Details
Stereochemistry | RACEMIC |
Molecular Formula | C4H3O4S.Au.2Na |
Molecular Weight | 390.075 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].[Na+].[Au+].[O-]C(=O)CC([S-])C([O-])=O
InChI
InChIKey=VXIHRIQNJCRFQX-UHFFFAOYSA-K
InChI=1S/C4H6O4S.Au.2Na/c5-3(6)1-2(9)4(7)8;;;/h2,9H,1H2,(H,5,6)(H,7,8);;;/q;3*+1/p-3
Sodium aurothiomalate (also known as gold sodium thiomalate) is a gold compound that is used for its immunosuppressive anti-rheumatic effects. It was indicated in the treatment of selected cases of active rheumatoid arthritis—both adult and juvenile type. The greatest benefit occurs in the early active stage. In late stages of the illness when cartilage and bone damage have occurred, gold can only check the progression of rheumatoid arthritis and prevent further structural damage to joints. It cannot repair damage caused by previously active disease. Gold Sodium Thiomalate should be used only as one part of a complete program of therapy; alone it is not a complete treatment. The mode of action is unknown, but was found, that aurothiomalate is able to inhibit Microsomal prostaglandin E synthase-1 (mPGES-1 expression. mPGES-1 is a terminal enzyme in the production of prostaglandin E2 (PGE2) and its expression is upregulated during inflammation. mPGES-1 is considered as a potential drug target for the treatment of arthritis to reduce adverse effects related to the current non-steroidal anti-inflammatory drugs (NSAIDs).
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5658 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25314295 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MYOCHRYSINE Approved UseGold Sodium Thiomalate is indicated in the treatment of selected cases of active rheumatoid arthritis—both adult and juvenile type. The greatest benefit occurs in the early active stage. In late stages of the illness when cartilage and bone damage have occurred, gold can only check the progression of rheumatoid arthritis and prevent further structural damage to joints. It cannot repair damage caused by previously active disease. Gold Sodium Thiomalate should be used only as one part of a complete program of therapy; alone it is not a complete treatment. |
|||
Palliative | Unknown Approved UseUnknown |
Sample Use Guides
Weekly Injections: 1st injection 10 mg; 2nd injection 25 mg; 3rd and sub sequent injections, 25 to 50 mg until there is toxicity or major clinical improvement, or, in the absence of either of these, the cumulative dose of Gold Sodium Thiomalate reaches one gram. Gold Sodium Thiomalate is continued until the cumulative dose reaches one gram unless toxicity or major clinical improvement occurs. If significant clinical improvement occurs before a cumulative dose of one gram has been administered, the dose may be decreased or the interval between injections increased as with maintenance therapy. Maintenance doses of 25 to 50 mg every other week for two to 20 weeks are recommended. If the clinical course remains stable, injections of 25 to 50 mg may be given every third and subsequently every fourth week indefinitely. Some patients may require maintenance treatment at intervals of one to three weeks. Should the arthritis exacerbate during maintenance therapy, weekly injections may be resumed temporarily until disease activity is suppressed.
Route of Administration:
Intramuscular
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25314295
mPGES-1 expression in primary human chondrocytes was enhanced when the cells were exposed to interleukin-1β (IL-1β) and mPGES-1 protein levels continued to increase up to the 96-h follow-up. The effect of aurothiomalate on mPGES-1 mRNA expression was dose-dependent (at concentration of Aurothiomalate: 2.5-50 uM) and was shown by a reduction in mPGES-1 protein levels (at 25 uM Aurothiomalate) and PGE2 production (at concentration of Aurothiomalate: 2.5-25 uM).
Name | Type | Language | ||
---|---|---|---|---|
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Systematic Name | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
DTXSID80872500
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
PRIMARY | |||
|
74916-57-7
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
PRIMARY | |||
|
HRS6S09A0H
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
PRIMARY | |||
|
3211
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
PRIMARY | |||
|
147828
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
PRIMARY | |||
|
22318
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
PRIMARY | |||
|
185826-27-1
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
ALTERNATIVE | |||
|
1096140-34-9
Created by
admin on Fri Dec 15 17:06:02 GMT 2023 , Edited by admin on Fri Dec 15 17:06:02 GMT 2023
|
ALTERNATIVE |
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD