sodium aurothiomalate Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4706	12244-57-4

Description:

Molecule

Description

Synonyms: sodium aurothiomalate aurolate aurothiomalate sodium gold sodium thiomalate sodium aurithiomalate myochrysine

A variable mixture of the mono- and disodium salts of gold thiomalic acid used mainly for its anti-inflammatory action in the treatment of rheumatoid arthritis. It is most effective in active progressive rheumatoid arthritis and of little or no value in the presence of extensive deformities or in the treatment of other forms of arthritis. Molecular weight: 390.07 Formula: C4H3AuNa2O4S CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: 80.26 ALOGS: ROTB: None

Drug dosage:

Dose	Unit	Route
2.40	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	70 %	Benet LZ, Broccatelli F, Oprea TI

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1992	YEAR INTRODUCED

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
Rheumatoid arthritis	862.56	87.55	689	15474	239526	46430373
Treatment failure	505.79	87.55	344	15819	92743	46577156
Drug ineffective	397.28	87.55	777	15386	677061	45992838
Contraindicated product administered	390.65	87.55	277	15886	79670	46590229
Granuloma skin	330.44	87.55	97	16066	3373	46666526
Sleep disorder	330.04	87.55	204	15959	46591	46623308
Blood parathyroid hormone decreased	320.68	87.55	100	16063	4281	46665618
Joint swelling	317.09	87.55	336	15827	165737	46504162
Drug hypersensitivity	316.15	87.55	404	15759	243421	46426478
Panniculitis	294.75	87.55	100	16063	5604	46664295
Drug intolerance	270.76	87.55	292	15871	146757	46523142
Rheumatoid nodule	260.52	87.55	103	16060	8917	46660982
Red blood cell sedimentation rate increased	259.04	87.55	136	16027	22753	46647146
Soft tissue disorder	250.58	87.55	82	16081	4104	46665795
Skin necrosis	237.17	87.55	95	16068	8509	46661390
Presbyacusis	204.76	87.55	64	16099	2758	46667141
Synovitis	204.09	87.55	169	15994	60906	46608993
Infection	202.60	87.55	240	15923	133352	46536547
Pleural thickening	201.54	87.55	62	16101	2533	46667366
Therapeutic product effect incomplete	196.55	87.55	184	15979	77969	46591930
Therapeutic product effect decreased	195.42	87.55	188	15975	82413	46587486
Pleural fibrosis	193.95	87.55	65	16098	3504	46666395
Blood magnesium increased	192.14	87.55	62	16101	2965	46666934
Drug tolerance decreased	191.50	87.55	62	16101	2997	46666902
C-reactive protein increased	189.27	87.55	159	16004	58431	46611468
Adverse reaction	184.47	87.55	78	16085	8012	46661887
Peripheral swelling	184.17	87.55	249	15914	157822	46512077
Inflammation	184.16	87.55	145	16018	48636	46621263
Deafness neurosensory	179.28	87.55	65	16098	4429	46665470
Ulcer	173.33	87.55	95	16068	17297	46652602
Basal cell carcinoma	171.97	87.55	100	16063	20387	46649512
Hypercalcaemia	169.47	87.55	100	16063	20946	46648953
Drug eruption	165.63	87.55	99	16064	21230	46648669
Pneumonia viral	164.92	87.55	68	16095	6556	46663343
Epigastric discomfort	164.43	87.55	65	16098	5619	46664280
Dyspnoea	156.55	87.55	5	16158	515543	46154356
Loss of personal independence in daily activities	152.14	87.55	139	16024	57044	46612855
Therapeutic response decreased	151.63	87.55	123	16040	43022	46626877
Musculoskeletal disorder	141.48	87.55	80	16083	15465	46654434
Demyelination	136.97	87.55	57	16106	5623	46664276
Skin ulcer	132.27	87.55	101	16062	32357	46637542
Deafness transitory	131.01	87.55	40	16123	1592	46668307
Gastric disorder	124.26	87.55	90	16073	26615	46643284
Arthropathy	118.11	87.55	146	16017	84554	46585345
Impaired gastric emptying	117.76	87.55	57	16106	8015	46661884
Cyst	117.53	87.55	65	16098	12035	46657864
Osteoarthritis	106.53	87.55	119	16044	61906	46607993
Musculoskeletal stiffness	105.82	87.55	149	16014	97844	46572055
Functional gastrointestinal disorder	104.69	87.55	40	16123	3154	46666745
Rash pruritic	103.21	87.55	100	16063	44115	46625784
Osteopenia	99.67	87.55	66	16097	16895	46653004
Fibromyalgia	99.59	87.55	90	16073	36373	46633526
Death	99.09	87.55	4	16159	335544	46334355
Renal impairment	98.55	87.55	125	16038	74247	46595652
C-reactive protein abnormal	97.38	87.55	71	16092	21199	46648700
Blood cholesterol increased	96.23	87.55	92	16071	39921	46629978
Condition aggravated	92.03	87.55	237	15926	244815	46425084
Liver function test abnormal	91.74	87.55	96	16067	46391	46623508
Blood potassium increased	90.08	87.55	62	16101	16905	46652994
Gastrointestinal pain	89.14	87.55	46	16117	7409	46662490
Gastrointestinal disorder	88.36	87.55	106	16057	59470	46610429

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
Joint swelling	474.01	160.74	204	4762	46742	29900770
Red blood cell sedimentation rate increased	457.53	160.74	125	4841	7170	29940342
Apparent death	436.05	160.74	104	4862	3438	29944074
Pulmonary thrombosis	366.70	160.74	102	4864	6241	29941271
Rheumatoid arthritis	309.89	160.74	146	4820	41051	29906461
Contraindicated product administered	306.67	160.74	113	4853	17118	29930394
Drug ineffective	288.23	160.74	314	4652	340073	29607439
Diverticulitis	286.98	160.74	108	4858	17337	29930175
Arthropathy	286.36	160.74	113	4853	20614	29926898
C-reactive protein increased	257.67	160.74	131	4835	43342	29904170
C-reactive protein abnormal	251.55	160.74	74	4892	5519	29941993
Terminal state	250.26	160.74	67	4899	3537	29943975
Drug intolerance	207.50	160.74	115	4851	45176	29902336
Thrombosis	190.03	160.74	106	4860	42125	29905387
Photosensitivity reaction	166.44	160.74	62	4904	9632	29937880

Pharmacologic Action:

Source	Code	Description
ATC	M01CB01	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS SPECIFIC ANTIRHEUMATIC AGENTS Gold preparations
CHEBI has role	CHEBI:35842	antirheumatic agent
CHEBI has role	CHEBI:37670	protease inhibitors
CHEBI has role	CHEBI:50904	allergene
CHEBI has role	CHEBI:67079	antiinflammatory agents
CHEBI has role	CHEBI:131699	deoxyribonucleic polymerase inhibitor
MeSH PA	D018501	Antirheumatic Agents

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Rheumatoid arthritis	indication	69896004	DOID:7148
Juvenile rheumatoid arthritis	indication	410795001
Psoriasis with arthropathy	off-label use	33339001
Felty's syndrome	off-label use	57160007	DOID:11042

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	6.07		DRUG MATRIX
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		IC50	5.62		DRUG MATRIX
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		IC50	6.09		DRUG MATRIX
Thioredoxin reductase 1, cytoplasmic	Enzyme	Q16881	TRXR1_HUMAN					WOMBAT-PK
Cathepsin L1	Enzyme	P07711	CATL1_HUMAN		IC50	4.05		CHEMBL

External reference:

ID	Source
D00992	KEGG_DRUG
4017995	VUID
N0000146340	NUI
4017995	VANDF
C0718739	UMLSCUI
CHEBI:35864	CHEBI
CHEMBL306043	ChEMBL_ID
DB09276	DRUGBANK_ID
D006052	MESH_DESCRIPTOR_UI
22318	PUBCHEM_CID
4154	INN_ID
E4768ZY6GM	UNII
203004	RXNORM
2006	MMSL
4795	MMSL
615	MMSL
620	MMSL
d00250	MMSL
002396	NDDF
387380005	SNOMEDCT_US
68702006	SNOMEDCT_US

Pharmaceutical products:

None