Triptorelin Peptide CAS 57773-63-4

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Triptorelin peptide, also known as Lupron, is a synthetic decapeptide compound with a chemical structure similar to natural GnRH. Its molecular formula is C55H74N16O13, with a molecular weight of 1186.36. Qu Pu Rui Lin is a white or almost white powder, almost odorless and tasteless. It is highly soluble in water, and its aqueous solution is acidic with a pKa of 5.3. It has high stability and a half-life of up to 4 weeks in an aqueous solution with a pH of 4.5. Under low temperature conditions, triptorelin can be stably stored for a long time. The three peptide bonds contained in the molecule of triptorelin are important factors in its stability. In solution, it is not easy to form polymers between the molecules of triptorelin, which helps to maintain its biological activity. The mechanism of action lies in binding to the GnRH receptor on the pituitary cell membrane, causing receptor mediated chemical signal transduction and inhibiting the secretion of gonadotropins. Due to its high affinity with natural GnRH, triptorelin can occupy the GnRH receptors on the pituitary cell membrane, thereby preventing the binding of natural GnRH to its receptors and inhibiting the secretion of FSH and LH. This further inhibits the function of the ovaries and testes, reducing the secretion of sex hormones.

Triptorelin peptide is an artificially synthesized peptide drug with a chemical structure similar to natural gonadotropin-releasing hormone (GnRH), but with stronger biological activity. Since its inception, Triptorelin peptide has been widely used in the medical field, particularly in the treatment of reproductive endocrine disorders and certain tumors. The following is a detailed description of its purpose:

The clinical application effect in the treatment of prostate cancer

 

Prostate specific antigen (PSA) is a glycoprotein secreted by prostate epithelial cells, and its levels are typically elevated in prostate cancer patients. PSA level is one of the important indicators for evaluating the condition and treatment effectiveness of prostate cancer. Multiple clinical studies have shown that the use of Triptorelin peptide significantly reduces PSA levels in prostate cancer patients. For example, in a study targeting patients with advanced prostate cancer, approximately 80% of patients treated with Triptorelin peptide experienced a decrease of over 50% in PSA levels within 3 months after treatment. Prostate cancer patients often experience lower urinary tract symptoms (such as frequent urination, urgency, pain, difficulty urinating, etc.), bone pain (such as lower back pain, hip pain, etc.), and sexual dysfunction. Triptorelin peptide treatment can significantly alleviate these symptoms and improve patients' quality of life. For example, in a study of prostate cancer patients with bone metastases, approximately 70% of patients treated with Triptorelin peptide showed significant relief in bone pain symptoms.

Extending survival and reducing the risk of tumor recurrence

 

Triptorelin peptide treatment can prolong the survival of prostate cancer patients. Multiple long-term follow-up studies have shown that patients who receive Triptorelin peptide castration treatment have significantly longer survival compared to those who do not receive castration treatment. For example, in a study targeting patients with locally advanced or metastatic prostate cancer, the median survival of patients receiving Triptorelin peptide castration treatment was approximately 12 months longer than those who did not receive castration treatment. For early prostate cancer patients, surgery or radiotherapy are the main treatment methods. However, some patients may still experience tumor recurrence after treatment. Triptorelin peptide, as an adjuvant therapy, can reduce the risk of tumor recurrence. For example, in a study targeting high-risk prostate cancer patients, patients treated with Triptorelin peptide in combination after surgery or radiation therapy had a 5-year recurrence free survival rate that was approximately 15% higher than those who did not receive adjuvant therapy.

Application in the treatment of endometriosis

 

Triptorelin peptide treatment can significantly alleviate symptoms such as dysmenorrhea, chronic pelvic pain, and sexual pain in patients with endometriosis. For example, in a randomized controlled trial of patients with endometriosis, patients treated with Triptorelin peptide showed a significant decrease in pain scores at 3 and 6 months after treatment compared to before treatment, and the efficacy was better than that of the placebo group. Imaging examination shows that Triptorelin peptide treatment can reduce the volume of lesions in some patients with endometriosis. Through examination methods such as ultrasound and magnetic resonance imaging (MRI), it can be observed that the size, quantity, and activity of ectopic lesions have improved after treatment. For endometriosis patients with fertility needs, Triptorelin peptide treatment can improve the pelvic environment, reduce adhesions, and increase the success rate of natural conception or assisted reproductive technologies. Some studies have reported that the pregnancy rate of patients undergoing in vitro fertilization embryo transfer (IVF-ET) has increased after pretreatment with Triptorelin peptide.

Application in the treatment of uterine fibroids

 

Triptorelin peptide treatment can significantly reduce the volume of uterine fibroids. Generally speaking, after 3-6 months of treatment, the volume of fibroids can shrink by 30% -50%. The reduction of fibroid volume can alleviate pressure on surrounding tissues and alleviate related symptoms. For patients with increased menstrual flow and prolonged periods caused by uterine fibroids, Triptorelin peptide treatment can significantly reduce menstrual flow and restore normal menstruation. This helps prevent and treat anemia, improving the quality of life for patients. Pre treatment with Triptorelin peptide before uterine fibroid surgery can reduce fibroid volume, decrease pelvic congestion, lower surgical difficulty and bleeding volume, and shorten surgical time. Especially for patients with large fibroids, severe adhesions, or planning to undergo laparoscopic surgery, preoperative use of Triptorelin peptide can improve the safety and success rate of the surgery.

There have been numerous descriptions of the experimental method for the synthesis of triptorelin peptide in the literature. In the following text, we will introduce one of these methods to briefly describe how we produce this product in the laboratory.

The specific experimental steps are as follows:

1. Synthesis of 2-bromo-4-aminobenzoate ethyl ester

Add ethyl 2-bromo-4-chlorobenzoate (30g, 0.1mol) and methanol (50mL) to a 250mL three necked bottle equipped with a stirrer, thermometer, and reflux condenser, heat to reflux, and after dissolution, add ammonia water (30mL). After the reaction is completed, pour the reaction solution into ice water, extract with ether, dry and distill, collect the fraction at 100 ℃, and obtain a colorless oily liquid of 2-bromo-4-aminobenzoate ethyl ester (27.5g, 99%) with a melting point of 73-74 ℃.

2. Synthesis of 2-bromo-4- (2 '- pyridyl) benzoyl chloride

In a 500mL three necked bottle equipped with a stirrer, thermometer, and reflux condenser, add ethyl 2-bromo-4-aminobenzoate (27.5g, 0.1mol) and methanol (30mL), heat until dissolved, then add an aqueous solution of sodium hydroxide (10g, 0.25mol) (20mL), and heat and reflux for 3 hours. After the reaction is complete, pour the reaction solution into ice water and extract with ether. After drying, distill and recover ether, collect the fraction at 170-173 ℃, and obtain sodium 2-bromo-4-aminobenzoate (25g). Place this product in a 500mL three necked bottle equipped with a stirrer, thermometer, and reflux condenser, add DMF (50mL), heat until dissolved, add ethyl 2-pyridinecarboxylate (18g, 0.1mol), heat and reflux for 3 hours. After the reaction is complete, pour the reaction solution into ice water and extract with ether. After drying, distill and recover ether, collect fractions at 185-187 ℃, and obtain ethyl 2-bromo-4- (2 '- pyridyl) benzoate (30g). Finally, add phosphorus trichloride (34g, 0.25mol) to anhydrous dichloromethane, heat until dissolved, cool to room temperature, add 2-bromo-4- (2 '- pyridyl) ethyl benzoate (30g), heat and reflux for 3 hours. After the reaction is complete, pour the reaction solution into ice water and extract with ether. Distill and recover ether and dichloromethane after drying, collect fractions at 83-85 ℃, and obtain a colorless oily liquid of 2-bromo-4- (2 '- pyridyl) benzoyl chloride (27g). Melting point: 66-68 ℃.

3. Synthetic Triptorelin

Add 2-bromo-4- (2 '- pyridyl) benzoyl chloride (15g, 0.05mol) and anhydrous tetrahydrofuran (50mL) to a 500mL three necked bottle equipped with a stirrer, thermometer, and reflux condenser. Heat until dissolved, then add N-ethyl-1,2-dihydro-4-pyrrolidone (8g, 0.07mol) and reflux for 3 hours. After the reaction is complete, pour the reaction solution into ice water and extract with ether. After drying, distill and recover tetrahydrofuran and ether, collect fractions at 165-167 ℃, and obtain white solid triptorelin (16g). Melting point: 168-171 ℃.

Triptorelin peptide is an antipsychotic drug, and its pharmacokinetics mainly include processes such as absorption, distribution, metabolism, and excretion.

1. Absorption:

After oral administration, triptorelin is rapidly absorbed with a bioavailability of approximately 100%. Food can slow down its absorption rate, but it does not affect the overall absorption amount. The drug is metabolized through the liver for the first time, producing the main active metabolites.

2. Distribution:

Triptorelin is widely distributed in the body, with a binding rate of up to 83% with plasma proteins. It can cross the blood-brain barrier and enter the central nervous system. Triptorelin can also be secreted through milk.

3. Metabolism:

Triptorelin is mainly metabolized in the liver through the CYP3A4 enzyme system. Metabolites include the active metabolite N-demethyltriptoreline, as well as other secondary metabolites. Metabolites have strong anti histamine and 5-HT2 receptor antagonistic effects.

4. Excretion:

The excretion of triptorelin is mainly through urine, accounting for about 73%, with the majority being metabolites. About 20% of drugs are excreted through feces.

5. Half life:

The half-life of triptorelin is 6-7 hours, while the half-life of its metabolite N-demethyltriptorelin is 9-12 hours. Therefore, triptorelin and its metabolites need to be administered daily or twice a day to maintain stable blood drug concentrations.

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