Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H32N2O3 |
Molecular Weight | 456.576 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(N(CC2=CC=C(OCCN3CCCCC3)C=C2)C4=C1C=C(O)C=C4)C5=CC=C(O)C=C5
InChI
InChIKey=JICOGKJOQXTAIP-UHFFFAOYSA-N
InChI=1S/C29H32N2O3/c1-21-27-19-25(33)11-14-28(27)31(29(21)23-7-9-24(32)10-8-23)20-22-5-12-26(13-6-22)34-18-17-30-15-3-2-4-16-30/h5-14,19,32-33H,2-4,15-18,20H2,1H3
Molecular Formula | C29H32N2O3 |
Molecular Weight | 456.576 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Pipendoxifene (ERA-923) is a selective estrogen receptor modulator with a distinct profile compared with tamoxifen. In particular, unlike tamoxifen, ERA-923 is devoid of uterotropic activity and does not stimulate the growth of endometrial tumors in the EnCa-101 (human endometrial adenocarcinoma that is continuously passaged in animals in the presence of estrogen) experimental mice model. These data may indicate that, in patients, ERA-923 will not increase the incidence of endometrial hyperplasia or cancer. ERA-923 inhibits estrogen-stimulated ER-alpha-dependent tumor growth with equal effects compared with tamoxifen in models sensitive to tamoxifen. ERA-923 partially or completely overcomes tamoxifen resistance. In vivo combination of temsirolimus and ERA-923 at certain doses and schedules completely inhibited breast carcinoma growth, while individual agents were only partially effective. Pipendoxifene had been in phase II clinical trial for the treatment of refractory metastatic breast cancer. However, this research has been discontinued.
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women. | 2002 Feb |
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Combination therapy for treating breast cancer using antiestrogen, ERA-923, and the mammalian target of rapamycin inhibitor, temsirolimus. | 2006 Sep |
|
Selective estrogen receptor modulators: an update on recent clinical findings. | 2008 Mar |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11831538
Once-daily 10-200 mg for 28 days
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:26:02 GMT 2023
by
admin
on
Fri Dec 15 15:26:02 GMT 2023
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Record UNII |
TPC5Q8496G
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Record Status |
Validated (UNII)
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Record Version |
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-
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NCI_THESAURUS |
C1821
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TPC5Q8496G
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300000034282
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6433099
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Pipendoxifene
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C1874
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DTXSID40870209
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DB05414
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198480-55-6
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8077
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CHEMBL44426
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