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BAY 1841788

Phase 1

Prostatic Neoplasms | Small molecule | Oncology |Bayer AG|Last Updated: Nov 6, 2018

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLED
Total Trials2
Total Enrollment24

FDA Designations

No designations recorded

Clinical trial landscape

BAY 1841788 · 2 trials · 1 indication

Phase 1 2
NCT03237416Drug-drug-interaction Study to Assess the Effect of Darolutamide on the Pharmacokinetics of Probe Substrates of CYP3A4 and P-gp in Healthy Male VolunteersProstatic Neoplasms
COMPLETED15 Analytics
NCT02363855Phase 1 Dose Escalation Study of BAY 1841788 in Japanese Metastatic Castration-resistant Prostate Cancer (mCRPC) SubjectsProstatic Neoplasms
COMPLETED9 Analytics
PHASE1COMPLETED
Drug-drug-interaction Study to Assess the Effect of Darolutamide on the Pharmacokinetics of Probe Substrates of CYP3A4 and P-gp in Healthy Male Volunteers
Prostatic NeoplasmsUnlock trial analytics
PHASE1COMPLETED
Phase 1 Dose Escalation Study of BAY 1841788 in Japanese Metastatic Castration-resistant Prostate Cancer (mCRPC) Subjects
Prostatic NeoplasmsUnlock trial analytics

Study Endpoints

Primary Endpoints

AUC in plasma of non-conjugated dabigatran (AUC(0-tlast), if AUC cannot be calculated)
Period 1, Day 1: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing Period 2, Day 3 and 9: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing

Exposure of non-conjugated dabigatran in plasma following a single administration of dabigatran etexilate AUC: area under the concentration vs. time curve from zero to infinity after single (first) dose AUC(0-tlast): AUC from time 0 to the last data point \> LLOQ

C(max) in plasma of non-conjugated dabigatran
Period 1, Day 1: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing Period 2, Day 3 and 9: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing

Maximum plasma concentration of non-conjugated dabigatran in plasma following a single administration of dabigatran etexilate Cmax: maximum observed drug concentration in measured matrix after single dose administration

AUC in plasma of midazolam (AUC(0-tlast), if AUC cannot be calculated)
PPeriod 1, Day 1: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing Period 2, Day 3 and 9: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing

Exposure of midazolam in plasma following a single administration of midazolam

C(max) in plasma of midazolam
Period 1, Day 1: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing Period 2, Day 3 and 9: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing

Maximum plasma concentration of midazolam in plasma following a single administration of midazolam

Number of participants with Treatment Emergent Adverse Event as measure of safety and tolerability
Up to 12 weeks
The intensity of an adverse event graded using the NCI CTCAE version 4.03
Up to 12 weeks

National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.03 (NCI CTCAE)

Plasma concentration of BAY 1841788 characterized by Cmax
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

Cmax: maximum drug concentration in plasma after single dose administration

Plasma concentration of BAY 1841788 characterized by tmax
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

tmax: time to reach maximum drug concentration in plasma after single (first) dose

Plasma concentration of BAY 1841788 characterized by AUC(0-12)
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

AUC(0-12):AUC from time 0 to 12 hours after administration

Plasma concentration of metabolite BAY 1896953 characterized by Cmax
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

Cmax: maximum drug concentration in plasma after single dose administration

Plasma concentration of metabolite BAY 1896953 characterized by tmax
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

tmax: time to reach maximum drug concentration in plasma after single (first) dose

Plasma concentration of metabolite BAY 1896953 characterized by AUC(0-12)
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

AUC(0-12):AUC from time 0 to 12 hours after administration

Plasma concentration of diastereomers BAY 1896951 characterized by Cmax
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

Cmax: maximum drug concentration in plasma after single dose administration

Plasma concentration of diastereomers BAY 1896951 characterized by tmax
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

tmax: time to reach maximum drug concentration in plasma after single (first) dose

Plasma concentration of diastereomers BAY 1896951 characterized by AUC(0-12)
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

AUC(0-12):AUC from time 0 to 12 hours after administration

Plasma concentration of diastereomers BAY 1896952 characterized by Cmax
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

Cmax: maximum drug concentration in plasma after single dose administration

Plasma concentration of diastereomers BAY 1896952 characterized by tmax
tmax: time to reach maximum drug concentration in plasma after single (first) dose

Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

Plasma concentration of diastereomers BAY 1896952 characterized by AUC(0-12)
Day -5 {pre dose, 0.5,1,1.5,3,5 ,8,12,24,36,48},Day -2 {before morning dose, 0.5,1,1.5,3,5,8, 12, 24, 36 and 48 h} ,Day 7 {before morning dose, 0.5, 1, 1.5,3,5,8,12 h (before evening dose)}

AUC(0-12):AUC from time 0 to 12 hours after administration

Secondary Endpoints

Number of subjects with study drug-related treatment-emergent Adverse Event (TEAE)
30 days following last intake of Investigational Product
AUC in plasma of total dabigatran (AUC(0-tlast), if AUC cannot be calculated)
Period 1, Day 1: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing Period 2, Day 3 and 9: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing
C(max) in plasma of total dabigatran
Period 1, Day 1: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing Period 2, Day 3 and 9: Predose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72 hours post dosing
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeOTHER

Treatment Arms

ArmTypeDescription
BAY1841788/Healthy subjectsEXPERIMENTALPeriod 1: intake of Midazolam and Dabigatran etexilate at day 1 followed by Period 2: intake of Darolutamide at days 1-11 (twice daily), intake of dabigatran etexilate at days 3 and 9, intake of Midazolam at day 9
BAY 1841788(ODM-201)EXPERIMENTALCohort 1: Safety, tolerability and PK of 300 mg dose given twice daily. Escalation to cohort 2 in case no safety relevant adverse event has been observed within 28 days after start of multiple dose (MD) Cohort 2: Safety, tolerability and PK of 600 mg dose given twice daily

Interventions

NameTypeDescription
Dabigatran etexilateDRUGIn Period 1, Day 1 a single dose of 75 mg will be administered after breakfast In Period 2, Day 3 a single dose of 75 mg will be administered prior to breakfast In Period 2, Day 9 a single dose of 75 mg will be administered after breakfast
MidazolamDRUGIn Period 1, Day 1 a single dose of 1 mg will be administered after breakfast In Period 2, Day 9 a single dose of 1 mg will be administered after breakfast
BAY1841788 (darolutamide)DRUGIn Period 2, Days 1-11 600 mg twice a day (as 2 x 300 mg tablets) will be administered after breakfast
BAY 1841788(ODM-201)DRUGCohort 1: Single dose 300 mg BAY 1841788, followed by twice daily administration of the same dose for 12 weeks Cohort 2: Single dose 2x300 mg BAY 1841788, followed by twice daily administration of the same dose for 12 weeks.
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Eligibility Criteria

Age Range45 Years to 65 Years
SexMALE
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy subject - as determined by the investigator or medically qualified designee based on medical evaluations including medical history, physical examination, laboratory tests and cardiac monitoring. * Gender: Male. * Age: 45 to 65 years (inclusive) at the screening visit. ...

Countries:GermanyJapan
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Frequently asked questions about BAY 1841788

What is BAY 1841788 used for?

BAY 1841788 is an investigational small molecule being studied for prostate cancer, specifically metastatic hormone-sensitive prostate cancer and metastatic castration-resistant prostate cancer. It has also been evaluated in healthy volunteers for pharmacokinetic and drug interaction studies. The drug is still in clinical development and has not been approved by the FDA.

What does BAY 1841788 target?

BAY 1841788 is an androgen receptor antagonist, meaning it blocks the action of androgens like testosterone, which can drive prostate cancer growth. By inhibiting the androgen receptor, the drug aims to slow or stop cancer progression. This mechanism is being tested in combination with standard therapies for metastatic prostate cancer.

Who makes BAY 1841788?

BAY 1841788 is being developed by Bayer AG, a German pharmaceutical company. Bayer's stock is traded over-the-counter under the ticker BAYRY. The company is conducting clinical trials to evaluate the drug's safety and efficacy in prostate cancer patients.

What phase is BAY 1841788 in?

BAY 1841788 is in Phase 1 clinical development. Two Phase 1 trials have been completed, including a dose escalation study in Japanese patients with metastatic castration-resistant prostate cancer and a drug interaction study in healthy volunteers. The drug remains investigational and is not yet approved.

What clinical trials is BAY 1841788 in?

BAY 1841788 has been studied in several completed trials. NCT02363855 was a Phase 1 dose escalation study in Japanese patients with metastatic castration-resistant prostate cancer. NCT02671097 and NCT03237416 were drug interaction studies in healthy volunteers. NCT02799602 was a Phase 3 trial combining darolutamide with standard therapy in metastatic hormone-sensitive prostate cancer.

Is BAY 1841788 the same as darolutamide?

Yes, BAY 1841788 is also known as darolutamide. Clinical trials listed under both names refer to the same drug. Darolutamide is the generic name used in later-stage studies, including the Phase 3 trial NCT02799602 for metastatic hormone-sensitive prostate cancer.