3 Months, Open-Label, Parallel-Group Study of the Pharmacodynamics, Pharmacokinetics and Safety of TAP-144SR 1-month Depot Gelatin-Free vs. Gelatin-Containing Formulation in Female Patients With Uterine Fibroids
Gonadotropin-releasing hormone, also called luteinizing hormone releasing hormone, is a
neuropeptide hormone released from the hypothalamus. Gonadotropin-releasing hormone binds to
specific gonadotropin-releasing hormone receptors in the cell membrane of pituitary gland
cells, inducing the cells to produce and release the gonadotropins: luteinizing hormone and
follicle-stimulating hormone. Luteinizing hormone and follicle-stimulating hormone are
released into the general circulation and stimulate the gonads to produce and release the
sex steroids: testosterone and estrogen. Follicle-stimulating hormone also controls
Suppression of gonadotropin secretion is an effective treatment for conditions such as
prostate cancer, endometriosis and central precocious puberty, because these conditions
respond to manipulation of the sex steroids. Suppression of gonadotropin secretion can be
achieved by administration of gonadotropin-releasing hormone agonists that, after an initial
transient stimulation of gonadotropin release, reversibly desensitize pituitary
gonadotropin-releasing hormone receptors. Desensitization is thought to occur by
down-regulation of the numbers of gonadotropin-releasing hormone receptors and uncoupling of
the receptors from the biochemical pathway that leads to gonadotropin release. Termination
of gonadotropin-releasing hormone agonist administration reverses the desensitization, and
gonadotropin and sex hormone levels return to normal.
There are several marketed gonadotropin-releasing hormone agonists, one of which is TAP-144
(leuprorelin), an active synthetic nonapeptide gonadotropin-releasing hormone analogue. In
the present study, the existing leuprorelin 1- month sustained release formulation will be
compared with a new gelatin-free 1-month sustained release formulation.
Allocation: Randomized, Endpoint Classification: Pharmacodynamics Study, Intervention Model: Parallel Assignment, Masking: Open Label, Primary Purpose: Treatment
Percentage of measured E2 (17β-estradiol) Serum Concentrations less than or equal to 30 pg/mL.
Weeks 5 through Final Visit.
Takeda Pharma GmbH
European Union: European Medicines Agency
ENG K001 GF