Comparison of PKs of 17-Beta-Estradiol Via Sublingual Placement Versus Swallowing in Male-to-Female Transgender Patients

NCT05428215 | Terminated Phase 4 FDA Drug

• 1 other identifier: 1737257
• Study Type: interventional
• Target: 2
• Locations: 1 country
• Sites: 1

Brief Summary

This crossover study will investigate the pharmacokinetics of oral versus sublingual administration of 17-beta-estradiol in the trans-female population.

Conditions

Gender Dysphoria

Keywords

estradiol; gender-affirming estrogen

Outcome Measures

Primary Outcomes (1)

• Estradiol absorption

  Mean area under the curve of estradiol

  Over 24 hours

Secondary Outcomes (5)

• Peak serum estradiol

  Peak over 24 hour period

• Serum estradiol Nadir

  24 hours from last estradiol administration

• Suppression of Testosterone

  24 hours from last estradiol administration on Study Day 14 and 28

• Serum estrone to estradiol ratio

  Hours from administration of estradiol: 0, 1, 2, 4, 6, and 8 hours

• Sex hormone binding globulin

  0 hours from estradiol administration on Study Day 14 and 28

Study Arms (2)

PO then SL

ACTIVE COMPARATOR

Subjects will administer 17-beta-estradiol orally (PO) for Study Day 1-14, followed by administration of 17-beta-estradiol sublingually (SL) for Study Day 15-28.

Drug: 17beta Estradiol

SL then PO

ACTIVE COMPARATOR

Subjects will administer 17-beta-estradiol sublingually (SL) for Study Day 1-14, followed by administration of 17-beta-estradiol orally (PO) for Study Day 15-28.

Drug: 17beta Estradiol

Interventions

17beta Estradiol DRUG

Subjects will take individualized therapeutic dose of 17-beta-estradiol via sublingual and oral administration

PO then SL; SL then PO

Eligibility Criteria

• Age: 18 Years+
• Gender Eligibility Details: Transgender male-to-female
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• English speaker
• Currently taking 17-beta-estradiol tablet daily via sublingual or oral route on dose therapeutic for gender-affirming therapy; steady dose for at least 4 weeks
• Serum estradiol and testosterone levels within target therapeutic range (75-200 pg/mL and \<55 ng/dL, respectively)

You may not qualify if:

• Active or history of deep venous thrombosis/pulmonary embolism
• Active or recent (within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction)
• Liver dysfunction
• History of breast cancer
• History of orchiectomy
• Known sensitivity or allergy to any components of the study medication
• Taking potent CYP3A4 inhibitors or inducers

Sponsors & Collaborators

• MaineHealth: lead

Study Sites (1)

Maine Medical Center

Portland, Maine, 04102, United States

Location

MeSH Terms

Conditions

Gender Dysphoria

Interventions

Estradiol

Condition Hierarchy (Ancestors)

Sexual Dysfunctions, Psychological; Mental Disorders

Intervention Hierarchy (Ancestors)

Estrenes; Estranes; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Estradiol Congeners; Gonadal Steroid Hormones; Gonadal Hormones; Hormones; Hormones, Hormone Substitutes, and Hormone Antagonists

Study Officials

• Katherine Davis, MD

  MaineHealth

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 4
• Allocation: RANDOMIZED
• Masking: TRIPLE
• Who Masked: CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Physician- MH Obstetrics and Gynecology

Model Details: Each subject will take their individualized dose of 17B-estradiol tablet orally for 2 weeks and sublingually for 2 weeks. The subject will then take their same dose of 17B-estradiol via the other means of administration for 2 weeks. The order in which this occurs will be randomized.

Study Record Dates

• First Submitted: January 11, 2022
• First Posted: June 23, 2022
• Study Start: December 29, 2022
• Primary Completion: July 20, 2023
• Study Completion: July 20, 2023
• Last Updated: July 27, 2023

Record last verified: 2023-07

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)