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

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

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.

Study Overview

• Status: Completed
• Conditions: Gram-Positive Infections
• Intervention / Treatment: Drug: IV Tedizolid Phosphate; Drug: Oral Suspension Tedizolid Phosphate

Detailed Description

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.

• Study Type: Interventional
• Enrollment (Actual): 47
• Phase: Phase 1

Contacts and Locations

Study Locations

• Bulgaria
  • Burgas, Bulgaria, 8127
    • UMHAT Deva Maria ( Site 2208)
  • Gabrovo, Bulgaria, 5300
    • MHAT Dr. Tota Venkova-Pediatrics ( Site 2218)
  • Montana, Bulgaria, 3400
    • MHAT "Dr. Stamen Iliev" Montana ( Site 2215)
  • Montana, Bulgaria, 3400
    • MHAT City Clinic Sv. Georgi EOOD ( Site 2202)
  • Pleven, Bulgaria, 5800
    • UMHAT Dr. Georgi Stranski EAD ( Site 2211)
  • Ruse, Bulgaria, 7002
    • MHAT Rousse-Neonatology ( Site 2213)
  • Ruse, Bulgaria, 7002
    • Multiprofile Hospital for Active Treatment - Ruse ( Site 2204)
  • Ruse, Bulgaria, 7002
    • UMHAT Kanev AD ( Site 2209)
  • Sliven, Bulgaria, 8800
    • MHAT Dr. Ival Seliminski ( Site 2212)
  • Gabrovo
    • Sevlievo, Gabrovo, Bulgaria, 5400
      • Medical Center - 1- Sevlievo EOOD ( Site 2207)
  • Vratsa
    • Kozloduy, Vratsa, Bulgaria, 3320
      • MHAT Sv. Ivan Rilski EOOD ( Site 2201)
• Colombia
  • Antioquia
    • Medellin, Antioquia, Colombia, 050010
      • Hospital San Vicente Fundacion ( Site 1103)
  • Atlantico
    • Barranquilla, Atlantico, Colombia, 080020
      • Clinica de la Costa S.A.S. ( Site 1106)
  • Distrito Capital De Bogota
    • Bogota, Distrito Capital De Bogota, Colombia, 111221
      • Fundacion Hospital Infantil Universitario de San Jose ( Site 1107)
  • Valle Del Cauca
    • Cali, Valle Del Cauca, Colombia, 760032
      • Fundacion Valle del Lili ( Site 1102)
• Norway
  • Akershus
    • Loerenskog, Akershus, Norway, 1478
      • Akershus Universitetssykehus HF ( Site 1604)
  • Hordaland
    • Bergen, Hordaland, Norway, 5021
      • Haukeland Universitetssjukehus ( Site 1602)
  • Rogaland
    • Stavanger, Rogaland, Norway, 4011
      • Stavanger Universitetssykehus, Helse Stavanger ( Site 1601)
  • Sor-Trondelag
    • Trondheim, Sor-Trondelag, Norway, 7006
      • St. Olavs Hospital. ( Site 1600)
• United Kingdom
  • Hampshire
    • Southampton, Hampshire, United Kingdom, SO16 6YD
      • University Hospital Southampton NHS Foundation Trust ( Site 1700)
  • Lancashire
    • Liverpool, Lancashire, United Kingdom, L12 2AP
      • Alder Hey Childrens NHS Foundation Trust Hospital ( Site 1703)
  • Newcastle Upon Tyne
    • Newcastle, Newcastle Upon Tyne, United Kingdom, NE1 4LP
      • Royal Victoria Infirmary ( Site 1702)
  • Oxfordshire
    • Oxford, Oxfordshire, United Kingdom, OX3 9DU
      • Oxford University Hospitals NHS Foundation Trust ( Site 1704)
• United States
  • Arkansas
    • Little Rock, Arkansas, United States, 72202
      • Arkansas Children's Hospital ( Site 1012)
  • California
    • Orange, California, United States, 92868
      • Children's Hospital of Orange County ( Site 1001)
    • San Diego, California, United States, 92123
      • Sharp Memorial Hospital ( Site 1021)
  • Illinois
    • Chicago, Illinois, United States, 60611
      • Ann & Robert H. Lurie Children's Hospital of Chicago ( Site 1022)
  • Louisiana
    • Baton Rouge, Louisiana, United States, 70808
      • Our Lady of the Lake Regional Medical Center. ( Site 1004)
  • Missouri
    • Saint Louis, Missouri, United States, 63110
      • Saint Louis Children's Hospital ( Site 1020)
  • Utah
    • Salt Lake City, Utah, United States, 84113
      • Primary Children's Hospital ( Site 1000)

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 1 day to 2 years (Child)
• Accepts Healthy Volunteers: No

Description

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Non-Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

9

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Part A Group 1 Cohort 1: Single Dose IV Tedizolid Phosphate 28 days to <6 months; Pediatric participants 28 days to <6 months of age will receive a single dose (SD) intravenous (IV) infusion of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg.	Drug: IV Tedizolid Phosphate; A single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.
Experimental: Part A Group 1 Cohort 2: Single Dose IV Tedizolid Phosphate 6 months to <24 months; Pediatric participants 6 months to <24 months of age will receive an SD IV infusion of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg.	Drug: IV Tedizolid Phosphate; A single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.
Experimental: Part A Group 2 Cohort 1: Single Dose IV Tedizolid Phosphate (full term) birth to <28 days; Full term (FT) neonates from birth to <28 days of age will receive an SD IV infusion of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg.	Drug: IV Tedizolid Phosphate; A single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.
Experimental: Part A Group 2 Cohort 2: Multiple Dose IV Tedizolid Phosphate (full term) birth to <28 days; FT neonates from birth to <28 days of age will receive multiple dose (MD) IV infusions of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg, administered twice daily for 3 days.	Drug: IV Tedizolid Phosphate; A single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.
Experimental: Part A Group 3 Cohort 1: Single Dose IV Tedizolid Phosphate (preterm) birth to <28 days; Preterm (PT) neonates from birth to <28 days of age will receive an SD IV infusion of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg.	Drug: IV Tedizolid Phosphate; A single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.
Experimental: Part A Group 3 Cohort 2: Multiple Dose IV Tedizolid Phosphate IV (preterm) birth to <28 days; PT neonates from birth to <28 days of age will receive MD IV infusions of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg, administered twice daily for 3 days.	Drug: IV Tedizolid Phosphate; A single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.
Experimental: Part B Group 4: Single Dose Oral Tedizolid Phosphate 28 days to <24 months; Pediatric participants 28 days to <24 months of age will receive an SD oral suspension of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg.	Drug: Oral Suspension Tedizolid Phosphate; A single dose of tedizolid phosphate administered as an oral suspension.
Experimental: Part B Group 5: Single Dose Oral Tedizolid Phosphate (full term) birth to <28 days; FT neonates from birth to <28 days of age will receive an SD oral suspension of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg.	Drug: Oral Suspension Tedizolid Phosphate; A single dose of tedizolid phosphate administered as an oral suspension.
Experimental: Part B Group 6: Single Dose Oral Tedizolid Phosphate (preterm) birth to <28 days; PT neonates from birth to <28 days of age will receive an SD oral suspension of tedizolid phosphate according to body weight: 3 mg/kg for body weight <10 kg or 2.5 mg/kg for body weight 10 to <30 kg.	Drug: Oral Suspension Tedizolid Phosphate; A single dose of tedizolid phosphate administered as an oral suspension.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
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	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: Area Under the Concentration-time Curve From Time 0 to Infinity (AUC0-inf) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: Maximum Concentration (Cmax) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: Time to Reach Maximum Concentration (Tmax) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: Apparent Terminal Half-life (t½) of Tedizolid Phosphate (Prodrug) After Single-dose IV Administration	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: AUC0-last of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: AUC0-inf of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: Cmax of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: Tmax of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: t½ of Tedizolid Phosphate (Prodrug) After Multiple-dose IV Administration	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: AUC0-24 of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate [AUC0-last]	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: AUC0-inf of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: Cmax of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: Tmax of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: t½ of Tedizolid (Active Metabolite) After Single-dose IV Administration of Tedizolid Phosphate	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.	1, 1.5, 3, 6, 12 and 24 hours post start of dosing
Part A: AUC0-12 of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate [AUC0-last]	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: Cmax of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: Tmax of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: AUC0-inf of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
Part A: t½ of Tedizolid (Active Metabolite) After Multiple-dose IV Administration of Tedizolid Phosphate	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.	Day 3: pre-dose, 1, 1.5, 3, 6 and 12 hours post start of dosing
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]	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.	1, 3, 5, 8, 12, and 24 hours post start of dosing
Part B: AUC0-inf of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension	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.	1, 3, 5, 8, 12, and 24 hours post start of dosing
Part B: Cmax of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension	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.	1, 3, 5, 8, 12, and 24 hours post start of dosing
Part B: Tmax of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension	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.	1, 3, 5, 8, 12, and 24 hours post start of dosing
Part B: t½ of Tedizolid (Active Metabolite) After Single-dose Administration of Tedizolid Phosphate Oral Suspension	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.	1, 3, 5, 8, 12, and 24 hours post start of dosing

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of Participants With an Adverse Event (AE)	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.	Up to approximately 21 days
Number of Participants That Discontinued Study Treatment Due to an AE	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.	Up to approximately 3 days

Collaborators and Investigators

• Sponsor: Merck Sharp & Dohme LLC
• Investigators: Study Director: Medical Director, Merck Sharp & Dohme LLC

Publications and helpful links

Helpful Links

• Merck Clinical Trials Information

Study record dates

Study Major Dates

• Study Start (Actual): February 6, 2019
• Primary Completion (Actual): March 18, 2023
• Study Completion (Actual): April 6, 2023

Study Registration Dates

• First Submitted: July 12, 2017
• First Submitted That Met QC Criteria: July 12, 2017
• First Posted (Actual): July 14, 2017

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: January 23, 2025
• Last Verified: January 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Infections; Anti-Bacterial Agents; Anti-Infective Agents; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protein Synthesis Inhibitors; Oxazolidinones; Tedizolid; Tedizolid phosphate
• Other Study ID Numbers: 1986-014; MK-1986-014 (Other Identifier: MSD Protocol Number); 2017-000953-38 (EudraCT Number)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: YES
• IPD Plan Description: http://engagezone.msd.com/doc/ProcedureAccessClinicalTrialData.pdf

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No