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

Phase 4

Terminated

• Conditions: Gender Dysphoria
• Interventions: Drug: 17beta Estradiol

• Registration Number: NCT05428215
• Lead Sponsor: MaineHealth

Brief Summary

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

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2022-01-11
• Study First Submitted QC: 2022-06-17
• Study First Posted: 2022-06-23
• Study Start: 2022-12-29
• Status Verified: 2023-07
• Primary Completion: 2023-07-20
• Study Completion: 2023-07-20
• Last Update Submitted: 2023-07-24
• Last Update Posted: 2023-07-27

Recruitment & Eligibility

• Status: TERMINATED
• Sex: Male
• Target Recruitment: 2

Inclusion Criteria

• 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)

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Exclusion Criteria

• 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

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
PO then SL	17beta Estradiol	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.
SL then PO	17beta Estradiol	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.

Primary Outcome Measures

Name	Time	Method
Estradiol absorption	Over 24 hours	Mean area under the curve of estradiol

Secondary Outcome Measures

Name	Time	Method
Serum estrone to estradiol ratio	Hours from administration of estradiol: 0, 1, 2, 4, 6, and 8 hours	E1:E2 ratio over 24 hour period with sublingual vs oral administration
Peak serum estradiol	Peak over 24 hour period	With subjects as own controls, compare peak E2 with sublingual vs oral administration
Serum estradiol Nadir	24 hours from last estradiol administration	Baseline serum estradiol level after 2 weeks of oral administration versus sublingual administration at same dose
Suppression of Testosterone	24 hours from last estradiol administration on Study Day 14 and 28	Testosterone level after 2 weeks of estradiol administration via oral and sublingual method, respectively
Sex hormone binding globulin	0 hours from estradiol administration on Study Day 14 and 28	SHBG after 2 weeks of estradiol sublingual vs oral administration

Trial Locations

Locations (1)

Maine Medical Center; 🇺🇸 Portland, Maine, United States