NCT02807363 is a Phase 2 clinical trial of Leuprolide Oral Tablet 4-mg QD in Endometriosis, sponsored by Enteris BioPharma Inc..

Who is sponsoring NCT02807363?

NCT02807363 is sponsored by Enteris BioPharma Inc..

What drugs are being tested in NCT02807363?

Interventions in NCT02807363: Leuprolide Oral Tablet 4-mg QD, Leuprolide Oral Tablet 4-mg BID, Leuprolide Depot, Leuprolide Oral Tablet 10-mg BID.

What condition does NCT02807363 study?

NCT02807363 studies Endometriosis.

Is NCT02807363 still recruiting?

NCT02807363 is currently completed. Last updated 11 February 2022.

Are results published for NCT02807363?

Yes — primary outcome results have been posted to ClinicalTrials.gov. See the outcomes section above for details.

Last reviewed 2022-02-11 · How we verify

NCT02807363

Name: Drug Landscape Pharmaceutical Database
Creator: Drug Landscape
Published: 2026-01-01
License: https://creativecommons.org/licenses/by/4.0/

A Study of Pharmacokinetic/Pharmacodynamic Profile of Orally Administered Leuprolide in Healthy Female Volunteers

Completed Phase 2 Results posted Last updated 11 February 2022

What this trial tests

Phase 2 trial testing Leuprolide Oral Tablet 4-mg QD in Endometriosis in 35 participants. Completed in 27 June 2018.

Timeline

23 August 2017

Primary endpoint
27 June 2018

27 June 2018

Quick facts

Lead sponsor	Enteris BioPharma Inc.
Phase	Phase 2
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	parallel
Masking	none
Primary purpose	treatment
Enrollment	35
Start date	23 August 2017
Primary completion	27 June 2018
Estimated completion	27 June 2018
Sites	1 location across Canada

Drugs / interventions tested

Leuprolide Oral Tablet 4-mg QD — full drug profile →
Leuprolide Oral Tablet 4-mg BID — full drug profile →
Leuprolide Depot — full drug profile →
Leuprolide Oral Tablet 10-mg BID — full drug profile →

Conditions studied

Endometriosis — all drugs for Endometriosis →

Sponsor

Enteris BioPharma Inc. — full company profile →

Who can join

Adults 18 to 49, female only, with Endometriosis. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Number of Participants With Adequacy of Suppression of Estradiol (E2) as Assessed by Estradiol Level Below 40 pg/mL Primary · Dosing Period: Day 8 to 28, Post-dosing: Day 1 to day 28 of post dosing period; Day 29 is the post dosing day 1

Criterion: E2 level is considered suppressed during the evaluation period if a value below pre-specified threshold was reported at least once during that period. The days in the row title indicate the evaluation interval.

Days 8,15, 22, 28 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	6
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	7
Leuprolide 1 Month Depot (Treatment C)	5
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	12

Days 15, 22, 28 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	5
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	7
Leuprolide 1 Month Depot (Treatment C)	5
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	12

Days 22, 28 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	4
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	6
Leuprolide 1 Month Depot (Treatment C)	5
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	9

Days 22 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	4
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	6
Leuprolide 1 Month Depot (Treatment C)	5
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	9

Entire 28-day Dosing Period

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	7
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	8
Leuprolide 1 Month Depot (Treatment C)	5
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	12

28-day Post-dosing Period

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	7
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	6
Leuprolide 1 Month Depot (Treatment C)	5
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	9

Ovulation Rate - Measured by Number of Subjects With Progesterone Levels Not Less Than 3000 pg/mL Primary · Dosing period: Day 1 to Day 28 and 28 day Post-Dosing Period; 29 day is post dosing day 1

Progesterone level is considered suppressed during the evaluation period if a value below pre-specified threshold (3000 pg/mL) was reported at least once during that period. The days in row title indicate the evaluation interval.

Days 8, 15, 22, 28 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	4
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	3
Leuprolide 1 Month Depot (Treatment C)	3
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	10

Days 15, 22, 28 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	2
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	2
Leuprolide 1 Month Depot (Treatment C)	0
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	0

Days 22, 28 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	2
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	2
Leuprolide 1 Month Depot (Treatment C)	0
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	0

Days 22 and 29

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	2
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	1
Leuprolide 1 Month Depot (Treatment C)	0
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	0

Entire 28-day Dosing Period

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	8
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	5
Leuprolide 1 Month Depot (Treatment C)	4
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	12

28-day Post-dosing Period

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	9
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	7
Leuprolide 1 Month Depot (Treatment C)	2
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	12

Number of Subjects Who Experienced Treatment Emergent Adverse Events (TEAE) Excluding Menstrual Disorders Primary · Dosing Period: Day 1 to day 28

The participant incidence of TEAEs was generally comparable during the dosing period across the treatment groups. Treatment C is a depot formulation established to release the drug over a period of 1 month. The data for adverse event was collected for day 1 to 28 of the dosing period.

Number of subjects with at least one TEAE

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	7
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	9
Leuprolide 1 Month Depot (Treatment C)	4
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	8

Number of subjects who discontinued due to TEAE

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	0
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	1
Leuprolide 1 Month Depot (Treatment C)	0
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	0

Number of Subjects Who Experienced Treatment-Emergent Adverse Events (TEAEs), Excluding Menstrual Disorders Primary · Post dosing period (starting day 1 to day 28 post dosing period)

Treatment C is a depot formulation established to release the drug over a period of 1 month. The data for post dosing adverse event was collected starting from day 1 to 28 post the 28th day of dosing.

Number of subjects with at least one TEAE

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	1
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	2
Leuprolide 1 Month Depot(Treatment C)	1
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	3

Number of subject who discontinued due to TEAEs

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	0
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	0
Leuprolide 1 Month Depot(Treatment C)	0
Leuprolide Oral Tablet, 10 mg BID (Treatment D)	0

Steady State Concentration Level, (Css) of Leuprolide Primary · Treatment Day 28 for oral groups; Treatment Days 22-29 for Lupron Depot group

Treatment A and B: Steady state concentration level calculated for oral tablets at the end of the fourth treatment week (Treatment Day 28) as the 24-hour AUCs divided by the duration of the dosing interval i.e. 24 hours. Treatment C: Steady state concentration level calculated for IM injection at the fourth treatment week (a mean of leuprolide levels on Days 22 and 29).

Group	Value	95% CI
Leuprolide Oral Tablet, 4 mg QD (Treatment A)	357.80	± 367.37
Leuprolide Oral Tablet, 4 mg BID (Treatment B)	688.27	± 258.01
Leuprolide 1 Month Depot (Treatment C)	180.95	± 101.04

Adverse events — posted to ClinicalTrials.gov

Time frame: Dosing period (day 1 to day 28) and post dosing period (day 1 to day 28). Reporting threshold: 0%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Leuprolide Oral Tablet, 4 mg QD (Treatment A)

Serious: 0/9 (0%)

Deaths: 0/9

Leuprolide Oral Tablet, 4 mg BID (Treatment B)

Serious: 0/9 (0%)

Deaths: 0/9

Leuprolide 1 Month Depot (Treatment C)

Serious: 0/5 (0%)

Deaths: 0/5

Leuprolide Oral Tablet, 10 mg BID (Treatment D)

Serious: 0/12 (0%)

Deaths: 0/12

Other adverse events (11 terms — click to expand)

Reaction	System	Leuprolide Oral Tablet, 4 …	Leuprolide Oral Tablet, 4 …	Leuprolide 1 Month Depot (…	Leuprolide Oral Tablet, 10…
Headache, disturbance in attention, dizziness, presyncope	Nervous system disorders	—	—	—	—
Nausea, Vomiting, Abdominal pain, abdominal pain upper, dry mouth, faeces soft	Gastrointestinal disorders	—	—	—	—
Breast tenderness. Metrorrhagia,	Reproductive system and breast disorders	—	—	—	—
hot flush	Vascular disorders	—	—	—	—
Nasopharyngitis, gastroenteritis, vaginitis gardnerella	Infections and infestations	—	—	—	—
Acne, erythema	Skin and subcutaneous tissue disorders	—	—	—	—
Cough, Oropharyngeal pain	Respiratory, thoracic and mediastinal disorders	—	—	—	—
Depressed mood, Insomnia	Psychiatric disorders	—	—	—	—
Axillary pain	General disorders	—	—	—	—
Procedural dizziness	Injury, poisoning and procedural complications	—	—	—	—
Myalgia	Musculoskeletal and connective tissue disorders	—	—	—	—

Data from ClinicalTrials.gov NCT02807363 adverse events section.

Sponsor's own description

This Phase 2a, pharmacokinetic/pharmacodynamic study will determine the safety and provide evaluation of the PK/PD metrics of three different oral doses selected upon the results of the study LOPDT-PH1-01 - 4 mg oral tablets administered over 28 days as QD and BID regimens and 10 mg oral tablets administered over 28 days as a BID regimen. The PK/PD profiles of the study drug will be compared to the leuprolide formulation approved for the treatment of endometriosis (a monthly intramuscular injection, Lupron Depot 3.75 mg). Major PK (e.g., a total exposure to leuprolide) and PD parameters (e.g., rates of the estradiol suppression and cessation of the menstrual period) will also be evaluated against the Lupron Depot historical data.

Publications & conference data

3 peer-reviewed publications reference this trial (live from Europe PMC):

Barriers and Strategies for Oral Peptide and Protein Therapeutics Delivery: Update on Clinical Advances.
Baral KC, Choi KY. · · 2025 · cited 39× · PMID 40284395 · DOI 10.3390/pharmaceutics17040397
The Hallmarks of Endometriosis.
Psilopatis I, Burghaus S, Au K, Hofbeck L, et al · · 2024 · cited 6× · PMID 38884026 · DOI 10.1055/a-2306-8759
Strategies for overcoming multiple barriers of oral administration of protein and peptide therapeutics.
Wang X, Wang K, Fang Y, Zhang Y, et al · · 2026 · PMID 41585434 · DOI 10.1016/j.mtbio.2026.102763

Verify or expand the search:

Other recruiting trials for Endometriosis

Currently open trials in the same condition.

NCT06559852 — The Impact of Yoga on Endometriosis-Related Pain · NA · recruiting
NCT07393295 — Efficacy and Tolerability of TENS in Endometriosis-related Pain · NA · recruiting
NCT07134023 — Educational Program for the Multidisciplinary Support of Patients With Endometriosis · NA · recruiting
NCT07240883 — ENDO1000 - A UK-wide Endometriosis Research Project · recruiting
NCT06974773 — Remote Electrical Stimulation as a Long-term Intervention for Endometriosis Flare Ups · NA · recruiting

Verify against primary sources

ClinicalTrials.gov — authoritative US registry record
WHO ICTRP — international registry index
EU Clinical Trials Register
Sponsor press releases (Google)

Data sources for this page

Trial protocol + status: ClinicalTrials.gov NCT02807363 (US National Library of Medicine, public domain)
Publications: Europe PMC API search by NCT ID, retrieved 9 June 2026
Drug + disease cross-links: matched in real time against Drug Landscape's normalised drug + company + condition tables
Sponsor: as reported to ClinicalTrials.gov by Enteris BioPharma Inc.
Last refreshed: 11 February 2022

Drug Landscape aggregates and links these public records for informational use only. Always verify against the primary source before clinical or regulatory decisions. Canonical URL: https://druglandscape.com/trial/NCT02807363.

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing