Phase 1
Completed N=23
A Study of the Effects of Posaconazole on Alectinib (RO5424802) Pharmacokinetics in Healthy Volunteers
Healthy Volunteer
Source: ClinicalTrials.gov NCT01984229 ↗
Enrolled (actual)
23
Serious AEs
0.0%
Results posted
Oct 2016
Primary outcomePrimary: Maximum Observed Plasma Concentration (Cmax) of Alectinib: Cohort A — 27.6; 35.0 nanograms per milliliter (ng/mL)
Summary
This open-label study will investigate whether multiple oral doses of posaconazole affect the single dose pharmacokinetics of alectinib in healthy volunteers.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Maximum Observed Plasma Concentration (Cmax) of Alectinib: Cohort A |
27.6; 35.0 | — |
| PRIMARY Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Alectinib: Cohort A |
634; 1030 | — |
| PRIMARY Cmax of Alectinib: Cohort B |
147; 171 | — |
| PRIMARY AUClast of Alectinib: Cohort B |
2770; 4910 | — |
| PRIMARY Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC0-inf) of RO5424802: Cohort B |
2850; 4990 | — |
| SECONDARY Cmax of RO5468924: Cohort A |
6.52; 2.54 | — |
| SECONDARY AUClast of RO5468924: Cohort A |
138; 65.1 | — |
| SECONDARY AUC0-inf of RO5468924: Cohort A |
201; 256 | — |
| SECONDARY Cmax of RO5468924: Cohort B |
59.6; 15.5 | — |
| SECONDARY AUClast of RO5468924: Cohort B |
1460; 910 | — |
| SECONDARY AUC0-inf of RO5468924: Cohort B |
1550; 1110 | — |
| SECONDARY Time to Reach Maximum Observed Plasma Concentration (Tmax) of Alectinib: Cohort A |
8.15; 8.00 | — |
| SECONDARY Tmax of Alectinib: Cohort B |
8.00; 8.00 | — |
| SECONDARY Tmax of RO5468924: Cohort A |
12.0; 11.9 | — |
| SECONDARY Tmax of RO5468924: Cohort B |
12.0; 11.9 | — |
| SECONDARY Metabolite/Parent Ratio for AUC0-inf: Cohort B |
0.541; 0.232 | — |
| SECONDARY Metabolite/Parent Ratio for Cmax: Cohort B |
0.393; 0.0953 | — |
| SECONDARY Terminal Half-life (t1/2) of Alectinib: Cohort A |
19.6; 26.9 | — |
| SECONDARY t1/2 of Alectinib: Cohort B |
18.4; 24.8 | — |
| SECONDARY t1/2 of RO5468924: Cohort A |
23.9; 79.6 | — |
| SECONDARY t1/2 of RO5468924: Cohort B |
25.3; 69.6 | — |
Eligibility Criteria
Inclusion Criteria
- Body mass index (BMI) between 18 to 32 kilogram per square meter (kg/m^2)
- Male volunteers must use effective contraception as outlined in the protocol
- Willingness to abstain from alcohol and xanthine-containing beverages or food (coffee, tea, cola, chocolate and "energy drinks") from 72 hours prior to the first dose until discharged
- Willingness to avoid prolonged sun exposure and guard against sunburn during study and follow-up
Exclusion Criteria
- Clinically significant medical history or findings in physical examination, vital signs, or laboratory test results prior to study start
- Positive screening tests for hepatitis B or C, human immunodeficiency virus (HIV), alcohol, drugs of abuse, or tobacco
- Women of childbearing potential, or males with pregnant or lactating partners
- Regular smoking within 6 months prior to first dosing. Participants should avoid smoky environments for at least 1 week prior to each cotinine screen
- Excessive alcohol consumption
- Use of any metabolic inducers (including herbals such as St. John's Wort) within 4 weeks or 5 half-lives (whichever is longer) before the first dose of study medication, including but not limited to: rifampin, rifabutin, glucocorticoids, carbamazepine, phenytoin and phenobarbital
- Strenuous activity, sunbathing, or contact sports are not allowed from 4 days prior to entry into the clinical site until study follow-up
- Participation in an investigational drug or device study within 45 days (or 6 months for biologic therapies) prior to first dosing
Data sourced from ClinicalTrials.gov (NCT01984229). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.