Tedizolid

Summary

Tedizolid (CHEMBL1257051) is an approved small-molecule antimicrobial agent (ATC J01XX11); indicated across 2 conditions including bacterial infectious disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J01XX11
• Indications: 2 conditions
• Clinical trials: 10
• Chemistry: 370.3 Da · C17H15FN6O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1257051
Name	Tedizolid
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	11234049
ChEBI	CHEBI:82717
ATC	J01XX11
Molecular formula	C17H15FN6O3
Molecular weight	370.3
InChIKey	XFALPSLJIHVRKE-GFCCVEGCSA-N

SMILES: CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4C[C@@H](OC4=O)CO)F

IUPAC name: (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one

ChEBI definition: A member of the class of pyridines that is pyridine which is substituted by a 2-methyl-2H-tetrazol-5-yl group at position 2 and by a 2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl group at position 5. It is used as its phosphate pro-drug used for the treatment of acute bacterial skin and skin structure infections caused by certain susceptible bacteria, including Staphylococcus aureus (including methicillin-resistant strains (MRSA) and methicillin-susceptible strains), various Streptococcus species, and Enterococcus faecalis.

Pharmacological roles (ChEBI): antimicrobial agent, protein synthesis inhibitor.

Other ChEBI roles (chemical / environmental): drug metabolite.

Also known as: Sivextro, Tedizolid, TR-700, Torezolid, torezolid, TEDIZOLID, Tedizolide, tedizolid

Patent coverage: 873 distinct patent families (1,778 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,689 (95%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Amine oxidase [flavin-containing] A, Amine oxidase [flavin-containing] B.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
MAOB	5.24	IC50	5700	nM	CHEMBL_ACT_16402689
MAOA	5.06	IC50	8700	nM	CHEMBL_ACT_16402687

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
bacterial infectious disease	4	MONDO:0005113	EFO:0000771

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 10.

Phase distribution

Phase	Trials
PHASE1	4
PHASE3	3
PHASE4	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05398679	PHASE4	RECRUITING	Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis
NCT03746327	PHASE4	COMPLETED	Efficacy and Tolerance of 4 Weeks of Tedizolid in Prosthetic Joint Infections Treated With Implant Removal
NCT01967225	PHASE3	COMPLETED	Safety and Efficacy of BAY1192631 in Japanese Patients With Methicillin-resistant Staphylococcus Aureus (MRSA) Infections
NCT02066402	PHASE3	COMPLETED	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)
NCT02276482	PHASE3	COMPLETED	Study of Tedizolid Phosphate in Adolescents With Complicated Skin and Soft Tissue Infection (cSSTI) (MK-1986-012)
NCT03009045	PHASE2	COMPLETED	Tolerability, Safety, and Efficacy of Tedizolid as Oral Treatment for Bone and Joint Infections (OTTER)
NCT02620787	PHASE1	COMPLETED	Tedizolid Tissue Penetration in Diabetic Patients With Wound Infections and Healthy Volunteers Via In Vivo Microdialysis
NCT02750761	PHASE1	COMPLETED	A Study of Oral and Intravenous (IV) Tedizolid Phosphate in Hospitalized Participants, Ages 2 to <12 Years, With Confirmed or Suspected Bacterial Infection (MK-1986-013)
NCT06609161	PHASE1	COMPLETED	A Study to Compare Oral Formulations of Tedizolid Phosphate in Healthy Adults (MK-1986-044)
NCT06733688	PHASE1	COMPLETED	A Study to Evaluate Oral Formulations of Tedizolid Phosphate in Healthy Participants (MK-1986-043)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).