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RO5186582

Phase 1

Healthy Volunteer | Small molecule | Other |Roche Holding AG|Last Updated: Nov 2, 2016

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment12

FDA Designations

No designations recorded

Clinical trial landscape

RO5186582 · 1 trial · 1 indication

Phase 1 1
NCT02254759A Study of RO5186582 Treatment on Cytochrome P450 (CYP) 3A4 Activity in Healthy ParticipantsHealthy Volunteer
COMPLETED12 Analytics
PHASE1COMPLETED
A Study of RO5186582 Treatment on Cytochrome P450 (CYP) 3A4 Activity in Healthy Participants
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Study Endpoints

Primary Endpoints

Bioavailability of Drug (F) for Oral Midazolam
Pre-dose [-0.5 hour (h)] and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10 and 14 h post-dose (pd) on Day (D) 2 and 18, and 22 h pd on D3 and 19
Total Plasma Clearence (CL) for IV Midazolam
Pre-dose [-10 minutes (min)] and 0.08 (5 min), 0.25 (15 min), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 14 h pd on D1 and D17, and 22 h pd on D2 and D18
Apparent Volume of Distribution at Steady-State (Vss) for IV Midazolam
Pre-dose (-10 min) and 0.08 (5 min), 0.25 (15 min), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 14 h pd on D1 and D17, and 22 h pd on D2 and D18
Maximum Observed Plasma Concentration (Cmax) for Oral Midazolam
Pre-dose (-0.5 h) and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10 and 14 h pd on D2 and 18, and 22 h pd on D3 and D19

Secondary Endpoints

Apparent Volume of Distribution (V/F) for Oral Midazolam
Pre-dose (-0.5 h) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 14 h pd on D2 and D18, and 22 h pd on D3 and D19
Area Under the Plasma Concentration Time Curve from Time Zero to Time Tau, Where Tau is the Dosing Interval (AUC0-tau) for RO5186582 and RO5271857 (metabolite of RO5186582)
D18: Pre-dose -0.17 h (10 min) and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10 and 12 h pd
Cmax for RO5186582 and RO5271857 (metabolite of RO5186582)
Pre-dose (10 min) and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10 and 12 h pd on D18 (timepoints relative to oral midazolam dosing are (- 2 h 10 min), -1.5, -1, -0.5, 0 h pre-dose and 1, 2, 3, 4, 6, 8, and 10 h pd)
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelCROSSOVER

Treatment Arms

ArmTypeDescription
IV Midazolam AloneOTHERA single 1 milligram (mg) dose of IV Midazolam on Day 1.
Oral Midazolam AloneOTHERA single 5 mg oral dose of midazolam on Day 2.
RO5186582 AloneEXPERIMENTALRO5186582 240 mg oral tablet twice daily (BID) for 14 days from Days 3 to 16.
RO5186582 Plus IV MidazolamEXPERIMENTALRO5186582 240 mg BID oral tablet in combination with a single 1 mg IV dose of midazolam on Day 17.
RO5186582 Plus Oral MidazolamEXPERIMENTALRO5186582 240 mg BID in combination with a single 5 mg oral dose of midazolam on Day 18.

Interventions

NameTypeDescription
Midazolam, IVDRUG2 milligrams per milliliter (mg/mL) midazolam solution for IV administration. For a 1 mg dose, the midazolam solution (0.5 mL of 2 mg/mL) will be injected at 2 milligrams per minute (mg/min).
Midazolam, oralDRUG0.1 mg/mL midazolam for oral administration. For a 5 mg dose, participants will receive 50 mL of 0.1 mg/mL midazolam.
RO5186582DRUGRO5186582 120 mg film-coated release tablet.
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Eligibility Criteria

Age Range18 Years to 60 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy participants with signed informed consent. Exclusion Criteria: * A history of epilepsy, convulsions or significant head injury * Significant history of drug allergy, as determined by the Investigator, or a known hypersensitivity to any of the ingredients of any of th...

Countries:United Kingdom
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Frequently asked questions about RO5186582

What is RO5186582 used for?

RO5186582 is an investigational small molecule being studied in healthy volunteers. It was evaluated in a Phase 1 clinical trial to assess its effect on cytochrome P450 (CYP) 3A4 activity. The drug is not approved for any indication and remains in clinical development.

Who makes RO5186582?

RO5186582 is being developed by Roche Holding AG, which trades under the ticker RHHBY. The company sponsored a Phase 1 study of the drug in healthy participants in the United Kingdom.

What phase is RO5186582 in?

RO5186582 is in Phase 1 clinical development. One Phase 1 trial has been completed, and there are no active trials currently listed for the drug. It is investigational and has not been approved by regulatory authorities.

What clinical trials is RO5186582 in?

RO5186582 was studied in one completed Phase 1 trial, NCT02254759, titled "A Study of RO5186582 Treatment on Cytochrome P450 (CYP) 3A4 Activity in Healthy Participants." The trial enrolled 12 healthy adults in the United Kingdom and was controlled but not randomized or double-blinded.

How does RO5186582 work?

RO5186582 is a small molecule that was studied for its effect on cytochrome P450 (CYP) 3A4 activity. The Phase 1 trial measured how the drug influences this enzyme, which is involved in drug metabolism. Its precise mechanism of action is not fully described in available data.

Is RO5186582 FDA approved?

RO5186582 is not FDA approved. It is an investigational drug that has completed a Phase 1 trial in healthy volunteers. The drug is still in clinical development, and no approval status has been established.