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Completed

NCT Number: NCT03217565

A Pharmacokinetic Study of Tedizolid Phosphate in Pediatric Participants With Gram-Positive Infections (MK-1986-014)

The primary objectives of this study are to describe the single-dose, and multiple dose pharmacokinetics (PK) of intravenous (IV) tedizolid phosphate, or a single dose oral suspension of tedizolid phosphate, when administered to pediatric participants, full-term neonates, and preterm neonates.

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Key information

Conditions

Gram-Positive Infections

Age range

1 day–24 month

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Medical Center - 1- Sevlievo EOOD ( Site 2207), Sevlievo, Gabrovo, Bulgaria

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About this study

Per protocol, PK analysis in Part A Group 1 will be conducted across ages in Cohorts 1 and 2 combined: Part A Group 1 Cohort 1 + Cohort 2: 28 days to <24 months.

Who can participate

Healthy volunteers accepted: No

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Is receiving prophylaxis for or has a confirmed or suspected infection with gram-positive bacteria and receiving concurrent antibiotic treatment with gram -positive antibacterial activity.
  • Is at least 1 kg in weight.
  • Is in stable condition as determined from medical history, physical examination, electrocardiogram (ECG), vital signs, and clinical laboratory evaluations.
  • Has no clinically significant ECG abnormalities.
  • Has sufficient vascular access to receive trial drug, and allow for required blood draws.
  • Is able to receive medication by mouth, for those dosed with oral suspension; dose administration via feeding tube is acceptable.

Exclusion criteria

  • Has a history of seizures, other than febrile seizures, clinically significant cardiac arrhythmia or condition, moderate or severe renal impairment, or any physical condition that could interfere with the interpretation of the study results, as determined by the Investigator.
  • Has used rifampin within 14 days prior to dosing.
  • Has used or will be using proton pump inhibitors, H2 blockers, or antacids (for participants in Part B, i.e, oral suspension dose) at any time from 24 hours prior to dosing through 24 hours after dosing..
  • Has a recent (3-month) history or current infection with viral hepatitis or other significant hepatic disease.
  • Has a history of drug allergy or hypersensitivity to oxazolidinones.
  • Has had significant blood loss.
  • Need for oral administration of topotecan, rosuvastatin, irinotecan, or methotrexate during administration of oral study drug.
  • Used monoamine oxidase inhibitors (MAOIs) or serotonergic agents including tricyclic antidepressants, selective serotonin reuptake inhibitors (SSRIs), and serotonin 5-hydroxytryptamine receptor agonists (triptans), meperidine, or buspirone within 14 days prior to study, or planned use while on study.
  • Has received another investigational product within the 30 days prior to enrollment.

Treatment and study plan

IV Tedizolid Phosphate

Drug

A single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.

Oral Suspension Tedizolid Phosphate

Drug

A single dose of tedizolid phosphate administered as an oral suspension.

Primary outcomes

  1. Part A: Area Under the Concentration-time Curve From Time 0 to Time of Last Quantifiable Drug Concentration (AUC0-last) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    AUC0-last of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of pharmacokinetic (PK) outcomes in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, tedizolid phosphate AUC0-last for multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol.

  2. Part A: Area Under the Concentration-time Curve From Time 0 to Infinity (AUC0-inf) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    AUC0-inf of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK outcomes in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, tedizolid phosphate AUC0-inf for multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol.

  3. Part A: Maximum Concentration (Cmax) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    Cmax of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK outcomes in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, tedizolid phosphate Cmax for multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol.

  4. Part A: Time to Reach Maximum Concentration (Tmax) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    Tmax of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK outcomes in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, tedizolid phosphate Tmax for multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol.

  5. Part A: Apparent Terminal Half-life (t½) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    t½ of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK outcomes in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, tedizolid phosphate t½ for multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol.

  6. Part A: AUC0-last of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    AUC0-last of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. As specified in the protocol, tedizolid phosphate AUC0-last for single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol. Participants in Group 2 Cohort 2 study arm did not meet the criteria for PK per protocol analysis population for this outcome and were excluded from this protocol-specified analysis.

  7. Part A: AUC0-inf of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    AUC0-inf of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. As specified in the protocol, tedizolid phosphate AUC0-inf for single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol. Participants in Group 2 Cohort 2 study arm did not meet the criteria for PK per protocol analysis population for this endpoint and were excluded from this protocol-specified analysis.

  8. Part A: Cmax of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    Cmax of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. As specified in the protocol, tedizolid phosphate Cmax for single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol. Participants in Group 2 Cohort 2 study arm did not meet the criteria for PK per protocol analysis population for this outcome and were excluded from this protocol-specified analysis.

  9. Part A: Tmax of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    Tmax of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. As specified in the protocol, tedizolid phosphate Tmax for single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol. Participants in Group 2 Cohort 2 study arm did not meet the criteria for PK per protocol analysis population for this outcome and were excluded from this protocol-specified analysis.

  10. Part A: t½ of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    t½ of tedizolid phosphate was quantified in participants receiving tedizolid phosphate. As specified in the protocol, tedizolid phosphate t½ for single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1) were not included in this outcome and have been reported separately in the record. Tedizolid phosphate PK analysis was not planned or conducted in Part B (Groups 4, 5, 6), per protocol. Participants in Group 2 Cohort 2 study arm did not meet the criteria for PK per protocol analysis population for this outcome and were excluded from this protocol-specified analysis.

  11. Part A: AUC0-24 of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate [AUC0-last]

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    AUC0-last of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK endpoints in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, AUC0-last for tedizolid metabolite in multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) and Part B (Groups 4, 5, 6) were not included in this endpoint and have been reported separately in the record.

  12. Part A: AUC0-inf of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    AUC0-inf of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK endpoints in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, AUC0-inf for tedizolid metabolite in multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) and Part B (Groups 4, 5, 6) were not included in this endpoint and have been reported separately in the record.

  13. Part A: Cmax of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    Cmax of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK endpoints in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, Cmax for tedizolid metabolite in multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) and Part B (Groups 4, 5, 6) were not included in this endpoint and have been reported separately in the record.

  14. Part A: Tmax of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    Tmax of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK endpoints in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, Tmax for tedizolid metabolite in multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) and Part B (Groups 4, 5, 6) were not included in this endpoint and have been reported separately in the record.

  15. Part A: t½ of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate

    Time frame: 1, 1.5, 3, 6, 12 and 24 hours post start of dosing

    t½ of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. Protocol specified analysis of PK endpoints in Group 1 was done irrespective of age (28 days to <24 months, across ages in Cohorts 1 and 2). As specified in the protocol, t½ for tedizolid metabolite in multiple dose (Part A Group 2 Cohort 2, Group 3 Cohort 2) and Part B (Groups 4, 5, 6) were not included in this endpoint and have been reported separately in the record.

  16. Part A: AUC0-12 of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate [AUC0-last]

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    AUC0-last of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single concentration listing. This was analyzed in the per protocol population consisting of the subset of participants who complied with the protocol sufficiently to ensure that these data would be likely to exhibit treatment effects, based on the underlying scientific model and had data available for this endpoint. As specified in the protocol, AUC0-last for tedizolid metabolite in single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1; Part B [Groups 4, 5, 6]) were not included in this endpoint and have been reported separately in the record.

  17. Part A: Cmax of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    Cmax of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single concentration listing. As specified in the protocol, Cmax for tedizolid metabolite in single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1; Part B [Groups 4, 5, 6]) were not included in this endpoint and have been reported separately in the record.

  18. Part A: Tmax of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    Tmax of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single listing. As specified in the protocol, Tmax for tedizolid metabolite in single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1; Part B [Groups 4, 5, 6]) were not included in this endpoint and have been reported separately in the record.

  19. Part A: AUC0-inf of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    AUC0-inf of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach to be used in this noncompartmental analysis would allow data collected to generate single concentration listing. However, protocol-specified PK sampling did not characterize the terminal elimination phase; therefore, AUC0-inf of tedizolid metabolite could not be estimated for multiple dose study arms (Part A Group 2 Cohort 2 and Part A Group 3 Cohort 2). As specified in the protocol, AUC0-inf for tedizolid metabolite in single dose (Part A Group 1[Cohorts 1 and 2],Group 2 Cohort 1, Group 3 Cohort 1; Part B[Groups 4, 5, 6]) were not included in this endpoint and have been reported separately in the record.

  20. Part A: t½ of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate

    Time frame: Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing

    t½ of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach to be used in this noncompartmental analysis would allow data collected to generate single listing. However, protocol-specified PK sampling did not characterize the terminal elimination phase; therefore, t½ could not be estimated for multiple dose study arms (Part A Group 2 Cohort 2 and Part A Group 3 Cohort 2). As specified in the protocol, t½ for tedizolid metabolite in single dose (Part A Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 3 Cohort 1; Part B [Groups 4, 5, 6]) were not included in this endpoint and have been reported separately in the record.

  21. Part B: Area Under the Concentration-time Curve From Time 0 to 24 Hours (AUC0-24) of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension [AUC0-last]

    Time frame: 1, 3, 5, 8, 12, and 24 hours post start of dosing

    AUC0-last of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single concentration listing. As specified in the protocol, AUC0-last for tedizolid metabolite in Part A (Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 2 Cohort 2, Group 3 Cohort 1, Group 3 Cohort 2) were not included in this endpoint and have been reported separately in the record.

  22. Part B: AUC0-inf of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension

    Time frame: 1, 3, 5, 8, 12, and 24 hours post start of dosing

    AUC0-inf of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single concentration listing. As specified in the protocol, AUC0-inf for tedizolid metabolite in Part A (Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 2 Cohort 2, Group 3 Cohort 1, Group 3 Cohort 2) were not included in this endpoint and have been reported separately in the record.

  23. Part B: Cmax of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension

    Time frame: 1, 3, 5, 8, 12, and 24 hours post start of dosing

    Cmax of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single concentration listing. As specified in the protocol, Cmax for tedizolid metabolite in Part A (Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 2 Cohort 2, Group 3 Cohort 1, Group 3 Cohort 2) were not included in this endpoint and have been reported separately in the record.

  24. Part B: Tmax of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension

    Time frame: 1, 3, 5, 8, 12, and 24 hours post start of dosing

    Tmax of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single listing. As specified in the protocol, Tmax for tedizolid metabolite in Part A (Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 2 Cohort 2, Group 3 Cohort 1, Group 3 Cohort 2) were not included in this endpoint and have been reported separately in the record.

  25. Part B: t½ of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension

    Time frame: 1, 3, 5, 8, 12, and 24 hours post start of dosing

    t½ of tedizolid (metabolite) was quantified in participants receiving tedizolid phosphate. The per protocol statistical approach used in this noncompartmental analysis allowed data collected to generate single listing. As specified in the protocol, t½ for tedizolid metabolite in Part A (Group 1 [Cohorts 1 and 2], Group 2 Cohort 1, Group 2 Cohort 2, Group 3 Cohort 1, Group 3 Cohort 2) were not included in this endpoint and have been reported separately in the record.

Secondary outcomes

  1. Number of Participants With an Adverse Event (AE)

    Time frame: Up to approximately 21 days

    An AE was defined as any untoward medical occurrence in a participant, temporally associated with the use of study treatment, whether or not considered related to the study treatment. The number of participants experiencing an AE was reported for each arm.

  2. Number of Participants That Discontinued Study Treatment Due to an AE

    Time frame: Up to approximately 3 days

    An AE was defined as any untoward medical occurrence in a participant, temporally associated with the use of study treatment, whether or not considered related to the study treatment. The number of participants that discontinued study treatment due to an AE was reported for each arm.

Sponsors and collaborators

Lead sponsor

Merck Sharp & Dohme LLC

Industry

Registry information

Official study title

A Phase 1, Single- and Multiple-Dose Safety and Pharmacokinetic Study of Oral and IV Tedizolid Phosphate (MK-1986) in Inpatients Under 2 Years Old

Important dates

Study start
2019
Primary completion
2023
Study completion
2023
First posted
Jul 14, 2017
Registry last updated
Feb 11, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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