Triptorelin Injection 11.25 Mg

Triptorelin Injection 11.25 mg serves as a core clinical intervention for childhood central precocious puberty, a specialized developmental disorder marked by early onset of puberty and shortened growth cycles, manifesting as premature secondary sexual characteristics and aberrant growth velocity. Without timely and standardized management, this condition disrupts normal physical and psychological development, creates mismatches between physiological maturation and mental cognition, compromises adult final height irreversibly, and induces psychological distress including inferiority, sensitivity, and anxiety, impairing social function and overall well-being. It overcomes the drawbacks of conventional therapies, exerting gentle and precise regulation of physiological signals to decelerate abnormal sexual development, prevent early epiphyseal fusion, preserve growth potential, and redirect pubertal progression toward a normal timeline, establishing itself as a vital clinical option to safeguard the healthy growth of children with central precocious puberty.

 

Our Products Description

 

triptorelin peptide

Triptorelin Injection 11.25 mg

triptorelin tablets

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Triptorelin COA

Certificate of Analysis
Compound name	Triptorelin
Grade	Pharmaceutical grade
CAS No.	57773-63-4
Quantity	30g
Packaging standard	PE bag+Al foil bag
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202601090066
MFG	Jan 9th 2026
EXP	Jan 8th 2029
Structure
Item	Enterprise standard	Analysis result
Appearance	White or almost white powder	Conformed
Water content	≤5.0%	0.54%
Loss on drying	≤1.0%	0.42%
Heavy Metals	Pb≤0.5ppm	N.D.
	As≤0.5ppm	N.D.
	Hg≤0.5ppm	N.D.
	Cd≤0.5ppm	N.D.
Purity (HPLC)	≥99.0%	99.98%
Single impurity	<0.8%	0.52%
Total microbial count	≤750cfu/g	95
E. Coli	≤2MPN/g	N.D.
Salmonella	N.D.	N.D.
Ethanol (by GC)	≤5000ppm	500ppm
Storage	Store in a sealed, dark, and dry place below -20°C

Symptom relief and abnormal regulation of endometriosis

The core problem caused by endometriosis lies in the detachment of endometrial tissue from the normal growth area, abnormal proliferation and accumulation in the pelvic cavity, which leads to a series of chain reactions of discomfort. This type of abnormal proliferation of tissues can disrupt the inherent physiological balance order of the pelvic cavity, disrupt the normal operation of various organs in the pelvic cavity, not only induce periodic pain reactions, but also lead to the swelling and adhesion of abnormal tissues in the pelvic cavity. In the long run, it can seriously affect the daily work and work efficiency of the population, and even cause emotional distress and anxiety, further increasing the physical and mental burden.

Triptorelin Injection 11.25 mg abandons the stiffness of traditional intervention methods and, with its gentle and precise regulatory logic, moderately regulates the physiological transmission signals related to estrogen in the body. It can effectively alleviate current discomfort symptoms and regulate the growth of abnormal tissues from the root, achieving a dual effect of symptom relief and abnormal tissue control. This can be analyzed in detail from two core dimensions:

01

Relieve various types of pain and discomfort, gradually restore pelvic comfort.

The pain caused by endometriosis is not a single manifestation, but presents obvious periodicity and diversity. The most typical one is the severe pain during menstruation, which often accompanies the onset of menstruation. When the severity is severe, it can cause symptoms such as pale complexion, cold sweat, and nausea and vomiting, seriously affecting normal walking and sleep; In addition, pelvic pain and bloating may also occur during non menstrual periods, and some people may also experience soreness and discomfort in the lumbar and sacral regions, especially after fatigue and prolonged sitting.

Which can significantly worsen and long-term affect daily activities and quality of life. It gently regulates estrogen related signaling in the body, reducing the stimulation response of abnormal proliferative tissues in the pelvic cavity to peripheral nerves and organs, gradually easing the severity of menstrual pain, relieving non menstrual pelvic pain and lumbar soreness, restoring a stable and comfortable state inside the pelvic cavity, reducing the interference of pain on daily life, work, and emotions, and helping people gradually return to a normal pace of life.

02

Reduce abnormal proliferative tissue and inhibit the further development and spread of lesions.

The essence of endometriosis is the abnormal growth and accumulation of endometrial tissue in other parts of the pelvic cavity, resulting in abnormal lesions of varying sizes and shapes. These types of lesions can continuously stimulate normal tissues and organs around the pelvic cavity, not only exacerbating pain symptoms, but also potentially causing pelvic adhesions, organ dysfunction, and other subsequent problems, further increasing the burden on the body.

Triptorelin Injection 11.25 mg precisely regulates the physiological messengers in the body, inhibits the growth and vitality of abnormal endometrial tissue, slows down its proliferation and accumulation rate, gradually reduces the volume of lesions, prevents further spread, enlargement, and expansion of lesions, reduces the stimulation and damage of abnormal tissue to pelvic organs, alleviates various troubles caused by diseases from the root, creates favorable conditions for self repair of the body, and helps people gradually improve pelvic health status.

Information source:

-Zhang Min, Li Juan Observation of the clinical application of triptorelin in preoperative intervention for uterine fibroids [J]. Primary Medicine Forum, 2020, 24 (12): 1689-1690
-Wang Li, Zhao Jing The effect of preoperative application of triptorelin on muscle mass volume and bleeding in patients with uterine fibroids [J]. Chinese Journal of Maternal and Child Health, 2019, 34 (18): 4187-4189

How to reduce the intervention effect of bleeding

Abnormal bleeding caused by uterine fibroids is one of the common preoperative troubles. Long term or frequent abnormal bleeding not only affects the patient's physical condition, but may also lead to preoperative physical weakness and increase surgical risks. This precisely regulates physiological signals in the body, reduces the frequency and amount of abnormal bleeding before surgery, and maintains a stable state of the body before surgery. This can be explained from two key dimensions:

Reduce the frequency of abnormal bleeding and relieve physical burden

Patients with uterine fibroids often experience irregular bleeding during non menstrual periods, excessive bleeding during menstrual periods, and other abnormal conditions. Such bleeding can disrupt the normal circulation of the body, leading to long-term discomfort such as fatigue and dizziness, which can affect preoperative physical reserves. Triptorelin Injection 11.25 mg can reduce the frequency of non menstrual bleeding, shorten the duration of menstrual bleeding, gradually restore stable bleeding, reduce the consumption of abnormal bleeding on the body, and create favorable conditions for preoperative body conditioning by regulating relevant physiological transmission mechanisms.

Control the amount of bleeding and reduce the risk of intraoperative bleeding

Excessive preoperative bleeding can lead to insufficient blood volume in patients, increase the risk of intraoperative anemia exacerbation, shock, and affect the safety of surgery. It can selectively inhibit the stimulation of muscle blocks on surrounding blood vessels, reduce the probability of vascular rupture and bleeding, slow down local blood circulation speed, control the amount of bleeding each time, avoid physical weakness caused by excessive bleeding before surgery, and lay a solid foundation for surgical safety.

Information source:

-Liu Yan, Chen Ming Clinical value analysis of preoperative treatment of uterine fibroids with triptorelin in improving anemia [J]. Journal of Practical Gynecological Endocrinology, 2021, 8 (05): 78-80

-Chen Li, Yang Fang Exploration of the efficacy and safety of preoperative application of triptorelin in uterine fibroids [J]. Chinese Journal of Practical Medicine, 2020, 15 (23): 123-125

 

Phase 1: Initial excitement (1-2 weeks, brief increase in testosterone, "flare effect")

1-7 days after the first administration of triptorelin, due to its high affinity binding to pituitary GnRHR, the receptor is continuously activated, triggering transient explosive secretion of LH and FSH, resulting in a brief increase in testosterone levels (peak 1.5-2 times baseline), which is called the "flare effect" (testosterone flicker).
Molecular mechanism: After binding to GnRHR, triptorelin activates the Gq-PLC-IP3 pathway, releasing Ca ² ⁺ from the endoplasmic reticulum. Gonadotropin producing cells (LH/FSH synthesis cells) rapidly degranulate, releasing a large amount of stored LH/FSH;

Simultaneously promoting the transcription of LH/FSH genes (LHB, FSHB), continuously releasing newly synthesized hormones, with LH peak reaching 20-50 mIU/mL and testosterone peak reaching 800-1500 ng/mL.
Clinical risk (aggravation of androgen dependent tumors): The flare effect lasts for 7-14 days, and a brief increase in testosterone can stimulate prostate cancer cell proliferation, worsen bone pain, and worsen urinary tract obstruction, especially in patients with advanced bone metastases, who may experience pathological fractures, spinal cord compression, and other emergencies.
Preventive strategy: Combination with anti androgen drugs (such as bicalutamide 50 mg/day), starting 1-2 weeks before the administration of triptorelin, to block the effect of testosterone on cancer cells and completely eliminate the clinical risk of flare effect.

Phase 2: Receptor desensitization (2-4 weeks, rapid decrease in testosterone)

After 2-4 weeks of continuous administration, pituitary gonadotropin cells' GnRHR is continuously occupied and overactivated by triptorelin, initiating the receptor negative feedback regulation mechanism and entering a desensitized state.
Molecular mechanism (receptor downregulation core):
Receptor internalization: Overactivated GnRHR rapidly engulfs the cell, fuses with lysosomes for degradation, and reduces the number of receptors on the cell membrane surface by 50% -70%;

Receptor desensitization: The remaining cell membrane receptors undergo conformational changes, resulting in loss of G protein coupling ability. Even when bound to triptorelin, downstream signaling pathways cannot be activated;

Gene transcriptional repression: GnRHR gene (GNRHR) transcription is downregulated, new receptor synthesis is reduced, and the total number of cell membrane receptors continues to decrease to 10% -20% of normal levels;
LH/FSH synthesis inhibition: After receptor desensitization, LH/FSH gene transcription (LHB, FSHB) is completely inhibited, and LH/FSH synthesis and release sharply decrease (to 5% -10% of baseline).
Dynamics of testosterone decline: After rapid reduction of LH, the raw material for testosterone synthesis in Leydig cells of the testes is cut off, and serum testosterone rapidly decreases from its peak: it drops to 200-300 ng/dL at 2 weeks, 50-100 ng/dL at 3 weeks, and remains stable at<50 ng/dL (castration level) at 4 weeks.

Phase 3: Long term inhibition (after 4 weeks, testosterone stable castration, reversible)

After continuous administration for 4 weeks, the pituitary gland was completely desensitized, GnRHR remained in a sustained low expression state, LH/FSH remained at extremely low levels (<1 mIU/mL), and testosterone remained stable at castration levels (<50 ng/dL, 90% of patients<20 ng/dL), achieving long-term and deep testosterone castration.
Molecular mechanism (sustained low hormone state): Long acting preparations of triptorelin are continuously released, maintaining a blood drug concentration of * *>0.06 ng/mL (effective inhibition threshold), continuously occupying the remaining GnRHR, preventing endogenous GnRH binding, and preventing the pituitary gland from restoring sensitivity to GnRH. LH/FSH secretion remains low, and testosterone synthesis continues to stagnate.

Reversibility (core feature): 3-6 months after discontinuation, GnRHR expression gradually returns (reaching 80% normal at 6 months), LH/FSH secretion returns to normal, testosterone levels gradually return to physiological levels (500-1000 ng/dL), and reproductive function can be reversibly restored, which is different from surgical castration (permanent irreversible).
The correlation between castration depth and efficacy: Patients with testosterone levels below 20 ng/dL (deep castration) experience a greater decrease in PSA levels (96% -98%), a 30% reduction in tumor progression risk, and a 20% extension in survival; Patients who maintain testosterone levels between 20-50 ng/dL (mild castration) have significantly reduced efficacy, therefore the clinical goal is testosterone levels below 20 ng/dL.

The overall effect of testosterone castration (prerequisite for androgen dependent tumor suppression)

Triptolide achieves dynamic regulation of testosterone from physiological level to transient increase, rapid decrease, and long-term castration through HPG axis three-level inhibition, completely depriving prostate cancer cells of androgen growth driving signals, laying a core foundation for inhibiting tumor proliferation, angiogenesis, and metastasis.
Equivalence of testosterone castration: The testosterone inhibitory effect of 3.75 mg/4 weeks of triptorelin is completely equivalent to bilateral orchidectomy (testosterone<50 ng/dL), but it preserves the reversibility of reproductive function, avoids surgical trauma, and has higher psychological acceptance. It has completely replaced surgical castration and become the preferred ADT for prostate cancer.

References：

1. Chinese Medical Association Urology Branch. Guidelines for Endocrine Therapy of Prostate Cancer (2025 Edition) [J]. Chinese Journal of Urology, 2025. (Testosterone Castration Grading, Flare Effect Prevention)
2. PMC. Triptorelin: Mechanisms of Action and Clinical Applications in Prostate Cancer [J]. 2024.( The molecular mechanism of receptor desensitization and the kinetics of testosterone reduction are studied on the Chinese urological tumor MDT platform. Expert consensus on testosterone monitoring in castration treatment for prostate cancer [J]. 2021. (Deep castration criteria, efficacy correlation)
3. Dingxiangyuan Medication Assistant. Adverse reactions and management of triptorelin acetate [Z]. 2026. (Clinical risk of flare effect)

 

In summary, the abnormal proliferation and ectopic accumulation of endometrial tissue in the pelvic cavity are the root cause of endometriosis, which seriously disrupts the pelvic physiological balance and the normal function of pelvic organs. It not only induces persistent periodic pain and pelvic tissue adhesion, but also imposes heavy physical and mental burdens on patients, affecting their daily life, work efficiency and emotional state. Timely and standardized intervention is crucial to alleviate discomfort, prevent disease progression, reduce physical and mental distress, and help patients restore normal quality of life.

References

-Zhao Xiao, Sun Jing Study on the effect of triptorelin on preoperative muscle mass reduction and intraoperative bleeding of uterine fibroids [J]. Journal of Modern Chinese and Western Medicine, 2019, 28 (30): 3367-3370

-Li Na, Zhang Yan The effect of preoperative intervention with triptorelin on anemia status and postoperative recovery in patients with uterine fibroids [J]. Journal of Clinical Rational Drug Use, 2022, 15 (11): 102-104

-Wang Jing, Li Li The application effect of triptorelin in preoperative treatment of uterine fibroids and its impact on patients' qi and blood status [J]. China Rural Medicine, 2020, 27 (08): 32-33

-Wang Yan, Liu Min Clinical observation of preoperative application of triptorelin to reduce the volume of uterine fibroids [J]. Journal of Practical Clinical Medicine, 2019, 23 (16): 89-91

FAQ

• What is triptorelin injection used for?

Triptorelin Injection 11.25 mg is used to treat advanced prostate cancer. It is a hormone that is similar to the one normally released from the hypothalamus gland in the brain. When given on a regular basis to men, it decreases testosterone levels which helps treat prostate cancer.

• How long does a triptorelin injection last?

There are 2 types of triptorelin. We given as an injection into a muscle (intramuscular). It can be given every 28 days (4 weeks), or as a longer-acting injection every 3 or 6 months.

• Where is the injection?

You usually have it as an injection into a muscle (intramuscular), in your buttock or upper thigh. If you're having a type called Gonapeptyl Depot, you can have the injection under the skin (subcutaneous injection) into your tummy (abdomen), thigh or top of your arm.

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