Tedizolid Phosphate

Summary

Tedizolid Phosphate (CHEMBL2105669) is an approved small-molecule antimicrobial agent; indicated across 9 conditions including skin disease caused by bacterial infection and skin disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 9 conditions
• Clinical trials: 15
• Chemistry: 450.3 Da · C17H16FN6O6P

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2105669
Name	Tedizolid Phosphate
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	11476460
ChEBI	CHEBI:83326
Molecular formula	C17H16FN6O6P
Molecular weight	450.3
InChIKey	QCGUSIANLFXSGE-GFCCVEGCSA-N

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

IUPAC name: [(5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)-3-pyridinyl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl dihydrogen phosphate

ChEBI definition: A phosphate monoester resulting from the formal condensation of equimolar amounts of phosphoric acid with the hydroxy group of tedizolid . It is a prodrug of tedizolid, used for the treatment of acute bacterial skin 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, prodrug.

Also known as: Sivextro, Tedizolid phosphate, TR-701 FA, TR-701FA, TEDIZOLID PHOSPHATE, TEDIZOLID (PHOSPHATE), Tedizolid (phosphate), TOREZOLID PHOSPHATE SODIUM

Parent form; salt/anhydrous children: CHEMBL5314419

Patent coverage: 135 distinct patent families (289 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 217 (75%) 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

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

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

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
skin disease caused by bacterial infection	4	MONDO:0024295	MONDO:0024295

6 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
skin disorder	3	MONDO:0005093	EFO:0000701
pneumonia	3	MONDO:0005249	EFO:0003106
bacterial infectious disease	3	MONDO:0005113	EFO:0000771
liver disorder	1	MONDO:0005154	EFO:0001421
kidney disorder	1	MONDO:0005240	EFO:0003086
gram-positive bacterial infections	1	MONDO:0021679	MONDO:0021679

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

Clinical trials

Total trials: 15.

Phase distribution

Phase	Trials
PHASE1	9
PHASE3	4
PHASE4	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02342418	PHASE4	COMPLETED	Single Dose PK of IV Tedizolid Phosphate in Morbidly Obese and Non-Obese Adults
NCT03746327	PHASE4	COMPLETED	Efficacy and Tolerance of 4 Weeks of Tedizolid in Prosthetic Joint Infections Treated With Implant Removal
NCT01170221	PHASE3	COMPLETED	TR-701 FA vs. Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections.
NCT01421511	PHASE3	COMPLETED	TR-701 FA vs Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections
NCT02019420	PHASE3	COMPLETED	Tedizolid Phosphate (TR-701 FA, MK-1986) vs Linezolid for the Treatment of Nosocomial Pneumonia (MK-1986-002)
NCT03176134	PHASE3	COMPLETED	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)
NCT00983255	PHASE1	COMPLETED	Ascending Dose Pharmacokinetic (PK) and Absolute Bioavailability (BA)
NCT01156077	PHASE1	COMPLETED	Pharmacokinetic (PK) Study of Oral and IV TR-701 FA in Adolescent Patients
NCT01271998	PHASE1	COMPLETED	Pulmonary Disposition of TR-700 Following Once-Daily Oral 200 mg
NCT01431833	PHASE1	COMPLETED	A PK and Safety Study in Subjects With Hepatic Impairment
NCT01452828	PHASE1	COMPLETED	A Pharmacokinetics and Safety Study in Subjects With Renal Impairment
NCT01461460	PHASE1	COMPLETED	A Thorough QT Study of TR-701free Acid (FA) in Healthy Subjects
NCT01496677	PHASE1	COMPLETED	Pharmacokinetics, Safety, and Tolerability of TR-701 Free Acid (FA) in Elderly Subjects
NCT01623401	PHASE1	COMPLETED	A Phase 1, Open-Label, 10 Day Safety Study
NCT02477514	PHASE1	COMPLETED	A Study to Evaluate the Effects of Tedizolid Phosphate on the Pharmacokinetics and Safety of Midazolam and Rosuvastatin (MK-1986-004)

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).