Phase 1
Completed N=32
A Study of Oral and Intravenous (IV) Tedizolid Phosphate in Hospitalized Participants, Ages 2 to <12 Years, With Confirmed or Suspected Bacterial Infection (MK-1986-013)
Gram-Positive Bacterial Infections
Source: ClinicalTrials.gov NCT02750761 ↗
Enrolled (actual)
32
Serious AEs
3.1%
Results posted
Dec 2019
Primary outcomePrimary: Maximum Observed Drug Concentration in Plasma (Cmax) of Tedizolid Phosphate (Prodrug) — 76.3; 82.4; 710; 234 ng/mL
Summary
This is a study to assess the pharmacokinetics (PK) of tedizolid phosphate and its active metabolite, tedizolid, and the safety of tedizolid phosphate following administration of a single IV (Part A) or oral suspension (Part B) administration to hospitalized participants ages 6 to <12 years (Groups 1 and 3, respectively), and 2 to <6 years (Groups 2 and 4, respectively).
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Maximum Observed Drug Concentration in Plasma (Cmax) of Tedizolid Phosphate (Prodrug) |
76.3; 82.4; 710; 234; NA; 9.4 | — |
| PRIMARY Time to Reach Peak Plasma Concentration (Tmax) of Tedizolid Phosphate (Prodrug) |
1.18; 1.10; 1.12; 1.02; NA; 6.0 | — |
| PRIMARY Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid Phosphate (Prodrug) From Time Zero to Last Detectable Measurement |
64.8; 63.6; 433; 182; NA; 14.1 | — |
| PRIMARY Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid Phosphate (Prodrug) From Time Zero to Infinity |
NA; NA; NA; 2000; NA; NA | — |
| PRIMARY Terminal Elimination Half-life (T1/2) of Tedizolid Phosphate (Prodrug) |
NA; NA; NA; 2.77; NA; NA | — |
| PRIMARY Clearance (CL) of Tedizolid Phosphate (Prodrug) in Participants Who Received Tedizolid Phosphate Intravenously (IV) |
NA; NA; NA; 24400 | — |
| PRIMARY Clearance (CL/F) of Tedizolid Phosphate in Participants Who Received Oral Tedizolid Phosphate (Prodrug) |
NA; NA | — |
| PRIMARY Maximum Observed Drug Concentration in Plasma (Cmax) of Tedizolid (the Active Metabolite) |
4960; 4140; 7460; 4190; 2590; 1820 | — |
| PRIMARY Time to Reach Peak Plasma Concentration (Tmax) of Tedizolid (the Active Metabolite) |
1.18; 1.10; 1.12; 1.00; 2.53; 3.08 | — |
| PRIMARY Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Last Detectable Measurement |
28200; 19700; 26800; 17100; 22700; 14600 | — |
| PRIMARY Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Infinity |
29600; 21000; 27300; 17300; 24900; 17200 | — |
| PRIMARY Terminal Elimination Half-life (T1/2) of Tedizolid (Active Metabolite) |
5.18; 4.93; 5.51; 5.76; 6.15; 6.79 | — |
| PRIMARY Clearance (CL) of Tedizolid (Active Metabolite) in Participants Who Received Tedizolid Phosphate Intravenously (IV) |
4164.60; 4145.73; 2582.66; 2461.08 | — |
| PRIMARY Clearance (CL/F) of Tedizolid (Active Metabolite) in Participants Who Received Oral Tedizolid Phosphate |
4073.32; 2090.77 | — |
| PRIMARY Dose Normalized Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Infinity |
5340; 6000 | — |
| SECONDARY Number of Participants Who Experienced at Least One Adverse Event |
2; 1; 2; 0; 3; 1 | — |
| SECONDARY Number of Participants Who Discontinued Study Drug Due to an Adverse Event |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Palatability of Oral Tedizolid Phosphate Suspension in Participants Who Received Oral Tedizolid Phosphate |
0; 0; 0; 1; 3; 2 | — |
Eligibility Criteria
Inclusion Criteria
- Receiving prophylaxis for or with a confirmed or suspected infection with Gram-positive bacteria and receiving concurrent antibiotic treatment with Gram-positive antibacterial activity;
- Weight >5th percentile and <95th percentile based on age;
- Stable condition as determined from medical history, physical examination, minimally 5-lead electrocardiogram (ECG), vital signs, and clinical laboratory evaluations;
- Females must be premenarchal, abstinent, or practicing an effective method of birth control;
Exclusion Criteria
- History of seizures, other than febrile seizures, clinically significant cardiac arrhythmia, cystic fibrosis, moderate or severe renal impairment, or any physical condition that could interfere with the study results;
- Recent (3 month) history or current infection with viral hepatitis or other significant hepatic disease;
- History of drug allergy or hypersensitivity to oxazolidinones;
- Pregnant or breast feeding;
- Significant blood loss within 60 days prior to study start;
- Any acute or chronic condition that would limit the participant's ability to complete and/or participate in this clinical study.
- Treatment with investigational medicinal product within 30 days before the infusion/dose of study drug.
- Oral administration of methotrexate, topotecan, irinotecan or rosuvastatin, during administration of oral study drug. Administration during the follow-up period is allowed, as is administration during treatment with IV study drug.
- Use of monoamine oxidase inhibitors or serotonergic agents including tricyclic antidepressants, selective serotonin reuptake inhibitors, and serotonin 5 hydroxytryptamine receptor agonists (triptans), meperidine, or buspirone within,14 days prior to study, or planned use while on study.
Data sourced from ClinicalTrials.gov (NCT02750761). 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.