RADEZOLID

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H23FN6O3
Molecular Weight	438.4548
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(=O)NC[C@H]1CN(C(=O)O1)C2=CC(F)=C(C=C2)C3=CC=C(CNCC4=CN=NN4)C=C3

InChI

InChIKey=BTTNOGHPGJANSW-IBGZPJMESA-N

InChI=1S/C22H23FN6O3/c1-14(30)25-12-19-13-29(22(31)32-19)18-6-7-20(21(23)8-18)16-4-2-15(3-5-16)9-24-10-17-11-26-28-27-17/h2-8,11,19,24H,9-10,12-13H2,1H3,(H,25,30)(H,26,27,28)/t19-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=22191526

Radezolid (RX-1741) is a novel oxazolidinone antibiotic agent and is the first biaryloxazolidinone in clinical development. It is being developed by Rib-X Pharmaceuticals, Inc. for the treatment of serious multi-drug–resistant infections. Radezolid has completed two phase-II clinical trialsfor the treatment of community-acquired pneumonia; uncomplicated skin and skin structure infections. The mechanism of action for this drug seems to be an inhibition of 50S ribosomal subunit.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial 70S ribosome 179 Target ID: CHEMBL2363135 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19649920/	Inhibitor 8297

Conditions

Condition	Modality	Highest Phase	Product
Community-acquired pneumonia 47 Sources: https://clinicaltrials.gov/ct2/show/NCT00640926	Curative	Phase II 1132	Unknown Approved Use Unknown
Infectious skin diseases 2 Sources: https://clinicaltrials.gov/ct2/show/NCT00646958	Curative	Phase II 1132	Unknown Approved Use Unknown
Skin infections 59 Sources: https://clinicaltrials.gov/ct2/show/NCT00646958	Curative	Phase II 1132	Unknown Approved Use Unknown
Streptococcal infections 11 Sources: https://clinicaltrials.gov/ct2/show/NCT00646958	Curative	Phase II 1132	Unknown Approved Use Unknown

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY110822	https://www.001chemical.com/chem/search?q=DY110822
1PlusChem LLC	1P00GUMP	https://www.1pchem.com/search?query=1P00GUMP
Angene	AGN-PC-0V9NGN	http://www.angenechemical.com/productshow/AGN-PC-0V9NGN.html
ApexBio Technology	A3749	https://www.apexbt.com/catalogsearch/result/?q=A3749
BLD Pharm	BD265893	http://www.bldpharm.com/search/Search.html?keyword=BD265893
Chem Scene	CS-0688	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0688
ChemShuttle	100830	https://www.chemshuttle.com/catalogsearch/result/?q=100830
Excenen	EX-A1247	http://www.excenen.com/searchresultlist.php?id=EX-A1247
Matrix Scientific	143685	http://www.matrixscientific.com/143685.html
MedChem Express	HY-14800	https://www.medchemexpress.com/search.html?q=HY-14800&ft=&fa=&fp=
MolPort	MolPort-046-417-009	https://www.molport.com/shop/molecule-link/MolPort-046-417-009
Molcore	MC110822	http://www.molcore.com/CatMC110822.html
eMolecules	252366894	https://orderbb.emolecules.com/search/#?query=252366894
eMolecules	275100914	https://orderbb.emolecules.com/search/#?query=275100914
eMolecules	300763928	https://orderbb.emolecules.com/search/#?query=300763928
eMolecules	44811498	https://orderbb.emolecules.com/search/#?query=44811498
mcule	MCULE-8381518477	https://mcule.com/MCULE-8381518477/
mcule	MCULE-9737591986	https://mcule.com/MCULE-9737591986/

PubMed

Title	Date	PubMed
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.	2010 Jun	20385852

Patents

Sample Use Guides

In Vivo Use Guide

300 mg/day, orally for 7-10 days

Route of Administration: Oral

In Vitro Use Guide

It was studied the mechanisms involved in radezolid accumulation in cells, using THP-1 macrophages as a model. Data were obtained after 2 h of incubation with 50 mg/liter radezolid. When cells were incubated at 4°C, the apparent cellular concentrations of radezolid decreased to about 35 to 40% of their control values. In parallel experiments, we observed that radezolid's accumulation was not modified by either ATP depletion or efflux pump inhibitors.

Name

Type

Language

RADEZOLID

Official Name

English

Radezolid [WHO-DD]

Common Name

English

RX-013

Code

English

RX-1741

Code

English

RX-103

Code

English

radezolid [INN]

Common Name

English

AND RX-01_667

Code

English

RADEZOLID [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C258