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EE/DRSP

Phase 1

Contraception | Small molecule | Endocrine |Bayer AG|Last Updated: Aug 7, 2013

Success Probability

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Trial Design

RandomizedACTIVE_CONTROLLED
Total Trials2
Total Enrollment92

FDA Designations

No designations recorded

Clinical trial landscape

EE/DRSP · 2 trials · 1 indication

Phase 1 2
NCT01253187Investigation of Bioequivalence of Ethinylestradiol (EE) and Drospirenone (DRSP) in Two Different Tablet Formulations: YAZ and YAZ + Levomefolate Calcium (Metafolin) & L-5-MTHF in Two Different Tablet Formulations: Levomefolate Calcium (Metafolin) and YAZ + Levomefolate Calcium (Metafolin)Contraception
COMPLETED44 Analytics
NCT01253174Investigation of Bioequivalence of Ethinylestradiol (EE) and Drospirenone (DRSP) in Two Different Tablet Formulations: Yasmin and Yasmin + Levomefolate Calcium (Metafolin) & L-5-MTHF in Two Different Tablet Formulations: Levomefolate Calcium (Metafolin) and Yasmin + Levomefolate Calcium (Metafolin)Contraception
COMPLETED48 Analytics
PHASE1COMPLETED
Investigation of Bioequivalence of Ethinylestradiol (EE) and Drospirenone (DRSP) in Two Different Tablet Formulations: YAZ and YAZ + Levomefolate Calcium (Metafolin) & L-5-MTHF in Two Different Tablet Formulations: Levomefolate Calcium (Metafolin) and YAZ + Levomefolate Calcium (Metafolin)
ContraceptionUnlock trial analytics
PHASE1COMPLETED
Investigation of Bioequivalence of Ethinylestradiol (EE) and Drospirenone (DRSP) in Two Different Tablet Formulations: Yasmin and Yasmin + Levomefolate Calcium (Metafolin) & L-5-MTHF in Two Different Tablet Formulations: Levomefolate Calcium (Metafolin) and Yasmin + Levomefolate Calcium (Metafolin)
ContraceptionUnlock trial analytics

Study Endpoints

Primary Endpoints

Mean Maximum Concentration (Cmax) of EE Incl. Bioequivalence (BE) Evaluation
up to 96 hours after administration

Cmax refers to the highest measured drug concentration which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample

Mean Area Under the Concentration-time Curve From Administration to the Last Measurement [AUC(0-tlast)] of EE Incl. Bioequivalence (BE) Evaluation
up to 96 hours after administration

The AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample

Mean Maximum Concentration (Cmax) of DRSP Incl. Bioequivalence (BE) Evaluation
up to 168 hours after administration

Cmax refers to the highest measured drug concentration which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample

Mean Area Under the Concentration-time Curve From Administration to the Last Measurement [AUC(0-tlast)] of DRSP Incl. Bioequivalence (BE) Evaluation
up to 168 hours after administration

The AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample

Mean Maximum Concentration (Cmax) of L-5-methyl-THF (Baseline Corrected) Incl. Bioequivalence (BE) Evaluation
up to 12 hours after administration

The baseline corrected Cmax is a measure of the highest measured drug concentration provided solely by the treatment after subtracting endogenous L-5-methyl-THF level. It is obtained by collecting a series of blood samples, measuring the concentrations of L-5-methyl-THF in each sample and by subtracting the pre-treatment concentration.

Mean Area Under the Concentration-time Curve From Administration to the Last Measurement [AUC(0-tlast)] of L-5-methyl-THF (Baseline Corrected) Incl. Bioequivalence (BE) Evaluation
up to 12 hours after administration

The baseline corrected AUC is a measure of the systemic drug exposure provided by the treatment excluding the endogenous L-5-methyl-THF level. It is obtained by collecting a series of blood samples, measuring the concentrations of L-5-methyl-THF in each sample and by subtracting the pre-treatment concentration.

Mean Maximum Concentration (Cmax) of L-5-methyl-THF (Baseline Uncorrected) Incl. Bioequivalence (BE) Evaluation
up to 12 hours after administration

The baseline uncorrected Cmax is a measure of the highest measured drug concentration including the endogenous L-5-methyl-THF level. It is obtained by collecting a series of blood samples and measuring the concentrations of L-5-methyl-THF in each sample.

Mean Area Under the Concentration-time Curve From Administration to the Last Measurement [AUC(0-tlast)] of L-5-methyl-THF (Baseline Uncorrected) Incl. Bioequivalence (BE) Evaluation
up to 12 hours after administration

The baseline uncorrected AUC is a measure of the systemic drug exposure provided by the treatment including the endogenous L-5-methyl-THF level. It is obtained by collecting a series of blood samples and measuring the concentrations of L-5-methyl-THF in each sample.

Mean Area Under the Concentration-time Curve (AUC) of DRSP Incl. Bioequivalence (BE) Evaluation
up to 168 hours after administration

The AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample

Secondary Endpoints

Time to Reach Maximum Concentration (Tmax) of EE
up to 96 hours after administration
Mean Area Under the Concentration-time Curve From Administration up to 72h AUC(0-72h) of DRSP
up to 72 hours after administration
Time to Reach Maximum Concentration (Tmax) of DRSP
up to 168 hours after administration
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
EE 0.02 mg/DRSP 3 mg (YAZ, BAY86-5300)EXPERIMENTALsingle oral administration of 1 film-coated SHT00186D tablet (YAZ), containing 0.020 mg ethinylestradiol (EE) + 3 mg drospirenone (DRSP)
EE 0.02mg/DRSP 3mg/L-5-MTHF Ca 0.451mg (EE20/DRSP/L-5-MTHF Ca)EXPERIMENTALsingle oral administration of 1 film-coated SHT04532B tablet, containing 0.020 mg ethinylestradiol (EE) + 3 mg drospirenone (DRSP) + 0.451 mg Metafolin (L-5-methyltetrahydrofolate calcium \[MTHF-Ca\])
L-5-MTHF Ca 0.451 mg (Metafolin)EXPERIMENTALsingle oral administration of 1 coated SHT04532C tablet, containing 0.451 mg Metafolin (L-5-methyltetrahydrofolate calcium \[MTHF-Ca\])
EE 0.03 mg/DRSP 3 mg (Yasmin, BAY86-5131)EXPERIMENTALsingle oral administration of 1 film-coated SHT470FA tablet (Yasmin with ethinylestradiol (EE) as free steroid), containing 0.030 mg EE + 3 mg drospirenone (DRSP)
EE 0.03mg/DRSP 3mg/L-5-MTHF Ca 0.451mg (EE30/DRSP/L-5-MTHF Ca)EXPERIMENTALsingle oral administration of 1 film-coated SHT04532A tablet (with ethinylestradiol (EE) as clathtrate), containing 0.030 mg EE + 3 mg drospirenone (DRSP) + 0.451 mg Metafolin (L-5-methyltetrahydrofolate calcium \[MTHF-Ca\])

Interventions

NameTypeDescription
EE 0.02 mg/DRSP 3 mg (YAZ, BAY86-5300)DRUGTreatment group A: Single 1 film-coated tablet (Ethinylestradiol \[EE\] 0.02mg / Drospirenone \[DRSP\] 3mg) taken orally under fasting condition at intervals of at least one menstrual cycle.
EE 0.02 mg/DRSP 3 mg/L-5-MTHF Ca 0.451 mg (EE20/DRSP/L-5-MTHF Ca)DRUGTreatment group B: Single 1 film-coated tablet (Ethinylestradiol \[EE\] 0.02mg / Drospirenone \[DRSP\] 3mg / L-5-methyltetrahydrofolate \[L-5-MTHF\] 0.451mg) taken orally under fasting condition at intervals of at least one menstrual cycle.
L-5-MTHF 0.451mg (Metafolin)DRUGTreatment group C: Single 1 coated tablet (L-5-methyltetrahydrofolate \[L-5-MTHF\] 0.451mg) taken orally under fasting condition at intervals of at least one menstrual cycle.
EE 0.03 mg/DRSP 3 mg (Yasmin, BAY86-5131)DRUGsingle oral administration of 1 coated tablet SH T470FA (Yasmin, film-coated tablets with ethinylestradiol (EE) as free steroid), containing 0.030 mg EE + 3 mg drospirenone (DRSP)
EE 0.03mg/DRSP 3mg/L-5-MTHF Ca 0.451mg (EE30/DRSP/L-5-MTHF Ca)DRUGsingle oral administration of 1 coated tablet SH T04532A (film-coated tablet with ethinylestradiol (EE) as clathtrate), containing 0.030 mg EE + 3 mg drospirenone (DRSP) + 0.451 mg Metafolin
L-5-MTHF Ca 0.451 mg (Metafolin)DRUGsingle oral administration of 1 coated tablet SH T04532C, containing 0.451 mg Metafolin
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Eligibility Criteria

Age Range18 Years to 38 Years
SexFEMALE
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy female volunteer * Age: 18 - 38 years inclusive * Body mass index (BMI)1: ≥ 19 and \< 28 kg/m² * Regular cyclic menstrual periods at screening OR when using combined oral contraceptives during the recruitment period reporting of natural cyclic menstrual periods prior t...

Countries:NetherlandsGermany
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Frequently asked questions about EE/DRSP

What is EE/DRSP used for?

EE/DRSP is a combination of ethinylestradiol and drospirenone being developed for contraception. It is an investigational small molecule in Phase 1 clinical development, studied in healthy female volunteers aged 18 years and older.

Who makes EE/DRSP?

EE/DRSP is being developed by Bayer AG, a pharmaceutical company traded on the OTC market under the ticker BAYRY. The drug is currently in Phase 1 clinical trials for contraception.

What phase is EE/DRSP in?

EE/DRSP is in Phase 1 clinical development. Two Phase 1 trials have been completed, with a total of 92 participants enrolled. The drug is investigational and not yet approved for use.

What clinical trials is EE/DRSP in?

EE/DRSP has been studied in two completed Phase 1 trials: NCT01253174, which enrolled 48 participants in Germany, and NCT01253187, which enrolled 44 participants in the Netherlands. Both trials investigated bioequivalence of different tablet formulations for contraception.

Is EE/DRSP the same as Yasmin or YAZ?

EE/DRSP refers to the combination of ethinylestradiol and drospirenone, which are the active ingredients in the tablet formulations Yasmin and YAZ. The clinical trials compared these formulations with versions containing levomefolate calcium.