Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMECVP9)

Drug Name

OP-0595 Drug Info

Synonyms

Nacubactam; 1452458-86-4; RG6080; RG-6080; UNII-832O37V7MZ; RO7079901; 832O37V7MZ; FPI-1459; 1452458-86-4 (free acid); RO-7079901; (1R,2S,5R)-2-((2-aminoethoxy)carbamoyl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate; Nacubactam [INN]; Nacubactam (USAN); Nacubactam [USAN:INN]; CHEMBL3989959; SCHEMBL15206610; SCHEMBL17975933; GTPL10833; MFCD28986228; OP0595; ZINC207610051; DB15353; SB17180; AS-35134; HY-109008; CS-0030506; D11329; Q27269383; (1R,2S,5R)-2-((2-Aminoethoxy)carbamoyl)-7-oxo- 1,6-diazabicyclo(3.2.1)octan-6-yl hydrogen sulfate; (2S,5R)-2-(2-Aminoethoxycarbamoyl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate; (2S,5R)-N-(2-Aminoethoxy)-7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide; [(2S,5R)-2-(2-aminoethoxycarbamoyl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] hydrogen sulfate; Sulfuric acid, mono((1R,2S,5R)-2-(((2-aminoethoxy)amino)carbonyl)-7-oxo-1,6-diazabicyclo(3.2.1)oct-6-yl) ester; Sulfuric acid, mono((1R,2S,5R)-2-(((2-aminoethoxy)amino)carbonyl)-7-oxo-1,6-diazabicyclo(3.2.1)oct-6-yl) ester, (-)-

Indication

Disease Entry	ICD 11	Status	REF
Bacterial infection	1A00-1C4Z	Phase 1	[1]

Cross-matching ID

PubChem CID: 73386748
CAS Number: CAS 1452458-86-4
TTD Drug ID: DMECVP9

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Staphylococcus Beta-lactamase (Stap-coc blaZ)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tazobactam	DM3XNUI	Appendicitis	DB10	Approved	[3]
Clavulanate	DM2FGRT	Bacteremia	1A73	Approved	[4]
CAZ AVI	DMPG4OM	Serious infection	1H0Z	Phase 3	[5]
Enmetazobactam	DMZKTYJ	Urinary tract infection	GC08	Phase 3	[6]
Vaborbactam	DMDCFXJ	Urinary tract infection	GC08	Phase 3	[7]
MK-7655	DMLMV0O	Bacterial infection	1A00-1C4Z	Phase 2	[8]
CXL	DM3JFZ2	Methicillin-resistant staphylococci infection	1A00-1A09	Phase 2	[9]
RASV-Sp	DM4VTX6	Streptococcus infection	1B53	Phase 1	[10]
ME-1071	DMEMQ5J	Bacterial infection	1A00-1C4Z	Phase 1	[11]
VNRX-5133	DMNZ6XH	Bacterial infection	1A00-1C4Z	Phase 1	[12]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Staphylococcus Beta-lactamase (Stap-coc blaZ)	TTHI19T	BLAC_STAAU	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT02134834) A Phase I Study to Assess Safety, Tolerability and Pharmacokinetics of OP0595. U.S. National Institutes of Health.
2	OP0595, a new diazabicyclooctane: mode of action as a serine -lactamase inhibitor, antibiotic and -lactam 'enhancer'. J Antimicrob Chemother. 2015 Oct;70(10):2779-86.
3	Selection of TNF-alpha binding affibody molecules using a beta-lactamase protein fragment complementation assay. N Biotechnol. 2009 Nov 30;26(5):251-9.
4	A sensitive coupled HPLC/electrospray mass spectrometry assay for SPM-1 metallo-beta-lactamase inhibitors. Assay Drug Dev Technol. 2009 Apr;7(2):170-9.
5	NXL104 irreversibly inhibits the -lactamase from Mycobacterium tuberculosis. Biochemistry. 2012 Jun 5;51(22):4551-7.
6	Pharmacodynamics of Cefepime Combined with the Novel Extended-Spectrum--Lactamase (ESBL) Inhibitor Enmetazobactam for Murine Pneumonia Caused by ESBL-Producing Klebsiella pneumoniae. Antimicrob Agents Chemother. 2020 May 21;64(6):e00180-20.
7	Vaborbactam: Spectrum of Beta-Lactamase Inhibition and Impact of Resistance Mechanisms on Activity in Enterobacteriaceae. Antimicrob Agents Chemother. 2017 Oct 24;61(11):e01443-17.
8	Discovery of MK-7655, a beta-lactamase inhibitor for combination with Primaxin . Bioorg Med Chem Lett. 2014 Feb 1;24(3):780-5.
9	Beta-Lactam Antibiotics Renaissance. Antibiotics. 2014, 3(2), 193-215.
10	WO patent application no. 2010,0456,20, Recombinant bacterium capable of eliciting an immune response against streptococcus pneumoniae.
11	Multidrug-resistant Gram-negative bacterial infections: are you ready for the challenge. Curr Clin Pharmacol. 2014 Feb;9(1):27-38.
12	Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo--lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. J Med Chem. 2020 Mar 26;63(6):2789-2801.