Tedizolid

Tedizolid is an antibacterial drug [see Microbiology (12.4) ] .

• SIVEXTRO is an oxazolidinone antibacterial indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible microorganisms in adult and pediatric patients (at least 26 weeks gestational age and weighing at least 1 kg) ( 1.1 ) Usage to Reduce Development of Drug-Resistant Bacteria To reduce the development of drug-resistant bacteria and maintain the effectiveness of SIVEXTRO and other antibacterial drugs, SIVEXTRO should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

• None.contraindicated

Do not administer SIVEXTRO Tablets to pediatric patients weighing less than 35 kg. ( 2.1 ) Adult Patients Intravenous and Oral Dosage : 200 mg administered once daily orally or as an intravenous (IV) infusion over 1 hour for 6 days as specified in Table 1 in the full prescribing information. ( 2.2 ) Pediatric Patients Intravenous Dosage (at least 26 weeks gestational age and weighing at least 1 kg): Weight-based dosing as an intravenous infusion as specified in Table 2 in the full prescribing information. ( 2.3 ) Pediatric Patients Oral Dosage (weighing greater than or equal to 35 kg): Weight-based dosing as an oral tablet administered once daily as specified in Table 3 in the full prescribing information. ( 2.3 ) 2.1 Important Administration Instructions for Pediatric Patients Weighing Less than 35 kg Do not administer SIVEXTRO Tablets to pediatric patients weighing less than 35 kg [see Dosage and Administration 2.3 ]. 2.2 Recommended Dosage for Adult Patients The recommended dosage of SIVEXTRO is 200 mg administered once daily for six (6) days either as an oral tablet (with or without food) or as an intravenous (IV) infusion in adult patients. The recommended dosage and administration of SIVEXTRO in adult patients are described in Table 1 .

Serotonin Syndrome: Monitor patients taking SIVEXTRO concomitantly with serotonergic agents for signs of serotonin syndrome. If signs or symptoms of serotonin syndrome occur, consider discontinuing SIVEXTRO and/or concomitant serotonergic agents. ( 5.1 ) Patients with neutropenia: The safety and efficacy of SIVEXTRO in patients with neutropenia (neutrophil counts <1000 cells/mm 3 ) have not been adequately evaluated. In an animal model of infection, the antibacterial activity of SIVEXTRO was reduced in the absence of granulocytes. Consider alternative therapies in neutropenic patients. ( 5.2 ) Clostridioides difficile -Associated Diarrhea: Evaluate if diarrhea occurs. ( 5.3 ) 5.1 Serotonin Syndrome Spontaneous reports of serotonin syndrome have been observed with the co-administration of oxazolidinones, including SIVEXTRO, and serotonergic agents. Commonly used serotonergic agents include serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, tricyclic antidepressants, buspirone, serotonin 5-HT1 receptor agonists (triptans), and opioids, including meperidine. Symptoms associated with serotonin syndrome may include hyperthermia, diaphoresis, agitation, hyperreflexia, clonus, pyrexia, opsoclonus, muscle rigidity, tremor, and hypertonia. Monitor patients for the emergence of serotonin syndrome with the concomitant use of SIVEXTRO and serotonergic agents. If signs or symptoms of serotonin syndrome occur, consider discontinuing SIVEXTRO and/or concomitant serotonergic agents as clinically appropriate and initiate supportive treatment.

The following clinically significant adverse reactions are described elsewhere in the labeling: Serotonin Syndrome [see Warnings and Precautions (5.1) ] Clostridioides difficile -Associated Diarrhea [see Warnings and Precautions (5.3) ] The most common adverse reactions (≥2%) in adult patients are nausea, headache, diarrhea, infusion- or injection-related adverse reactions, vomiting, and dizziness. ( 6.1 ) The most common adverse reactions (>2%) in pediatric patients (12 years to less than 18 years of age) are phlebitis and increased hepatic transaminases. ( 6.1 ) The most common adverse reactions (>2%) in pediatric patients (less than 12 years of age) are infusion- or injection-related adverse reactions and vomiting. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme LLC at 1-877-888-4231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be compared directly to rates from clinical trials of another drug and may not reflect rates observed in practice. Clinical Trials Experience in Adult Patients Adverse reactions were evaluated for 1425 adult patients treated with SIVEXTRO in two Phase 2 and four Phase 3 clinical trials (three Phase 3 trials for 6 days of therapy and one Phase 3 trial for 7-21 days of therapy). The median age of adult patients treated with SIVEXTRO in the Phase 2 and Phase 3 trials was 44 years, ranging between 17 and 94 years old.

Pregnancy: Based on animal data, SIVEXTRO may cause fetal harm. Advise pregnant women of the potential risks to a fetus. ( 8.1 ) 8.1 Pregnancy Risk Summary Based on animal reproduction studies, SIVEXTRO may cause fetal harm when administered to pregnant women. The available data on the use of SIVEXTRO in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Advise pregnant women of the potential risks to a fetus. Fetal developmental toxicities were observed in mice and rats treated with SIVEXTRO. In embryo-fetal studies in mice and rats, tedizolid phosphate was shown to produce fetal developmental toxicities in mice and maternal toxicity and fetal developmental toxicities in rats. Tedizolid phosphate administered orally during organogenesis to pregnant animals was associated with reduced fetal weights and an increased incidence of costal cartilage anomalies in the absence of maternal toxicity in mice; and maternal toxicity, decreased fetal weights, and increased skeletal variations in rats at plasma exposures approximately 4 and 6 times respectively, the human plasma exposure at the maximum recommended human dose (MRHD) of 200 mg/day.

Metabolism

Tedizolid phosphate is a prodrug that is converted by phosphatases to tedizolid, the microbiologically active moiety, following oral and intravenous administration. Only the pharmacokinetic profile of tedizolid is discussed further due to negligible systemic exposure of tedizolid phosphate following oral and intravenous administration.

In the event of overdosage, SIVEXTRO should be discontinued and general supportive treatment given. Hemodialysis does not result in meaningful removal of tedizolid from systemic circulation.

• Jun 20, 2014NDANDA205435Cubist Pharms Llc
• Jun 20, 2014NDANDA205436Cubist Pharms Llc

1. 1Off Label Use11014%
2. 2Product Use In Unapproved Indication8812%
3. 3Thrombocytopenia597.7%
4. 4Anaemia445.8%
5. 5Nausea435.6%
6. 6No Adverse Event415.4%
7. 7Drug Ineffective364.7%
8. 8Product Availability Issue334.3%
9. 9Product Dose Omission Issue324.2%
10. 10Pancytopenia303.9%
11. 11Diarrhoea263.4%
12. 12Rash253.3%
13. 13Serotonin Syndrome212.7%
14. 14Vomiting212.7%
15. 15Death192.5%

The 10 most recently updated of 40 ClinicalTrials.gov registrations naming Tedizolid as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis
  Recruiting · Phase 4 · Interventional · 360 enrolled · Fundacion Clinic per a la Recerca Biomédica
  NCT05398679updated 2026-02-25
• Pathogenicity Factors of Staphylococcus Pettenkoferi in Foot Wounds and Osteitis in Diabetic Patients
  Active not recruiting · Observational · 230 enrolled · Centre Hospitalier Universitaire de Nīmes
  NCT06688084updated 2025-11-17
• Tedizolid Neuropathies
  Completed · Observational · 5 enrolled · Hospices Civils de Lyon
  NCT07143240updated 2025-08-27
• 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)
  Completed · Phase 3 · Interventional · 100 enrolled · Merck Sharp & Dohme LLC
  NCT03176134updated 2025-07-31
• Efficacy and Tolerance of 4 Weeks of Tedizolid in Prosthetic Joint Infections Treated With Implant Removal
  Completed · Phase 4 · Interventional · 30 enrolled · Fundacion Clinic per a la Recerca Biomédica
  NCT03746327updated 2025-03-12
• A Pharmacokinetic Study of Tedizolid Phosphate in Pediatric Participants With Gram-Positive Infections (MK-1986-014)
  Completed · Phase 1 · Interventional · 47 enrolled · Merck Sharp & Dohme LLC
  NCT03217565updated 2025-02-11
• Evaluation of the Early Bactericidal Activity of Tedizolid and Linezolide Against Mycobacterium Tuberculosis (TEDITUB)
  Recruiting · Phase 2 · Interventional · 60 enrolled · Assistance Publique - Hôpitaux de Paris
  NCT05534750updated 2025-02-03
• A Study to Evaluate Oral Formulations of Tedizolid Phosphate in Healthy Participants (MK-1986-043)
  Completed · Phase 1 · Interventional · 36 enrolled · Merck Sharp & Dohme LLC
  NCT06733688updated 2024-12-13
• A Study to Compare Oral Formulations of Tedizolid Phosphate in Healthy Adults (MK-1986-044)
  Completed · Phase 1 · Interventional · 18 enrolled · Merck Sharp & Dohme LLC
  NCT06609161updated 2024-09-27
• Tolerability, Safety, and Efficacy of Tedizolid as Oral Treatment for Bone and Joint Infections (OTTER)
  Completed · Phase 2 · Interventional · 44 enrolled · Lundquist Institute for Biomedical Innovation at Harbor-UCLA Medical Center
  NCT03009045updated 2023-12-13

Frequently asked questions

How does Tedizolid work?

Tedizolid is an antibacterial drug [see Microbiology (12.4) ] .

What is Tedizolid used for?

According to FDA labeling, Tedizolid carries indications including: SIVEXTRO is an oxazolidinone antibacterial indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible microorganisms in adult and pediatric patients (at least 26 weeks gestational age and weighing at least 1 kg) ( 1.1 ) Usage to Reduce Development of Drug-Resistant Bacteria To reduce the development of drug-resistant bacteria and maintain the effectiveness of SIVEXTRO and other antibacterial drugs, SIVEXTRO should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tedizolid?

Tedizolid is classified as Other antibacterials, Oxazolidinone Antibacterial, Breast Cancer Resistance Protein Inhibitors, Protein Synthesis Inhibitors, Decreased Protein Synthesis.

What are the brand names for Tedizolid?

Tedizolid is marketed under brand names including Sivextro.

What are the contraindications for Tedizolid?

Tedizolid labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.