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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

Phase 2
18 Years
Not Enrolling
Uterine Fibroids

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Trial Information

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.

Inclusion Criteria:

- Female patients with measurable uterine fibroids confirmed by vaginal or abdominal
ultrasound, deemed otherwise healthy.

- A body mass index in the range 18 to 28.

- Oestradiol, progesterone, luteinizing hormone and follicle stimulating hormone
results within the range of normal ovarian function.

- Regular menstruation (except for symptoms of fibroids).

- Females of childbearing potential who are sexually active must agree to use barrier
contraception, and can neither be pregnant nor lactating from Screening throughout
the duration of the study.

Exclusion Criteria:

- Acute pelvioperitonitis, ovarian cysts, persistent corpus luteum.

- History of bilateral oophorectomy, hysterectomy, or hypophysectomy.

- Clinically relevant abnormal history, physical findings, or laboratory values at the
pre-study screening assessment that could interfere with the objectives of the study
or the safety of the patient.

- Presence of acute or chronic illness or history of chronic illness sufficient to
invalidate the patient participation in the study or make it unnecessarily hazardous.

- Impaired endocrine, thyroid, hepatic, respiratory or renal function, diabetes
mellitus, coronary heart disease, or history of any psychotic mental illness.

- Presence or history of severe adverse reaction to any drug.

- Participation in other clinical studies of a new chemical entity or a prescription
medicine within the previous 3 months.

- Presence or history of drug or alcohol abuse, or smoking of more than 10 cigarettes

- Evidence of drug abuse on urine testing.

- Positive test for hepatitis B, hepatitis C, human immune deficiency virus 1 or human
immune deficiency virus 2.

- Severe bleedings from fibroids.

- Anemia (hemoglobin less than 11 g/dL), loss of more than 400 mL blood during the 3
months before the study.

- Use of oral contraceptives or other estrogen containing medication, progestins,
danazol, progesterone antagonists, antiandrogens, steroids or gonadotropins which
might affect sex steroid production or activity or assay (e.g. norethindrone) within
30 days prior to study enrolment.

Type of Study:


Study Design:

Allocation: Randomized, Endpoint Classification: Pharmacodynamics Study, Intervention Model: Parallel Assignment, Masking: Open Label, Primary Purpose: Treatment

Outcome Measure:

Percentage of measured E2 (17β-estradiol) Serum Concentrations less than or equal to 30 pg/mL.

Outcome Time Frame:

Weeks 5 through Final Visit.

Safety Issue:


Principal Investigator

Medical Director

Investigator Role:

Study Director

Investigator Affiliation:

Takeda Pharma GmbH


European Union: European Medicines Agency

Study ID:




Start Date:

June 2006

Completion Date:

July 2007

Related Keywords:

  • Uterine Fibroids
  • Leiomyoma
  • Uterine Fibroids
  • Drug Therapy
  • Uterine Neoplasms
  • Fibroid Tumor
  • Leiomyoma
  • Myofibroma