Phase 1
Completed N=99
A Study to Investigate the Safety, Tolerability, and Pharmacokinetics (PK) of Oseltamivir and Its Carboxylate Metabolite, RO0640802 in Healthy Participants
Healthy Volunteer
Source: ClinicalTrials.gov NCT02717754 ↗
Enrolled (actual)
99
Serious AEs
0.0%
Results posted
Jun 2016
Primary outcomePrimary: Area Under the Plasma Concentration-Time Curve From Time 0 to 12 Hour (AUC0-12h) of Oseltamivir and RO0640802 at Steady State — 581; 1143; 4147; 7966 ng*hour/mL
Summary
This multi-center, randomized, double-blind, multiple-dose, placebo-controlled, parallel-group study will assess the safety and PK of oseltamivir (Tamiflu) and its carboxylate metabolite, RO0640802 in healthy participants. Participants will be randomized to receive 100 milligrams (mg) oseltamivir, 200 mg oseltamivir, or placebo, all administered intravenously twice daily (BID). The anticipated time on study treatment is 5 days.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration-Time Curve From Time 0 to 12 Hour (AUC0-12h) of Oseltamivir and RO0640802 at Steady State |
581; 1143; 4147; 7966 | — |
| PRIMARY Maximum Plasma Concentration (Cmax) of Oseltamivir and RO0640802 at Steady State |
266; 496; 488; 960 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time 0 to Infinity (AUC0-inf) of Oseltamivir and RO0640802 |
612; 1139; 3606; 7336 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time 0 to Last Measurable Concentration (AUC0-last) of Oseltamivir and RO0640802 |
609; 1136; 2273; 4566; 580; 1142 | — |
| SECONDARY Cmax of Oseltamivir and RO0640802 |
284; 503; 301; 577 | — |
| SECONDARY Time to Reach Maximum Plasma Concentration (Tmax) of Oseltamivir and RO0640802 |
1.85; 1.65; 3.90; 3.95; 1.64; 1.81 | — |
| SECONDARY Half-Life (t1/2) of Oseltamivir and RO0640802 |
1.22; 1.53; 6.89; 7.17; 1.40; 1.88 | — |
| SECONDARY Volume of Distribution (Vd) of Oseltamivir and RO0640802 |
171; 183; 250; 251; 189; 192 | — |
| SECONDARY Clearance (CL) of Oseltamivir and RO0640802 |
289; 393; 26.0; 25.4; 192; 179 | — |
| SECONDARY Minimum Plasma Concentration (Cmin) of RO0640802 |
131; 264; 209; 388; 235; 450 | — |
Eligibility Criteria
Inclusion Criteria
- Participants with Body Mass Index (BMI) 18-34 kilograms per meter square (kg/m^2), inclusive
- Male participants who are willing to use barrier contraception for the duration of the study and for 3 months following the end of treatment
- Female participants who are of non-child bearing potential
- Female participants who are of child bearing potential utilizing two effective methods of contraception for the duration of the study and for 3 months following the end of treatment
Exclusion Criteria
- Evidence of clinically significant disease or disorder (for example, renal, cardiac, bronchopulmonary)
- Any other condition or disease which would place the participant at undue risk, or interfere with the assessment, or with the ability of the participant to complete the study
- Clinically significant orthostatic hypotension present at screening or history of clinically significant hypotensive episodes or symptoms of fainting, dizziness, or lightheadedness.
- Participants with abnormal electrocardiogram (ECG), bradycardia or mean QTc at screening
- Positive result for Hepatitis B, Hepatitis C, human immunodeficiency virus (HIV) 1 or 2 at screening
- Renal impairment
- Transplant recipients
- A known clinically relevant history of allergy or hypersensitivity
- Any clinically relevant abnormal laboratory test results
- A clinically relevant history of abuse of alcohol or other drugs of abuse
- Any major illness within 30 days prior to the screening examination
- Smoking of more than 10 cigarettes a day or an equivalent amount of tobacco in the form of cigars or pipe
- Participation in a clinical study with an investigational drug within 3 months prior to Day 1
- Donation/loss of more than 500 milliliters (mL) of blood within 3 months prior to Day 1
- Positive pregnancy test at screening or Day -1 and lactating women
Data sourced from ClinicalTrials.gov (NCT02717754). 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.