Diphereline®

1. Overview of Diphereline

Diphereline is a drug containing the active ingredient Triptorelin — a synthetic peptide belonging to the group of GnRH agonists.
Triptorelin inhibits the production of gonadotropins (LH, FSH), and thereby inhibits the production of sex hormones (testosterone in males, estrogen in females).
Diphereline is formulated as a lyophilized powder + solvent, to be reconstituted into an injectable suspension — with various release versions (monthly, quarterly injections, etc.) depending on the dosage.

2. Ingredients & Dosage Forms

• Main active ingredient: Triptorelin (usually as acetate or embonate/pamoate depending on the version).

• Some common forms/dosages:

  • 0.1 mg — lyophilized powder for injection (often used for purposes such as reproductive assistance, infertility, uterine fibroids, cycle dependence)

  • 3.75 mg — 1-month prolonged-release form (intramuscular IM injection).

  • 11.25 mg — ~3-month prolonged-release form.

  • Other forms may exist (depending on manufacturer/country), depending on treatment needs and physician's guidance.

• Excipients/additives: include substances to create a prolonged-release suspension such as polymers (e.g., D,L-lactide/glycolide), mannitol, sodium carmellose, polysorbate 80, etc.

3. Mechanism of Action

Triptorelin in Diphereline acts as a GnRH (gonadotropin-releasing hormone) agonist. Upon injection, the drug initially stimulates the pituitary gland to release LH and FSH — causing a temporary surge in hormones — then continued use will "desensitize" the pituitary gland to GnRH, leading to reduced production of LH & FSH. The result is the inhibition of sex hormone production (testosterone/estrogen).
Thus, the drug reduces sex hormones — effective in hormone-dependent diseases such as prostate cancer, endometriosis, uterine fibroids, precocious puberty, etc.

4. Indications / Uses

Diphereline is used in various situations, depending on the dose and formulation. The main indications include:

• Treatment of Prostate cancer — especially advanced, hormone-dependent, or metastatic cases. It can be used as monotherapy or in combination with radiotherapy.

• Treatment of Central precocious puberty in children: used to "block" sex hormone production, delaying puberty when it occurs early.

• Assistance in treating female infertility (in artificial insemination/IVF protocols): with the aim of inhibiting sex hormones, controlling ovulation, in combination with gonadotropins to stimulate cyclical ovulation.

5. Dosage & Administration

Depending on the indication, Diphereline will have different doses and frequencies of use:

• 3.75 mg form (1-month release): intramuscular injection every 4 weeks.

• 11.25 mg form (~3-month release): injection every 3 months.

• 0.1 mg form (lyophilized powder for subcutaneous injection — commonly used in reproductive assistance or infertility): dose and duration depend on the regimen prescribed by the doctor. The drug should only be administered via injection (intramuscular or subcutaneous), not intravenously.

6. Side Effects, Contraindications & Precautions

Contraindications

• Hypersensitivity to triptorelin or any excipients of the drug.

• Pregnant or breastfeeding women — usually not used.

Side Effects & Precautions

• Some common reactions: hot flashes, increased sweating, flushing, mood changes, bone/joint pain, fatigue, pain at the injection site.

• May cause reduced bone density with long-term use (due to inhibition of sex hormones).

• For gynecological diseases (such as endometriosis, uterine fibroids), treatment should usually not be prolonged beyond 6 months.

• When used for IVF/infertility — strict monitoring under the guidance of a specialist doctor is required.

7. Assessment & General Role

Diphereline — with its active ingredient Triptorelin — has a clear mechanism of action: inhibiting sex hormones, thus playing an important role in the treatment of hormone-dependent diseases (prostate cancer, endometriosis, uterine fibroids), as well as regulating sexual development (precocious puberty) or assisting reproduction (IVF).
Thanks to various formulations with different release rates, Diphereline allows flexibility in treatment depending on the pathology, age, weight, and clinical needs.