Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C33H47NO3 |
| Molecular Weight | 505.7312 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 6 / 6 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@H](CCOC3=CC=C(CN(CC)CC)C=C3OC)[C@@]1(C)CC[C@]4([H])C5=C(C[C@@H](C)[C@@]24[H])C=C(O)C=C5
InChI
InChIKey=OHCPNHFLPCVWRG-MWSJHZLTSA-N
InChI=1S/C33H47NO3/c1-6-34(7-2)21-23-8-13-30(31(19-23)36-5)37-17-15-25-9-12-29-32-22(3)18-24-20-26(35)10-11-27(24)28(32)14-16-33(25,29)4/h8,10-11,13,19-20,22,25,28-29,32,35H,6-7,9,12,14-18,21H2,1-5H3/t22-,25-,28-,29+,32-,33-/m1/s1
| Molecular Formula | C33H47NO3 |
| Molecular Weight | 505.7312 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 5 / 6 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
TAS-108 (also known as SR-16234) is a selective estrogen receptor modulator (SERM) and has been reported to have estrogen receptor (ER) α antagonistic activity and a strong affinity with a weak partial agonistic activity to ERβ receptor. It is known that ERs play a central role in the diverse actions of estrogen. TAS-108 was studied in phase II clinical trials to treat recurrent or recurrent inoperable breast cancer. In addition, TAS-108 participated in Japan in a phase II clinical trial in Endometriosis patients. The phase III studies are being planned with the drug.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Both N- and C-terminal transactivation functions of DNA-bound ERalpha are blocked by a novel synthetic estrogen ligand. | 2003 Dec 19 |
|
| TAS-108, a novel oral steroidal antiestrogenic agent, is a pure antagonist on estrogen receptor alpha and a partial agonist on estrogen receptor beta with low uterotrophic effect. | 2005 Jan 1 |
|
| Safety, tolerability and pharmacokinetics of TAS-108, a novel anti-oestrogen, in healthy post-menopausal Japanese women: a phase I single oral dose study. | 2009 May |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:14:01 UTC 2023
by
admin
on
Sat Dec 16 11:14:01 UTC 2023
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| Record UNII |
42U0C8VOLO
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| Record Status |
Validated (UNII)
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| Record Version |
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9874875
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42U0C8VOLO
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229634-97-3
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DTXSID601117925
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admin on Sat Dec 16 11:14:01 UTC 2023 , Edited by admin on Sat Dec 16 11:14:01 UTC 2023
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ACTIVE MOIETY |
