Clinical data | |
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Trade names | Zonalta |
Other names | 4-Hydroxy-N-desmethyltamoxifen; Desmethylhydroxytamoxifen |
Routes of administration | By mouth |
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PDB ligand | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.208.548 |
Chemical and physical data | |
Formula | C25H27NO2 |
Molar mass | 373.496 g·mol−1 |
3D model (JSmol) | |
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Endoxifen, also known as 4-hydroxy-N-desmethyltamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group as well as a protein kinase C (PKC) inhibitor. It is under development for the treatment of estrogen receptor-positive breast cancer and for the treatment of mania in bipolar disorder.[1][2] It is taken by mouth.[2]
Endoxifen is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). [3][4][5] The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce endoxifen and afimoxifene (4-hydroxytamoxifen).[6]
Currently, endoxifen is approved by Drugs Controller General of India for the acute treatment of manic episode with or without mixed features of Bipolar I disorder.[7] It is manufactured and sold by Intas Pharmaceuticals under the brand name Zonalta.[8]