Page last updated: 2024-11-12
metapristone
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
metapristone: a potential cancer metastatic chemopreventive agent derived from mifepristone (RU486); structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 10070462 |
| CHEMBL ID | 1608 |
| SCHEMBL ID | 4020579 |
| MeSH ID | M000599185 |
Synonyms (32)
| Synonym |
|---|
| ru 42633 |
| desmethylmifepristone |
| CHEMBL1608 , |
| SCHEMBL4020579 |
| bdbm50292750 |
| 17beta-hydroxy-17alpha-propynyl-11beta-(4-n-methylaminophenyl)-estra-4,9-dien-3-one |
| 17beta-hydroxy-11beta-[4-(methylamino)-phenyl]-17alpha-(1-propinyl)-estra-4,9-dien-3-one |
| 104004-96-8 |
| n-desmethyl-ru 486 |
| estra-4,9-dien-3-one, 17-hydroxy-11-(4-(methylamino)phenyl)-17-(1-propynyl)-, (11beta,17beta)- |
| metapristone |
| k1p8ogj86j , |
| unii-k1p8ogj86j |
| ru-42633 |
| n-demethyl mifepristone |
| n-methylaminopristone |
| estra-4,9-dien-3-one, 17-hydroxy-11-(4-(methylamino)phenyl)-17-(1-propynyl)-, (11.beta.,17.beta.)- |
| estra-4,9-dien-3-one, 17-hydroxy-11-(4-(methylamino)phenyl)-17-(1-propyn-1-yl)-, (11.beta.,17.beta.)- |
| mifepristone, n-monodemethyl |
| AKOS025294003 |
| n-desmethyl mifepristone |
| DTXSID60146216 |
| (8s,11r,13s,14s,17s)-17-hydroxy-13-methyl-11-[4-(methylamino)phenyl]-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one |
| J-001090 |
| (11r,13s,14s,17s)-17-hydroxy-13-methyl-11-(4-(methylamino)phenyl)-17-(prop-1-ynyl)-6,7,8,11,12,13,14,15,16,17-decahydro-1h-cyclopenta[a]phenanthren-3(2h)-one |
| Q27281827 |
| (11beta,17beta)-17-hydroxy-11-[4-(methylamino)phenyl]-17-(1-propyn-1-yl)-estra-4,9-dien-3-one |
| EN300-6762714 |
| (1s,3as,3bs,10r,11as)-1-hydroxy-11a-methyl-10-[4-(methylamino)phenyl]-1-(prop-1-yn-1-yl)-1h,2h,3h,3ah,3bh,4h,5h,7h,8h,9h,10h,11h,11ah-cyclopenta[a]phenanthren-7-one |
| ru42633 |
| (8s,11r,13s,14s,17s)-17-hydroxy-13-methyl-11-(4-(methylamino)phenyl)-17-(prop-1-ynyl)-6,7,8,11,12,13,14,15,16,17-decahydro-1h-cyclopenta[a]phenanthren-3(2h)-one |
| Z3028399069 |
Research Excerpts
Treatment
| Excerpt | Reference | Relevance |
|---|---|---|
| "Metapristone-treatment caused the cell arrest at the G0/G1 stage, and the inhibition of colony formation in B16F10 cells." | ( Metapristone (RU486 derivative) inhibits cell proliferation and migration as melanoma metastatic chemopreventive agent. Chen, J; Jia, L; Liu, J; Liu, W; Wang, J; Zheng, N, 2017) | 2.62 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " There was a wide variability (up to ten-fold) in the pharmacokinetic parameters within each dose group." | ( Pharmacokinetic study of RU 486 and its metabolites after oral administration of single doses to pregnant and non-pregnant women. Fotherby, K; He, CH; Shi, YE; Van Look, PF; Xu, JQ; Ye, ZH; Zhang, GQ, 1993) | 0.29 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " They gave the same dosage of mifepristone to 12 similar women, but took fetal blood samples at 24 or 48 hours post treatment." | ( Transplacental passage of mifepristone and its influence on maternal and fetal steroid concentrations in the second trimester of pregnancy. Ferguson, J; Hill, NC; MacKenzie, IZ; Selinger, M, 1991) | 0.28 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (1)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Progesterone receptor | Homo sapiens (human) | IC50 (µMol) | 0.0001 | 0.0000 | 0.5807 | 10.0000 | AID345893; AID345895; AID461850 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (18)
Molecular Functions (15)
Ceullar Components (6)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Progesterone receptor | Homo sapiens (human) |
| nucleoplasm | Progesterone receptor | Homo sapiens (human) |
| mitochondrial outer membrane | Progesterone receptor | Homo sapiens (human) |
| cytosol | Progesterone receptor | Homo sapiens (human) |
| chromatin | Progesterone receptor | Homo sapiens (human) |
| nucleus | Progesterone receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (8)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID461850 | Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells. |
| AID1381653 | Antiproliferative activity against human HCC1937 cells after 48 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer. |
| AID461851 | Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity relative to mifepristone | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells. |
| AID1381652 | Antiproliferative activity against human SUM149PT cells after 48 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer. |
| AID345895 | Antagonist activity at progesterone receptor in human T47D-C124 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of progesterone-induced luciferase transactivation activity after 24 hrs | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Syntheses and antigestagenic activity of mifepristone derivatives. |
| AID345894 | Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs relative to mifepristone | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Syntheses and antigestagenic activity of mifepristone derivatives. |
| AID345893 | Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Syntheses and antigestagenic activity of mifepristone derivatives. |
| AID345896 | Antagonist activity at progesterone receptor in human T47D-C124 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of progesterone-induced luciferase transactivation activity after 24 hrs relative to mifepristone | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Syntheses and antigestagenic activity of mifepristone derivatives. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (16)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (6.25) | 18.7374 |
| 1990's | 2 (12.50) | 18.2507 |
| 2000's | 1 (6.25) | 29.6817 |
| 2010's | 12 (75.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 113.03
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (113.03) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (6.25%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15 (93.75%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||