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Phase 1 Completed N=32 Treatment

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

OutcomeResultp-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.
View full record on ClinicalTrials.gov →

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.

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