Drug intelligence / Profile preview

triptoreline + estradiol

Development stage
Unknown
Lead developer
Rouen University Hospital
Modality
Peptides, Small Molecules
Administration
Intravenous, Percutaneous
01

Overview

Triptoreline + estradiol is a combination hormonal regimen evaluated in the MESURE (MEdical versus SUrgical management of Rectal Endometriosis) Phase 3 randomized clinical trial (NCT01973816). This regimen consists of triptoreline, a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH), and estradiol, a naturally occurring steroid hormone. Triptoreline acts as a GnRH receptor agonist that, upon continuous administration, induces pituitary desensitization and suppresses the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to a profound hypoestrogenic state and therapeutic amenorrhea, which is used to treat deep rectal endometriosis by shrinking endometriotic lesions. Estradiol is co-administered as "add-back" therapy to mitigate the side effects associated with estrogen deficiency, such as bone mineral density loss and vasomotor symptoms. In the MESURE trial, triptoreline was administered as a 11.25 mg intravenous dose in two consecutive 3-month cures, paired with daily 0.5% percutaneous estradiol gel.

Other names
triptorelin + estradioltriptoreline and estradioltriptoreline/estradiol
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)GPER1 (G protein-coupled estrogen receptor 1)ESR1 (ERα)ESR2 (ERβ)

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