Triptorelin

human trialNo statistically significant difference in overall survival was reported between triptorelin-based treatment arms¹⁴

human trialTriptorelin pamoate 22.5 mg (6-month prolonged release formulation) achieves luteinizing hormone (LH) suppression in Chinese children with central precocious puberty¹⁶

human trialAt month 6, 100% of patients achieved LH suppression (stimulated peak LH ≤ 5 IU/L after gonadotropin-releasing hormone stimulation)¹⁶

human trialLH suppression was maintained at month 12 in 98.5% of patients¹⁶

human trialMean basal and peak LH and follicle-stimulating hormone levels were suppressed throughout follow-up¹⁶

human trialAll patients at months 3 to 12 had sex hormone suppression to prepubertal levels¹⁶

human trialStable or reduced breast development was seen for 98.4% of girls at month 6 and 93.5% at month 12¹⁶

human trialAll boys had regression or stable genital development until month 12¹⁶

human trialMean growth velocity decreased from 9.82 cm/year at baseline to 5.88 cm/year at month 6 and 5.17 cm/year at month 12¹⁶

human trialMean bone age/chronological age ratio decreased from 1.27 at baseline to 1.23 at month 6 and 1.21 at month 12¹⁶

human trial64.5% of girls showed decreased uterine length at month 6 and 12 versus baseline¹⁶

human trial75.0% of boys showed stable testicular volume versus baseline¹⁶

human trial11.25 mg/90 days formulation suppresses pituitary-gonadal axis in short-term trials¹⁷

human trial22.5 mg/6 month formulation suppresses pituitary-gonadal axis¹⁷

human trialQuarterly formulation able to suppress pituitary-gonadal axis and pubertal development with similar end-results as monthly formulation¹⁷

human trialTriptorelin (Decapeptyl) is a 1-month formulation GnRHa approved in the EU as adjuvant treatment in combination with tamoxifen or aromatase inhibitor for endocrine-responsive early-stage breast cancer in premenopausal women at high risk of recurrence¹⁸

human trialOvarian function suppression with triptorelin added to tamoxifen provided significant benefit in premenopausal breast cancer patients after adjusting for prognostic factors¹⁸

human trialOFS plus tamoxifen produced more pronounced benefits in disease control and increased overall survival in higher-risk patients who had previously received chemotherapy¹⁸

human trialOFS plus exemestane produced more pronounced benefits in disease control compared with OFS plus tamoxifen¹⁸

human trialGonadotropin-releasing hormone analogues (including triptorelin) are associated with relief of pain due to endometriosis¹⁹

human trialGonadotropin-releasing hormone analogues (including triptorelin) are associated with increased clinical pregnancy rates in women with endometriosis¹⁹

human trialCastrate serum testosterone levels were achieved in a geometric mean time of 18.8 days²¹

human trialBy day 29, 97.5% of patients had castrate serum testosterone levels²¹

human trialCastrate serum testosterone levels were maintained from months 2 to 12 in 93.0% of patients²¹

human trialPrior to the second injection at month 6, 98.3% of patients had castrate serum testosterone levels²¹

human trial98.3% of patients had castrate serum testosterone levels at study completion²¹

human studyDECAPEPTYL-induced down-regulation of the pituitary can prevent the LH surge and thereby prevent premature ovulation and/or follicular luteinisation⁴

human studyFollowing the first administration, there is a transient surge in circulating levels of luteinizing hormone (LH), follicle-stimulating hormone (FSH), testosterone, and estradiol⁶

human studyAfter chronic and continuous administration, usually 2 to 4 weeks after initiation of therapy, a sustained decrease in LH and FSH secretion and marked reduction of testicular and ovarian steroidogenesis is observed⁶

human studyIn men, a reduction of serum testosterone concentration to a level typically seen in surgically castrated men is obtained⁶

human studyTriptorelin acetate microspheres demonstrated effectiveness in patients with locally advanced and metastatic prostate cancer⁷

human studyTriptorelin elicited significantly higher FSH peaks than gonadorelin, while LH peaks were comparable¹³

human studyFSH/LH ratios were higher after triptorelin compared to gonadorelin¹³

human studyOptimal diagnostic LH peak cut-off of 7.14 IU/L following triptorelin administration showed sensitivity 94% and specificity 96%¹³

human studySubcutaneous triptorelin provides excellent diagnostic accuracy for CPP diagnosis, comparable to gonadorelin¹³

human studyTriptorelin improves pain symptoms caused by endometriosis²⁰

human studyTriptorelin reduces the volume of endometriotic nodules during treatment²⁰

expert opinionMonitoring of testosterone levels needs to improve in routine practice and physicians should not overlook the benefits of continued ADT in their patients when introducing one of the various new treatment options for CRPC³

expert opinionGnRH analogs are considered the therapy of choice for central precocious puberty and generally have supplanted medroxyprogesterone in this form of precocity¹²

expert opinionGnRH analogs are ineffective as primary therapy in the treatment of GnRH-independent precocious puberty, including familial male precocious puberty (testotoxicosis), congenital virilizing adrenal hyperplasia, and McCune-Albright syndrome¹²

expert opinionThe drug has shown significant efficacy in both clinical and real-world settings²⁹

human trialGnRH agonists offer the advantage of sustained efficacy even after one or two days of withdrawal, while the effect disappears as soon as administration is stopped²²

human studyAfter administration of triptorelin there is an initial and transient increase in circulating follicle-stimulating hormone (FSH) and luteinising hormone (LH) levels (flare-up)⁴

human studyContinued administration of triptorelin results in decreased FSH and LH secretion with a consequent marked reduction in gonadal hormone production⁴

human studyTriptorelin is a potent inhibitor of gonadotropin secretion when given continuously and in therapeutic doses⁶

human studyGnRH-a have been used to induce a hypoestrogenic status in women with endometriosis with the aim to cause an improvement in pain symptoms similar to that observed after menopause²⁰

in vitroPLGA is the key component of long acting drug products responsible for providing sustained release in a controlled manner²⁴

expert opinionAndrogen deprivation therapy (ADT) aims to reduce testosterone to levels obtained by surgical castration³

expert opinionTriptorelin is a gonadotrophin releasing hormone (GnRH) agonist that inhibits gonadotrophin secretion when given continuously and in therapeutic doses⁴

expert opinionGnRH causes the pituitary gland to release two more hormones called luteinizing hormone (LH) and follicle-stimulating hormone (FSH)¹¹

expert opinionTreatments for CPP weaken the effects of GnRH signaling on the pituitary gland, reducing the release of hormones that cause puberty¹¹

expert opinionTriptorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin)¹²

expert opinionTriptorelin is structurally related to leuprolide and goserelin¹²

expert opinionTriptorelin is a gonadotropin-releasing hormone (GnRH) analogue with enhanced affinity for GnRH receptors and a prolonged half-life due to its resistance to enzymatic degradation.²⁸

expert opinionTriptorelin acts as an agonist analog of gonadotropin-releasing hormone, repressing expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).²⁸

expert opinionIt is a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2).²⁸

expert opinionTriptorelin acetate is a synthetic peptide analogue of gonadotropin-releasing hormone (GnRH)²⁹

expert opinionTriptorelin acetate falls under the category of GnRH agonists²⁹

expert opinionTriptorelin acetate binds to GnRH receptors in the pituitary gland, causing an initial surge in LH and FSH levels, followed by a downregulation of these receptors and a consequent decrease in the production of sex hormones such as testosterone and estrogen²⁹

theoreticalTriptorelin is a Luteinizing Hormone-Releasing Hormone (LHRH) Analog¹

theoreticalTriptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH or GnRH) with greater potency than the naturally occurring LHRH⁶

human trial3.75 mg/28 day triptorelin depot formulation used in trials comparing treated and untreated children until adult height¹⁷

human trial6-month formulation of triptorelin embonate designed to deliver 22.5 mg of triptorelin over a 6-month period²¹

human trialDelayed-release formulations of triptorelin allow doses to be spaced by intervals of several weeks, or even three months²²

human studySustained-release 1-, 3- and 6-month formulations of triptorelin, administered intramuscularly or subcutaneously, have been developed to provide improved flexibility and convenience for the patient³

expert opinionAdminister 3.75-mg formulation of triptorelin pamoate (Trelstar) by IM injection every 4 weeks (28 days), 11.25-mg formulation (Trelstar) every 12 weeks, or the 22.5-mg extended-release formulation (Trelstar, Triptodur) every 24 weeks¹²

expert opinionFor central precocious puberty in pediatric patients ≥2 years of age: 22.5 mg every 24 weeks as the 22.5-mg formulation¹²

expert opinionFor prostate cancer: 3.75 mg every 4 weeks (28 days) as the 3.75-mg formulation, 11.25 mg every 12 weeks as the 11.25-mg formulation, or 22.5 mg every 24 weeks as the 22.5-mg formulation¹²

expert opinionFor early-stage breast cancer: 3.75 mg every 4 weeks has been used in combination with endocrine therapy¹²

expert opinionTriptorelin acetate is typically administered via intramuscular or subcutaneous injection²⁹

expert opinionThe drug is available in various formulations, including monthly, quarterly, and semi-annual doses²⁹

human trialFollowing intramuscular administration, serum testosterone levels initially increased, followed by a rapid, sustained decrease²¹

human trialThe biological half life of triptorelin injected by the subcutaneous route is 10 times greater than that observed after intravenous injection because of the progressive release of the peptide from the injection site²²

human studyPituitary suppression is maintained for at least 6 days after stopping administration⁴

human studyAfter discontinuation of DECAPEPTYL, LH levels return to baseline after approximately 2 weeks⁴

human studySystemic bioavailability of triptorelin is close to 100% after subcutaneous administration⁴

human studyFollowing a single dose of triptorelin 250 micrograms s.c. in healthy male subjects, the mean maximum plasma concentration was 5.68 ng/mL⁴

human studyMaximum plasma concentrations were reached approximately 45 minutes after s.c. administration⁴

human studyFollowing i.v. bolus injection of 500 micrograms triptorelin, the drug is distributed and eliminated according to a 3-compartment model with half-lives of 3.2 minutes, 46.1 minutes, and 5.1 hours⁴

human studyThe estimated volume of distribution at steady-state of triptorelin was 28.9 L⁴

human studyThe mean terminal half-life was 5.1 hours following i.v. bolus injection of 500 micrograms triptorelin to 19 female subjects⁴

human studyAverage total clearance was estimated to 107 mL/min⁴

human studyRenal clearance over 24 hours was on average 25.3 mL/min⁴

human studyMean percentage of the dose recovered in urine over 24 hours was 16.7%⁴

human studyFollowing a single intramuscular (IM) injection of TRELSTAR ää DEPOT to healthy male volunteers, serum testosterone levels first increased, peaking on day 4, and declined thereafter to low levels by week 4⁶

human studyIn healthy volunteers, testosterone serum levels returned to near baseline by week 8⁶

human studyAfter intravenous (IV) bolus administration, triptorelin is distributed and eliminated according to a 3-compartment model and corresponding half-lives are approximately 6 minutes, 45 minutes, and 3 hours⁶

human studyTriptorelin pamoate is not active when given orally⁶

human studyIntramuscular injection of the depot formulation provides plasma concentrations of triptorelin over a period of 1 month⁶

human studyThe plasma concentrations declined to 0.084 ng/mL at 4 weeks⁶

human studyThe volume of distribution following an IV bolus dose of 0.5 mg of triptorelin peptide was 30-33 L in healthy male volunteers⁶

human studyThere is no evidence that triptorelin, at clinically relevant concentrations, binds to plasma proteins⁶

human studyThe metabolism of triptorelin in humans is unknown, but is unlikely to involve hepatic microsomal enzymes (cytochrome P-450)⁶

human studyTriptorelin acetate microspheres has characterized pharmacokinetics in prostate cancer patients⁷

human studyPeak LH occurred predominantly at 180 min after triptorelin in both CPP and NPT groups (78% and 90%, respectively)¹³

human studyTriptorelin half-life increase is similar to renal impairment²³

human studyPatients with hepatic impairment had 2- to 4-fold higher exposure (AUC) values than younger²³

human studyThe elimination half-life for patients with hepatic impairment was 6.6 h (Group II), 7.7 h (Group III) and 7.6 h (Group IV), but significantly longer than in healthy volunteers (2.8 h for Group I).²⁸

in vitroTrelstar contains PLGA with lactide:glycolide ratio of 52:48²⁴

in vitroPLGA in Trelstar possesses ester end-caps²⁴

expert opinionTriptorelin is excreted by the kidney.²⁸

expert opinionIn the management of prostate cancer, testosterone levels generally begin to decline within a week of the first injection, with castration levels achieved within 2 to 4 weeks²⁹

expert opinionIn the treatment of precocious puberty, the clinical effects of hormone suppression can be observed within the first few weeks of therapy²⁹

human trialTriptorelin acetate microspheres have a safety profile suitable for use in prostate cancer treatment⁸

human trialThe most common adverse reactions (≥ 5%) during TRELSTAR 3.75 mg therapy included hot flushes, skeletal pain, impotence, and headache⁹

human trialThe most common adverse reactions (≥ 5%) during TRELSTAR 11.25 mg therapy included hot flushes, skeletal pain, headache, edema in legs, and leg pain⁹

human trialThe most common adverse reactions (≥ 5%) during TRELSTAR 22.5 mg therapy included hot flushes, erectile dysfunction, and testicular atrophy⁹

human trialAnaphylactic shock, hypersensitivity, and angioedema have been reported with TRELSTAR⁹

human trialThe use of GnRH agonists may lead to an increased risk of metabolic changes such as hyperglycemia, diabetes, hyperlipidemia, and non-alcoholic fatty liver disease⁹

human trialIncreased risk of myocardial infarction, sudden cardiac death and stroke has been reported in men treated with GnRH agonists⁹

human trialConvulsions have occurred in patients treated with GnRH analogs including TRELSTAR with or without a history of predisposing factors⁹

human trialAndrogen deprivation therapy with TRELSTAR may prolong the QT interval⁹

human trialTRELSTAR may cause fetal harm and may impair fertility in females and males of reproductive potential⁹

human trialThis transient increase in testosterone may worsen prostate cancer and result in spinal cord compression and urinary tract obstruction¹⁰

human trialThe use of GnRH agonists may lead to an increased risk of metabolic changes such as hyperglycemia, diabetes, hyperlipidemia, and non-alcoholic fatty liver disease¹⁰

human trialIncreased risk of myocardial infarction, sudden cardiac death and stroke has been reported in men¹⁰

human trialConvulsions have occurred in patients treated with GnRH analogs including TRELSTAR with or without a history of predisposing factors¹⁰

human trialSevere Cutaneous Adverse Reactions (SCARs) have been reported in patients receiving GnRH agonists, including triptorelin products¹⁰

human trialAndrogen deprivation therapy may prolong the QT interval¹⁰

human trialAnaphylactic shock, hypersensitivity, and angioedema have been reported¹⁰

human trialTRELSTAR may cause fetal harm¹⁰

human trialTRELSTAR may impair fertility¹⁰

human trialMost common adverse reactions (≥ 5%) during TRELSTAR 3.75 mg therapy included hot flushes, skeletal pain, impotence, and headache¹⁰

human trialMost common adverse reactions (≥ 5%) during TRELSTAR 11.25 mg therapy included hot flushes, skeletal pain, headache, edema in legs, and leg pain¹⁰

human trialMost common adverse reactions (≥ 5%) during TRELSTAR 22.5 mg therapy included hot flushes, erectile dysfunction, and testicular atrophy¹⁰

human trialTriptodur was also found to be safe and well tolerated with no unexpected side effects¹¹

human trialThe most common side effects of Triptodur include injection site reactions, menstrual (vaginal) bleeding, hot flush, headache, cough, and infections¹¹

human trial13 patients (19.7%) had 22 drug-related treatment emergent adverse events; no grade ≥ 3 TEAEs were reported¹⁶

human trialOFS plus tamoxifen combination showed increased endocrine symptom burden, with more frequent vasomotor symptoms and thromboembolic events¹⁸

human trialOFS plus exemestane combination showed increased musculoskeletal symptoms, decreased libido, osteoporosis and fractures¹⁸

human trialGonadotropin-releasing hormone analogues (including triptorelin) are associated with a higher incidence of adverse events¹⁹

human trialTriptorelin embonate 22.5 mg was generally well tolerated in patients with advanced prostate cancer²¹

human trialAdverse events were of mild severity in the majority of patients²¹

human trialDrug-related adverse events were consistent with the pharmacological action of triptorelin, including hot flushes²¹

human trialInjection-site reactions occurred in 6.7% of triptorelin embonate recipients²¹

human trialGnRH agonists induce initial hyperstimulation of the gonadotrophs (flare up) characteristic of the superagonistic effect, while GnRH antagonists do not²²

human studyMost patients receiving ADT progress to castration-resistant prostate cancer (CRPC)³

human studyThese effects are usually reversible after cessation of therapy⁶

human studyTriptorelin acetate microspheres has established safety profile in patients with locally advanced and metastatic prostate cancer⁷

human studyAnaphylactic shock, hypersensitivity, and angioedema have been reported with triptorelin¹²

human studyIncreased gonadotropin and sex steroid concentrations and subsequent transient increase in clinical signs and symptoms of puberty (e.g., vaginal bleeding) may occur during initial weeks of therapy or following subsequent doses in pediatric patients with precocious puberty¹²

human studyPossible worsening of signs and/or symptoms of prostate cancer and/or development of new manifestations (e.g., bone pain, neuropathy, hematuria, urethral or bladder outlet obstruction) due to transient increase in serum testosterone concentrations during initial weeks of therapy¹²

human studyPossible spinal cord compression contributing to weakness or paralysis in patients with prostate cancer; possibly fatal¹²

human studyAmong 18,541,994 eligible FAERS reports, 4018 primary suspect reports involving triptorelin were identified¹⁵

human studyDisproportionality analysis revealed 102 statistically significant Preferred Terms (PTs) for adverse events¹⁵

human studyUnexpected statistical signals warranting further investigation included defiant behavior and Alzheimer's dementia¹⁵

human studyThe median time-to-onset (TTO) of adverse events was 132 days (interquartile range [IQR] 36-361 days)¹⁵

human studyAdverse event reporting exhibited a bimodal distribution, with the highest proportions occurring within the first month (22.59%) and after more than one year (25.07%) following administration¹⁵

human studyDistinct statistical signal profiles were observed between genders¹⁵

human studyNo long term-adverse events on reproductive function are reported with triptorelin depot in CPP treatment¹⁷

human studyRare but serious adverse events may occur with triptorelin depot¹⁷

expert opinionCommon side effects may include hot flashes, decreased libido, erectile dysfunction, and injection site reactions such as pain, redness, and swelling²⁹

expert opinionMore serious but less common side effects can include bone pain, mental/mood changes such as depression, and cardiovascular events like heart attack and stroke²⁹

expert opinionContraindications for Triptorelin acetate include pregnancy, as the drug can cause harm to the fetus, and hypersensitivity to GnRH, GnRH agonists, or any other components of the formulation²⁹

expert opinionConcurrent use of hormone therapy or medications that affect pituitary function can interfere with the action of Triptorelin acetate²⁹

expert opinionDrugs that prolong the QT interval, such as certain antiarrhythmics, antipsychotics, and antibiotics, should be used with caution as Triptorelin acetate may exacerbate this condition²⁹

human trialTriptorelin is approved for palliative treatment of advanced prostate cancer¹²

human trialTriptorelin is approved for treatment of central precocious puberty (CPP) in pediatric patients ≥2 years of age¹²

human trialTriptorelin was used as adjuvant treatment for hormone receptor-positive early breast cancer in premenopausal patients¹⁴

human studyOvarian suppression with triptorelin in combination with endocrine therapy (i.e., anastrozole, exemestane, letrozole, tamoxifen) as adjuvant therapy in premenopausal women with early-stage hormone receptor-positive breast cancer may be considered a reasonable choice¹²

human studyRapid-acting subcutaneous triptorelin has been proposed as a reliable alternative to native GnRH for GnRH stimulation testing¹³

human studyTriptorelin offers a practical and reliable diagnostic alternative in clinical practice for CPP diagnosis¹³

human studyTriptorelin is a gonadotropin-releasing hormone (GnRH) agonist approved by the FDA for treating advanced prostate cancer, endometriosis, and central precocious puberty (CPP) in children aged ≥2 years¹⁵

human studyTriptorelin depot is largely used to treat central precocious puberty (CPP) in children¹⁷

expert opinionTriptorelin depot treatment of CPP should be restricted to tertiary pediatric endocrinology centers¹⁷

expert opinionTriptorelin is one of the most commonly used GnRH-a²⁰

expert opinionPre-operative administration of triptorelin prior to surgical excision of endometriomas may be useful in preserving the ovarian reserve²⁰

expert opinionTriptorelin is used to treat prostate cancer as part of androgen deprivation therapy.²⁸

expert opinionTriptorelin is used for hormone replacement therapy to suppress testosterone or estrogen levels in transgender people.²⁸

expert opinionTriptorelin can be used as a puberty blocker in the case of precocious puberty.²⁸

expert opinionIt is a pivotal drug in the treatment of hormone-responsive cancers such as prostate cancer²⁹

expert opinionTriptorelin acetate plays a crucial role in managing endometriosis, uterine fibroids, and precocious puberty²⁹