A Cross-over Study Examining the Bioequivalence of 3 Test Formulations to a Reference Formulation of Alectinib (RO5424802) in Healthy Volunteers
A Randomized, Open-Label, Single Dose, Cross-Over Study to Investigate the Bioequivalence of Three RO5424802 Test Formulations Versus a Reference Formulation Following Oral Administration in Healthy Subjects
1 other identifier
interventional
97
1 country
1
Brief Summary
This 2-part, single center, open-label, randomized, single-dose, 4-sequence, 4-period cross-over study will compare the bioequivalence of three test RO5424802 capsule formulations with the reference capsule formulation in healthy adult volunteers. All participants in both fasted (Part 1) and fed (Part 2) conditions of the study will receive each of 4 treatments (Ro542-4802/F03 \[RO5424802 with 50 percentage (%) sodium lauryl sulfate (SLS) (reference)\], Ro542-4802/F07 \[RO5424802 with 25% SLS (test)\], Ro542-4802/F14 \[RO5424802 with 12.5% SLS (test)\] and Ro542-4802/F08 \[RO5424802 with 3% SLS (test)\] in a randomized sequence. Each treatment will be given as a single 600 milligrams (mg) oral administration in an upright position on Day 1 after an overnight fast, followed by a 10-day washout period. Total time on study is expected to last up to 75 days, for each enrolled participant.
Trial Health
Trial Health Score
Automated assessment based on enrollment pace, timeline, and geographic reach
participants targeted
Target at P75+ for phase_1
Started Feb 2014
Shorter than P25 for phase_1
1 active site
Health score is calculated from publicly available data and should be used for screening purposes only.
Trial Relationships
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Study Timeline
Key milestones and dates
Study Start
First participant enrolled
February 1, 2014
CompletedFirst Submitted
Initial submission to the registry
February 26, 2014
CompletedFirst Posted
Study publicly available on registry
February 28, 2014
CompletedPrimary Completion
Last participant's last visit for primary outcome
September 1, 2014
CompletedStudy Completion
Last participant's last visit for all outcomes
September 1, 2014
CompletedResults Posted
Study results publicly available
October 18, 2016
CompletedDecember 11, 2023
March 1, 2023
7 months
February 26, 2014
August 25, 2016
March 9, 2023
Conditions
Outcome Measures
Primary Outcomes (3)
Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC[0-inf]) of Alectinib
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).
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
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC[0-last]) of Alectinib
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.
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
Maximum Observed Plasma Concentration (Cmax) of Alectinib
Cmax is the maximum observed plasma alectinib concentration, presented in nanogram per milliliter (ng/mL).
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
Secondary Outcomes (18)
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
AUC(0-inf) 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
AUC(0-last) 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
- +13 more secondary outcomes
Study Arms (4)
Ro542-4802/F03;Ro542-4802/F07;Ro542-4802/F14;Ro542-4802/F08
EXPERIMENTALParticipants 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/F14
EXPERIMENTALParticipants 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/F03
EXPERIMENTALParticipants 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/F07
EXPERIMENTALParticipants 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.
Interventions
Participants will receive Ro542-4802/F03 (containing 50% SLS) 600 mg capsules orally on Day 1.
Participants will receive Ro542-4802/F07 (containing 25% SLS) 600 mg capsules orally on Day 1.
Participants will receive Ro542-4802/F08 (containing 3% SLS) 600 mg capsules orally on Day 1.
Participants will receive Ro542-4802/F14 (containing 12.5% SLS) 600 mg capsules orally on Day 1.
Eligibility Criteria
You may qualify if:
- 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 before first dosing)
- Male participants and their partners of child-bearing potential must be willing to use two effective contraceptive methods as defined by protocol
- Willing to abstain from xanthine-containing beverages and food (coffee, tea, cola, chocolate, and "energy drinks") from 72 hours prior to Day -1 through the study
- Willing to abstain from grapefruit, pomelo, star fruit or Seville orange containing products from day 7 prior study start until study end
- Willing to avoid prolonged sun exposure while taking RO5424802 and through follow-up
You may not qualify if:
- Pregnant or lactating women, men with female partners who are pregnant or lactating, or women of child bearing potential
- Clinically significant abnormalities on physical examination, vital signs, or laboratory test results during screening or prior to admission to the study unit
- Positive test for drugs of abuse, alcohol or cotinine test at screening or prior to admission to the study unit or suspicion of regular consumption of drug(s) of abuse
- History of recent alcohol consumption exceeding 2 standard drinks per day on average. Alcohol consuming is prohibited from 72 hours prior to study start until the end of the study
- Participants with any risk factors or family history for QT/QTcF and electrocardiogram (ECG) abnormalities
- A history of any concurrent clinically significant hematologic, renal, hepatic, pulmonary, neurological, psychiatric, allergies, gastrointestinal, metabolic or endocrine disorder, or cardiovascular disease or infections
- Positive screening test for hepatitis B, C, or human immunodeficiency virus (HIV)
- Use of any medications (prescriptions or over-the-counter), within 2 weeks or 5 half-lives (whichever is longer) before the first dose of study medication with exception of acetaminophen up to 2 grams (g) per day up to 48 hours prior to dosing, not to exceed 4 g total during the week prior to dosing
- Routine or chronic use of more than 2 g of acetaminophen daily
- Use of any herbal supplements (for example, St. John's Wort) or any metabolic inducers within 4 weeks or 5 half-lives (whichever is longer) before the first dose of study medication, including but not limited to the following drugs: rifampin, rifabutin, glucocorticoids, carbamazepine, phenytoin, and phenobarbital
- Strenuous activity, sunbathing or contact sports are not allowed from 4 days prior to study start until the end of the study
- Participation in an investigational drug or device study within 45 days or 5 half-lives (whichever time period is longer), or 6 months for biologic therapies, prior to first dosing
- Donation of blood over 450 milliliters (mL) within 45 days prior to screening
Contact the study team to confirm eligibility.
Sponsors & Collaborators
Study Sites (1)
Unknown Facility
Austin, Texas, 78744, United States
Results Point of Contact
- Title
- Medical Communications
- Organization
- Hoffmann-La Roche
Study Officials
- STUDY DIRECTOR
Clinical Trials
Hoffmann-La Roche
Publication Agreements
- PI is Sponsor Employee
- No
- Restriction Type
- OTHER
- Restrictive Agreement
- Yes
Study Design
- Study Type
- interventional
- Phase
- phase 1
- Allocation
- RANDOMIZED
- Masking
- NONE
- Purpose
- TREATMENT
- Intervention Model
- CROSSOVER
- Sponsor Type
- INDUSTRY
- Responsible Party
- SPONSOR
Study Record Dates
First Submitted
February 26, 2014
First Posted
February 28, 2014
Study Start
February 1, 2014
Primary Completion
September 1, 2014
Study Completion
September 1, 2014
Last Updated
December 11, 2023
Results First Posted
October 18, 2016
Record last verified: 2023-03