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Ethinylestradiol

Phase 1

Healthy | Small molecule | Other |Johnson & Johnson|Last Updated: Apr 27, 2025

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Market & Valuation

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Trial Design

UNCONTROLLED
Total Trials2
Total Enrollment42

FDA Designations

No designations recorded

Clinical trial landscape

Ethinylestradiol · 2 trials · 1 indication

Phase 1 2
NCT03249402A Study to Evaluate the Effect of Multiple Oral Doses of JNJ-42847922 on the Steady-state Pharmacokinetics of an Oral Contraceptive Containing Ethinyl Estradiol and Levonorgestrel in Healthy Female Adult ParticipantsHealthy
COMPLETED24 Analytics
NCT02652650A Study to Investigate the Effect of JNJ-63623872 at Steady-state on the Steady-state Pharmacokinetics of Ethinylestradiol and NorethindroneHealthy
COMPLETED18 Analytics
PHASE1COMPLETED
A Study to Evaluate the Effect of Multiple Oral Doses of JNJ-42847922 on the Steady-state Pharmacokinetics of an Oral Contraceptive Containing Ethinyl Estradiol and Levonorgestrel in Healthy Female Adult Participants
HealthyUnlock trial analytics
PHASE1COMPLETED
A Study to Investigate the Effect of JNJ-63623872 at Steady-state on the Steady-state Pharmacokinetics of Ethinylestradiol and Norethindrone
HealthyUnlock trial analytics

Study Endpoints

Primary Endpoints

Maximum Observed Plasma Concentration (Cmax) in Cycle 1
Cycle 1: Predose (Day 21), 30 minute (min), 1 hour (h), 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 14h, 18h, 20h, 24h, 28h, 36h, 48h and 72h Postdose

The Cmax is the maximum observed plasma concentration.

Maximum Observed Plasma Concentration (Cmax) in Cycle 2
Cycle 2: Predose (Day 21), 30 minute (min), 1 hour (h), 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 14h, 18h, 20h, 24h, 28h, 36h, 48h and 72h Postdose

The Cmax is the maximum observed plasma concentration.

Trough Plasma Concentration (Ctrough) in Cycle 1
Cycle1: Predose (Day 21)

The (Ctrough) is the observed plasma concentration just prior to the beginning of a dosing interval.

Trough Plasma Concentration (Ctrough) in Cycle 2
Cycle 2: Predose (Day 21)

The (Ctrough) is the observed plasma concentration just prior to the beginning of a dosing interval.

Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC[0-24]) at Cycle 1
Cycle 1: Predose (Day 21), 30 minute (min), 1 hour (h), 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 14h, 18h, 20h, Day 22: 24h Postdose

The AUC (0-24) is the area under the plasma concentration-time curve from time zero to 24 hours.

Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC[0-24]) at Cycle 2
Cycle 2: Predose (Day 21), 30 minute (min), 1 hour (h), 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 14h, 18h, 20h, Day 22: 24h Postdose

The AUC (0-24) is the area under the plasma concentration-time curve from time zero to 24 hours.

Observed Analyte Concentration Just Prior to the Beginning or at the End of a Dosing Interval (Ctrough) of JNJ-63623872
Post-dose on Days 75 and 76 of Cycle III

Ctrough is the observed analyte concentration just prior to the beginning or at the end of a dosing Interval.

Observed Analyte Concentration at 12 Hours Post Dosing (C12h) of JNJ-63623872
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle II

C12h is the observed analyte concentration at 12 hours post dosing.

Minimum Observed Analyte Concentration (Cmin) of JNJ-63623872
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle II

Cmin is the minimum observed analyte concentration.

Maximum Observed Analyte Concentration (Cmax) of JNJ-63623872
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle II

Cmax is the maximum observed analyte concentration.

Time To Reach The Maximum Observed Analyte Concentration (Tmax) of JNJ-63623872
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle II

Tmax is the actual sampling time to reach the maximum observed analyte concentration.

Area Under the Analyte Concentration versus Time Curve (AUC) From Time of Administration up to 12 Hours Post Dosing (AUC12h) of JNJ-63623872
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle II

AUC12h is the area under the analyte concentration versus time curve (AUC) from time of administration up to 12 hours post dosing.

Average Steady-State Plasma Concentration (Cavg) of JNJ-63623872
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle II

Cavg is the average steady-state plasma concentration.

Percentage Fluctuation (FI) of JNJ-63623872
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle II

FI is the percentage fluctuation(variation between maximum and minimum concentration at steady-state), calculated as: 100 multiplied (\[Cmax - Cmin\] / Cavg).

Observed Analyte Concentration Just Prior to the Beginning or at the End of a Dosing Interval (Ctrough) of Ethinylestradiol
Post-dose on Days 47 and 48 of Cycle II; post-dose on Days 75 and 76 of Cycle III

Ctrough is the observed analyte concentration just prior to the beginning or at the end of a dosing Interval.

Observed Analyte Concentration Just Prior to the Beginning or at the End of a Dosing Interval (Ctrough) of Norethindrone
Post-dose on Days 47 and 48 of Cycle II; post-dose on Days 75 and 76 of Cycle III

Ctrough is the observed analyte concentration just prior to the beginning or at the end of a dosing Interval.

Observed Analyte Concentration at 24 Hours Post Dosing (C24h) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

C24h is the observed analyte concentration at 24 hours post dosing.

Observed Analyte Concentration at 24 Hours Post Dosing (C24h) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

C24h is the observed analyte concentration at 24 hours post dosing.

Minimum Observed Analyte Concentration (Cmin) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Cmin is the minimum observed analyte concentration.

Minimum Observed Analyte Concentration (Cmin) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Cmin is the minimum observed analyte concentration.

Maximum Observed Analyte Concentration (Cmax) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Cmax is the maximum observed analyte concentration.

Maximum Observed Analyte Concentration (Cmax) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Cmax is the maximum observed analyte concentration.

Time To Reach The Maximum Observed Analyte Concentration (Tmax) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Tmax is the actual sampling time to reach the maximum observed analyte concentration.

Time To Reach The Maximum Observed Analyte Concentration (Tmax) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Tmax is the actual sampling time to reach the maximum observed analyte concentration.

Area Under the Analyte Concentration versus Time Curve (auc) From Time of Administration up to 24 Hours Post Dosing (AUC24h) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

AUC24h is the area under the analyte concentration versus time curve (AUC) from time of administration up to 24 hours post dosing.

Area Under the Analyte Concentration versus Time Curve (auc) From Time of Administration up to 24 Hours Post Dosing (AUC24h) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

AUC24h is the area under the analyte concentration versus time curve (AUC) from time of administration up to 24 hours post dosing.

Average Steady-State Plasma Concentration (Cavg) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Cavg average steady-state plasma concentration.

Average Steady-State Plasma Concentration (Cavg) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Cavg average steady-state plasma concentration.

Percentage Fluctuation (FI) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

FI is the percentage fluctuation(variation between maximum and minimum concentration at steady-state), calculated as: 100 multiplied (\[Cmax - Cmin\] / Cavg).

Percentage Fluctuation (FI) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

FI is the percentage fluctuation(variation between maximum and minimum concentration at steady-state), calculated as: 100 multiplied (\[Cmax - Cmin\] / Cavg).

Ratio of Individual Cmax Values Between Test and Reference Treatment (Ratio Cmax, test/ref) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Ratio Cmax, test/ref is the ratio of individual Cmax values between test and reference treatment of ethinylestradiol.

Ratio of Individual Cmax Values Between Test and Reference Treatment (Ratio Cmax, test/ref) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Ratio Cmax, test/ref is the ratio of individual Cmax values between test and reference treatment of Norethindrone.

Ratio of Individual AUC24h Values Between Test and Reference Treatment (Ratio AUC24h, test/ref) of Ethinylestradiol
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Ratio AUC24h, test/ref is the ratio of individual AUC24h values between test and reference treatment of Ethinylestradiol.

Ratio of Individual AUC24h Values Between Test and Reference Treatment (Ratio AUC24h, test/ref) of Norethindrone
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 49 of Cycle II; Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 9 and 12 hours post-dose on Day 77 of Cycle III

Ratio AUC24h, test/ref is the ratio of individual AUC24h values between test and reference treatment of Norethindrone.

Secondary Endpoints

Number of Participants With Adverse Events as a Measure of Safety and Tolerability
Up to 87 Days
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeOTHER

Treatment Arms

ArmTypeDescription
Oral Contraceptive Tablet + JNJ-42847922EXPERIMENTALAll participants will receive one oral contraceptive (OC) tablet containing ethinyl estradiol (EE) 0.03 milligram (mg) and levonorgestrel (LN) 0.15 mg once daily on Days 1 to 21 for both cycle 1 and cycle 2. In addition, in cycle 2, participants will receive 40 mg of JNJ-42847922 once daily on Days 14 to 21. Participants will not be given OC tablet on Days 22 to 28 during cycle 1 and cycle 2 (tablet-free period).
Ethinylestradiol/NorethindroneEXPERIMENTALDuring the first oral contraceptive (OC) cycle participants will receive ethinylestradiol/norethindrone 35 microgram (mcg)/1 milligram (mg) alone once daily (qd) for 21 days on Days 1 to 21 (Cycle I: lead-in). During the second OC cycle (from Day 29 to Day 56), participants will receive ethinylestradiol/norethindrone 35 mcg/1 mg alone qd for 21 days on Days 29 to 49 (Cycle II: OC alone, reference). During the third OC cycle (from Day 57 to Day 84), participants will receive ethinylestradiol/norethindrone 35 mcg/1 mg qd for 21 days on Days 57 to 77 and in addition JNJ-63623872, 600 mg twice daily (bid) for 5 days on Days 73 to 77 (Cycle III: OC plus JNJ-63623872, test).

Interventions

NameTypeDescription
Ethinyl Estradiol + LevonorgestrelDRUGParticipants will receive one OC tablet containing EE 0.03 mg and LN 0.15 mg once daily on Days 1 to 21 in cycles 1 and 2.
JNJ-42847922DRUGParticipants will receive 40 mg of JNJ-42847922 once daily on Days 14 to 21 in cycle 2.
EthinylestradiolDRUGParticipants will receive 35 microgram (mcg) alone once daily (qd) for 21 days on Days 1 to 21 (Cycle I: lead-in) during first OC cycle; Days 29 to 49 (Cycle II: OC alone, reference) during the second OC cycle and Days 57 to 77 during third OC cycle.
NorethindroneDRUGParticipants will receive 1 milligram (mg) alone once daily (qd) for 21 days on Days 1 to 21 (Cycle I: lead-in) during first OC cycle; Days 29 to 49 (Cycle II: OC alone, reference) during the second OC cycle and Days 57 to 77 during third OC cycle.
JNJ-63623872DRUGParticipants will receive 600 mg twice daily (bid) for 5 days on Days 73 to 77 (Cycle III: OC plus JNJ-63623872, test) during third OC cycle under fed conditions.
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Eligibility Criteria

Age Range18 Years to 45 Years
SexFEMALE
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Be female of childbearing potential (women with tubal ligation are not accepted) * Have a body weight equal to or over 45 kilogram (kg) and a body mass index (BMI) 23 within the range of 18 to 30 kilogram / square meter (kg/m\^2) inclusive * Have a systolic blood pressure betw...

Countries:Belgium
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Frequently asked questions about Ethinylestradiol

What is Ethinylestradiol used for?

Ethinylestradiol is an investigational small molecule being studied in healthy female volunteers as part of drug interaction trials. It is used in these trials as a component of oral contraceptives to evaluate how other investigational drugs affect its pharmacokinetics. It is not approved for any indication and remains in clinical development.

Who makes Ethinylestradiol?

Ethinylestradiol is being developed by Johnson & Johnson, traded on the New York Stock Exchange under the ticker JNJ. The company is conducting Phase 1 clinical trials to study the drug's interactions with other investigational compounds in healthy female participants.

What phase is Ethinylestradiol in?

Ethinylestradiol is in Phase 1 clinical development. It is an investigational drug and has not been approved by regulatory authorities. Two Phase 1 trials have been completed, with no active trials currently ongoing, and the drug is being studied only in healthy volunteers.

What clinical trials is Ethinylestradiol in?

Ethinylestradiol has been studied in two completed Phase 1 trials. NCT02652650 evaluated its interaction with JNJ-63623872 in 18 healthy women in Belgium. NCT03249402 evaluated its interaction with JNJ-42847922 in 24 healthy women in Belgium. Both trials were uncontrolled and not blinded.

How does Ethinylestradiol work?

Ethinylestradiol is a synthetic estrogen used in oral contraceptives. It works by binding to estrogen receptors, which helps regulate the menstrual cycle and prevent ovulation. In the studied trials, it was administered as part of combination oral contraceptives to assess potential drug interactions.

Is Ethinylestradiol the same as ethinyl estradiol?

Ethinylestradiol is the same compound as ethinyl estradiol, a synthetic form of estrogen used in oral contraceptives. In clinical trial records, it is sometimes spelled as ethinyl estradiol, but both names refer to the identical drug substance.