Clinical data | |
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Trade names | Resatorvid |
Identifiers | |
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CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C15H17ClFNO4S |
Molar mass | 361.81 g·mol−1 |
3D model ( JSmol) | |
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Resatorvid (TAK-242) is a cyclohexane derivative that was invented by scientists at Takeda in a drug discovery campaign to identify inhibitors of the receptor TLR4. [1] It binds directly to cysteine residue 747 [1] intracellularly, preventing TLR4 binding with TIRAP and thus preventing downstream signal transduction. [2]
A randomized, double-blinded Phase III trial of resatorvid in sepsis was halted early due to lack of efficacy, and the compound has become a widely used tool compound in biological research. [1]
It has antiinflammatory and neuroprotective effects in preclinical models. [3] It has been explored in preclinical studies of several forms of cancer, including multiple myeloma, breast cancer, and ovarian cancer, [4] and has been suggested for study in skin cancers. [5]
Efforts have been made to improve resatorvid by making prodrugs and deuterated derivatives. [3]
Clinical data | |
---|---|
Trade names | Resatorvid |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C15H17ClFNO4S |
Molar mass | 361.81 g·mol−1 |
3D model ( JSmol) | |
| |
|
Resatorvid (TAK-242) is a cyclohexane derivative that was invented by scientists at Takeda in a drug discovery campaign to identify inhibitors of the receptor TLR4. [1] It binds directly to cysteine residue 747 [1] intracellularly, preventing TLR4 binding with TIRAP and thus preventing downstream signal transduction. [2]
A randomized, double-blinded Phase III trial of resatorvid in sepsis was halted early due to lack of efficacy, and the compound has become a widely used tool compound in biological research. [1]
It has antiinflammatory and neuroprotective effects in preclinical models. [3] It has been explored in preclinical studies of several forms of cancer, including multiple myeloma, breast cancer, and ovarian cancer, [4] and has been suggested for study in skin cancers. [5]
Efforts have been made to improve resatorvid by making prodrugs and deuterated derivatives. [3]