious Puberty (CPP): Used to inhibit premature activation of the hypothalamus-pituitary-gonadal axis, delaying bone age progression and protecting final adult height.

Endometriosis: Induces a hypoestrogenic state (pseudomenopause), inhibiting the growth of ectopic endometrial lesions and relieving pain symptoms.

Uterine Fibroids: Reduces fibroid volume preoperatively, decreasing intraoperative bleeding; or used for conservative treatment of patients with anemia.

Assisted Reproductive Technology (ART): Used in IVF cycles for down-regulation to prevent premature LH surges and achieve synchronized control of follicle development.

Breast Cancer: Used for ovarian castration treatment of hormone receptor-positive premenopausal breast cancer.

 

Storage Conditions:

To ensure the physical structure of the microsphere formulation and the bioactivity of the peptides, triptorelin has strict storage requirements: Unreconstituted (lyophilized powder/microspheres): Must be stored in a refrigerated environment at 2°C to 8°C (36°F to 46°F), protected from light and moisture. Freezing is strictly prohibited to avoid damaging the sustained-release structure of the microspheres.

Reconstituted (suspension): The reconstituted solution must be used immediately and cannot be stored or reused.

Transportation Requirements: Cold chain equipment should be used during transportation, avoiding severe vibration and direct sunlight.

 

FAQ
Q: What is the minimum order quantity?

A: The minimum order quantity is 10 bottles/set.

Q: How long does it take to ship? A: In-stock orders will be shipped within 24 hours.

Q: What purity level can you provide?

A: Standard purity 99%.

Q: Which courier service do you use?

A: FedEx, DHL, UPS, and postal services are available.

Q: How long does shipping take?

A: Approximately 10-15 days.

Q: Can you provide a COA (Certificate of Account) quality inspection report and HPLC (High-Performance Computing) report?

A: Yes, all goods undergo professional testing before shipment.

Q: Do you support OEM branding?

A: OEM branding is supported, subject to minimum order quantity requirements.

Q: What are your after-sales service terms?

A: After the customer receives the goods, if the quality problem is confirmed to be caused by our production, they can enjoy free replacement or refund. We adhere to a pragmatic and responsible service principle, actively responding to and properly handling all kinds of issues, without shirking responsibility or avoiding problems, and fully protecting customer rights.

Q: What payment methods are available?

A: We support bank transfer, Bitcoin, Transferwise, and Xoom.

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