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Tedizolid

Phase 3

Acute Bacterial Skin and Skin Structure Infections | Small molecule | Infectious Disease |Merck & Company, Inc.|Last Updated: Jul 31, 2025

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Trial Design

RandomizedACTIVE_CONTROLLEDDMC
Total Trials1
Total Enrollment100

FDA Designations

No designations recorded

Clinical trial landscape

Tedizolid · 6 trials · 6 indications

Phase 3 3Phase 1 3
NCT03176134A Study of Safety and Efficacy of MK-1986 (Tedizolid Phosphate) and Comparator in Participants From Birth to Less Than 12 Years of Age With Acute Bacterial Skin and Skin Structure Infections (MK-1986-018)Acute Bacterial Skin and Skin Structure Infections
COMPLETED100 Analytics
NCT02066402Efficacy and Safety of Intravenous to Oral 6-Day Tedizolid Phosphate vs. Intravenous to Oral 10-Day Linezolid in Patients With Acute Bacterial Skin and Skin Structure Infection (ABSSSI)Bacterial Infections
COMPLETED598 Analytics
NCT02019420Tedizolid Phosphate (TR-701 FA, MK-1986) vs Linezolid for the Treatment of Nosocomial Pneumonia (MK-1986-002)Pneumonia
COMPLETED726 Analytics
PHASE3COMPLETED
A Study of Safety and Efficacy of MK-1986 (Tedizolid Phosphate) and Comparator in Participants From Birth to Less Than 12 Years of Age With Acute Bacterial Skin and Skin Structure Infections (MK-1986-018)
Acute Bacterial Skin and Skin Structure InfectionsUnlock trial analytics
PHASE3COMPLETED
Efficacy and Safety of Intravenous to Oral 6-Day Tedizolid Phosphate vs. Intravenous to Oral 10-Day Linezolid in Patients With Acute Bacterial Skin and Skin Structure Infection (ABSSSI)
Bacterial InfectionsUnlock trial analytics
PHASE3COMPLETED
Tedizolid Phosphate (TR-701 FA, MK-1986) vs Linezolid for the Treatment of Nosocomial Pneumonia (MK-1986-002)
PneumoniaUnlock trial analytics

Study Endpoints

Primary Endpoints

Number of Participants Who Experienced an Adverse Event (AE)
Up to approximately 35 days

An AE was any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. An AE can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a study intervention. Number of participants who experienced an AE were reported.

Number of Participants Who Discontinued Study Treatment Due to an AE
Up to approximately day 15

An AE was any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. An AE can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a study intervention. Number of participants who experienced an AE were reported. The number of participants who discontinued study treatment due to an AE were reported.

Number of Participants With Hematopoietic Cytopenias
Up to approximately 35 days

Hematopoietic cytopenia is a condition where there is a lower-than-normal amount of one or multiple kinds of blood cells. A standardized Medical Dictionary for Regulatory Activities (MedDRA) query for hematopoietic cytopenia was conducted. The number of participants with a hematopoietic cytopenia were reported.

Percentage of Participants With Early Clinical Response at 48-72 Hours After the First Infusion of Study Drug in the ITT Analysis Set.
Baseline and 48-72 hours visit

Early clinical response is defined as responder if there is \>=20% reduction in the area of erythema, edema, and/or induration (length × width) of the primary acute bacterial skin and skin structure infections (ABSSSI) lesion, compared with baseline at the 48-72 Hour visit.

Number of Participants With All-Cause Mortality in the Intent-to-Treat (ITT) Population
Up to 28 days

The numbers of participants with all-cause mortality within 28 days after randomization was determined in the ITT population. Any participants who were lost to follow-up and not known to be alive or deceased by Day 28 were imputed as deceased.

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
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.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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]
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.

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

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

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

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

Maximum Observed Drug Concentration in Plasma (Cmax) of Tedizolid Phosphate (Prodrug)
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Cmax of tedizolid phosphate in participants ages 6 to \<12 years (Group 1) and 2 to \<6 years (Group 2). Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Time to Reach Peak Plasma Concentration (Tmax) of Tedizolid Phosphate (Prodrug)
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Time to reach peak plasma concentration (Tmax) of tedizolid phosphate in participants ages 6 to \<12 years (Group 1) and 2 to \<6 years (Group 2). Tedizolid phosphate concentrations were below the lower limit of quantification in Group 3 and Group 4. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid Phosphate (Prodrug) From Time Zero to Last Detectable Measurement
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Area under the plasma concentration time curve (AUC) of tedizolid phosphate from time zero to last detectable measurement following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid Phosphate (Prodrug) From Time Zero to Infinity
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Area under the plasma concentration time curve (AUC) of tedizolid phosphate from time zero to infinity following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Terminal Elimination Half-life (T1/2) of Tedizolid Phosphate (Prodrug)
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Terminal elimination half-life (T1/2) of tedizolid phosphate following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Clearance (CL) of Tedizolid Phosphate (Prodrug) in Participants Who Received Tedizolid Phosphate Intravenously (IV)
Group 1 (6 to <12 years): Day 1 immediately after infusion and at 1.5, 2, 3, 4, 6, 12, and 24 hours. Group 2 (2 to <6 years): Day 1 immediately after infusion and at 3, 6, 12, 24 and 48 hours.

CL of IV tedizolid phosphate in participants ages 6 to \<12 years (Group 1) and 2 to \<6 years (Group 2).

Clearance (CL/F) of Tedizolid Phosphate in Participants Who Received Oral Tedizolid Phosphate (Prodrug)
Group 3 (6 to <12 years): at 1, 2, 3, 4, 6, 8, 12, and 24 hours after the dose; Group 4 (2 to <6 years): at 3, 6, 9, 12, 24 and 48 hours after the dose

CL/F of oral suspension tedizolid phosphate and its active metabolite, tedizolid, in participants ages 6 to \<12 years (Group 3) and 2 to \<6 years (Groups 4).

Maximum Observed Drug Concentration in Plasma (Cmax) of Tedizolid (the Active Metabolite)
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Maximum observed drug concentration in plasma (Cmax) of tedizolid (active metabolite) following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Time to Reach Peak Plasma Concentration (Tmax) of Tedizolid (the Active Metabolite)
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Time to reach peak plasma concentration (Tmax) of tedizolid (active metabolite) following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Last Detectable Measurement
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Area under the plasma concentration time curve (AUC) of tedizolid (active metabolite) from time zero to last detectable measurement following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Infinity
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Area under the plasma concentration time curve (AUC) of tedizolid (active metabolite) from time zero to infinity following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Terminal Elimination Half-life (T1/2) of Tedizolid (Active Metabolite)
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

Terminal elimination half-life (T1/2) of tedizolid (active metabolite) following administration of IV or oral dose. Pharmacokinetic sampling occurred at the following time points: Group 1 (6 to \<12 years): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (IV): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (6 to \<12 years): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (2 to \<6 years): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Clearance (CL) of Tedizolid (Active Metabolite) in Participants Who Received Tedizolid Phosphate Intravenously (IV)
Group 1 (6 to <12 years): Day 1 immediately after infusion and at 1.5, 2, 3, 4, 6, 12, and 24 hours. Group 2 (2 to <6 years): Day 1 immediately after infusion and at 3, 6, 12, 24 and 48 hours.

CL of IV tedizolid phosphate and its active metabolite, tedizolid, in participants ages 6 to \<12 years (Group 1) and 2 to \<6 years (Group 2).

Clearance (CL/F) of Tedizolid (Active Metabolite) in Participants Who Received Oral Tedizolid Phosphate
Group 3 (6 to <12 years): at 1, 2, 3, 4, 6, 8, 12, and 24 hours after the dose; Group 4 (2 to <6 years): at 3, 6, 9, 12, 24 and 48 hours after the dose

CL/F of tedizolid, in participants ages 6 to \<12 years (Group 3) and 2 to \<6 years (Groups 4).

Dose Normalized Area Under the Plasma Concentration Time Curve (AUC) of Tedizolid (Active Metabolite) From Time Zero to Infinity
IV: immediately after the end of the infusion, and various time points up to 48 hours after the start of infusion as described above. Oral: at various time points up to 48 hours after the dose as described above.

The area under the plasma concentration time curve (AUC) of tedizolid (active metabolite) from time zero to infinity following administration of IV or oral dose, normalized to dosage, was calculated. Per protocol, this outcome used pooled groups as follows: The IV Group pooled Groups 1 and 2, who received tedizolid phosphate via intravenous (IV) administration; the Oral Group pooled groups 3 and 4, who received tedizolid phosphate via oral administration. Pharmacokinetic sampling occurred at the following time points: Group 1 (part of the IV Group): Day 1 immediately after infusion and 1.5, 2, 3, 4, 6, 12, and 24 hours; Group 2 (part of the IV Group): Day 1 immediately after infusion and 3, 6, 12, 24 and 48 hours; Group 3 (part of the Oral Group): Day 1 at 1, 2, 3, 4, 6, 8, 12, and 24 hours after oral dose; Group 4 (part of the Oral Group): Day 1 at 3, 6, 9, 12, 24 and 48 hours after oral dose.

Area under the concentration versus time curve, from 0 to last observed/measured non-zero concentration (AUC0-t) of midazolam alone or in combination with tedizolid phosphate
Days 1 and 14: pre-dose, 0.25, 0.5, 1, 1.5, 3, 4.5, 6, 8, 12, 24 hours
AUC0-t of rosuvastatin alone or in combination with tedizolid phosphate
Days 3 and 16: pre-dose, 1, 3, 4, 5, 6, 8, 16, 24, 36, 48 hours
Area under the concentration versus time curve from 0 to infinity (AUC0-inf) of midazolam alone or in combination with tedizolid phosphate
Days 1 and 14: pre-dose, 0.25, 0.5, 1, 1.5, 3, 4.5, 6, 8, 12, 24 hours
AUC0-inf of rosuvastatin alone or in combination with tedizolid phosphate
Days 3 and 16: pre-dose, 1, 3, 4, 5, 6, 8, 16, 24, 36, 48 hours
Maximum observed plasma concentration (Cmax) of midazolam alone or in combination with tedizolid phosphate
Days 1 and 14: pre-dose, 0.25, 0.5, 1, 1.5, 3, 4.5, 6, 8, 12, 24 hours
Cmax of rosuvastatin alone or in combination with tedizolid phosphate
Days 3 and 16: pre-dose, 1, 3, 4, 5, 6, 8, 16, 24, 36, 48 hours

Secondary Endpoints

Percentage of Participants With Clinical Response (CR) Per Investigator Assessment
Up to approximately 25 days
Percentage of Clinically Evaluable (CE) Participants With CR Per Investigator Assessment
Up to approximately 25 days
Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the ITT Analysis Set
Baseline and EOT visit (Day 11)
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Study Design & Arms

AllocationRANDOMIZED
MaskingSINGLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Cohort 1: Tedizolid phosphate 6 to <12 YearsEXPERIMENTALParticipants will receive tedizolid phosphate once-daily single 200-mg dose (body weight ≥50 kg) or twice-daily 2-mg/kg doses (body weight 30 kg to \<50 kg); or twice-daily 2.5-mg/kg doses (body weight 3.2 kg to \<30 kg), by IV and/or oral suspension for 6 to 10 days.
Cohort 1: Comparator 6 to <12 YearsACTIVE_COMPARATORParticipants will receive comparator IV and/or oral per local standard of care for 10 to 14 days.
Cohort 2: Tedizolid phosphate 2 to <6 YearsEXPERIMENTALParticipants will receive tedizolid phosphate once-daily single 200-mg dose (body weight ≥50 kg) or twice-daily 2-mg/kg doses (body weight 30 kg to \<50 kg); or twice-daily 2.5-mg/kg doses (body weight 3.2 kg to \<30 kg), by IV and/or oral suspension for 6 to 10 days.
Cohort 2: Comparator 2 to <6 YearsACTIVE_COMPARATORParticipants will receive comparator IV and/or oral per local standard of care for 10 to 14 days.
Cohort 3: Tedizolid phosphate 28 Days to <2 YearsEXPERIMENTALParticipants will receive tedizolid phosphate once-daily single 200-mg dose (body weight ≥50 kg) or twice-daily 2-mg/kg doses (body weight 30 kg to \<50 kg); or twice-daily 2.5-mg/kg doses (body weight 3.2 kg to \<30 kg), by IV and/or oral suspension for 6 to 10 days.
Cohort 3: Comparator 28 Days to <2 YearsACTIVE_COMPARATORParticipants will receive comparator IV and/or oral per local standard of care for 10 to 14 days.
Cohort 4: Tedizolid phosphate Birth to <28 Days Term and Preterm NeonatesEXPERIMENTALParticipants will receive tedizolid phosphate ≤200 mg daily dose, IV and/or oral suspension for 6 to 10 days. Exact mg/kg dose is to be determined based on results of another study (NCT03217565) covering the age range.
Cohort 4: Comparator Birth to <28 Days Term and Preterm NeonatesACTIVE_COMPARATORParticipants will receive comparator IV and/or oral per local standard of care for 10 to14 days.
Tedizolid Phosphate (Sivextro, BAY119-2631)EXPERIMENTALParticipants received 200 mg Tedizolid Phosphate once daily intravenous (I.V.) infusion to oral for 6 days, followed by 4 days of placebo.
LinezolidACTIVE_COMPARATORParticipants received 600 mg Linezolid twice daily I.V. infusion to oral for 10 days.
Tedizolid phosphate IVEXPERIMENTALVentilated HABP/VABP participants receive tedizolid phosphate 200 mg IV once daily for 7 days, or for 14 days for concurrent bacteremia.
Linezolid IVACTIVE_COMPARATORVentilated HABP/VABP participants receive linezolid 600 mg IV every 12 hours for 10 days, or for 14 days for concurrent bacteremia.
Part A Group 1 Cohort 1: Single Dose IV Tedizolid Phosphate 28 days to <6 monthsEXPERIMENTALPediatric 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.
Part A Group 1 Cohort 2: Single Dose IV Tedizolid Phosphate 6 months to <24 monthsEXPERIMENTALPediatric 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.
Part A Group 2 Cohort 1: Single Dose IV Tedizolid Phosphate (full term) birth to <28 daysEXPERIMENTALFull 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.
Part A Group 2 Cohort 2: Multiple Dose IV Tedizolid Phosphate (full term) birth to <28 daysEXPERIMENTALFT 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.
Part A Group 3 Cohort 1: Single Dose IV Tedizolid Phosphate (preterm) birth to <28 daysEXPERIMENTALPreterm (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.
Part A Group 3 Cohort 2: Multiple Dose IV Tedizolid Phosphate IV (preterm) birth to <28 daysEXPERIMENTALPT 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.
Part B Group 4: Single Dose Oral Tedizolid Phosphate 28 days to <24 monthsEXPERIMENTALPediatric 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.
Part B Group 5: Single Dose Oral Tedizolid Phosphate (full term) birth to <28 daysEXPERIMENTALFT 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.
Part B Group 6: Single Dose Oral Tedizolid Phosphate (preterm) birth to <28 daysEXPERIMENTALPT 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.
Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 years)EXPERIMENTALParticipants 6 to \<12 years of age received a single intravenous infusion of tedizolid phosphate dosed at 5 mg/kg of total body weight. Maximum dose is 200 mg of tedizolid phosphate.
Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 years)EXPERIMENTALParticipants 6 to \<12 years of age received a single intravenous infusion of tedizolid phosphate dosed at 4 mg/kg of total body weight. Maximum dose is 200 mg of tedizolid phosphate.
Group 2 Cohort 1: Tedizolid IV 6 mg/kg (2 to <6 years)EXPERIMENTALParticipants 2 to \<6 years of age received a single intravenous infusion of tedizolid phosphate dosed at 6 mg/kg of total body weight. Maximum dose is 200 mg of tedizolid phosphate.
Group 2 Cohort 2: Tedizolid IV 3 mg/kg (2 to <6 years)EXPERIMENTALParticipants 2 to \<6 years of age received a single intravenous infusion of tedizolid phosphate dosed at 3 mg/kg of total body weight. Maximum dose is 200 mg of tedizolid phosphate.
Group 3: Tedizolid oral 4 mg/kg (6 to <12 years)EXPERIMENTALParticipants 6 to \<12 years of age received a single dose of tedizolid phosphate oral suspension dosed at 4 mg/kg of total body weight. Maximum dose is 200 mg of tedizolid phosphate.
Group 4: Tedizolid oral 3 mg/kg (2 to <6 years)EXPERIMENTALParticipants 2 to \<6 years of age received a single dose of tedizolid phosphate oral suspension dosed at 3 mg/kg of total body weight. Maximum dose is 200 mg of tedizolid phosphate.
Experimental ArmEXPERIMENTALDay 1: participants will receive midazolam (2 mg); Day 3: participants will receive rosuvastatin (10 mg); Days 5-13: participants will receive tedizolid phosphate (200 mg); Day 14: participants will receive tedizolid phosphate (200 mg) plus midazolam (2 mg); Day 15: participants will receive tedizolid phosphate (200 mg); Day 16: participants will receive tedizolid phosphate (200 mg) plus rosuvastatin (10 mg); Day 17: participants will receive tedizolid phosphate (200 mg)

Interventions

NameTypeDescription
Tedizolid phosphateDRUGTedizolid phosphate IV solution or oral suspension
ComparatorDRUGVancomycin IV, linezolid IV or oral (outside European Union only), clindamycin IV or oral, flucloxacillin IV or oral, cefazolin IV, or cephalexin oral provided locally by the trial site and administered per local standard of care
Tedizolid (BAY119-2631)DRUG50 % of the participants will be randomized to this arm and will receive 200 mg Tedizolid once daily i.v to oral from 1-6 days
Placebo Tedizolid (BAY119-2631)DRUG50 % of the participants will be randomized to this arm and will receive 200 mg Placebo Tedizolid once daily i.v to oral from 7-10 days
LinezolidDRUG50 % of the participants will be randomized to this arm and will receive 600 mg Linezolid twice daily i.v. to oral from 1-10 days
Placebo LinezolidDRUG50 % of the participants will be randomized to this arm and will receive 600 mg Placebo Linezolid twice daily i.v. to oral from 1-10 days
IV Tedizolid PhosphateDRUGA single dose, or twice daily dose for 3 days, of tedizolid phosphate administered IV.
Oral Suspension Tedizolid PhosphateDRUGA single dose of tedizolid phosphate administered as an oral suspension.
Tedizolid Phosphate (IV)DRUG200 mg/vial powder for injection
Tedizolid Phosphate (oral suspension)DRUGPowder for oral suspension 20 mg/mL following reconstitution
midazolamDRUG2 mg (1 mL of 2 mg/mL oral syrup) administered as a single dose on Days 1 and 14
rosuvastatinDRUG10 mg tablet administered as a single oral dose on Days 3 and 16
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Eligibility Criteria

Age Range1 Day to 11 Years
SexALL
Healthy VolunteersNo
Study Sites58

Inclusion Criteria: * Has a parent/legally acceptable representative who is able to give documented informed consent * Has acute bacterial skin and skin structure infections (ABSSSI), defined as ≥1 of the following: 1) cellulitis/erysipelas, 2) major cutaneous abscess, or 3) wound infection * Local...

Countries:United StatesBrazilBulgariaGeorgiaGermanyGuatemalaLatviaLithuaniaMexicoPolandRussiaSouth AfricaTurkey (Türkiye)UkraineChinaPhilippinesTaiwanColombiaNorwayUnited Kingdom
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Frequently asked questions about Tedizolid

What is Tedizolid used for?

Tedizolid is an oxazolidinone antibiotic used for bacterial infections, including gram-positive bacterial infections and acute bacterial skin and skin structure infections (ABSSSI). It is being studied for these indications in clinical trials.

What does Tedizolid target?

Tedizolid is a small molecule antibiotic that targets bacterial protein synthesis. It binds to the 50S ribosomal subunit, inhibiting translation and preventing bacterial growth. This mechanism is effective against gram-positive bacteria, including resistant strains.

Who makes Tedizolid?

Tedizolid is developed by Merck & Company, Inc., which trades under the ticker symbol MRK on the New York Stock Exchange. Merck is conducting clinical trials to evaluate the drug for various bacterial infections.

What phase is Tedizolid in?

Tedizolid is in Phase 3 clinical development for bacterial infections. It is an investigational drug and has not been approved by regulatory authorities. Multiple Phase 3 trials have been completed to assess its efficacy and safety.

What clinical trials is Tedizolid in?

Tedizolid has been studied in several clinical trials, including NCT02019420 for nosocomial pneumonia, NCT02066402 for ABSSSI, NCT03176134 for pediatric ABSSSI, and NCT03217565 for pharmacokinetics in pediatric gram-positive infections. All trials are completed.

Is Tedizolid the same as Sivextro?

Tedizolid is also known as tedizolid phosphate, which is the prodrug form. The drug is marketed under the brand name Sivextro in some regions. Clinical trials often refer to it as MK-1986 or TR-701 FA.