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Phase 1 N=8 Randomized Treatment

Evaluating Drug Interactions Between Doravirine With Estradiol and Spironolactone in Healthy Transgender Women

Transgender Health · Gender Dysphoria · Transgender Women · Human Immunodeficiency Virus

Enrolled (actual)
8
Serious AEs
0.0%
Results posted
Mar 2025
Primary outcome: Primary: Doravirine Area Under the Plasma Concentration Versus Time Curve From 0 Hours to Infinity (AUC0-∞) — 17798.14; 18413.21 hr*ng/mL

Study Design & Population

Study type
Interventional
Phase
Phase 1
Interventions
Doravirine/Lamivudine/Tenofovir (Drug); Spironolactone 100mg (Drug); Estradiol 2mg (Drug); Placebo (Other)
Age
Adult · 18+ yrs
Sex
Female
Sponsor
Thomas Jefferson University
Primary completion
Oct 2022

Outcome Measures

OutcomeResultp-value
PRIMARY
Doravirine Area Under the Plasma Concentration Versus Time Curve From 0 Hours to Infinity (AUC0-∞)
17798.14; 18413.21
PRIMARY
Doravirine Maximum Concentration (Cmax)
745.46; 799.67
PRIMARY
Doravirine Trough Concentration (C24)
283.74; 292.89
PRIMARY
Tenofovir Disoproxil Fumarate Area Under the Plasma Concentration Versus Time Curve From 0 Hours to Infinity (AUC0-∞)
2370.6; 2031.84
PRIMARY
Tenofovir Disoproxil Fumarate Maximum Concentration (Cmax)
178.84; 129.95
PRIMARY
Tenofovir Disoproxil Fumarate Trough Concentration (C24)
29.59; 26
PRIMARY
Estradiol Area Under the Plasma Concentration Versus Time Curve From 0 Hours to Infinity (AUC0-∞)
9370.25; 9677.31
PRIMARY
Estradiol Maximum Concentration (Cmax)
118.08; 105.14
PRIMARY
Estradiol Trough Concentration (C12)
100.26; 92.01

Summary

Transgender women living with Human Immunodeficiency Virus (HIV) may prioritize gender-affirming hormonal therapy over antiretroviral drug therapy. Hormonal therapy typically consists of oral estradiol and spironolactone, which induce drug-metabolizing enzymes after prolonged administration. This study evaluates the bi-directional potential drug interaction between the antiretroviral drug, doravirine, when co-administered with estradiol and spironolactone.

Eligibility Criteria

Inclusion Criteria

  • Healthy self-identified transgender women (male-to-female) between 18-45 years old at the time of screening
  • Have not undergone an orchiectomy
  • Receiving oral estradiol and spironolactone for >/= 3 months prior to study entry with a self-reported adherence to prescribed doses of >/= 90%
  • Agree to abstain from alcohol consumption throughout the duration of the study
  • Be willing to briefly interrupt hormonal therapy prior to and during the study
  • If on pre-exposure prophylaxis (PrEP) therapy containing tenofovir alafenamide or tenofovir disoproxil fumarate, willing to discontinue PrEP at least 2 weeks before study start and for the duration of the study
  • Agree to use condoms for all sexual activity prior to the start and throughout the duration of the study
  • Evidence of a personal signed and dated informed consent document indicating that the participant has been informed of all pertinent aspects of the study

Exclusion Criteria

  • Presence of clinically significant acute or chronic disease, that in the investigator's opinion, would compromise the participant's safety during the study
  • Use of injectable or transdermal estradiol
  • Use of any other hormonal replacement therapy, wit h the exception of oral estradiol and spironolactone
  • Current use of any antiretroviral drug. This will not be exclusionary if participants reported discontinuing within 30 days of screening
  • Creatinine clearance </= 60 mL/min, as estimated by the Cockcroft-Gault equation
  • Known anaphylactic or severe systemic reactions to any components of doravirine, lamivudine, or tenofovir disoproxil fumarate
  • Positive HIV, hepatitis B or Hepatitis C virus at screening. Evidence of prior hepatitis B infection and immunity is not exclusionary. Positive hepatitis C antibody with negative viral load or documented antiviral hepatitis C treatment with one post treatment non-detectable hepatitis C viral load is not exclusionary
  • Recent significant blood or plasma donation
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT04283656). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.

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