I. Basic Information

Chemical Structure: Composed of 10 amino acids with the sequence Pyro-Glu-His-Trp-Ser-Tyr-D-Leu-Arg-Pro-Gly-NH2. The acetate form increases stability and water solubility.

CAS Number: 33515 - 09 - 2 (free base); for the acetate form, the CAS number is 74381 - 53 - 6.
Molecular Weight: Approximately 1182.4 g/mol for the free base, slightly higher for the acetate.
Synonyms: Gonadorelin acetate, Luteinizing Hormone - Releasing Hormone (LHRH) analog.

II. Mechanism of Action
Physiological Effects:
Under normal physiological conditions, GnRH is secreted by the hypothalamus, periodically stimulating the pituitary gland to release luteinizing hormone (LH) and follicle - stimulating hormone (FSH), regulating the synthesis of sex hormones (such as estrogen, testosterone, etc.) in the gonads (ovaries/testes) and gamete production (ovulation, sperm maturation).
Gonadorelin acetate has a stronger binding ability to endogenous GnRH receptors, and its effect is dose - dependent:
Pulsatile low - dose administration: Mimicking the physiological secretion pattern, it promotes the release of LH/FSH, inducing ovulation or sperm production.
Continuous high - dose administration: It will lead to desensitization of pituitary GnRH receptors, inhibiting the secretion of LH/FSH, thus suppressing the synthesis of sex hormones (the effect of "medical castration").

Core mechanism:
Ovulation induction / Reproductive treatment: Stimulate ovarian ovulation through pulsatile drug administration, applicable to infertile patients with hypothalamic amenorrhea, etc.
Treatment of hormone-dependent diseases: Inhibit sex hormones through continuous drug administration, used for prostate cancer, breast cancer, uterine fibroids, endometriosis, etc.

Female:

Hypothalamic ovulatory disorder: Such as hypogonadotropic amenorrhea, induce follicular development and ovulation through pulsatile administration.

Assisted Reproductive Technology (ART): Used in combination with ovulation-stimulating drugs to regulate follicular synchronization (such as the "down-regulation" pretreatment in the in vitro fertilization cycle).

Male:

Hypogonadotropic hypogonadism: Pulsatile administration promotes testosterone synthesis and spermatogenesis, improving infertility.

III.Dosage Forms and Administration

1.Common Dosage Forms

Injection:

Short-acting preparation: Gonadorelin Acetate Injection (e.g., 100 µg/vial), which needs to be injected daily or every other day.

Long-acting sustained-release preparation: Microspheres (e.g., 3.75 mg, 11.25 mg), injected once every 2 - 4 weeks to maintain the drug concentration.

Nasal Spray: Some countries have nasal spray dosage forms (e.g., 100 µg/spray), but due to the low bioavailability (about 10%), it is rarely used clinically.

2.Dosage and Administration

Reproductive Ovulation Induction:

Pulsatile administration: Subcutaneously inject 5 - 20 µg every 90 minutes through a portable infusion pump until the follicles mature.

Prostate Cancer/Endometriosis:

Long-acting preparation: 3.75 mg subcutaneous injection, once every 4 weeks. A transient "flare-up" reaction may occur after the first administration (a transient increase in testosterone/estrogen, and anti-androgen drugs need to be used in combination for prevention).

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