Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C29H37NO4 |
Molecular Weight | 463.6084 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@](O)(C(=O)COC)[C@@]1(C)C[C@]([H])(C3=CC=C(C=C3)N(C)C)C4=C5CCC(=O)C=C5CC[C@@]24[H]
InChI
InChIKey=BHERMCLNVOVDPU-DQFOBABISA-N
InChI=1S/C29H37NO4/c1-28-16-24(18-5-8-20(9-6-18)30(2)3)27-22-12-10-21(31)15-19(22)7-11-23(27)25(28)13-14-29(28,33)26(32)17-34-4/h5-6,8-9,15,23-25,33H,7,10-14,16-17H2,1-4H3/t23-,24+,25-,28-,29-/m0/s1
DescriptionSources: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C104057https://www.ncbi.nlm.nih.gov/pubmed/22028249 | https://clinicaltrials.gov/ct2/show/NCT01728454 | https://clinicaltrials.gov/ct2/show/NCT00874302 | https://www.globenewswire.com/news-release/2017/07/17/1047288/0/en/Repros-Announces-Proellex-Development-Program-Will-Remain-on-Partial-Clinical-Hold-by-the-FDA.html | https://clinicaltrials.gov/ct2/show/NCT01800422
Sources: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C104057https://www.ncbi.nlm.nih.gov/pubmed/22028249 | https://clinicaltrials.gov/ct2/show/NCT01728454 | https://clinicaltrials.gov/ct2/show/NCT00874302 | https://www.globenewswire.com/news-release/2017/07/17/1047288/0/en/Repros-Announces-Proellex-Development-Program-Will-Remain-on-Partial-Clinical-Hold-by-the-FDA.html | https://clinicaltrials.gov/ct2/show/NCT01800422
Telapristone acetate, a selective progesterone receptor modulator (SPRM), was developed for the long-term treatment of symptoms associated with endometriosis and uterine fibroids. It is known, that the progesterone is a steroid hormone that plays an important role in the breast. Deregulation of the progesterone-signaling pathway is implicated in the formation, development, and progression of breast cancer. Thus, the telapristone acetate is studied in phase II clinical trial in stage I-II primary breast cancer. Besides, telapristone acetate participated in phase III clinical trials in pre-menopausal anemic women with symptomatic uterine fibroids. However, FDA terminated these studies because of the safety.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01728454
Endometriosis: capsules (6 and 12 mg), once a day for 18 weeks
Route of Administration:
Oral
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NCI_THESAURUS |
C1891
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65703MV349
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20761503
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300000036965
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198414-30-1
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DTXSID00173586
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9273
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TELAPRISTONE
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C104057
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ACTIVE MOIETY
PRODRUG (METABOLITE ACTIVE)