Progesterone Microspheres Pharmacokinetic - Pharmacodynamic (PK-PD) Study

Randomized, Controlled, Open-label, Parallel, Clinical Trial to Assess Pharmacokinetics and Endometrial Effect of an Injectable Formulation of Progesterone Microspheres in Doses of 50 mg, 100 mg, 200 mg and 300 mg, in Postmenopausal Women.

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01176175

Enrollment

Registered

2010-08-05

Start date

2010-08-31

Completion date

2011-02-28

Last updated

2011-10-13

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Infertility

Keywords

Progesterone, Microspheres, postmenopausal, Luteal phase support

Brief summary

Phase: I pharmacokinetic - pharmacodynamic (PK-PD) study. Main objective: To establish the minimum effective dose of progesterone microspheres suspension, which administered by weekly intramuscular injection, will be able to induce transformation from a proliferative endometrium to a secretory endometrium. Study design: Randomized, controlled, open-label, parallel, dose-response clinical trial. Sites: 1 Subjects: 48 postmenopausal women.

Detailed description

Sites: 1 Phase: 1 Main objective:To establish the minimum effective dose of progesterone microspheres suspension, which administered by weekly intramuscular injection, will be able to induce transformation from a proliferative endometrium to a secretory endometrium. Secondary objectives: * To determine and compare the steady-state pharmacokinetic profile of investigational products. * To evaluate safety profile of investigational products in the study subjects. * To evaluate local tolerability of investigational products in the study subjects. Study design:Randomized, controlled, open-label, parallel, dose-response clinical trial. Investigational products: * Progesterone microspheres intramuscular injectable suspension 50 mg * Progesterone microspheres intramuscular injectable suspension 100 mg * Progesterone microspheres intramuscular injectable suspension 200 mg * Progesterone microspheres intramuscular injectable suspension 300 mg Study subjects: 48 healthy postmenopausal women, 45 - 60 years. Brief description: After written informed consent, 48 eligible women will receive pretreatment with oral estradiol valerate, then, 14 days later, those with adequate endometrial thickness evaluated through ultrasound will be randomized to study treatments (one IM injection each 7 days, for a total of 7 doses). 10 days after the first progesterone dose, an endometrial biopsy will be obtained. Blood samples will be obtained for pharmacokinetic study.

Interventions

DRUGProgesterone

Progesterone microspheres injectable suspension 50 mg, intramuscular weekly injection for a total of 7 doses.

Study design

Allocation

RANDOMIZED

Intervention model

PARALLEL

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

FEMALE

Age

45 Years to 60 Years

Healthy volunteers

Yes

Inclusion criteria

* Female * 45 to 60 years old * Able to read and write * Postmenopausal * Body Mass Index equal or below 34.99 kg/m2 * Healthy * Normal uterus * Time availability

Exclusion criteria

* Hypersensitivity to progesterone or related compounds * Hypersensitivity to estrogens * Hysterectomy * History or present hormone-dependent tumor * History or present uterine cervix dysplasia * Abnormal and clinically-significant laboratory test results * Family history of breast cancer * History of thromboembolic disease * Non-controlled hypertension * History of stroke * History of cardiac valve surgery * Renal failure * Hepatic failure * Non-controlled diabetes * Severe gastrointestinal disease * History of serious neurologic disease * Reduced mobility * Anemia * Previous or concomitant hormonal therapy * Previous or concomitant therapy with inhibitors or inductors of cytochrome

Design outcomes

Primary

Measure	Time frame	Description
Endometrial dating through histopathologic criteria.	10 days	Endometrial dating according Noyes criteria as a measure of efficacy. At the moment of the biopsy, study subjects would have received 25 days of estradiol valerate pretreatment and 10 days of progesterone (investigational product); thus simulating the 25th day of a menstrual cycle. Efficacy will be measured as number of biopsies that have histological date according to cronological date.

Secondary

Measure	Time frame	Description
Pharmacokinetics	0 -60 days.	Progesterone plasmatic concentrations and pharmacokinetic parameters.
Adverse events	0 - 65 days	Number of Participants with Adverse Events as a Measure of Safety and Tolerability Pain Scores on a Visual Analog Scale

Countries

Mexico

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026