All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
	2268	57-66-9

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: probenecid benecid probecid probenecid acid

The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy. Molecular weight: 285.36 Formula: C13H19NO4S CLOGP: 3.37 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 74.68 ALOGS: -2.83 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
1	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	1.20 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	58.52 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.13 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.25 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.13 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5.90 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
April 26, 1951	FDA

FDA Adverse Event Reporting System (Female)

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
Adenovirus infection	62.70	44.50	12	417	3559	63485034
Aplastic anaemia	56.21	44.50	13	416	9556	63479037

FDA Adverse Event Reporting System (Male)

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
Adenovirus infection	100.81	22.77	25	1079	5232	34950595
Lip haemorrhage	32.68	22.77	7	1097	763	34955064
Platelet transfusion	23.01	22.77	6	1098	1520	34954307

FDA Adverse Event Reporting System (Geriatric)

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
Adenovirus infection	166.73	23.98	37	1406	8410	79734535
Aplastic anaemia	62.91	23.98	20	1423	17885	79725060
Pancreatitis acute	33.99	23.98	17	1426	49587	79693358
Lip haemorrhage	33.50	23.98	7	1436	1187	79741758
Cystitis haemorrhagic	31.19	23.98	10	1433	9162	79733783

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	M04AB01	MUSCULO-SKELETAL SYSTEM ANTIGOUT PREPARATIONS ANTIGOUT PREPARATIONS Preparations increasing uric acid excretion
MeSH PA	D000277	Adjuvants, Pharmaceutic
MeSH PA	D018501	Antirheumatic Agents
MeSH PA	D006074	Gout Suppressants
MeSH PA	D010592	Pharmaceutic Aids
MeSH PA	D014528	Uricosuric Agents
CHEBI has role	CHEBI:35841	uricosuric drugs

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

Disease	Relation	SNOMED_ID	DOID
Hyperuricemia	indication	35885006	DOID:1920
Articular gout	indication	48440001	DOID:13189
Chronic gouty arthritis	indication	68451005
Adjunct Treatment to Inhibit Renal Drug Excretion	indication
Peptic ulcer	contraindication	13200003	DOID:750
Acute nephropathy	contraindication	58574008
Hepatic failure	contraindication	59927004
Diarrhea	contraindication	62315008
Leukopenia	contraindication	84828003	DOID:615
Kidney disease	contraindication	90708001	DOID:557
Anemia due to enzyme deficiency	contraindication	111577008
Disorder of muscle	contraindication	129565002	DOID:423
Disease of blood AND/OR blood-forming organ	contraindication	191124002	DOID:74
Impaired renal function disorder	contraindication	197663003
Rhabdomyolysis	contraindication	240131006
Renal dialysis	contraindication	265764009
Infectious mononucleosis	contraindication	271558008	DOID:8568
Uric acid renal calculus	contraindication	274401005
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Aplastic anemia	contraindication	306058006	DOID:12449
Bone marrow depression	contraindication	307762000
Pseudomembranous enterocolitis	contraindication	397683000
Granulocytopenic disorder	contraindication	417672002
Vomiting	contraindication	422400008
Uric Acid Nephropathy Gout	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.46	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Solute carrier family 22 member 11	Transporter	Q9NSA0	S22AB_HUMAN	INHIBITOR	IC50	4.26		CHEMBL	CHEMBL
Solute carrier family 22 member 6	Transporter	Q4U2R8	S22A6_HUMAN	INHIBITOR	IC50	4.90		IUPHAR	CHEMBL
Solute carrier family 22 member 8	Transporter	Q8TCC7	S22A8_HUMAN	INHIBITOR	IC50	5.05		CHEMBL	CHEMBL
Solute carrier family 22 member 12	Transporter	Q96S37	S22AC_HUMAN		IC50	4.30		CHEMBL
UDP-glucuronosyltransferase 1-7	Enzyme	Q9HAW7	UD17_HUMAN		Ki	4.02		CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	6.44		CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		Ki	5.90		CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Ki	6.37		CHEMBL
Solute carrier family 22 member 6	Transporter		S22A6_MOUSE		Ki	5.20		CHEMBL
Solute carrier family 22 member 20	Transporter		S22AK_MOUSE		Ki	5.08		CHEMBL
Transient receptor potential cation channel subfamily V member 2	Ion channel		TRPV2_RAT	ACTIVATOR	EC50	4.50		IUPHAR

External reference:

ID	Source
4017872	VUID
N0000146225	NUI
D00475	KEGG_DRUG
4017872	VANDF
C0033209	UMLSCUI
CHEBI:8426	CHEBI
RTO	PDB_CHEM_ID
CHEMBL897	ChEMBL_ID
DB01032	DRUGBANK_ID
D011339	MESH_DESCRIPTOR_UI
4911	PUBCHEM_CID
4357	IUPHAR_LIGAND_ID
563	INN_ID
PO572Z7917	UNII
8698	RXNORM
128	MMSL
5356	MMSL
d00031	MMSL
002321	NDDF
387365004	SNOMEDCT_US
66094001	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1367	TABLET, FILM COATED	500 mg	ORAL	ANDA	13 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1367	TABLET, FILM COATED	500 mg	ORAL	ANDA	13 sections
Probenecid and Colchicine	HUMAN PRESCRIPTION DRUG LABEL	2	0591-5325	TABLET	500 mg	ORAL	ANDA	13 sections
Probenecid and Colchicine	HUMAN PRESCRIPTION DRUG LABEL	2	0591-5325	TABLET	500 mg	ORAL	ANDA	13 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5347	TABLET, FILM COATED	500 mg	ORAL	ANDA	12 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5347	TABLET, FILM COATED	500 mg	ORAL	ANDA	12 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	10135-541	TABLET, FILM COATED	500 mg	ORAL	ANDA	14 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	10135-541	TABLET, FILM COATED	500 mg	ORAL	ANDA	14 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	11819-282	TABLET, FILM COATED	500 mg	ORAL	ANDA	12 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	43353-839	TABLET, FILM COATED	500 mg	ORAL	ANDA	14 sections
Probenecid and Colchicine	Human Prescription Drug Label	2	50742-263	TABLET	500 mg	ORAL	ANDA	13 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	54868-0159	TABLET, FILM COATED	500 mg	ORAL	ANDA	12 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8213	TABLET, FILM COATED	500 mg	ORAL	ANDA	12 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	68151-1993	TABLET, FILM COATED	500 mg	ORAL	ANDA	13 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	69367-154	TABLET	500 mg	ORAL	ANDA	13 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	71335-1697	TABLET, FILM COATED	500 mg	ORAL	ANDA	13 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	71626-999	TABLET, FILM COATED	500 mg	ORAL	ANDA	13 sections
Probenecid	HUMAN PRESCRIPTION DRUG LABEL	1	83008-020	TABLET, FILM COATED	500 mg	ORAL	ANDA	14 sections