NCT02042196

Brief Summary

As women get older and go through menopause, levels of the female reproductive hormone estradiol decrease to low levels. Also with aging, the functioning of the arteries declines. Over time this vascular dysfunction can lead to health problems such as high blood pressure and heart disease. This study is being done to help determine what causes arteries to become unhealthy in postmenopausal women, who have low levels of the female reproductive hormone estradiol. In this study we will test whether low levels of tetrahydrobiopterin (BH4), a natural substance in the body that can cause the arteries to expand, explains why arteries become unhealthy in women with low levels of estradiol. To answer this question, we will study how vascular function changes with a medication that causes a short-term increase in BH4 levels when estradiol is lowered with a medication, compared to when estradiol is normal. We will also determine whether the administration of the antioxidant vitamin C, along with the medication to increase BH4 levels, will normalize vascular health in perimenopausal and postmenopausal women, and in women who have their estradiol levels lowered.

Trial Health

87
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
100

participants targeted

Target at P75+ for early_phase_1

Timeline
Completed

Started Dec 2013

Typical duration for early_phase_1

Geographic Reach
1 country

1 active site

Status
completed

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

Study Start

First participant enrolled

December 1, 2013

Completed
2 months until next milestone

First Submitted

Initial submission to the registry

January 17, 2014

Completed
5 days until next milestone

First Posted

Study publicly available on registry

January 22, 2014

Completed
2.3 years until next milestone

Primary Completion

Last participant's last visit for primary outcome

May 2, 2016

Completed
Same day until next milestone

Study Completion

Last participant's last visit for all outcomes

May 2, 2016

Completed
Last Updated

July 11, 2019

Status Verified

July 1, 2019

Enrollment Period

2.4 years

First QC Date

January 17, 2014

Last Update Submit

July 9, 2019

Conditions

Keywords

endothelial functionwomenestrogen deficiencysex hormonesadiposityoxidative stressantioxidants

Outcome Measures

Primary Outcomes (1)

  • Change in brachial artery flow-mediated dilation

    4-5 years

Secondary Outcomes (1)

  • Change in carotid artery compliance and endothelial cell protein expression

    4-5 years

Study Arms (3)

Pre or Early perimenopausal 1

EXPERIMENTAL

Baseline experiment: Subjects randomized to either 1) KUVAN (10mg/kg body weight) crossover to placebo OR 2) placebo crossover to KUVAN Hormone modification: GnRH antagonist with Cetrotide (0.25mg/d) + placebo transdermal patch, then subjects randomized again to either 1) KUVAN crossover to placebo OR 2) placebo crossover to KUVAN

Drug: KUVANDrug: PlaceboDrug: CetrotideDrug: Placebo transdermal patch

Pre or Early Perimenopausal 2

EXPERIMENTAL

Baseline experiment: Subjects randomized to either 1) KUVAN crossover to placebo OR 2) placebo crossover to KUVAN Hormone modification: Estrogen add-back with Cetrotide + Climara (0.075mg/d), then subjects randomized again to either 1) KUVAN crossover to placebo OR 2) placebo crossover to KUVAN

Drug: KUVANDrug: PlaceboDrug: CetrotideDrug: Climara

Late Perimenopausal and Postmenopausal

EXPERIMENTAL

Subjects randomized to either 1) KUVAN crossover to placebo OR 2) placebo crossover to KUVAN No hormone modification.

Drug: KUVANDrug: Placebo

Interventions

KUVANDRUG

KUVAN will be given orally at 10mg/kg dose per body weight. KUVAN will be dissolved in 4-8oz water and consumed within 15 minutes.

Also known as: Tetrahydrobiopterin or BH4
Late Perimenopausal and PostmenopausalPre or Early Perimenopausal 2Pre or Early perimenopausal 1

Placebo pills designed to match the dissolvable KUVAN pills

Also known as: Control
Late Perimenopausal and PostmenopausalPre or Early Perimenopausal 2Pre or Early perimenopausal 1

Cetrotide (0.25mg/d) will be taken daily for 10 days via abdominal subcutaneous injection.

Also known as: Cetrorelix acetate
Pre or Early Perimenopausal 2Pre or Early perimenopausal 1

0.075mg/d transdermal patch will be placed on skin.

Also known as: Estradiol transdermal patch
Pre or Early Perimenopausal 2

Inactive transdermal patch

Also known as: Control
Pre or Early perimenopausal 1

Eligibility Criteria

Age18 Years - 70 Years
Sexfemale
Healthy VolunteersYes
Age GroupsAdult (18-64), Older Adult (65+)

You may qualify if:

  • age criteria established for pre-, peri- and postmenopausal women, and if postmenopausal at least 1 year beyond menopause
  • resting blood pressure \<140/90 mmHg 81; 2) plasma glucose concentrations \<110 mg/dl under fasting conditions
  • sedentary or recreationally active (\<3 days of vigorous aerobic exercise)
  • no use of OCs, HT, or other medications that might influence cardiovascular function
  • nonsmokers
  • no use of vitamin supplements, NSAIDS or willing to stop use for duration of the study
  • not taking any other medications that would interact with cetrotide, E2 patch, or Kuvan® to confound interpretation of results

You may not qualify if:

  • history of or active estrogen-dependent neoplasms, acute liver or gallbladder disease, vaginal bleeding, venous thromboembolism, hypertriglyceridemia, and CVD
  • known allergy to transdermal patch, GnRHant (i.e., hypersensitivity to cetrorelix, extrinsic peptide hormones, mannitol, GnRH, benzyl alcohol - the vehicle for injection of cetrorelix), or KUVAN
  • history of stomach ulcer or bleeding
  • other contraindications to HRT, GnRHant, and KUVAN (i.e., taking Levodopa, medications that can inhibit folate metabolism including methotrexate)
  • pregnant or currently breastfeeding
  • Other conditions for which individuals will be excluded from the study include: diabetes, active infection, history of seizures or disease that affects the nervous system, sepsis or an abnormal resting ECG

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Study Sites (1)

University of Colorado Denver

Aurora, Colorado, 80045, United States

Location

MeSH Terms

Conditions

Obesity

Interventions

sapropterincetrorelixEstradiol

Condition Hierarchy (Ancestors)

OverweightOvernutritionNutrition DisordersNutritional and Metabolic DiseasesBody WeightSigns and SymptomsPathological Conditions, Signs and Symptoms

Intervention Hierarchy (Ancestors)

EstrenesEstranesSteroidsFused-Ring CompoundsPolycyclic CompoundsEstradiol CongenersGonadal Steroid HormonesGonadal HormonesHormonesHormones, Hormone Substitutes, and Hormone Antagonists

Study Officials

  • Kerrie Moreau, PhD

    University of Colorado School of Medicine

    PRINCIPAL INVESTIGATOR

Study Design

Study Type
interventional
Phase
early phase 1
Allocation
RANDOMIZED
Masking
QUADRUPLE
Who Masked
PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
Purpose
BASIC SCIENCE
Intervention Model
PARALLEL
Sponsor Type
OTHER
Responsible Party
SPONSOR

Study Record Dates

First Submitted

January 17, 2014

First Posted

January 22, 2014

Study Start

December 1, 2013

Primary Completion

May 2, 2016

Study Completion

May 2, 2016

Last Updated

July 11, 2019

Record last verified: 2019-07

Locations