Triptorelin

Mechanism (as reported)

A review of endometriosis research described GnRH agonists as used to induce a hypoestrogenic status in women with endometriosis; triptorelin is presented as one of the commonly used GnRH agonists in that context. (PMID: 24832495)

Key findings (each cites a source)

• A review reported that studies of triptorelin in endometriosis demonstrated efficacy for improving pain symptoms associated with endometriosis, and that this was supported by reductions in the volume of endometriotic nodules during treatment. [PMID 24832495]
• In advanced prostate cancer, results from a noncomparative multicentre pivotal trial reported that a 6-month formulation of triptorelin embonate achieved and maintained castrate serum testosterone levels, with castrate levels achieved by day 29 in 97.5% of patients and maintained from months 2 to 12 in 93.0% of patients. [PMID 20166771]
• In advanced prostate cancer, the same trial reported that adverse events were generally of mild severity in the majority of patients and that injection-site reactions occurred in 6.7% of triptorelin embonate recipients. [PMID 20166771]
• A phase 3 open-label single-arm trial in Chinese children with central precocious puberty reported that at month 6, all patients had luteinizing hormone (LH) suppression (stimulated peak LH ≤5 IU/L) and that this was maintained at month 12 in 98.5% of patients. [PMID 39412628]
• In the phase 3 CPP trial, mean basal and peak LH and follicle-stimulating hormone levels were reported as suppressed throughout follow-up, and sex hormone suppression to prepubertal levels was reported for all patients at months 3 to 12. [PMID 39412628]
• In the phase 3 CPP trial, drug-related treatment emergent adverse events were reported in 19.7% of patients, and no grade ≥3 treatment emergent adverse events were reported. [PMID 39412628]
• A review of triptorelin depot use in children with CPP reported that long experience is available and summarized that quarterly formulation seems able to suppress the pituitary-gonadal axis and pubertal development and to determine similar end-results as monthly formulation, while noting that additional trials are needed and some uncertainties remain to be optimized. [PMID 29957076]
• A study investigated silk fibroin-based nanoparticle-loaded polymeric microneedles for transdermal delivery of triptorelin and reported increased transdermal release of triptorelin (~65%), a prolonged drug half-life, and increased relative bioavailability after administration to rats. [PMID 37387211]
• In the microneedle study, surging levels of luteinizing hormone and estradiol in plasma and their subsequent prolonged downregulation were reported as indicating the potential therapeutic role of the system in ART regimens. [PMID 37387211]