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RO5424802

Phase 1

Healthy Volunteer | Small molecule | Other |Roche Holding AG|Last Updated: Dec 11, 2023

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials3
Total Enrollment127

FDA Designations

No designations recorded

Clinical trial landscape

RO5424802 · 3 trials · 1 indication

Phase 1 3
NCT02074553A Cross-over Study Examining the Bioequivalence of 3 Test Formulations to a Reference Formulation of Alectinib (RO5424802) in Healthy VolunteersHealthy Volunteer
COMPLETED97 Analytics
NCT01981005A Study of the Elimination, Pharmacokinetics, and Metabolism of RO5424802Healthy Volunteer
COMPLETED6 Analytics
NCT01940510A Study of the Effect of Multiple Doses of Rifampin on the Single Dose Pharmacokinetics of RO5424802Healthy Volunteer
COMPLETED24 Analytics
PHASE1COMPLETED
A Cross-over Study Examining the Bioequivalence of 3 Test Formulations to a Reference Formulation of Alectinib (RO5424802) in Healthy Volunteers
Healthy VolunteerUnlock trial analytics
PHASE1COMPLETED
A Study of the Elimination, Pharmacokinetics, and Metabolism of RO5424802
Healthy VolunteerUnlock trial analytics
PHASE1COMPLETED
A Study of the Effect of Multiple Doses of Rifampin on the Single Dose Pharmacokinetics of RO5424802
Healthy VolunteerUnlock trial analytics

Study Endpoints

Primary Endpoints

Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC[0-inf]) of Alectinib
Predose (0 hour), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 60, 72, and 96 hours postdose

AUC(0-inf) is the area under the alectinib plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). AUC is a measure of the plasma concentration of a drug over time. AUC(0-inf) is presented in nanogram times (\*) hour per milliliter (ng\*hour/mL).

Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC[0-last]) of Alectinib
Predose (0 hour), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 60, 72, and 96 hours postdose

AUC(0-last) is the area under the alectinib plasma concentration versus time curve from time zero to the time of last measured concentration of alectinib. AUC is a measure of the plasma concentration of a drug over time. AUC(0-last) is presented in ng\*hour/mL.

Maximum Observed Plasma Concentration (Cmax) of Alectinib
Predose (0 hour), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 60, 72, and 96 hours postdose

Cmax is the maximum observed plasma alectinib concentration, presented in nanogram per milliliter (ng/mL).

Elimination: Amount of drug excreted in urine/feces over the study period
Days 11 to 15
Pharmacokinetics: Bioavailability (Area under the plasma concentration-time curve [AUC]) after administration of RO5424802
Days 1 to 25

Secondary Endpoints

Time to Reach Maximum Observed Plasma Concentration (Tmax) of Alectinib
Predose (0 hour), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 60, 72, and 96 hours postdose
Cmax of RO5468924
Predose (0 hour), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 60, 72, and 96 hours postdose
Tmax of RO5468924
Predose (0 hour), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 60, 72, and 96 hours postdose
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Ro542-4802/F03;Ro542-4802/F07;Ro542-4802/F14;Ro542-4802/F08EXPERIMENTALParticipants will receive Ro542-4802/F03 (containing 50% SLS) capsules orally on Day 1 of first intervention period; then Ro542-4802/F07 (containing 25% SLS) capsules orally on Day 1 of second intervention period; then Ro542-4802/F14 (containing 12.5% SLS) capsules orally on Day 1 of third intervention period; followed by Ro542-4802/F08 (containing 3% SLS) capsules orally on Day 1 of fourth intervention period during both fasted (Part 1) and fed (Part 2) conditions. A washout period of at least 10 days will be maintained between each period.
Ro542-4802/F07;Ro542-4802/F08;Ro542-4802/F03;Ro542-4802/F14EXPERIMENTALParticipants will receive Ro542-4802/F07 (containing 25% SLS) capsules orally on Day 1 of first intervention period; then Ro542-4802/F08 (containing 3% SLS capsules orally on Day 1 in second intervention period; then Ro542-4802/F03 (containing 50% SLS) (containing 12.5% SLS) capsules orally on Day 1 of third intervention period; followed by Ro542-4802/F14 (containing 12.5% SLS) capsules orally on Day 1 of the fourth intervention period during both fasted (Part 1) and fed (Part 2) conditions. A washout period of at least 10 days will be maintained between each period.
Ro542-4802/F08;Ro542-4802/F14;Ro542-4802/F07;Ro542-4802/F03EXPERIMENTALParticipants will receive Ro542-4802/F08 (containing 3% SLS) capsules orally on Day 1 of first intervention period; then Ro542-4802/F14 (containing 12.5% SLS) capsules orally on Day 1 in second intervention period; then Ro542-4802/F07 (containing 25% SLS) capsules orally on Day 1 of third intervention period; followed by Ro542-4802/F03 (containing 50% SLS) capsules orally on Day 1 of the fourth intervention period during both fasted (Part 1) and fed (Part 2) conditions. A washout period of at least 10 days will be maintained between each period.
Ro542-4802/F14;Ro542-4802/F03;Ro542-4802/F08;Ro542-4802/F07EXPERIMENTALParticipants will receive Ro542-4802/F14 (containing 12.5% SLS) capsules orally on Day 1 of first intervention period; then Ro542-4802/F03 (containing 50% SLS) capsules orally on Day 1 in second intervention period; then Ro542-4802/F08 (containing 3% SLS) capsules orally on Day 1 of third intervention period; followed by Ro542-4802/F07 (containing 25% SLS) capsules orally on Day 1 of the fourth intervention period during both fasted (Part 1) and fed (Part 2) conditions. A washout period of at least 10 days will be maintained between each period.
RO5424802EXPERIMENTAL -
Healthy subjectsEXPERIMENTAL -

Interventions

NameTypeDescription
Ro542-4802/F03 (Reference)DRUGParticipants will receive Ro542-4802/F03 (containing 50% SLS) 600 mg capsules orally on Day 1.
Ro542-4802/F07 (Test)DRUGParticipants will receive Ro542-4802/F07 (containing 25% SLS) 600 mg capsules orally on Day 1.
Ro542-4802/F08 (Test)DRUGParticipants will receive Ro542-4802/F08 (containing 3% SLS) 600 mg capsules orally on Day 1.
Ro542-4802/F14 (Test)DRUGParticipants will receive Ro542-4802/F14 (containing 12.5% SLS) 600 mg capsules orally on Day 1.
RO5424802DRUGSingle oral doses followed by IV or oral administration of a 14C-labeled tracer
rifampinDRUGMultiple doses Days 8-16 and Days 17-20
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy male and surgically sterile or post-menopausal female participants 18-55 years of age * Body mass index (BMI) between 18 to 32 kilograms per meter-squared (kg/m\^2) * Non-smoking participants and former smoking participants (who have not smoked for the past six months ...

Countries:United StatesNetherlands
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Frequently asked questions about RO5424802

What is RO5424802 used for?

RO5424802 is an investigational small molecule being studied in healthy volunteers. It is not approved for any disease and remains in clinical development. All completed trials for RO5424802 enrolled healthy volunteers to assess pharmacokinetics, drug interactions, elimination, and formulation bioequivalence.

Who makes RO5424802?

RO5424802 is being developed by Roche Holding AG, traded on the OTC market under the ticker RHHBY. The company has sponsored Phase 1 clinical trials of the drug in healthy volunteers.

What phase is RO5424802 in?

RO5424802 is in Phase 1 clinical development. All three trials of the drug are Phase 1 studies that have been completed. The drug is investigational and has not been approved by regulatory authorities.

What clinical trials is RO5424802 in?

RO5424802 has three completed Phase 1 trials: NCT01940510, a rifampin drug interaction study; NCT01981005, an elimination, pharmacokinetics, and metabolism study; and NCT02074553, a bioequivalence study of three test formulations versus a reference formulation. Total enrollment across these trials was 127 healthy volunteers.

Is RO5424802 the same as alectinib?

Yes, RO5424802 is also known as alectinib. One completed trial, NCT02074553, explicitly refers to alectinib (RO5424802) in its title, confirming that the two names refer to the same drug.