Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C31H39NO5 |
Molecular Weight | 505.6451 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@](OC(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=JVBGZFRPTRKSBB-MJBQOYBXSA-N
InChI=1S/C31H39NO5/c1-19(33)37-31(28(35)18-36-5)15-14-27-25-12-8-21-16-23(34)11-13-24(21)29(25)26(17-30(27,31)2)20-6-9-22(10-7-20)32(3)4/h6-7,9-10,16,25-27H,8,11-15,17-18H2,1-5H3/t25-,26+,27-,30-,31-/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
PubMed
Title | Date | PubMed |
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Population pharmacokinetics of telapristone (CDB-4124) and its active monodemethylated metabolite CDB-4453, with a mixture model for total clearance. | 2011 Dec |
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A peek into the drug development scenario of endometriosis - A systematic review. | 2017 Jun |
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Mechanism of Telapristone Acetate (CDB4124) on Progesterone Receptor Action in Breast Cancer Cells. | 2018 Oct 1 |
Patents
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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C1891
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ACTIVE MOIETY
METABOLITE ACTIVE (PARENT)
SUBSTANCE RECORD