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sulbactam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
beta-lactamase inhibitors	2492	68373-14-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sulbactam penicillanic acid dioxide sulbactam sodium	A beta-lactamase inhibitor with very weak antibacterial action. The compound prevents antibiotic destruction of beta-lactam antibiotics by inhibiting beta-lactamases, thus extending their spectrum activity. Combinations of sulbactam with beta-lactam antibiotics have been used successfully for the therapy of infections caused by organisms resistant to the antibiotic alone. Molecular weight: 233.24 Formula: C8H11NO5S CLOGP: 0.31 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 91.75 ALOGS: -0.68 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sulbactam
penicillanic acid dioxide
sulbactam sodium

A beta-lactamase inhibitor with very weak antibacterial action. The compound prevents antibiotic destruction of beta-lactam antibiotics by inhibiting beta-lactamases, thus extending their spectrum activity. Combinations of sulbactam with beta-lactam antibiotics have been used successfully for the therapy of infections caused by organisms resistant to the antibiotic alone.

Molecular weight: 233.24
Formula: C8H11NO5S
CLOGP: 0.31
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 91.75
ALOGS: -0.68
ROTB: 1

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1	g	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	5.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	285.97 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	1.10 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.62 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.32 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 31, 1986	FDA	PFIZER

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Enterocolitis haemorrhagic	68.55	26.81	14	1665	1452	63485891
Hepatic function abnormal	53.84	26.81	24	1655	37118	63450225
Culture stool positive	40.45	26.81	7	1672	295	63487048
Stevens-Johnson syndrome	32.58	26.81	15	1664	24935	63462408
Toxic epidermal necrolysis	32.36	26.81	15	1664	25319	63462024
Klebsiella infection	31.97	26.81	11	1668	8555	63478788
Epidermolysis	28.90	26.81	6	1673	673	63486670

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac septal defect	66.43	21.44	12	1904	307	34954708
Kidney duplex	63.48	21.44	12	1904	396	34954619
Enterocolitis haemorrhagic	42.32	21.44	10	1906	973	34954042
Hepatic function abnormal	40.59	21.44	27	1889	44336	34910679
Interstitial lung disease	25.37	21.44	24	1892	65258	34889757
Aspartate aminotransferase increased	24.60	21.44	24	1892	67759	34887256
Pyrexia	23.16	21.44	54	1862	332959	34622056

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Enterocolitis haemorrhagic	106.93	22.18	23	2942	2171	79739252
Hepatic function abnormal	70.51	22.18	40	2925	73067	79668356
Culture stool positive	44.73	22.18	9	2956	612	79740811
Aspartate aminotransferase increased	37.35	22.18	35	2930	138606	79602817
Toxic epidermal necrolysis	31.52	22.18	20	2945	44561	79696862
Stevens-Johnson syndrome	31.31	22.18	19	2946	39147	79702276
Rash	27.61	22.18	64	2901	578294	79163129
Alanine aminotransferase increased	27.49	22.18	32	2933	162538	79578885
Interstitial lung disease	25.75	22.18	26	2939	112574	79628849
Klebsiella infection	24.87	22.18	12	2953	15708	79725715

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J01CG01	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE BETA-LACTAM ANTIBACTERIALS, PENICILLINS Beta-lactamase inhibitors
FDA EPC	N0000175930	beta Lactamase Inhibitor
FDA MoA	N0000000202	beta Lactamase Inhibitors
MeSH PA	D000900	Anti-Bacterial Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D065093	beta-Lactamase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Infection of skin AND/OR subcutaneous tissue	indication	19824006
Infection due to Escherichia coli	indication	71057007
Rhinoscleroma	indication	72409005	DOID:11336
Cholangitis	indication	82403002	DOID:9446
Female genital tract infection	indication	125585007
Infectious disease of abdomen	indication	128070006
Infection due to Enterobacteriaceae	indication	128945009
Bacterial peritonitis	indication	197171003
Infection due to Staphylococcus aureus	indication	406602003
Ventilator-associated bacterial pneumonia caused by acinetobacter baumannii-calcoaceticus complex	indication	429271009

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.1	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL	XACDURO (COPACKAGED)	ENTASIS THERAP	N216974	May 23, 2023	RX	POWDER	INTRAVENOUS	9623014	April 2, 2033	TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP)
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL	XACDURO (COPACKAGED)	ENTASIS THERAP	N216974	May 23, 2023	RX	POWDER	INTRAVENOUS	10376499	Nov. 17, 2035	TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP)
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL	XACDURO (COPACKAGED)	ENTASIS THERAP	N216974	May 23, 2023	RX	POWDER	INTRAVENOUS	9968593	Nov. 17, 2035	TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP)

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL	XACDURO (COPACKAGED)	ENTASIS THERAP	N216974	May 23, 2023	RX	POWDER	INTRAVENOUS	May 23, 2028	NEW CHEMICAL ENTITY
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL	XACDURO (COPACKAGED)	ENTASIS THERAP	N216974	May 23, 2023	RX	POWDER	INTRAVENOUS	May 23, 2033	GENERATING ANTIBIOTIC INCENTIVES NOW

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Serine beta-lactamase-like protein LACTB, mitochondrial	Enzyme	P83111	LACTB_HUMAN		IC50	5.01	WOMBAT-PK
Beta-lactamase TEM	Enzyme		BLAT_ECOLX	INHIBITOR	Ki	6.10	CHEMBL	CHEMBL
Beta-lactamase	Enzyme		AMPC_ECOLI		IC50	4.18	CHEMBL
Beta-lactamase SHV-1	Enzyme		BLA1_ECOLX		IC50	5.41	CHEMBL
Beta-lactamase	Enzyme		AMPC_ENTCL		IC50	6	CHEMBL
Beta-lactamase OXA-1	Enzyme		BLO1_ECOLX		IC50	4.66	CHEMBL
Beta-lactamase	Enzyme		AMPC_PSEAE		IC50	4.57	CHEMBL
Beta-lactamase	Enzyme		A1E3K9_ECOLX		IC50	5.21	CHEMBL
Beta-lactamase	Enzyme		A8RR46_BACCS		IC50	7.12	CHEMBL
Carbapenem-hydrolizing beta-lactamase SFC-1	Enzyme		Q6JP75_SERFO		IC50	4.64	CHEMBL

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External reference:

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ID	Source
0RN	PDB_CHEM_ID
002811	NDDF
002812	NDDF
10167	RXNORM
10769	IUPHAR_LIGAND_ID
130313	PUBCHEM_CID
398916003	SNOMEDCT_US
4019381	VANDF
4019937	VUID
4019937	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0409-2689	INJECTION, POWDER, FOR SOLUTION	0.50 g	INTRAVENOUS	ANDA	25 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0409-2689	INJECTION, POWDER, FOR SOLUTION	0.50 g	INTRAVENOUS	ANDA	25 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0409-2987	INJECTION, POWDER, FOR SOLUTION	1 g	INTRAVENOUS	ANDA	25 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0409-2987	INJECTION, POWDER, FOR SOLUTION	1 g	INTRAVENOUS	ANDA	25 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0641-6116	INJECTION, POWDER, FOR SOLUTION	0.50 g	INTRAVENOUS	ANDA	24 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0641-6117	INJECTION, POWDER, FOR SOLUTION	1 g	INTRAVENOUS	ANDA	24 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0641-6118	INJECTION, POWDER, FOR SOLUTION	50 mg	INTRAVENOUS	ANDA	24 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0641-6119	INJECTION, POWDER, FOR SOLUTION	0.50 g	INTRAVENOUS	ANDA	25 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0641-6120	INJECTION, POWDER, FOR SOLUTION	1 g	INTRAVENOUS	ANDA	25 sections
Ampicillin and Sulbactam	HUMAN PRESCRIPTION DRUG LABEL	2	0641-6121	INJECTION, POWDER, FOR SOLUTION	50 mg	INTRAVENOUS	ANDA	24 sections

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