Page last updated: 2024-11-06

mifepristone

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Description

Mifepristone, also known as RU-486, is a synthetic steroid that acts as a progesterone receptor antagonist. It was first synthesized in 1980 by scientists at Roussel Uclaf in France. Mifepristone blocks the effects of progesterone, a hormone that is essential for pregnancy. This blockage can prevent the implantation of a fertilized egg in the uterus or cause the detachment of an already implanted embryo.
Mifepristone is used for medical abortion, in combination with a prostaglandin such as misoprostol, and it can also be used for managing heavy menstrual bleeding and treating uterine fibroids.
Mifepristone is a controversial drug due to its use in abortion. However, it is also a safe and effective treatment option for many medical conditions. It has been extensively studied and its safety and efficacy have been established.
Mifepristone is important for reproductive health and access to safe abortion services. It is studied to further understand its mechanisms of action, potential applications in other medical conditions, and to improve its accessibility and affordability.'

Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID55245
CHEMBL ID438575
CHEMBL ID1276308
CHEBI ID50692
SCHEMBL ID16087
MeSH IDM0024116

Synonyms (189)

Synonym
BIDD:PXR0123
MLS001074115
BRD-K37270826-001-04-5
gtpl2805
BSPBIO_000238
MLS000069785 ,
korlym
smr000058481
c-1073 ,
mifeprex
ci-1073
ru-38486
corlux
pictovir
vx-410
mifegyne
PRESTWICK3_000299
(11beta,17beta)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-prop-1-yn-1-ylestra-4,9-dien-3-one
nsc652104
EU-0100801
mifepristone, >=98%
ru 486
11beta-(4-(dimethylamino)phenyl)-17beta-hydroxy-17-(1-propynyl)estra-4,9-dien-3-on
11beta-(4-(dimethylamino)phenyl)-17-hydroxy-21-methyl-19-nor-17alpha-pregna-4,9-dien-20-m-3-on
mifepristone [usan:inn:ban]
hsdb 6841
(11beta,17beta)-11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one
ru 486-6
estra-4,9-dien-3-one, 11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(1-propynyl)-, (11-beta,17-beta)-
brn 5779404
11beta-(4-(n,n-dimethylamino)phenyl)-17alpha-(prop-1-ynyl)-delta4,9-estradiene-17beta-ol-3-one
17-beta-hydroxy-11-beta-(4-dimethylaminophenyl-1)-17-alpha-(prop-1-ynyl)oestra-4,9-dien-3-one
11beta-(p-(dimethylamino)phenyl)-17beta-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one
estra-4,9-dien-3-one, 11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(1-propynyl)-, (11beta,17beta)-
c29h35no2
r 38486
mifepristona [spanish]
mifepristonum [latin]
ru 38486
SPECTRUM5_002045
PRESTWICK_570
cas-84371-65-3
LOPAC0_000801
HSCI1_000369
BPBIO1_000262
NCGC00179632-01
estra-4,9-dien-3-one, 11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-, (11b,17b)-
(8s,11r,13s,14s,17s)-11-(4-dimethylaminophenyl)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
vgx-410c
vgx-410
83203-42-3
pictovir (tm)
ru486
PRESTWICK2_000299
CHEBI:50692 ,
11-(4-dimethylamino-phenyl)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,13,14,15,16,17-dodec ahydro-cyclopenta[a]phenanthren-3-one
mifepristone
C07652
84371-65-3
ru-486
DB00834
cpd000058481
D00585
mifepristone (jan/usan/inn)
korlym (tn)
mifeprex (tn)
NCGC00025179-05
PRESTWICK1_000299
PRESTWICK0_000299
SPBIO_002457
bdbm18627
(10s,11s,14s,15s,17r)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0;{2,7}.0;{11,15}]heptadeca-1,6-dien-5-one
ru486 (tetramethyl-rhodamine conjugated)
HMS2090L22
HMS2052L05
M 8046
NCGC00025179-08
HMS1568L20
chembl438575
bdbm50072024
(11r,13s,14s,17s)-11-(4-dimethylamino-phenyl)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydro-cyclopenta[a]phenanthren-3-one
A840767
(8s,11r,13s,14s,17s)-11-[4-(dimethylamino)phenyl]-13-methyl-17-oxidanyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
(8s,11r,13s,14s,17s)-11-[4-(dimethylamino)phenyl]-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
NCGC00025179-07
NCGC00025179-09
NCGC00025179-06
HMS3262B03
HMS2095L20
unii-320t6rnw1f
320t6rnw1f ,
mifepristonum
ccris 9332
mifepristona
nsc 759862
dtxsid5023322 ,
NCGC00255152-01
dtxcid303322
tox21_301841
nsc-759862
CHEMBL1276308
MLS001424271
tox21_110952
HMS2230P21
CCG-101164
mifepriston
CS-1435
NCGC00025179-13
LP00801
(11beta,17beta)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propyn-1-yl)estra-4,9-dien-3-one
estra-4,9-dien-3-one, 11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propyn-1-yl)-, (11beta,17beta)-
mifepristone [hsdb]
mifepristone [jan]
mifepristone [usan]
mifepristone [inn]
mifepristone [mi]
mifepristone [orange book]
17beta-hydroxy-11beta-[4-(dimethylamino)-phenyl]-17alpha-(prop-1-ynyl)-estra-4,9-dien-3-one
mifepristone [mart.]
mifepristone [vandf]
mifepristone [usp-rs]
mifepristone [who-dd]
1NHZ
AKOS015895416
S2606
HY-13683
NC00414
SCHEMBL16087
NCGC00025179-12
tox21_110952_1
2W8Y
tox21_500801
NCGC00261486-01
(11?,17?)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one
Q-201405
11ss-[p-(dimethylamino)fenyl]-17ss-hydroxy- 17-(1-propynyl)estra-4,9-dien-3-on
VKHAHZOOUSRJNA-GCNJZUOMSA-N
11.beta.-[4-(dimethylamino)phenyl]-17.beta.-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one
(11beta,17beta)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one
HB2783
(8s,11r,13s,14s,17s)-11-(4-(dimethylamino)phenyl)-17-hydroxy-13-methyl-17-(prop-1-yn-1-yl)-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydro-3h-cyclopenta[a]phenanthren-3-one
HMS3649J08
OPERA_ID_562
(10s,11s,14s,15s,17r)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one
sr-01000721888
SR-01000721888-4
sr-01000076011
SR-01000076011-5
mifepristone, united states pharmacopeia (usp) reference standard
mifepristone 1.0 mg/ml in acetonitrile
SR-01000076011-1
SR-01000076011-3
HMS3712L20
ru-486; mifepristone
ru486;c-1073
Q411240
mifepristone (mifeprex) ,
HMS3676D17
122742-25-0
AS-13938
SR-01000076011-9
BCP02145
HMS3412D17
BRD-K37270826-001-31-8
SDCCGSBI-0050778.P002
NCGC00025179-23
HMS3884D12
11beta-(4-dimethylamino)phenyl-17beta-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one
(1s,3as,3bs,10r,11as)-10-[4-(dimethylamino)phenyl]-1-hydroxy-11a-methyl-1-(prop-1-yn-1-yl)-1h,2h,3h,3ah,3bh,4h,5h,7h,8h,9h,10h,11h,11ah-cyclopenta[a]phenanthren-7-one
EN300-117256
estra-4,9-dien-3-one, 11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propyn-1-yl)-, (11.beta.,17.beta.)-
HY-13683R
mifepristone (standard)
CS-0694789
Z1501480424
11-((4-dimethylamino) phenyl)-17-hydroxy-17-(1-propynyl) estra-4,9-dien-3-one
11beta-(4-(dimethylamino)phenyl)-17beta-hydroxy-17-(prop-1-yn-1-yl)estra-4,9-dien-3-one
mifepristonum (latin)
ru 38486(o'neil, m.j. (ed.). the merck index - an encyclopedia of chemicals, drugs, and biologicals. 13th edition, whitehouse station, nj: merck and co., inc., 2001., p. 1103)
11beta-(4-(n,n-dimethylamino)phenyl)-17alpha-(prop-1-ynyl)-delta 4,9-estradiene- 17beta-ol-3-one(o'neil, m.j. (ed.). the merck index - an encyclopedia of chemicals, drugs, and biologicals. 13th edition, whitehouse station, nj: merck and co., inc., 2001
(11beta,17beta)-11-(4-(dimethylamino)-phenyl)-17-hydroxy-17-(1-propynyl)estra- 4,9-dien-3-one(o'neil, m.j. (ed.). the merck index - an encyclopedia of chemicals, drugs, and biologicals. 13th edition, whitehouse station, nj: merck and co., inc., 2001.,
g03xb01
11beta-(4-(dimethylamino)phenyl)-17beta-hydroxy-17alpha-(prop-1-yn-1-yl)estra-4,9-dien-3-one
11 beta-(4-(n,n-dimethylamino)phenyl)-17alpha-(propyl-1-ynyl)-delta-4,9-estradiene-17 beta-ol-3-one
(aa beta, 17 beta)-11-(4-(dimethylamino)-phenyl)-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one
mifepristone (mart.)
mifegyne(o'neil, m.j. (ed.). the merck index - an encyclopedia of chemicals, drugs, and biologicals. 13th edition, whitehouse station, nj: merck and co., inc., 2001., p. 1103)
11-(4-dimethylamino-phenyl)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,13,14,15,16,17-dodec ahydro-cyclopenta(a)phenanthren-3-one
mifepristone (usp-rs)

Research Excerpts

Overview

Mifepristone (RU486) is a chemical contraceptive marketed in more than 55 countries and used by hundreds of millions of women worldwide. It is a non-selective progesterone (PR), glucocorticoid (GR), and androgen receptor (AR) antagonist with antidepressant and anxiolytic effects.

ExcerptReferenceRelevance
"Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-endometriotic activities. "( Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
Gray, DW; Hoekstra, WJ; Jones, DG; Kallander, LS; Liang, X; Madauss, KP; Noe, RA; Stewart, EL; Thompson, SK; Williams, SP, 2005
)
2.07
"Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-diabetic activities. "( Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
Allan, G; Demarest, K; Fiordeliso, JJ; Gunnet, J; Jiang, W; Linton, O; Lundeen, S; Sui, Z; Tannenbaum, P; Xu, J; Zhu, P, 2007
)
1.78
"Mifepristone (RU486) is a chemical contraceptive marketed in more than 55 countries and used by hundreds of millions of women worldwide. "( Similarities and differences between embryonic implantation and CTC invasion: Exploring the roles of abortifacients in cancer metastasis chemoprevention.
Jia, L; Li, Y; Lu, Y; Xie, H; Zhong, C; Zhou, G, 2022
)
2.16
"Mifepristone (RU-486) is a drug used clinically to induce preterm labor."( The Impact of Mouse Preterm Birth Induction by RU-486 on Microglial Activation and Subsequent Hypomyelination.
Bokobza, C; Csaba, Z; Faivre, V; Gressens, P; Guenoun, D; Morin, C; Sautet, I; Schwendimann, L; Van Steenwinckel, J; Young-Ten, P, 2022
)
1.44
"Mifepristone is a non-selective progesterone (PR), glucocorticoid (GR), and androgen receptor (AR) antagonist with antidepressant and anxiolytic effects. "( Mifepristone's effects on depression- and anxiety-like behavior in rodents.
Nayana, J; Shankaranarayana Rao, BS; Srikumar, BN, 2022
)
3.61
"Mifepristone (RU-486) is a selective progesterone receptor modulator that has antagonist properties on the uterus and cervix. "( Clinical Update on Uses for Mifepristone in Obstetrics and Gynecology.
Bryant, AG; Givens, M; Hagey, JM, 2022
)
2.46
"Mifepristone is a safe and effective medication both for its approved use in first-trimester medication abortion and other off-label uses. "( Clinical Update on Uses for Mifepristone in Obstetrics and Gynecology.
Bryant, AG; Givens, M; Hagey, JM, 2022
)
2.46
"Mifepristone is an anti-progesterone shown to improve outcomes when used in conjunction with misoprostol for first trimester abortion."( Combination therapy with mifepristone and misoprostol for the management of first trimester miscarriage: Improved success.
Dunford, A; Fyfe, R, 2018
)
1.51
"Mifepristone, which is an orally active synthetic steroid with antiprogesterone activity, is known as an ovarian toxicant. "( Histopathologic Characterization of Mifepristone-induced Ovarian Toxicity in Cynomolgus Monkeys.
Goto, A; Goto, T; Hayakawa, K; Horie, K; Hosokawa, S; Nakano-Ito, K; Ohta, E; Seki, Y; Taketa, Y, 2018
)
2.2
"Mifepristone is a progesterone receptor modulator that has been shown to alter endometrial receptivity. "( Effect of mifepristone on the transcriptomic signature of endometrial receptivity.
Boggavarapu, NR; Gemzell-Danielsson, K; Lalitkumar, PG; Miravet-Valenciano, J; Navarro, R; Ruiz-Alonso, M; Simon, C; von Grothusen, C, 2018
)
2.33
"Mifepristone acts as a PPAR γ agonist, and relieves cerebral ischemia-reperfusion injury by restoring the balance between MMPs and TIMPs and inhibiting inflammatory cytokines."( Mifepristone alleviates cerebral ischemia-reperfusion injury in rats by stimulating PPAR γ.
Bi, YH; Chen, JL; Jiang, DX; Sun, XH; Wang, SW; Wu, XJ, 2018
)
3.37
"Mifepristone (RU486) is a born-for-woman molecule discovered three decades ago. "( The unique pharmacological characteristics of mifepristone (RU486): from terminating pregnancy to preventing cancer metastasis.
Chen, J; Gao, Y; Jia, L; Liu, Z; Shao, J; Wang, J; Xu, J; Yu, S, 2014
)
2.1
"Mifepristone (RU486) is a chemical abortifacient used by hundreds of millions of women world-wide. "( A novel UPLC/MS/MS method for rapid determination of metapristone in rat plasma, a new cancer metastasis chemopreventive agent derived from mifepristone (RU486).
Chen, JZ; Gao, Y; Jia, L; Jiang, Z; Shao, JW; Wang, JC; Zeng, RJ; Zhu, YW, 2014
)
2.05
"Mifepristone is a synthetic orally active steroid with potent antiglucocorticoid, antiprogestogen and a weak anti-androgen activity, used primarily for termination of pregnancy."( Mifepristone: current knowledge and emerging prospects.
Kakade, AS; Kulkarni, YS, 2014
)
2.57
"Mifepristone is a well-tolerated treatment."( The Role of Mifepristone in Meningiomas Management: A Systematic Review of the Literature.
Cossu, G; Daniel, RT; Levivier, M; Messerer, M, 2015
)
1.52
"Mifepristone is an oral antiprogestational agent reported to have modest activity in a phase II study."( Double-Blind Phase III Randomized Trial of the Antiprogestin Agent Mifepristone in the Treatment of Unresectable Meningioma: SWOG S9005.
Ahmadi, J; Feun, LG; Fredericks, RK; Grunberg, S; Ji, Y; Kabbinavar, FF; Rankin, C; Russell, CA; Schott, A; Sherrod, AE; Stelzer, KJ; Townsend, JJ; Verschraegen, C, 2015
)
1.37
"Mifepristone (RU486) is an oral first-line contraceptive used by hundreds of millions of women, and recently it was tested for anticancer activity in both genders worldwide. "( Thirty-day rat toxicity study reveals reversible liver toxicity of mifepristone (RU486) and metapristone.
Ho, RJ; Jia, L; Li, T; Liu, J; Tu, X; Wan, L; Wang, J; Xiao, Y; Xu, H; Yan, C; Yang, X; Yu, S; Zhu, Y, 2016
)
2.11
"Mifepristone (RU 486) is a compound that is structurally related to steroid hormones, which is derived from the estrane progestins. "( Genomic and Nongenomic Effects of Mifepristone at the Cardiovascular Level: A Review.
Cairrão, E; Feiteiro, J; Mariana, M; Verde, I, 2017
)
2.18
"Mifepristone is a rapidly effective treatment of hypercortisolism, but requires close monitoring of potentially severe hypokalemia, hypertension, and clinical signs of adrenal insufficiency. "( Merits and pitfalls of mifepristone in Cushing's syndrome.
Allolio, B; Bouchard, P; Brue, T; Castinetti, F; Chanson, P; Conte-Devolx, B; Do Cao, C; Fassnacht, M; Hahner, S; Johanssen, S; Morange, I; Ouzounian, S; Picó, A; Terzolo, M; Young, J, 2009
)
2.11
"Mifepristone (MF) is a potent antiprogestin, but was unable to antagonize the PG-induced cell density reduction."( Levonorgestrel, medroxyprogesterone and progesterone cause a concentration-dependent reduction in endometrial cancer (Ishikawa) cell density, and high concentrations of progesterone and mifepristone act in synergy.
Jaeger, R; Moe, BT; Orbo, A; Sager, G; Vereide, AB, 2009
)
1.27
"Mifepristone is a synthetic steroid compound that has been applied to terminate early pregnancy for many years. "( Association of the G2014G genotype in estrogen receptor 1 gene with failure of the mifepristone-induced termination of early pregnancy.
Han, W; He, B; Wang, J; Wang, N; Zhang, S; Zhao, H, 2010
)
2.03
"Mifepristone is a synthetic selective progesterone-receptor modulator (SPRM) that is widely used around the globe in the field of reproductive medicine. "( Mifepristone: pharmacology and clinical impact in reproductive medicine, endocrinology and oncology.
Appleman, LJ; Im, A, 2010
)
3.25
"Mifepristone is a glucocorticoid receptor inhibitor shown in vitro to have anti-HIV activity and anti-simian immunodeficiency virus activity in a macaque model. "( Phase I/II trial of the anti-HIV activity of mifepristone in HIV-infected subjects ACTG 5200.
Brizz, B; Cavert, W; Daar, ES; Lertora, J; Para, MF; Patterson, KB; Reeds, D; Rosenkranz, SL; Schouten, J; Tebas, P; Weiner, D; White, CJ; Yu, S, 2010
)
2.06
"Mifepristone is a safe, effective and relatively cheap drug that plays an important role in women's health care and is widely used for early medical abortion in many countries. "( Early medical abortion: legal and medical developments in Australia.
Petersen, KA, 2010
)
1.8
"Mifepristone is a synthetic progesterone antagonist that is being used widely for the treatment of various conditions such as endometriosis, glaucoma, meningiomas, breast, ovarian and prostate cancer, as well as for research purposes, in the conditional induction of gene expression by using artificial plasmid-based systems. "( Atypical induction of the unfolded protein response by mifepristone.
Dioufa, N; Kassi, E; Kiaris, H; Papavassiliou, AG, 2010
)
2.05
"Mifepristone is a glucocorticoid and progestin antagonist under investigation for the treatment of Cushing's syndrome. "( Impact of mifepristone, a glucocorticoid/progesterone antagonist, on HDL cholesterol, HDL particle concentration, and HDL function.
Amory, JK; Cox, CJ; Gross, C; Heinecke, JW; Ishida, B; Kane, J; Krauss, RM; Page, ST; Purnell, JQ; Schaefer, PM; Tang, C; Vaisar, T; Weinstein, RL, 2012
)
2.22
"Mifepristone (RU486) is a high-affinity, nonselective antagonist of the glucocorticoid receptor."( Successful long-term treatment of Cushing disease with mifepristone (RU486).
Basina, M; Feldman, D; Hoffman, AR; Liu, H,
)
1.1
"Mifepristone is a progesterone receptor antagonist widely used in obstetrics. "( Modulation of free corticotrophin-releasing hormone, adrenal and placental steroid hormone levels induced by mifepristone during pregnancy.
Blot, P; Ceccaldi, PF; Ducarme, G; Guibourdenche, J; Luton, D; Nicolas, M; Saada, J, 2012
)
2.03
"Mifepristone is a glucocorticoid receptor antagonist now available for use in patients with CS."( A new therapeutic approach in the medical treatment of Cushing's syndrome: glucocorticoid receptor blockade with mifepristone.
Biller, BM; Fleseriu, M; Gross, C; Molitch, ME; Schteingart, DE; Vaughan, TB,
)
1.06
"Mifepristone is a potent antiglucocorticoid, the administration of which results in a dose-dependent activation of the hypothalamic-pituitary-adrenal axis. "( Termination of pregnancy with mifepristone and prostaglandin suppresses transiently circulating glucocorticoid bioactivity.
Heikinheimo, O; Honkanen, H; Jänne, OA; Raivio, T; Ranta, S, 2003
)
2.05
"Mifepristone (MIF) is an antiprogestin with potent anti-glucocorticoid and anti-androgen activity. "( Induction of antiproliferation and apoptosis in estrogen receptor negative MDA-231 human breast cancer cells by mifepristone and 4-hydroxytamoxifen combination therapy: a role for TGFbeta1.
Barrett, JT; El Etreby, F; Hou, M; Kallab, AM; Liang, Y; Schoenlein, PV, 2003
)
1.97
"Mifepristone (RU486) is a recently introduced abortifacient that is largely unstudied in terms of drug-drug interactions."( From bench to bedside: utilization of an in vitro model to predict potential drug-drug interactions in the kidney: the digoxin-mifepristone example.
Ito, S; Koren, G; Woodland, C, 2003
)
1.25
"Mifepristone is an excellent agent for emergency contraception."( Progesterone antagonists and progesterone receptor modulators.
Spitz, IM, 2003
)
1.04
"Mifepristone is a potent antagonist of steroid hormone receptors such as glucocorticoid and progesterone receptors. "( Antiandrogen effects of mifepristone on coactivator and corepressor interactions with the androgen receptor.
Coghlan, M; Gelmann, EP; Song, LN, 2004
)
2.07
"Mifepristone is an excellent agent for use as an emergency "postcoital" contraceptive."( Progesterone antagonists and progesterone receptor modulators: an overview.
Spitz, IM, 2003
)
1.04
"Mifepristone is a progesterone receptor antagonist that has been demonstrated to decrease BTB caused by the levonorgestrel subdermal implant (Norplant)."( Mifepristone for the prevention of breakthrough bleeding in new starters of depo-medroxyprogesterone acetate.
Felix, JC; Jain, JK; Kuo, J; Lu, JJ; Nicosia, AF; Nucatola, DL, 2003
)
2.48
"Mifepristone is a potent agent used in emergency contraception (EC). "( A multiparametric study of the action of mifepristone used in emergency contraception using the Rhesus monkey as a primate model.
Dhawan, L; Ghosh, D; Lalitkumar, PG; Sengupta, J, 2003
)
2.03
"Mifepristone is an effective progesterone receptor antagonist. "( [Effects of mifepristone on the proliferation, apoptosis, and cis-platinum (DDP) sensitivity of chemo-resistant human ovarian cancer cells].
Li, GY; Li, XJ; Lin, TC; Wang, G; Xiao, P; Zheng, WT, 2004
)
2.15
"Mifepristone appears to be a useful intervention for psychotic depression, leading to significant improvements even after a 1-week course of administration. "( An 8-week open-label trial of a 6-day course of mifepristone for the treatment of psychotic depression.
El Sheshai, A; Fawzy, W; Fayek, M; Kingsbury, SJ; Loza, N; Rady, A; Simpson, GM, 2005
)
2.03
"Mifepristone is a potent antagonist of the glucocorticoid receptor and blocks the central actions of cortisol."( C-1073 (mifepristone) in the adjunctive treatment of Alzheimer's disease.
Belanoff, J; DeBattista, C, 2005
)
1.48
"The mifepristone-treated rat is a valid model for investigation of the vascular deficits seen in PCOS."( Aortic function is compromised in a rat model of polycystic ovary syndrome.
Bruckdorfer, R; Dooley, A; El-Mahdi, E; Hardiman, P; Lakhani, K; Leonard, A; McLellan, S; Seifalian, A; Sundaresan, M; Yang, W, 2006
)
0.81
"Mifepristone is a potent glucocorticoid and progesterone receptor antagonist. "( The use of mifepristone in the treatment of neuropsychiatric disorders.
Belanoff, J; DeBattista, C, 2006
)
2.17
"Like mifepristone, it is a glucocorticoid antagonist in vivo."( Molecular properties and preclinical pharmacology of JNJ-1250132, a steroidal progesterone receptor modulator that inhibits binding of the receptor to DNA in vitro.
Allan, GF; Clancy, J; Lai, MT; Musto, A; Palmer, E; Palmer, S, 2006
)
0.79
"Mifepristone (RU486) is an oral antiprogestational and, to a lesser extent, antiglucocorticoid agent commonly used for short-term (single-day) therapy. "( Long-term administration of mifepristone (RU486): clinical tolerance during extended treatment of meningioma.
Ahmadi, J; Grunberg, SM; Russell, CA; Sadun, A; Sitruk-Ware, R; Spitz, IM; Weiss, MH, 2006
)
2.07
"Mifepristone is a progesterone antagonist that has been studied for a number of clinical applications. "( Clinical applications of mifepristone.
Ho, PC; Tang, OS, 2006
)
2.08
"Mifepristone (RU-486) is a potent antagonist of steroid hormone receptors such as glucocoticoid and progesterone receptors. "( Antiandrogenic and apoptotic effects of RU-486 on animal prostate.
Berrios, H; Bratoeff, E; Cabeza, M; Gómez, G; Guzmán, A; Heuze, I; Rosales, AM, 2007
)
1.78
"Mifepristone is an antagonist of the glucocorticoid receptor (GR) that also has significant agonist activity in some cell types. "( The glucocorticoid agonist activities of mifepristone (RU486) and progesterone are dependent on glucocorticoid receptor levels but not on EC50 values.
Danielsen, M; Jonklaas, J; Zhang, S, 2007
)
2.05
"Mifepristone is a potent AR antagonist that functions by competing with androgen, preventing AR coactivator binding and by enhancing binding of AR corepressors."( A phase II study of mifepristone (RU-486) in castration-resistant prostate cancer, with a correlative assessment of androgen-related hormones.
Balk, SP; Barb, D; Bubley, GJ; Gelmann, EP; Kantoff, PW; Manola, J; Mantzoros, C; Oh, WK; Smith, M; Taplin, ME, 2008
)
1.39
"Mifepristone is a potent oral antiprogestogen which acts at the level of the receptor, having a high affinity for the progesterone receptor. "( Mifepristone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential.
Brogden, RN; Faulds, D; Goa, KL, 1993
)
3.17
"Mifepristone is an antiprogesterone that binds with progesterone receptors without releasing the biological effect of progesterone."( [Treatment in miscarriage and abortion. Widened use of drugs has many advantages].
Bygdeman, M, 1994
)
1.01
"Mifepristone (RU 486) is an antiprogestin which interacts with progesterone at the receptor level. "( Early luteal phase treatment with mifepristone (RU 486) for fertility regulation.
Bygdeman, M; Gemzell-Danielsson, K; Svalander, P; Swahn, ML, 1993
)
2.01
"Mifepristone (RU-486) is an antiprogestin which interacts with progesterone at the receptor level. "( Early luteal phase treatment with mifepristone (RU 486) for fertility regulation.
Bygdeman, M; Gemzell-Danielsson, K; Svalander, P; Swahn, ML, 1993
)
2.01
"Mifepristone (RU 486) is a steroid that binds to the progesterone receptor and acts as a progesterone antagonist. "( Cervical ripening with mifepristone (RU 486) in first trimester abortion. An electron microscope study.
Christensen, NJ; Rådestad, A; Thyberg, J, 1993
)
2.04
"Mifepristone is a potent antagonist of glucocorticoid and progesterone receptors. "( Mifepristone: treatment of Cushing's syndrome.
Cutler, GB; Sartor, O, 1996
)
3.18
"Mifepristone (RU486) is a progesterone receptor (PgR) antagonist that has been shown to be active in some preclinical hormone-dependent breast cancer tumor models and to produce a few responses in patients with pretreated metastatic disease in two small trials. "( Phase II study of the progesterone antagonist mifepristone in patients with untreated metastatic breast carcinoma: a National Cancer Institute of Canada Clinical Trials Group study.
Eisenhauer, EA; Fisher, B; Norris, B; Panasci, L; Perrault, D; Pritchard, KI; Vandenberg, T, 1996
)
2
"Mifepristone is a steroidal antiprogestin and antiglucocorticoid acting at the receptor level. "( Clinical pharmacokinetics of mifepristone.
Heikinheimo, O, 1997
)
2.03
"Mifepristone is an effective inductive agent for cervical ripening and initiation of labor in term pregnancy, and can improve the outcome of labor induction."( [Mifepristone for induction of labor].
Li, E; Su, H; Weng, L, 1996
)
2.65
"Mifepristone is a potent antagonist of progesterone and glucocorticoids."( Mifepristone. Auxiliary therapeutic use in cancer and related disorders.
Koide, SS, 1998
)
2.46
"Mifepristone is a highly effective and well-tolerated emergency contraceptive when given in a dose of 600 mg within 72 h of unprotected coitus. "( Comparison of three single doses of mifepristone as emergency contraception: a randomised trial. Task Force on Postovulatory Methods of Fertility Regulation.
, 1999
)
2.02
"Mifepristone is a synthetic steroid bearing a propyne substitution on carbon 17 and this suggested to us that it may act as a mechanism-based inhibitor of the CYP isoforms responsible for its metabolism."( Mechanism-based inhibition of rat liver microsomal diazepam C3-hydroxylase by mifepristone associated with loss of spectrally detectable cytochrome P450.
Gomi, RJ; Mason, SR; Reilly, PE, 1999
)
1.25
"Mifepristone (RU 486) is a synthetic steroid obtained by Bailieu in the year 1982. "( [Mifepristone (RU-486), from hell to purgatory].
Botella Llusiá, J, 1999
)
2.66
"Mifepristone is an effective cervical priming agent when orally administered 48 hours before vacuum aspiration for termination of first-trimester pregnancy. "( Mifepristone versus vaginally administered misoprostol for cervical priming before first-trimester termination of pregnancy: a randomized, controlled study.
Ashok, PW; Flett, GM; Templeton, A, 2000
)
3.19
"Mifepristone is an effective late post-coital contraceptive, which can be offered to women who decline the IUCD."( Mifepristone as a late post-coital contraceptive.
Ashok, PW; Flett, GM; Templeton, A; Wagaarachchi, PT, 2001
)
2.47
"Mifepristone (RU486) is a potent antiprogestagen, and at high doses it also acts as an antiglucocorticoid drug. "( Long-term mifepristone (RU486) therapy resulting in massive benign endometrial hyperplasia.
Isacson, C; New, MI; Newfield, RS; Spitz, IM, 2001
)
2.16
"Mifepristone is an antiprogestin available for pregnancy termination in combination with a prostaglandin such as misoprostol. "( Mifepristone.
DeHart, RM; Morehead, MS, 2001
)
3.2
"Mifepristone is an orally-active progesterone receptor antagonist. "( Mifepristone: a potential postcoital contraceptive.
Ho, PC, 2001
)
3.2
"Mifepristone is a safe and effective drug for treating uterine leiomyoma. "( [Effects of mifepristone on estrogen and progestin receptors in human uterine leiomyoma].
Jin, J; Wang, H, 2000
)
2.13
"Mifepristone is an orally active compound with nearly 40% bioavailability after first pass effect."( The potential of mifepristone (RU486) as a female contraceptive drug.
Sarkar, NN, 2002
)
1.38
"Mifepristone is an orally active progesterone antagonist. "( Mifepristone: contraceptive and non-contraceptive uses.
Ho, PC; Tang, OS; Yu Ng, EH, 2002
)
3.2
"Mifepristone (RU 486) is a potent antigestagen and antiglucocorticoid which when given at a dose of 25-600 mg disrupts folliculogenesis, inhibits ovulation and induces menses in healthy women. "( Inhibition of ovulation by low-dose mifepristone (RU 486).
Baird, DT; Hillier, H; Ledger, WL; Sweeting, VM, 1992
)
2
"Mifepristone is a safe alternative for the termination of pregnancy when the beta human chorionic gonadotropin is below 20,000 IU/L."( Abortion: epidemiology, safety, and technique.
Blumenthal, PD, 1992
)
0.9
"Mifepristone (RU 486) is a synthetic steroid with potent antiprogestational and antiglucocorticoid properties that provides an effective medical method of inducing abortion in early pregnancy. "( Mifepristone (RU 486) compared with high-dose estrogen and progestogen for emergency postcoital contraception.
Baird, DT; Dewar, M; Glasier, A; Mackie, M; Thong, KJ, 1992
)
3.17
"Mifepristone is a highly effective postcoital contraceptive agent that, if used more widely, could help reduce the number of unplanned and unwanted pregnancies."( Mifepristone (RU 486) compared with high-dose estrogen and progestogen for emergency postcoital contraception.
Baird, DT; Dewar, M; Glasier, A; Mackie, M; Thong, KJ, 1992
)
3.17
"Mifepristone (RU 486) is a synthetic steroid with potent antiprogestational and antiglucocorticoid properties that offers an effective medical means of inducing abortion in early pregnancy. "( Mifepristone (RU 486) compared with high-dose estrogen and progestogen for emergency postcoital contraception.
Baird, DT; Dewar, M; Glasier, A; Mackie, M; Thong, KJ, 1992
)
3.17
"Mifepristone is a specific glucocorticoid receptor antagonist that has been shown to lower intraocular pressure modestly when applied topically to rabbit eyes. "( Mifepristone blocks specific glucocorticoid receptor binding in rabbit iris-ciliary body.
Munden, PM; Schmidt, TJ, 1992
)
3.17
"Mifepristone (RU 486) is a compound with progesterone as well as cortisol-blocking activities. "( The endocrine effects of long-term treatment with mifepristone (RU 486).
de Jong, FH; Koper, JW; Lamberts, SW, 1991
)
1.98
"Mifepristone is a highly effective cervical priming agent, and has the advantages of being an oral preparation associated with few side effects."( Pre-operative cervical preparation before first trimester vacuum aspiration: a randomized controlled comparison between gemeprost and mifepristone (RU 486).
Henshaw, RC; Templeton, AA, 1991
)
1.93
"Mifepristone is a highly effective cervical priming agent and has the advantages of being an oral preparation and resulting in few side effects."( Pre-operative cervical preparation before first trimester vacuum aspiration: a randomized controlled comparison between gemeprost and mifepristone (RU 486).
Henshaw, RC; Templeton, AA, 1991
)
1.11
"Mifepristone (RU 486) is an anti-progesterone steroid and it is known to be effective in terminating early pregnancies."( [Use of mifepristone (RU 486) in pregnancy (excluding abortion on demand). The first clinical trials].
Grall, F; Sylvestre, L, 1991
)
1.44
"Mifepristone is an effective abortifacient in combination with an exogenous prostaglandin but its mechanism of action is unknown. "( Effects of mifepristone in vivo on decidual prostaglandin synthesis and metabolism.
Baird, DT; Glasier, AF; Kelly, RW; McNeilly, AS; Norman, JE; Wu, WX, 1991
)
2.11
"Mifepristone is an effective abortifacient in combination with an exogenous prostaglandin (PG) but its mechanism is unknown. "( Effects of mifepristone in vivo on decidual prostaglandin synthesis and metabolism.
Baird, DT; Glasier, AF; Kelly, RW; McNeilly, AS; Norman, JE; Wu, WX, 1991
)
2.11
"The Mifepristone treatment is a simple and safe alternative to vacuum aspiration for termination of early pregnancies."( Mifepristone or vacuum aspiration in termination of early pregnancy.
Legarth, J; Michelsen, JW; Peen, UB, 1991
)
2.2
"Mifepristone is an antiprogesterone steroid which is able to terminate early pregnancy with a success rate of 80 p."( [Antiprogesterone, prostaglandin analogues and the early interruption of pregnancy].
Maria, B, 1990
)
1
"Mifepristone is a synthetic 19-norsteroid with strong progesterone receptor antagonist properties."( Induction of abortion in early pregnancy with mifepristone.
Olund, A; Somell, C, 1990
)
1.26
"Mifepristone, (RU 486), is an antiprogesterone which, when administered alone will terminate early pregnancy in 80% of cases. "( Termination of early pregnancy using mifepristone in combination with prostaglandin analogs.
Maria, B; Stampf, F, 1989
)
1.99
"Mifepristone is a synthetic steroid antagonist to progesterone which operates by competitively binding with the progesterone receptors."( [The antiprogesterone action of mifepristone].
Haspels, AA, 1989
)
1.18
"Mifepristone is a safe and useful adjuvant therapy in mid-trimester prostaglandin termination."( Efficacy of the antiprogestin mifepristone (RU 486) prior to prostaglandin termination of pregnancy.
Bahzad, C; Templeton, AA; Urquhart, DR, 1989
)
1.29
"Mifepristone (RU 486) is a new steroid which is a progesterone antagonist and which is able to interrupt early pregnancy without any major side-effects. "( Termination of early pregnancy by a single dose of mifepristone (RU 486), a progesterone antagonist.
Goepp, A; Maria, B; Stampf, F; Ulmann, A, 1988
)
1.97
"Mifepristone is a 19-nor-steroid with an affinity for the progesterone receptor 3 times that of progesterone, and an affinity for the glucocorticoid receptor 2 times that of dexamethasone."( The use of anti-progesterones as a medical IUD.
Loriaux, DL; Nieman, LK, 1988
)
0.9
"Mifepristone (RU 486) is a new steroid which is a progesterone antagonist and which is able to interrupt early pregnancy. "( [Early pregnancy interruption using an antiprogesterone steroid: Mifepristone (RU 486)].
Chaneac, M; Maria, B; Stampf, F; Ulmann, A, 1988
)
1.96

Effects

Mifepristone (RU-486) has theoretical potential as a softening agent on the pregnant and nonpregnant cervix. It has anti-progesterone effects and has a role in managing intrauterine pregnancy loss and termination of pregnancy. Mifepristsone/misoprostol has been rapidly incorporated into abortion services in Canada.

ExcerptReferenceRelevance
"Mifepristone has an effect on free CRH level and changes the estriol-progesterone balance."( Modulation of free corticotrophin-releasing hormone, adrenal and placental steroid hormone levels induced by mifepristone during pregnancy.
Blot, P; Ceccaldi, PF; Ducarme, G; Guibourdenche, J; Luton, D; Nicolas, M; Saada, J, 2012
)
2.03
"Mifepristone has been available in Canada with a normal prescription since November 2017."( Abortion Safety and Use with Normally Prescribed Mifepristone in Canada.
Darling, EK; Dunn, S; Gayowsky, A; Kaczorowski, J; Laba, TL; Law, MR; McGrail, K; Norman, WV; Schummers, L, 2022
)
1.7
"Mifepristone (RU-486) has been approved for abortion in Taiwan since 2000. "( Mifepristone (RU-486
Feng, LY; Hsieh, YP; Li, JH; Wang, YJ; Wu, LT, 2022
)
3.61
"Mifepristone has many uses outside of induced abortion, but these are less well known and underutilized by clinicians because of challenges in accessing and prescribing this medication."( Clinical Update on Uses for Mifepristone in Obstetrics and Gynecology.
Bryant, AG; Givens, M; Hagey, JM, 2022
)
1.74
"Mifepristone has been used to treat endometriosis, but it can cause a constellation of endometrial alterations. "( Distinct clinicopathological features of ovarian endometriosis after long-term exposure to mifepristone.
Pan, Y; Shi, H; Wu, T, 2022
)
2.38
"Mifepristone (RU-486) has anti-progesterone effects and has a role in managing intrauterine pregnancy loss and termination of pregnancy."( Have we overlooked the role of mifepristone for the medical management of tubal ectopic pregnancy?
Balachander, S; Mol, BW; Oltman, J; Woolner, AMF, 2023
)
1.92
"Mifepristone/misoprostol has been rapidly incorporated into abortion services in Canada."( Trends in medication abortion provision before and after the introduction of mifepristone: A study of the National Abortion Federation's Canadian member services.
Doctoroff, J; Foster, AM; Mark, A; Yalahow, A, 2020
)
2.23
"Mifepristone has also been shown to decrease alcohol consumption and craving for alcohol in humans with AUD."( Glucocorticoid receptor modulators decrease alcohol self-administration in male rats.
de Guglielmo, G; George, O; Gregory-Flores, A; Hunt, HJ; Koob, GF; Mason, BJ; McGinn, MA; Schlosburg, JE; Tunstall, BJ; Vendruscolo, LF, 2021
)
1.34
"Mifepristone has been used for first-trimester abortion and contraception. "( Mifepristone regulates macrophage-mediated natural killer cells function in decidua.
Cao, L; Guo, Q; Huang, L; Niu, X; Tang, Y, 2021
)
3.51
"Mifepristone also has beneficial effects in animal models of diabetes and patients with antipsychotic treatment-induced obesity."( Mifepristone enhances insulin-stimulated Akt phosphorylation and glucose uptake in skeletal muscle cells.
Bernal-Sore, I; Del Campo, A; Díaz-Castro, F; Donoso-Barraza, C; Lavandero, S; Navarro-Marquez, M; Osorio-Fuentealba, C; Porras, O; Troncoso, R, 2018
)
2.64
"Mifepristone has gained great interest in its potential as a novel agent against human cancers, including prostate cancer (PCa). "( Mifepristone Has Limited Activity to Enhance the
Kucuk, O; Li, X; Mamouni, K; Wu, D; Yang, Y, 2017
)
3.34
"Mifepristone has been demonstrated to cause palliation from murine and human cancer, even in cancers not known to be positive for expression of progesterone receptors. "( Mifepristone causing complete remission of rapidly advancing leukemia with measurement of progesterone-induced blocking factor.
Check, D; Check, JH; Cohen, R; Sarumi, M, 2014
)
3.29
"Mifepristone has the potential to improve access for rural and remote populations, reduce wait times and alleviate privacy concerns, but only if the medication abortion regimen is affordable and available at a range of service delivery points and provision requirements are aligned with the global evidence."( "They made me go through like weeks of appointments and everything": Documenting women's experiences seeking abortion care in Yukon territory, Canada.
Cano, JK; Foster, AM, 2016
)
1.16
"Mifepristone has become an integral part of abortion provision in the United States and likely has contributed to a trend toward very early abortions. "( Effect of mifepristone on abortion access in the United States.
Finer, LB; Wei, J, 2009
)
2.2
"Mifepristone has not proven to be an effective agent in the treatment of patients with recurrent or persistent ovarian, peritoneal and fallopian tube cancers."( A phase II evaluation of mifepristone in the treatment of recurrent or persistent epithelial ovarian, fallopian or primary peritoneal cancer: a gynecologic oncology group study.
Brady, WE; Hoffman, JS; Mannel, RS; Rocereto, TF; Rotmensch, J; Shahin, MS; Small, L, 2010
)
2.11
"Mifepristone has also served as an invaluable tool in the study of steroid hormone biology."( Mifepristone: pharmacology and clinical impact in reproductive medicine, endocrinology and oncology.
Appleman, LJ; Im, A, 2010
)
2.52
"Mifepristone has not only been shown to down-regulate PIBF expression by human leukemic cell lines but has also been shown to prolong and improve the length of life of mice with spontaneous leukemia."( Mifepristone treatment improves length and quality of survival of mice with spontaneous lung cancer.
Check, JH; Chern, J; Dix, E; Sansoucie, L, 2010
)
2.52
"Mifepristone has been demonstrated to improve longevity and quality of life in mice with spontaneous murine cancer without progesterone receptors and in human colon cancer. "( Efficacy of the progesterone receptor antagonist mifepristone for palliative therapy of patients with a variety of advanced cancer types.
Check, D; Check, JH; Cohen, R; Dix, E; Wilson, C, 2010
)
2.06
"Mifepristone treatment has 2 main drawbacks: (1) the blockade of glucocorticoid receptors leads to increased ACTH and cortisol levels, making it difficult to adapt the treatment and diagnose adrenal deficiency, and (2) increased cortisol levels can also lead to severe hypokalemia."( Medical treatment of Cushing's syndrome: glucocorticoid receptor antagonists and mifepristone.
Brue, T; Castinetti, F; Conte-Devolx, B, 2010
)
1.31
"Mifepristone has recently become available in Australia but its use is restricted."( Mifepristone in South Australia -- the first 1343 tablets.
Messenger, H; Mulligan, E, 2011
)
3.25
"Mifepristone has been added to regimens for early and second trimester abortions - both medical and surgical abortions. "( Mifepristone in South Australia -- the first 1343 tablets.
Messenger, H; Mulligan, E, 2011
)
3.25
"Mifepristone (MF) has been largely used in reproductive medicine due to its capacity to modulate the progesterone receptor (PR). "( Antiprogestin mifepristone inhibits the growth of cancer cells of reproductive and non-reproductive origin regardless of progesterone receptor expression.
Brandhagen, BN; Goyeneche, AA; Ortbahn, CT; Telleria, CM; Tieszen, CR, 2011
)
2.17
"Mifepristone has unique major antagonist properties allowing its use for pregnancy termination."( The immninent dawn of SPRMs in obstetrics and gynecology.
Bouchard, P; Chabbert-Buffet, N; Pintiaux, A, 2012
)
1.1
"Mifepristone has an effect on free CRH level and changes the estriol-progesterone balance."( Modulation of free corticotrophin-releasing hormone, adrenal and placental steroid hormone levels induced by mifepristone during pregnancy.
Blot, P; Ceccaldi, PF; Ducarme, G; Guibourdenche, J; Luton, D; Nicolas, M; Saada, J, 2012
)
2.03
"Mifepristone has been shown to decrease fibroid size."( Mifepristone for uterine fibroids.
Orozco, LJ; Ramírez-Morera, A; Steed, A; Stone, P; Tristan, M, 2012
)
2.54
"Mifepristone has been available in the US since 2000. "( Progesterone use to reverse the effects of mifepristone.
Davenport, ML; Delgado, G, 2012
)
2.08
"Mifepristone has been used to treat excessive cortisol production by blocking the action of cortisol at the level of the glucocorticoid receptor."( Mifepristone: is there a place in the treatment of Cushing's disease?
Carmichael, JD; Fleseriu, M, 2013
)
2.55
"Mifepristone has differential effects on eNOS expression in the epithelium and endothelium in the human endometrium at the time of implantation. "( Effects of mifepristone on expression of endothelial nitric oxide synthase in human endometrium during the implantation phase.
Gemzell-Danielsson, K; Qiu, X; Sun, X, 2003
)
2.15
"Mifepristone has potent reversal effect on MDR in SGC7901/VCR via inhibiting the function of MRP and P-gp, modulating the expression of Bcl-2 and Bax proteins, and enhancing the sensitivity to anticancer agent VCR."( Reversal of multidrug resistance in drug-resistant human gastric cancer cell line SGC7901/VCR by antiprogestin drug mifepristone.
Bai, J; Du, YH; Hu, K; Li, DQ; Wang, Y; Wang, ZB; Zhao, J, 2004
)
1.98
"Mifepristone has been used for both medical termination of pregnancy and emergency contraception. "( Effects of mifepristone on vascular endothelial growth factor and thrombospondin-1 mRNA in Ishikawa cells: implication for the endometrial effects of mifepristone.
Archer, DF; Mirkin, S, 2004
)
2.16
"Mifepristone has high patient acceptability and few side effects compared to the standard Yuzpe regimen for EC."( Mifepristone versus the Yuzpe regimen (PC4) for emergency contraception.
Ashok, PW; Flett, GM; Hamoda, H; Templeton, A, 2004
)
3.21
"Mifepristone has intrinsic neuroprotective and antioxidant potential which could offer additional benefits as well."( Glucocorticoids may initiate Alzheimer's disease: a potential therapeutic role for mifepristone (RU-486).
Anand, KS; Dhikav, V, 2007
)
1.29
"Mifepristone has possible antidepressant properties related to its anti-glucocorticoid activity."( Psychiatric outcomes following medical and surgical abortion.
Creinin, MD; Hanusa, BH; Rothschild, AJ; Sit, D; Wisner, KL, 2007
)
1.06
"Mifepristone has been shown to be an effective postcoital contraceptive with a likely emergency role, since its repeated use modifies the menstrual cycle."( Mifepristone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential.
Brogden, RN; Faulds, D; Goa, KL, 1993
)
2.45
"Mifepristone has been used clinically for medical termination of pregnancy."( Inhibitory effect of mifepristone (RU 486) on ovulation in the isolated perfused rat ovary.
Brännström, M, 1993
)
1.33
"Mifepristone has also been used for labor induction."( Drug therapy during labor and delivery.
Kelsey, JJ; Prevost, RR, 1994
)
1.01
"Mifepristone (RU 486) has many therapeutic possibilities, which largely exceed simple interruption of pregnancy. "( [Mifepristone (RU 486): present status, prospectives].
Baulieu, EE; Peyron, R; Ulmann, A, 1995
)
2.64
"Mifepristone has been also reported to be effective as a postcoital agent, and it is being evaluated in the treatment of meningioma, recurrent breast cancer, Cushing's syndrome, and glaucoma."( Mifepristone (RU 486) in the United States. What does the future hold?
Rosenfield, A, 1993
)
2.45
"Mifepristone (RU-486) has recently been granted approval from the Food and Drug Administration for the early termination of pregnancy. "( Pregnancy interruption using mifepristone (RU-486). A new choice for women in the USA.
Mackenzie, SJ; Yeo, S,
)
1.87
"Mifepristone has been demonstrated to act on hypothalamic, pituitary, ovarian, and uterine tissue. "( Fertility impairment after mifepristone treatment to rats at proestrus. Actions on the hypothalamic-hypophyseal-ovarian axis.
Deis, RP; Mezzadri, MR; Telleria, CM, 1997
)
2.04
"Mifepristone (RU 486) has received recent attention for its effects as an abortifacient. "( Mifepristone (RU 486): current knowledge and future prospects.
Anastasio, GD; Goldberg, JR; Plescia, MG,
)
3.02
"Mifepristone has been studied in various doses and has been shown to be very effective but is not yet commercially available."( Intrauterine contraceptive devices and antigestagens as emergency contraception.
Webb, AM, 1997
)
1.02
"Mifepristone has activity against ovarian cancer resistant to cisplatin and paclitaxel. "( Phase II study of mifepristone (RU486) in refractory ovarian cancer.
Aikins, JA; Paulson, J; Rocereto, TF; Saul, HM, 2000
)
2.08
"Mifepristone has much more significant effects on the chorionic villi than on the decidua."( [Effect of mifepristone on cell-cycle kinetics of human placental chorio-trophoblastic and decidual cell].
Wu, S; Zhang, L; Zhou, X, 1999
)
1.41
"Mifepristone has been shown to be effective as a contraceptive if administered in the early luteal phase."( Feasibility of administering mifepristone as a once a month contraceptive pill.
Baird, DT; Brown, A; Glasier, AF; Hapangama, DK, 2001
)
1.32
"Mifepristone has been used for a number of other indications, but further studies are needed before such treatment can be recommended."( Mifepristone: contraceptive and non-contraceptive uses.
Ho, PC; Tang, OS; Yu Ng, EH, 2002
)
2.48
"Mifepristone (RU-486) has theoretical potential as a softening agent on the pregnant and nonpregnant cervix. "( Effect of mifepristone on dilatation of the pregnant and non-pregnant cervix.
Gupta, JK; Johnson, N, 1990
)
2.12
"Mifepristone (RU 38486) has no effect on G6PD activity, but it inhibits the R5020 stimulation of G6PD activity."( Sex steroid hormone modulation of NADPH pathways in MCF-7 cells.
Bader, C; Monet, JD; Thomas, M, 1990
)
1

Actions

Mifepristone can increase the expression of caspase 3 in both eutopic and ectopic endometria. It can also inhibit ovulation, prevent implantation and induce menstrual bleeding at the time of expected menses. Mifepristsone did not increase life span of virgin females or males.

ExcerptReferenceRelevance
"Mifepristone induced an increase in tumor-infiltrating lymphocytes; a decrease in hormone receptor and pSer118ER expression; and an increase in calregulin, p21, p15, and activated caspase 3 expression."( Beneficial Effects of Mifepristone Treatment in Patients with Breast Cancer Selected by the Progesterone Receptor Isoform Ratio: Results from the MIPRA Trial.
Abascal, MF; Abba, MC; Acosta Haab, G; Belizán, JM; Burruchaga, J; Caillet-Bois, I; Castets, A; Elía, A; Fabris, V; Gass, H; Helguero, LA; Lamb, CA; Lanari, C; Liguori, M; Lovisi, S; Martínez-Vazquez, P; Muñoz, J; Novaro, V; Pataccini, G; Rojas, P; Saldain, L; Sánchez, J; Spengler, E; Vanzulli, SI, 2023
)
1.95
"Mifepristone did not cause a clinically meaningful QTc prolongation in healthy volunteers at plasma concent rations of mifepristone and its main metabolites that clearly exceeded those seen in a previous TQT study."( Assessment of the cardiac safety and pharmacokinetics of a short course, twice daily dose of orally-administered mifepristone in healthy male subjects.
Bullingham, R; Combs, DL; Darpo, B; Ferber, G; Hafez, K, 2013
)
2.04
"Mifepristone can increase the expression of caspase 3 in both eutopic and ectopic endometria and initiate cell apoptosis in both eutopic and ectopic endometria. "( The influence of mifepristone to caspase 3 expression in adenomyosis.
Jiang, X; Wang, S; Wang, Y, 2014
)
2.18
"Mifepristone did not increase life span of virgin females or males."( The progesterone antagonist mifepristone/RU486 blocks the negative effect on life span caused by mating in female Drosophila.
Brookes, N; Keroles, D; Landis, GN; Salomon, MP; Sekimura, T; Tower, J, 2015
)
1.43
"Mifepristone was found to suppress expression of the progesterone-induced blocking factor (PIBF). "( Mifepristone treatment improves length and quality of survival of mice with spontaneous leukemia.
Amadi, N; Check, JH; Chern, J; Katz, Y; Sansoucie, L, 2009
)
3.24
"Mifepristone can inhibit the effects of progesterone by down-regulating the expressions of HLA-G, HLA-E and HLA-F mRNA in trophoblasts during the first trimester."( [Mifepristone inhibits the progesterone-induced expressions of HLA-G, -E, -F genes in trophoblasts during first trimester].
Liao, AH; Wang, Y; Zeng, B; Zhang, Y, 2012
)
2.73
"Mifepristone did not increase the time for abortion by more than the prespecified margin (3 min). "( Mifepristone vs. osmotic dilator insertion for cervical preparation prior to surgical abortion at 14-16 weeks: a randomized trial.
Borgatta, L; Finneseth, M; Hou, MY; Mark, A; Roncari, D; Sonalkar, S; Vragovic, O, 2012
)
3.26
"Mifepristone may act to enhance the sensitivity of COC1/DDP cells to cisplatin, possibly through regulating Bcl-2 and Bax protein expressions."( [Enhanced sensitivity of ovarian cell line to cisplatin induced by mifepristone and its mechanism].
Qin, TN; Wang, LL, 2002
)
1.99
"Mifepristone can inhibit the growth of chemo-resistant human ovarian carcinoma cells,and enhance its DDP sensitivity. "( [Effects of mifepristone on the proliferation, apoptosis, and cis-platinum (DDP) sensitivity of chemo-resistant human ovarian cancer cells].
Li, GY; Li, XJ; Lin, TC; Wang, G; Xiao, P; Zheng, WT, 2004
)
2.15
"Mifepristone seems to inhibit OVCAR-3 cell proliferation by down-regulating bcl-2 and up-regulating caspase-3 activity."( Effects of progesterone and anti-progestin (mifepristone) treatment on proliferation and apoptosis of the human ovarian cancer cell line, OVCAR-3.
Bringuier, AF; Daraï, E; Dufournet Etienne, C; Fauvet, R; Feldmann, G; Poncelet, C, 2006
)
1.32
"Mifepristone may inhibit proliferation and promote apoptosis of trophoblasts in early pregnant chorionic villi."( [Effects of mifepristone on proliferation and apoptosis in early chorionic villi].
Cao, Z; Han, Z; Yang, Y, 1998
)
2.12
"Mifepristone was able to inhibit p65-associated HAT activity to the same extent as dexamethasone but failed to inhibit the natural promoter to an equal extent due to an inability to recruit HDAC2 to the p65-associated HAT complex."( p65-activated histone acetyltransferase activity is repressed by glucocorticoids: mifepristone fails to recruit HDAC2 to the p65-HAT complex.
Adcock, IM; Barnes, PJ; Cosio, B; Ito, K; Jazrawi, E, 2001
)
1.26
"Mifepristone will also inhibit ovulation, prevent implantation and induce menstrual bleeding at the time of expected menses."( Antigestogens: the holy grail of contraception.
Baird, DT, 2001
)
1.03

Treatment

Pretreatment with mifepristone, both icv (80 microg/rat) and ip (10 mg/kg) injected, did not modify the response to icv and ip N/OFQ. Treatment with m ifepriston decreased immobility and increased swimming (but not climbing) behavior in the FST.

ExcerptReferenceRelevance
"Mifepristone treatment for advanced cancer has demonstrated considerable improvement in both length and quality of life in patients who no longer have any other treatment options. "( New Insights as to Why Progesterone Receptor Modulators, such as Mifepristone, Seem to Be More Effective in Treating Cancers that Are Devoid of the Classical Nuclear Progesterone Receptor.
Check, D; Check, JH, 2021
)
2.3
"Mifepristone treatment decreased some hematological parameters mildly and increased plasma volume."( Estradiol dominance induces hemodilution and mild hematological alterations in mifepristone-treated rats.
Kishida, T; Souma, S; Takakura, I; Yokoi, R, 2022
)
1.67
"Mifepristone pre-treatments abolish DEP and PFOS effects, confirming their GR agonist profile, also corroborated by molecular docking."( Effects of endocrine disrupting chemicals on the expression of RACK1 and LPS-induced THP-1 cell activation.
Buoso, E; Corsini, E; Galbiati, V; Iulini, M; Linciano, P; Maddalon, A; Marinovich, M; Masi, M; Racchi, M, 2022
)
1.44
"Mifepristone treatment had no effect in male mice, but significantly lowered hepatic triglyceride and cholesterol levels in female mice."( Glucocorticoid receptor modulator CORT125385 alleviates diet-induced hepatosteatosis in male and female mice.
Gentenaar, M; Hunt, H; Kroon, J; Meijer, OC; Moll, TJA, 2023
)
1.63
"Mifepristone pretreatment plus misoprostol administration vs misoprostol alone."( Cost-effectiveness of Mifepristone Pretreatment for the Medical Management of Nonviable Early Pregnancy: Secondary Analysis of a Randomized Clinical Trial.
Atrio, J; Chen, M; Harvie, HS; Koelper, N; Loza-Avalos, SE; Nagendra, D; Schreiber, CA; Sonalkar, S, 2020
)
2.32
"The mifepristone pretreatment group had higher QALYs (0.0820 [95% CI, 0.0815-0.0825] vs 0.0806 [95% CI, 0.0800-0.0812]; P = .001) and a higher completion rate after first treatment (83.8% vs 67.1%; P < .001) than the group receiving misoprostol alone."( Cost-effectiveness of Mifepristone Pretreatment for the Medical Management of Nonviable Early Pregnancy: Secondary Analysis of a Randomized Clinical Trial.
Atrio, J; Chen, M; Harvie, HS; Koelper, N; Loza-Avalos, SE; Nagendra, D; Schreiber, CA; Sonalkar, S, 2020
)
1.35
"Mifepristone treatment demonstrated reduction in serum progesterone level and corpus luteum diameter, and elevation in ovarian caspase-3 and cleaved caspase-3 levels."( Effect of GnRH-antagonist, mifepristone and letrozole on preventing ovarian hyperstimulation syndrome in rat model.
Chen, Y; Luo, J; Qi, Q; Wang, Y; Xie, Q, 2021
)
1.64
"Mifepristone pretreatment increased the severity of pain but not bleeding and resulted in a shorter trajectory of symptoms during medical management of EPL."( The effect of mifepristone pretreatment on bleeding and pain during medical management of early pregnancy loss.
Flynn, AN; Jiang, E; Koelper, N; Martin, B; McAllister, A; Roe, AH; Schreiber, CA, 2021
)
2.42
"Mifepristone pretreatment decreases the duration of heavy bleeding and there was a trend toward decreased duration of pain during medical management of miscarriage, indicating that this medication improves the efficiency, in addition to the efficacy, of this treatment."( The effect of mifepristone pretreatment on bleeding and pain during medical management of early pregnancy loss.
Flynn, AN; Jiang, E; Koelper, N; Martin, B; McAllister, A; Roe, AH; Schreiber, CA, 2021
)
2.42
"Mifepristone treatment reduces VS cell viability more significantly than cells derived from patient meningiomas, while healthy human Schwann cells remain unaffected."( Computational repositioning and preclinical validation of mifepristone for human vestibular schwannoma.
Brown, AS; Kohane, IS; Landegger, LD; Lewis, RM; Patel, CJ; Perlis, RH; Sagers, JE; Sahin, MI; Stankovic, KM; Vasilijic, S; Welling, DB, 2018
)
1.45
"Mifepristone treatment consisted of 200 mg administered on day LH + 2. "( Effect of mifepristone on the transcriptomic signature of endometrial receptivity.
Boggavarapu, NR; Gemzell-Danielsson, K; Lalitkumar, PG; Miravet-Valenciano, J; Navarro, R; Ruiz-Alonso, M; Simon, C; von Grothusen, C, 2018
)
2.33
"Mifepristone treatment prior to LNG-IUS insertion results in significantly lower bleeding and spotting rates but no significant reduction post insertion."( Mifepristone treatment prior to insertion of a levonorgestrel releasing intrauterine system for improved bleeding control - a randomized controlled trial.
Gemzell-Danielsson, K; Kopp Kallner, H; Papaikonomou, K; Söderdahl, F, 2018
)
3.37
"Mifepristone treatment influenced locomotor response to repeated amphetamine injections, but this effect during the initial phase did not affect the expression of sensitization after a withdrawal period."( Mifepristone treatment affects the response to repeated amphetamine injections, but does not attenuate the expression of sensitization.
Boshuizen, MC; de Kloet, ER; van der Veen, R, 2013
)
2.55
"Mifepristone treatment for CS results in progressive clinical improvement. "( Global clinical response in Cushing's syndrome patients treated with mifepristone.
Braunstein, GD; Feldman, D; Gross, C; Katznelson, L; Loriaux, DL; Schteingart, DE, 2014
)
2.08
"Mifepristone treatment significantly reduced leiomyoma volume from 135.3 ± 22.9 cc at enrollment to 101.2 ± 22.4 cc after 3 months of treatment. "( Vaginal mifepristone for the treatment of symptomatic uterine leiomyomata: an open-label study.
Gilboa, Y; Goldchmit, C; Jakobson-Setton, A; Katz, D; Seidman, DS; Tadir, Y; Yerushalmi, GM, 2014
)
2.28
"The mifepristone-treated hatchlings were assayed for imprinting ability on post-hatching day 2 and for social behaviors on day 3."( Impaired imprinting and social behaviors in chicks exposed to mifepristone, a glucocorticoid receptor antagonist, during the final week of embryogenesis.
Kagami, K; Nishigori, H, 2014
)
1.12
"Mifepristone treatment alone was not cytotoxic in any cell line."( Glucocorticoid receptor activation inhibits chemotherapy-induced cell death in high-grade serous ovarian carcinoma.
Baker, GM; Conzen, SD; Fleming, GF; Kocherginsky, M; Lengyel, E; Skor, MN; Stringer-Reasor, EM, 2015
)
1.14
"Mifepristone treatment provided rapid improvement in glycemic control, insulin resistance, and hypertension as well as significant diminishment of her myopathy and fatigue."( Mifepristone Treatment of Cushing's Syndrome in a Pediatric Patient.
Banerjee, RR; Feldman, BJ; Katznelson, L; Marina, N, 2015
)
2.58
"Mifepristone treatment was not associated with improvement in self-reported physical health (p=0.838) or in other self-reported measures of mental health."( A randomized, double-blind, placebo-controlled, crossover trial of mifepristone in Gulf War veterans with chronic multisymptom illness.
Caramanica, K; Golier, JA; Harvey, PD; Makotkine, I; Michaelides, AC; Schmeidler, J; Yehuda, R, 2016
)
1.39
"Mifepristone treatment inhibited protein production of these genes, most notably with versican expression."( Mifepristone inhibits extracellular matrix formation in uterine leiomyoma.
Britten, J; Catherino, WH; Cox, J; Malik, M; Patel, A, 2016
)
2.6
"Mifepristone treatment induces reduced menstrual bleeding and amenorrhea and also has a direct effect on endometrial arterioles."( Aquaporin 1 is expressed in the human endometrium during normal cycle and increases after mifepristone treatment.
Gemzell-Danielsson, K; Hildenbrand, A; Lalitkumar, PG; Mints, M; Nielsen, S; Stavreus-Evers, A, 2008
)
1.29
"Mifepristone treatment induced lactotrope activation with development of the rough endoplasmic reticulum and Golgi complex with prolactin immunoreactive small newly formed and large mature secretory granules."( Pituitary changes involved in prolactin secretion induced by mifepristone and naloxone during late pregnancy.
Deis, R; Ezquer, M; Gabutti, CV; Maldonado, C; Soaje, M, 2009
)
1.32
"Mifepristone treatment significantly reduced the bleeding days (P = 0.001) and increased serum haemoglobin values (P = 0.046)."( Mifepristone for treatment of uterine leiomyoma. A prospective randomized placebo controlled trial.
Engman, M; Gemzell-Danielsson, K; Granberg, S; Lalitkumar, PG; Meng, CX; Williams, AR, 2009
)
2.52
"Mifepristone treated women were less likely to undergo caesarean section (RR 0.74, 95% CI 0.60 to 0.92) but more likely to have an instrumental delivery (RR 1.43, 95% CI 1.04 to 1.96)."( Mifepristone for induction of labour.
Hapangama, D; Neilson, JP, 2009
)
2.52
"Mifepristone treatment has 2 main drawbacks: (1) the blockade of glucocorticoid receptors leads to increased ACTH and cortisol levels, making it difficult to adapt the treatment and diagnose adrenal deficiency, and (2) increased cortisol levels can also lead to severe hypokalemia."( Medical treatment of Cushing's syndrome: glucocorticoid receptor antagonists and mifepristone.
Brue, T; Castinetti, F; Conte-Devolx, B, 2010
)
1.31
"Mifepristone (RU486) treatment can interfere with cortisol signaling that can lead to suppression of tumor immunity."( Treatment combining RU486 and Ad5IL-12 vector attenuates the growth of experimentally formed prostate tumors and induces changes in the sentinel lymph nodes of mice.
Braciak, TA; DeLaney, A; Gabaglia, CR; Gauldie, J; Gee, J; Graham, FL; Halder, R; Sercarz, EE, 2010
)
1.08
"Mifepristone treatment completely abolished the stressor-induced elevation in plasma cortisol and glucose levels seen in the control fish."( Central and peripheral glucocorticoid receptors are involved in the plasma cortisol response to an acute stressor in rainbow trout.
Alderman, SL; Bernier, NJ; McGuire, A; Vijayan, MM, 2012
)
1.1
"Mifepristone treatment decreased HDL-C and HDL particle concentration by 26 and 25%, respectively, but did not alter pre-β HDL concentration."( Impact of mifepristone, a glucocorticoid/progesterone antagonist, on HDL cholesterol, HDL particle concentration, and HDL function.
Amory, JK; Cox, CJ; Gross, C; Heinecke, JW; Ishida, B; Kane, J; Krauss, RM; Page, ST; Purnell, JQ; Schaefer, PM; Tang, C; Vaisar, T; Weinstein, RL, 2012
)
1.5
"Mifepristone treatment was associated with a time-limited increase in cortisol awakening response and with a sustained improvement in SWM performance, which was evident 7 weeks after the cessation of treatment."( A randomized trial to examine the effect of mifepristone on neuropsychological performance and mood in patients with bipolar depression.
Bulmer, S; Ferrier, IN; Gallagher, P; Herron, LJ; Porter, RJ; Smith, MS; Watson, S; Young, AH, 2012
)
1.36
"Mifepristone treatment rescues the pathologically induced cognitive impairments and markedly reduces amyloid beta (Aβ)-load and levels, as well as tau pathologies. "( Mifepristone alters amyloid precursor protein processing to preclude amyloid beta and also reduces tau pathology.
Baglietto-Vargas, D; Green, KN; LaFerla, FM; Martinez-Coria, H; Medeiros, R, 2013
)
3.28
"Mifepristone-treated cells displayed a long, thin, spindle-like shape with boundaries resembling those of loosely adhered cells. "( Cytostasis and morphological changes induced by mifepristone in human metastatic cancer cells involve cytoskeletal filamentous actin reorganization and impairment of cell adhesion dynamics.
Brandhagen, BN; Goyeneche, AA; Telleria, CM; Tieszen, CR; Tracy, MS; Ulmer, TM, 2013
)
2.09
"Mifepristone treatment reduced the prevalence and severity of dysmenorrhea, menorrhagia, and pelvic pressure."( Systematic review of mifepristone for the treatment of uterine leiomyomata.
Jackson, R; Jacoby, AF; Pritts, EA; Steinauer, J, 2004
)
1.36
"The mifepristone treatment decreased the MHC 2X profile in R."( Effect of glucocorticoïd receptor ligands on myosin heavy chains expression in rat skeletal muscles during controllable stress.
Favot, L; Hartmann, N; Martrette, JM; Westphal, A, 2004
)
0.8
"The mifepristone-treated rat is a valid model for investigation of the vascular deficits seen in PCOS."( Aortic function is compromised in a rat model of polycystic ovary syndrome.
Bruckdorfer, R; Dooley, A; El-Mahdi, E; Hardiman, P; Lakhani, K; Leonard, A; McLellan, S; Seifalian, A; Sundaresan, M; Yang, W, 2006
)
0.81
"In mifepristone-treated women the cervix was about 1 mm more dilated at operation and further mechanical dilatation was needed less frequently than in placebo-treated controls."( Cervical ripening with mifepristone (RU 486) in late first trimester abortion. World Health Organization Task Force on Postovulatory Methods of Fertility Regulation.
, 1994
)
1.11
"Mifepristone treatment partially reverted the PRL increase induced by progesterone."( Mifepristone treatment demonstrates the participation of adrenal glucocorticoids in the regulation of oestrogen-induced prolactin secretion in ovariectomized rats.
Carón, RW; Deis, RP; Salicioni, AM, 1994
)
2.45
"Mifepristone treatment increased the levels of estradiol, cortisol and testosterone in serum and decidual cytosol (p < 0.05 or p < 0.01)."( Tissue and serum levels of steroid hormones and RU 486 after administration of mifepristone.
Bai, XM; Shi, WL; Wang, JD; Zhang, GQ, 1994
)
1.24
"Mifepristone treatment did not affect plasma insulin or corticosterone levels but resulted in a significant reduction in plasma aldosterone concentration."( Effects of the glucocorticoid II receptor antagonist mifepristone on hypertension in the obese Zucker rat.
Clapham, JC; Turner, NC, 1997
)
1.27
"Mifepristone-treated rats had decreased preovulatory surges of LH and prolactin (PRL), and hypersecretion of LH, PRL, and progesterone at estrus."( Fertility impairment after mifepristone treatment to rats at proestrus. Actions on the hypothalamic-hypophyseal-ovarian axis.
Deis, RP; Mezzadri, MR; Telleria, CM, 1997
)
1.32
"Mifepristone pretreatment significantly reduced the apoptosis and caspase-3 activity after burn injury, whereas blocking FasL activity had only minimal effects."( Glucocorticoid-induced, caspase-dependent organ apoptosis early after burn injury.
Clare-Salzler, M; Copeland, EM; Edwards, CK; Fukuzuka, K; Moldawer, LL; Mozingo, DW, 2000
)
1.03
"6%) mifepristone-treated women and seven (10.8%) placebo-treated women delivered vaginally on day 1 (P =.60)."( Mifepristone for preinduction cervical ripening beyond 41 weeks' gestation: a randomized controlled trial.
Fassett, MJ; Mishell, DR; Wing, DA, 2000
)
2.23
"Mifepristone treated women were more likely to have delivered within 48 and 96 hours of treatment than were placebo treated/no treatment women - 48 hours: RR 2.82, 95% CI 1.82-4.36; 96 hours: RR 3.40, 95% CI 1.96-5.92."( Mifepristone for induction of labour.
Neilson, JP, 2000
)
2.47
"Mifepristone pretreatment significantly reduced apoptosis in both T- and B-cell populations in intraepithelial lymphocytes after the burn injury."( Glucocorticoid and Fas ligand induced mucosal lymphocyte apoptosis after burn injury.
Clare-Salzer, M; Copeland, EM; Edwards, CK; Fukuzuka, K; Moldawer, LL; Mozingo, DW, 2000
)
1.03
"Mifepristone treatment reduced ER and PR staining."( [The immunohistochemical studies on estradiol and progesterone receptors in human decidua after terminating early pregnancy by mifepristone].
Chen, X; Huang, L; Shi, Y, 1999
)
1.23
"Mifepristone treatment resulted in a threefold increase in plasma corticosterone levels in lean Zucker rats, but it did not change corticosterone secretion in obese animals."( Differential hypothalamic arginine vasopressin response to glucocorticoid receptor antagonism in lean and obese Zucker rats.
Huupponen, R; Jolkkonen, J; Koulu, M; Pesonen, U, 1992
)
1
"Mifepristone treatment resulted in control of tumour growth (= stable disease) in six of 10 patients who had shown recent evidence of tumour growth."( Mifepristone (RU 486) treatment of meningiomas.
Avezaat, CJ; Braakman, R; de Jong, H; Koper, JW; Lamberts, SW; Tanghe, HL; Wijngaarde, R, 1992
)
2.45
"Mifepristone treatment resulted in control of tumor growth (stable disease) in 6 of 10 patients who had shown recent evidence of tumor growth."( Mifepristone (RU 486) treatment of meningiomas.
Avezaat, CJ; Braakman, R; de Jong, H; Koper, JW; Lamberts, SW; Tanghe, HL; Wijngaarde, R, 1992
)
2.45
"The mifepristone treatment significantly increased plasma corticosterone levels in lean animals, but not in obese animals."( Effects of repeated administration of mifepristone and 8-OH-DPAT on expression of preproneuropeptide Y mRNA in the arcuate nucleus of obese Zucker rats.
Huupponen, R; Koulu, M; Pesonen, U; Rouru, J, 1991
)
1.03
"The Mifepristone treatment is a simple and safe alternative to vacuum aspiration for termination of early pregnancies."( Mifepristone or vacuum aspiration in termination of early pregnancy.
Legarth, J; Michelsen, JW; Peen, UB, 1991
)
2.2
"The mifepristone treatment is simple and a safe alternative to vacuum aspiration for termination of early pregnancies."( Mifepristone or vacuum aspiration in termination of early pregnancy.
Legarth, J; Michelsen, JW; Peen, UB, 1991
)
2.2
"In mifepristone-treated women the cervix was on average between 0.9 and 1.2 mm more dilated at operation, but the effect was not dose related."( The use of mifepristone (RU 486) for cervical preparation in first trimester pregnancy termination by vacuum aspiration. World Health Organization. Task Force on Post-ovulatory Methods for Fertility Regulation.
, 1990
)
1.18
"Mifepristone treatment (600 mg per day for 2 days) was considered to be effective in 29 of 46 patients (63%)."( Induction of labor with mifepristone (RU 486) in intrauterine fetal death.
Cabrol, D; Cronje, H; Dubois, C; Gonnet, JM; Guillot, M; Maria, B; Moodley, J; Oury, JF; Thoulon, JM; Treisser, A, 1990
)
1.31
"Pretreatment with mifepristone combined with estradiol valerate did not increase the complete expulsion rate significantly comparing with pretreatment with mifepristone (P = 0.222)."( A retrospective study of estrogen in the pretreatment for medical management of early pregnancy loss and the inference from intrauterine adhesion.
Cao, C; Chen, M; Hu, Z; Shu, C; Yang, X; Zhou, Q, 2022
)
1.04
"A treatment with mifepristone, injected every 3 days between PNDs 4 and16, prevented functional and structural alterations induced by MSEW."( Early life stress induces visual dysfunction and retinal structural alterations in adult mice.
Berardino, B; Calanni, JS; Canepa, E; Dieguez, HH; Dorfman, D; González Fleitas, MF; Repetto, EM; Rosenstein, RE; Villarreal, A, 2023
)
1.24
"Pretreatment with mifepristone followed by misoprostol bucally resulted in a shorter treatment time for medical management of fetal death than treatment with misoprostol alone. "( Mifepristone pretreatment followed by misoprostol 200 mcg buccal for the medical management of intrauterine fetal death at 14-28 weeks: A randomized, placebo-controlled, double blind trial.
Bousieguez, M; Bracken, H; Ha, DQ; Linh, NTH; Ngoc, NTN; Ortiz, MA; Paredes, NR; Quyet, VB; Winikoff, B, 2020
)
2.33
"Treatment with mifepristone and misoprostol or with matched placebo and misoprostol tablets."( Cost-effectiveness of mifepristone and misoprostol versus misoprostol alone for the management of missed miscarriage: an economic evaluation based on the MifeMiso trial.
Ahmed, A; Beeson, LE; Bender-Atik, R; Bhatia, K; Bottomley, C; Brewin, J; Cheed, V; Cheong, Y; Choudhary, M; Chu, JJ; Coomarasamy, A; Debs, S; Devall, AJ; Gallos, ID; Gupta, P; Hamilton, J; Hardy, P; Hassan, I; Hinshaw, K; Hodge, FS; Horne, AW; Izzat, F; Jeve, Y; Jones, LL; Kumar, CS; La Fontaine Papadopoulos, JH; Naftalin, J; Nunes, N; Okeke Ogwulu, CB; Oliver, A; Pringle, S; Quenby, S; Roberts, TE; Ross, J; Shahid, A; Small, R; Underwood, M; Watkins, L; Williams, EV; Yongzhong, S, 2021
)
1.29
"Pretreatment with mifepristone followed by treatment with misoprostol resulted in a higher likelihood of successful management of first-trimester pregnancy loss than treatment with misoprostol alone. "( Mifepristone Pretreatment for the Medical Management of Early Pregnancy Loss.
Atrio, J; Barnhart, KT; Creinin, MD; Ratcliffe, SJ; Schreiber, CA; Sonalkar, S, 2018
)
2.26
"Treatment with mifepristone was most commonly prompted by psychosis, uncontrolled glucose and/or hypertension."( Mifepristone in the treatment of the ectopic adrenocorticotropic hormone syndrome.
Auchus, RJ; Turcu, AF; Wannachalee, T, 2018
)
2.26
"Pretreatment with mifepristone decreased expulsion time."( Second-trimester postabortion care for ruptured membranes, fetal demise, and incomplete abortion.
Borgatta, L; Edelman, A; Mark, AG, 2015
)
0.74
"Pretreatment with mifepristone before induction of labor following late intrauterine fetal death is an effective and safe regimen. "( Induction of Labor Using Misoprostol With or Without Mifepristone in Intrauterine Death.
Agrawal, A; Basnet, P; Rai, R; Rizal, P; Thakur, A,
)
0.71
"Treatment with mifepristone had no significant impact on mRNA expression in these cells."( Ovarian steroid hormones modulate the expression of progesterone receptors and histone acetylation patterns in uterine leiomyoma cells.
Branchini, G; Brum, IS; Capp, E; Corleta, HVE; Pizzolato, LS; Sant'Anna, GDS, 2017
)
0.79
"Treatment with mifepristone did not affect cortisol levels, whereas an increase in serum testosterone was noted."( The effect of mifepristone on breast cell proliferation in premenopausal women evaluated through fine needle aspiration cytology.
Engman, M; Gemzell-Danielsson, K; Skoog, L; Söderqvist, G, 2008
)
1.05
"Pretreatment with mifepristone, both icv (80 microg/rat) and ip (10 mg/kg) injected, did not modify the response to icv and ip N/OFQ."( The hypothalamus-pituitary-adrenal axis does not influence the protective effects of nociceptin/orphanin FQ on the rat gastric mucosa.
Agostini, S; Broccardo, M; Grandi, D; Guerrini, R; Improta, G; Morini, G; Petrella, C; Scaccianoce, S; Solenghi, E, 2009
)
0.68
"Treatment with mifepristone was associated with significant improvement in HRQOL, which was explained in part by reduction in pain (28%, P<0.001) and bleeding (18%, P<0.001)."( Improved quality of life is partly explained by fewer symptoms after treatment of fibroids with mifepristone.
Feng, C; Fiscella, K; Meldrum, S, 2010
)
0.92
"Treatment with mifepristone decreased immobility and increased swimming (but not climbing) behavior in the FST, consistent with anti-depressant action."( Mifepristone decreases depression-like behavior and modulates neuroendocrine and central hypothalamic-pituitary-adrenocortical axis responsiveness to stress.
Herman, JP; Solomon, MB; Wulsin, AC, 2010
)
2.14
"Pretreatment with mifepristone resulted in more than twice the chance of complete uterine evacuation in 15 hours (79.8% compared with 36.9%, relative risk 2.16, 95% confidence interval 1.70-2.75). "( Mifepristone and misoprostol compared with misoprostol alone for second-trimester abortion: a randomized controlled trial.
Blum, J; Minh, NTH; Nga, NTB; Ngoc, NTN; Phan, VQ; Raghavan, S; Shochet, T; Winikoff, B, 2011
)
2.15
"Treatment with mifepristone reduced HDL-C, HDL particle concentration, and serum HDL cholesterol efflux in postmenopausal women. "( Impact of mifepristone, a glucocorticoid/progesterone antagonist, on HDL cholesterol, HDL particle concentration, and HDL function.
Amory, JK; Cox, CJ; Gross, C; Heinecke, JW; Ishida, B; Kane, J; Krauss, RM; Page, ST; Purnell, JQ; Schaefer, PM; Tang, C; Vaisar, T; Weinstein, RL, 2012
)
1.13
"Treatment with mifepristone significantly reduced serum progesterone levels in all women, when compared with the controls (13.2 nM vs."( Mifepristone-induced vaginal bleeding is associated with increased immunostaining for cyclooxygenase-2 and decrease in prostaglandin dehydrogenase in luteal phase endometrium.
Baird, DT; Critchley, HO; Hapangama, DK; Henderson, TA, 2002
)
2.1
"Treatment with mifepristone, a competitive antagonist of the progesterone receptor, resulted in a significant and rapid fall in concentrations of inhibin pro-alpha C, identifying a link between production of pro-alpha C and luteal steroidogenesis."( Changes in circulating concentrations of inhibins A and pro-alpha C during first trimester medical termination of pregnancy.
Anobile, CJ; Lahiri, S; Ledger, WL; Stewart, P, 2003
)
0.66
"Treatment with mifepristone increased progesterone receptor isoform B concentration in epithelial and stromal cells in the Fallopian tube and also increased progesterone receptor isoform B concentration in the glandular cells of the endometrium."( Progesterone receptor isoform B in the human fallopian tube and endometrium following mifepristone.
Christow, A; Gemzell-Danielsson, K; Marions, L; Sun, X, 2003
)
0.88
"Pretreatment with mifepristone represents a major improvement."( [Mifepristone for induction of second trimester abortion].
Backe, B; Heimstad, R, 2003
)
1.55
"Treatment with mifepristone significantly decreased eNOS expression in the endometrial glandular epithelium but did not affect endothelial eNOS."( Effects of mifepristone on expression of endothelial nitric oxide synthase in human endometrium during the implantation phase.
Gemzell-Danielsson, K; Qiu, X; Sun, X, 2003
)
1.05
"Pretreatment with mifepristone (20 microM) for two hours did not induce significant differences in short-term reactions."( Ciliary motility in bovine oviducts for sensing rapid non-genomic reactions upon exposure to progesterone.
Schuchter, U; Walt, H; Wessel, T, 2004
)
0.65
"Pretreatment with mifepristone, a glucocorticoid receptor antagonist, blocked the antiemetic effect of dexamethasone in the bilateral nuclei tractus solitarii."( Dexamethasone has a central antiemetic mechanism in decerebrated cats.
Chai, CY; Ho, CM; Ho, ST; Tsai, SK; Wang, JJ, 2004
)
0.65
"Pretreatment with mifepristone (5 mg /kg, i.p.), an antagonist of progesterone receptors, inhibited the effects of the low dose of progesterone, but did not show any antagonistic effect on the high dose-induced changes."( Effects of progesterone on apneic events during behaviorally defined sleep in male rats.
Haji, A; Ohi, Y; Takeda, R; Yamazaki, H, 2005
)
0.65
"Treatment with mifepristone increased the immunostaining on HER1 in the epithelium and the stroma of the endometrium, which was not seen in the fallopian tube."( Expression of heparin-binding epidermal growth factor-like growth factor and its receptors in the human fallopian tube and endometrium after treatment with mifepristone.
Gemzell-Danielsson, K; Li, HZ; Stâbi, B; Stavreus-Evers, A; Sun, XX, 2006
)
0.87
"Treatment with mifepristone has a limited effect on HB-EGF and its receptors in the fallopian tube, while the increase in HER1 and HER4 in the endometrium probably reflects defective endometrial maturation."( Expression of heparin-binding epidermal growth factor-like growth factor and its receptors in the human fallopian tube and endometrium after treatment with mifepristone.
Gemzell-Danielsson, K; Li, HZ; Stâbi, B; Stavreus-Evers, A; Sun, XX, 2006
)
0.88
"Pre-treatment with mifepristone is more effective at earlier gestational weeks."( Misoprostol-only versus mifepristone plus misoprostol in induction of labor following intrauterine fetal death.
Heikinheimo, O; Nuutila, M; Väyrynen, W, 2007
)
0.97
"Treatment with mifepristone retarded the follicular growth rate in all women (P = 0.01). "( Effect of daily low dose mifepristone on the ovarian cycle and on dynamics of follicle growth.
Baird, DT; Cameron, ST; Thong, KJ, 1995
)
0.95
"Pretreatment with mifepristone, but not progesterone, induced a significant increase in cervical dilatation."( Effects of mifepristone and progesterone on collagen synthesis in the human uterine cervix.
Bokström, H; Norström, A, 1995
)
1
"Pretreatment with mifepristone significantly prevented or reduced suppression of several macrophage functions following injury, including superoxide production and C albicans killing. "( Glucocorticoid receptor blockade reverses postinjury macrophage suppression.
Cech, AC; Daly, JM; Gallagher, H; Shou, J, 1994
)
0.62
"Pretreatment with mifepristone before an injury prevented suppression of several macrophage functions. "( Glucocorticoid receptor blockade reverses postinjury macrophage suppression.
Cech, AC; Daly, JM; Gallagher, H; Shou, J, 1994
)
0.62
"Treatment with mifepristone on day 19 produced a simultaneous rise in serum prolactin and a fall in serum progesterone and GH by 08.00 h on day 21."( Correlation of growth hormone secretion during pregnancy with circulating prolactin in rats.
Deis, RP; Jahn, GA; Rastrilla, AM, 1993
)
0.63
"Pretreatment with mifepristone reduces the demand for adenosine triphosphate production from phosphocreatine breakdown and downregulates Na(+)-K+ adenosine triphosphatase activity during sepsis."( Glucocorticoid receptor antagonism by mifepristone alters phosphocreatine breakdown during sepsis.
Jacobs, DO; Mitsuo, T; Prechek, D; Rounds, J; Wilmore, DW, 1996
)
0.9
"Treatment with mifepristone inhibited ovulation in four of the six subjects."( Effects of daily low dose mifepristone on endometrial maturation and proliferation.
Baird, DT; Buckley, CH; Cameron, ST; Critchley, HO; Thong, KJ; Williams, AR, 1996
)
0.93
"Treatment with mifepristone in the early luteal phase did not disrupt the cycle length but women reported slight vaginal bleeding in 15% of the cycles."( Feasibility of administering mifepristone as a once a month contraceptive pill.
Baird, DT; Brown, A; Glasier, AF; Hapangama, DK, 2001
)
0.94
"Treatment with mifepristone increased the progesterone receptor concentration in epithelial and stromal cells and increased the estrogen receptor concentration in epithelial cells."( Effect of mifepristone and levonorgestrel on expression of steroid receptors in the human Fallopian tube.
Christow, A; Gemzell-Danielsson, K; Sun, X, 2002
)
1.06
"Treatment with mifepristone and levonorgestrel before ovulation inhibited the luteinizing hormone surge showing no significant differences between the means of luteinizing hormone measurements. "( Emergency contraception with mifepristone and levonorgestrel: mechanism of action.
Gemzell Danielsson, K; Hultenby, K; Lindell, I; Marions, L; Ståbi, B; Sun, X, 2002
)
0.96
"Treatment with mifepristone for 4 days (10 mg/kg orally twice daily) significantly (P less than 0.05) stimulated corticosterone secretion in lean but not in obese rats."( The glucocorticoid antagonist mifepristone reveals abnormal regulation of the adrenocortical system in obese Zucker rats.
Heikinheimo, O; Huupponen, R; Koulu, M; Pesonen, U, 1992
)
0.91
"Pretreatment with mifepristone 36 hours prior to termination of pregnancy resulted in an increased production of PGF2 alpha in tissue culture (p less than 0.01)."( Effects of mifepristone in vivo on decidual prostaglandin synthesis and metabolism.
Baird, DT; Glasier, AF; Kelly, RW; McNeilly, AS; Norman, JE; Wu, WX, 1991
)
0.99
"Pretreatment with mifepristone 36 hours prior to termination of pregnancy resulted in an increased production of PGF2alpha in tissue culture (p0.01)."( Effects of mifepristone in vivo on decidual prostaglandin synthesis and metabolism.
Baird, DT; Glasier, AF; Kelly, RW; McNeilly, AS; Norman, JE; Wu, WX, 1991
)
0.99
"Pretreatment with mifepristone significantly reduced the amount of force required to dilate the cervix to 10 mm. "( Pretreatment of the primigravid uterine cervix with mifepristone 30 h prior to termination of pregnancy: a double blind study.
Cohn, M; Stewart, P, 1991
)
0.87
"Pretreatment with mifepristone significantly reduced the amount of force required to dilate the cervix to 10 mm."( Pretreatment of the primigravid uterine cervix with mifepristone 30 h prior to termination of pregnancy: a double blind study.
Cohn, M; Stewart, P, 1991
)
0.85

Toxicity

Women on Web uses telemedicine to help women access mifepristone and misoprostol in countries with no safe care for termination of pregnancy (TOP)

ExcerptReferenceRelevance
" Mifepristone is a safe alternative for the termination of pregnancy when the beta human chorionic gonadotropin is below 20,000 IU/L."( Abortion: epidemiology, safety, and technique.
Blumenthal, PD, 1992
)
1
" In all sites, both medical failures (an adverse effect resulting in a medically indicated surgical intervention) and acceptability failures (failure to complete the entire regimen) contributed substantially to the gross failure rates for medical abortion."( Safety, efficacy, and acceptability of medical abortion in China, Cuba, and India: a comparative trial of mifepristone-misoprostol versus surgical abortion.
Cabezas, E; Coyaji, KJ; Du, MK; Ellertson, C; Eschen, A; Gu, S; Krishna, UR; Sivin, I; Winikoff, B; Xiao, B, 1997
)
0.51
"Although serious adverse events of early abortion have been studied, little attention has been paid to the more common side effects experienced by early medical or surgical abortion clients."( Side effects of mifepristone-misoprostol abortion versus surgical abortion. Data from a trial in China, Cuba, and India.
Coyaji, K; Ellertson, C; Elul, B; Winikoff, B, 1999
)
0.65
" Some of these concerns include potentially increased risks of cardiovascular events (including arterial and venous disease), worries about possible effects on future fertility, feared teratogenic consequences following method failure or inadvertent use during pregnancy, exaggerated or extreme fears of adverse tolerability, and concerns about drug interactions with other medications."( How safe is emergency contraception?
Ellertson, C; Norris Turner, A, 2002
)
0.31
"At a July 19 hearing, the Food and Drug Administration's Advisory Committee for Reproductive Health Drugs found mifepristone to be safe and effective in inducing abortions early in pregnancy and recommended that the drug be approved for marketing in the US."( FDA panel finds mifepristone safe and effective.
, 1996
)
0.85
" However, attention should be paid in clinical practice to the rare, but severe adverse events caused by this treatment."( [Side effect of mifepristone in combination with misoprostol for medical abortion].
Jiang, S; Lei, ZW; Li, Q; Li, YP; Lü, L; Zou, Y, 2004
)
0.67
" Given that cigarette smoking is highly prevalent in some of these patient groups and nicotine has been shown to reduce toxic consequences of NMDA receptor function, it may be suggested that nicotine intake may attenuate the neurotoxic effects of hypercortisolemia."( (-)-nicotine ameliorates corticosterone's potentiation of N-methyl-d-aspartate receptor-mediated cornu ammonis 1 toxicity.
Harris, BR; Littleton, JM; Mulholland, PJ; Prendergast, MA; Self, RL, 2004
)
0.32
"Medical abortion with the option of home administration of misoprostol is safe and feasible for introduction into the Vietnamese healthcare system."( Is home-based administration of prostaglandin safe and feasible for medical abortion? Results from a multisite study in Vietnam.
Blum, J; Durocher, JM; Mai, TT; Ngoc, NT; Nhan, VQ; Winikoff, B, 2004
)
0.32
" Use of drug is safe and non-invasive and training is simple and complications are minimal."( Making unsafe abortion safe: medical method.
Pradhan, P, 2004
)
0.32
"The systematic analysis of morbidity and mortality for the Food and Drug Administration (FDA)-approved medical abortion regimen using mifepristone is possible using data from the FDA's Adverse Event Reporting System."( Analysis of severe adverse events related to the use of mifepristone as an abortifacient.
Gary, MM; Harrison, DJ, 2006
)
0.78
"To assess mifepristone's mortality, morbidity, sentinel events, and quality of postmarketing surveillance using mifepristone adverse event reports (AERs)."( Analysis of severe adverse events related to the use of mifepristone as an abortifacient.
Gary, MM; Harrison, DJ, 2006
)
0.98
"Six hundred seven unique mifepristone AERs submitted to the FDA over a 4 year span were coded using the National Cancer Institute's Common Terminology Criteria for Adverse Events."( Analysis of severe adverse events related to the use of mifepristone as an abortifacient.
Gary, MM; Harrison, DJ, 2006
)
0.88
"To increase access to safe abortion in rural India, the feasibility and acceptability of mifepristone-misoprostol abortion was assessed in a typical government run primary health center (PHC) in Nagpur district, Maharashtra State, that does not offer surgical abortion services and must refer off-site for emergency and backup services."( Increasing access to safe abortion services in rural India: experiences with medical abortion in a primary health center.
Anand, A; Elul, B; Kalyanwala, S; Mundle, S; Ughade, S, 2007
)
0.56
" This study suggests that introduction of medical abortion at lower levels of the health-care system could increase access to safe abortion in rural India."( Increasing access to safe abortion services in rural India: experiences with medical abortion in a primary health center.
Anand, A; Elul, B; Kalyanwala, S; Mundle, S; Ughade, S, 2007
)
0.34
"Women on Web is a service that uses telemedicine to help women access mifepristone and misoprostol in countries with no safe care for termination of pregnancy (TOP)."( Using telemedicine for termination of pregnancy with mifepristone and misoprostol in settings where there is no access to safe services.
Davies, S; Gemzell-Danielsson, K; Gomperts, RJ; Jelinska, K; Kleiverda, G, 2008
)
0.83
" The 2 groups reported similar adverse effects."( Feasibility, efficacy, safety, and acceptability of mifepristone-misoprostol for medical abortion in the Democratic People's Republic of Korea.
Choe, YS; Jang, MC; Kim, OS; Ko, WS; Pyo, HS; Tran, NT, 2010
)
0.61
"The high efficacy and acceptability of medical abortion among rural and urban women suggest that medical abortion is a safe alternative to surgical abortion and can be scaled up to other reproductive health clinics in both rural and urban areas of the Democratic People's Republic of Korea, provided that there is appropriate training and supervision."( Feasibility, efficacy, safety, and acceptability of mifepristone-misoprostol for medical abortion in the Democratic People's Republic of Korea.
Choe, YS; Jang, MC; Kim, OS; Ko, WS; Pyo, HS; Tran, NT, 2010
)
0.61
" We assessed whether early fi rst-trimester medical abortion provided by midlevel providers (government-trained, certified nurses and auxiliary nurse midwives) was as safe and effective as that provided by doctors in Nepal."( Can midlevel health-care providers administer early medical abortion as safely and effectively as doctors? A randomised controlled equivalence trial in Nepal.
Baird, DT; Huong, NT; Meirik, O; Shah, I; Tamang, A; Thapa, K; Wang, D; Warriner, IK, 2011
)
0.37
"To determine the risks of short term adverse events in adolescent and older women undergoing medical abortion."( Comparison of rates of adverse events in adolescent and adult women undergoing medical abortion: population register based study.
Gissler, M; Heikinheimo, O; Hemminki, E; Mentula, M; Niinimäki, M; Suhonen, S, 2011
)
0.37
"Incidence of adverse events (haemorrhage, infection, incomplete abortion, surgical evacuation, psychiatric morbidity, injury, thromboembolic disease, and death) among adolescent (<18 years) and older (≥ 18 years) women through record linkage of Finnish registries and genital Chlamydia trachomatis infections detected concomitantly with abortion and linked with data from the abortion register for 2004-6."( Comparison of rates of adverse events in adolescent and adult women undergoing medical abortion: population register based study.
Gissler, M; Heikinheimo, O; Hemminki, E; Mentula, M; Niinimäki, M; Suhonen, S, 2011
)
0.37
" The incidence of adverse events among adolescents was similar or lower than that among the adults."( Comparison of rates of adverse events in adolescent and adult women undergoing medical abortion: population register based study.
Gissler, M; Heikinheimo, O; Hemminki, E; Mentula, M; Niinimäki, M; Suhonen, S, 2011
)
0.37
"The incidence of adverse events after medical abortion was similar or lower among adolescents than among older women."( Comparison of rates of adverse events in adolescent and adult women undergoing medical abortion: population register based study.
Gissler, M; Heikinheimo, O; Hemminki, E; Mentula, M; Niinimäki, M; Suhonen, S, 2011
)
0.37
"Home-based abortion is safe under the conditions in place in the included studies."( Comparative effectiveness, safety and acceptability of medical abortion at home and in a clinic: a systematic review.
Free, C; Ngo, TD; Park, MH; Shakur, H, 2011
)
0.37
" The requirement of full antagonist activity for substantial side effect dissociation was demonstrated in primary human preadipocytes, hepatocytes, and osteoblasts in which effects on adipogenesis, key genes involved in gluconeogenesis, and genes important for bone formation were examined, respectively."( The antagonists but not partial agonists of glucocorticoid receptor ligands show substantial side effect dissociation.
Braden, T; Dietz, JD; Du, S; Hegde, SG; Hu, X; Hummert, S; Lee, J; Long, KR; Obukowicz, MG; Rouw, S; Tunca, C; Webb, EG; Webber, RK, 2011
)
0.37
" The association could indicate that the duration or degree of exposure to toxic proteins is important for pathology, or that age itself increases susceptibility to protein toxicity."( Ageing increases vulnerability to aβ42 toxicity in Drosophila.
Hardy, J; Kerr, F; Lovestone, S; Martinez, P; Partridge, L; Rogers, I, 2012
)
0.38
"Buccal misoprostol 800 mcg and sublingual misoprostol 800 mcg show high efficacy when used with 200 mg mifepristone for early pregnancy termination but have different side effect profiles."( A randomized clinical trial comparing the short-term side effects of sublingual and buccal routes of misoprostol administration for medical abortions up to 63 days' gestation.
Chai, J; Ho, PC; Wong, CY, 2013
)
0.6
"The provision of safe abortion services to women who need them has the potential to drastically reduce or eliminate maternal deaths due to unsafe abortion."( A review of evidence for safe abortion care.
Brahmi, D; Jackson, E; Kapp, N; Tang, J; Whyte, P, 2013
)
0.39
"Systematic reviews pertaining to the evidence for safe abortion services, from pre-abortion care, medical and surgical methods of abortion and post-abortion care were evaluated for relevant outcomes, primarily those relating to safety, effectiveness and women's preference."( A review of evidence for safe abortion care.
Brahmi, D; Jackson, E; Kapp, N; Tang, J; Whyte, P, 2013
)
0.39
"Evidence-based guidelines assist health care providers and policymakers to utilize the best data available to provide safe abortion care and prevent the millions of deaths and disabilities that result from unsafe abortion."( A review of evidence for safe abortion care.
Brahmi, D; Jackson, E; Kapp, N; Tang, J; Whyte, P, 2013
)
0.39
"To analyze rates of significant adverse events and outcomes in women having a medical abortion at Planned Parenthood health centers in 2009 and 2010 and to identify changes in the rates of adverse events and outcomes between the 2 years."( Significant adverse events and outcomes after medical abortion.
Cleland, K; Creinin, MD; Nshom, M; Nucatola, D; Trussell, J, 2013
)
0.39
" We evaluated the incidence of six clinically significant adverse events (hospital admission, blood transfusion, emergency department treatment, intravenous antibiotics administration, infection, and death) and two significant outcomes (ongoing pregnancy and ectopic pregnancy diagnosed after medical abortion treatment was initiated)."( Significant adverse events and outcomes after medical abortion.
Cleland, K; Creinin, MD; Nshom, M; Nucatola, D; Trussell, J, 2013
)
0.39
"Among 233,805 medical abortions provided in 2009 and 2010, significant adverse events or outcomes were reported in 1,530 cases (0."( Significant adverse events and outcomes after medical abortion.
Cleland, K; Creinin, MD; Nshom, M; Nucatola, D; Trussell, J, 2013
)
0.39
"To present evidence of MA's contributions to reduced complications, describe strategies to enhance safe MA, and highlight existing barriers to access in LAC, while examining MA's role in newly legal abortion services."( Medical abortion: a path to safe, high-quality abortion care in Latin America and the Caribbean.
Dzuba, IG; Peña, M; Winikoff, B, 2013
)
0.39
" Lower doses of mifepristone combined with 200 µg of misoprostol are as effective and safe as higher doses of this combination for the termination of ultra-early pregnancy with lower possibility of vaginal bleeding and side effects."( Effectiveness and Safety of Lower Doses of Mifepristone Combined With Misoprostol for the Termination of Ultra-Early Pregnancy: A Dose-Ranging Randomized Controlled Trial.
Chen, DJ; Chen, WL; Li, CL; Liu, MX; Song, LP; Wang, Y; Zhang, ZF, 2015
)
1.03
" Cases were identified for this descriptive study from our electronic practice management (EPM) database, and our electronic database on adverse events was queried for information on efficacy and safety."( Efficacy and safety of medical abortion using mifepristone and buccal misoprostol through 63 days.
Cleland, K; Gatter, M; Nucatola, DL, 2015
)
0.68
"An evidence-based regimen of 200 mg of mifepristone orally followed by home use of 800 mcg of buccal misoprostol 24-48 h later is safe and effective through 63 days estimated gestational age."( Efficacy and safety of medical abortion using mifepristone and buccal misoprostol through 63 days.
Cleland, K; Gatter, M; Nucatola, DL, 2015
)
0.94
" The study illustrates positive steps forward being taken in making abortion safe and preventing and reducing unsafe abortion practices in Cambodia."( Towards safe abortion access: an exploratory study of medical abortion in Cambodia.
Cockroft, M; Delvaux, T; Ith, L; Petitet, PH, 2015
)
0.42
"Data show that an outpatient regimen of 200-mg mifepristone followed by a single dose of misoprostol is safe and effective for medical abortion for up to 70 days from last menstrual period (LMP)."( Outpatient medical abortion is safe and effective through 70 days gestation.
Abbas, D; Chong, E; Raymond, EG, 2015
)
0.67
" The outcome measures were the success abortion rate, induction to abortion interval, the amount of bleeding, reoccurrence of menstruation and adverse events."( [Efficacy and safety of mifepristone combined with misoprostol for termination of pregnancy between 8 and 16 weeks of gestation].
Chang, Q; Di, W; Dong, B; Huang, Z; Jing, X; Li, Y; Qian, J; Ren, M; Shen, H; Shi, H; Song, W; Wu, S; Yao, C; Zheng, S, 2015
)
0.72
" Two cases of incomplete abortion were serious adverse events (SAE) relating to treatment."( [Efficacy and safety of mifepristone combined with misoprostol for termination of pregnancy between 8 and 16 weeks of gestation].
Chang, Q; Di, W; Dong, B; Huang, Z; Jing, X; Li, Y; Qian, J; Ren, M; Shen, H; Shi, H; Song, W; Wu, S; Yao, C; Zheng, S, 2015
)
0.72
"Oral or vaginal misoprostol combined with mifepristone, is effective and safe for termination of pregnancy between 8 and 16 weeks of gestation."( [Efficacy and safety of mifepristone combined with misoprostol for termination of pregnancy between 8 and 16 weeks of gestation].
Chang, Q; Di, W; Dong, B; Huang, Z; Jing, X; Li, Y; Qian, J; Ren, M; Shen, H; Shi, H; Song, W; Wu, S; Yao, C; Zheng, S, 2015
)
0.99
" Interestingly, the acute toxic death could not be reached at the maximum administrable dose (5 g/kg)."( Aspirin, lysine, mifepristone and doxycycline combined can effectively and safely prevent and treat cancer metastasis: prevent seeds from gemmating on soil.
Dong, H; Gao, Y; Jia, L; Li, T; Lu, Y; Ma, J; Shao, J; Tu, X; Wan, L; Wang, J; Xie, F; Xie, J; Xu, B; Xu, H; Zhang, T; Zhu, Y, 2015
)
0.76
"Abortion services were legalized in India in 1972, however, the access to safe abortion services is restricted, especially in rural areas."( Improving access to safe abortion in a rural primary care setting in India: experience of a service delivery intervention.
Iyengar, K; Iyengar, SD, 2016
)
0.43
"The results of our intervention indicate that integrating medical abortion into primary care settings is feasible and has a potential to improve access to safe abortion services in rural areas."( Improving access to safe abortion in a rural primary care setting in India: experience of a service delivery intervention.
Iyengar, K; Iyengar, SD, 2016
)
0.43
" Mifepristone and misoprostol is safe and effective method for the second-trimester pregnancy termination."( Mifepristone and misoprostol is safe and effective method in the second-trimester pregnancy termination.
Immonen, E; Nissi, R; Santala, M; Talvensaari-Mattila, A, 2016
)
2.79
" Secondary end points were rates of unscheduled reattendance, time required for and cost of hospital observation and follow-up, vaginal bleeding, adverse effects, menstrual disturbance in the posttreatment period, and satisfaction rating."( Efficacy, Safety, and Acceptability of Low-Dose Mifepristone and Self-Administered Misoprostol for Ultra-Early Medical Abortion: A Randomized Controlled Trial.
He, H; Li, CL; Liao, YM; Mo, XT; Song, LP; Tang, SY; Zhou, LJGY, 2017
)
0.71
" There were 674 serious adverse events (5."( Efficacy and safety of mifepristone-buccal misoprostol for early medical abortion in an Australian clinical setting.
Goldstone, P; Hawtin, K; Walker, C, 2017
)
0.77
"Mifepristone-buccal misoprostol is an effective and safe alternative to surgical termination of pregnancy up to 63 days gestation."( Efficacy and safety of mifepristone-buccal misoprostol for early medical abortion in an Australian clinical setting.
Goldstone, P; Hawtin, K; Walker, C, 2017
)
2.21
"Despite a liberal abortion law, access to safe abortion services in South Africa is challenging for many women."( The costs and cost effectiveness of providing first-trimester, medical and surgical safe abortion services in KwaZulu-Natal Province, South Africa.
Blanchard, K; Devjee, J; Fetters, T; Lince-Deroche, N; Moodley, J; Sinanovic, E, 2017
)
0.46
"This was an implementation study at four referral facilities and 28 Felsher Obstetric Points in two districts to train their midwives and family nurses to deliver safe and effective abortion care with co-packaged mifepristone-misoprostol and provide contraceptives postabortion."( Provision of medical abortion by midlevel healthcare providers in Kyrgyzstan: testing an intervention to expand safe abortion services to underserved rural and periurban areas.
Boobekova, A; Davletova, A; Johnson, BR; Kazakbaeva, C; Kondrateva, Y; Landoulsi, S; Lazdane, G; Maksutova, E; Monolbaev, K; Seuc Jo, AH, 2018
)
0.67
" This locally generated evidence can be used by the Kyrgyz Ministry of Health to reduce unintended pregnancy and expand safe abortion care to women in underserved periurban and rural settings."( Provision of medical abortion by midlevel healthcare providers in Kyrgyzstan: testing an intervention to expand safe abortion services to underserved rural and periurban areas.
Boobekova, A; Davletova, A; Johnson, BR; Kazakbaeva, C; Kondrateva, Y; Landoulsi, S; Lazdane, G; Maksutova, E; Monolbaev, K; Seuc Jo, AH, 2018
)
0.48
"Expanding access to medication abortion through pharmacies is a promising avenue to reach women with safe and convenient care, yet no pharmacy provision interventions have been evaluated."( Effectiveness and safety of early medication abortion provided in pharmacies by auxiliary nurse-midwives: A non-inferiority study in Nepal.
Blum, M; Darney, PD; Grossman, D; Harper, CC; Maharjan, D; Puri, M; Regmi, K; Rocca, CH; Shrestha, P, 2018
)
0.48
" No serious adverse events occurred."( Effectiveness and safety of early medication abortion provided in pharmacies by auxiliary nurse-midwives: A non-inferiority study in Nepal.
Blum, M; Darney, PD; Grossman, D; Harper, CC; Maharjan, D; Puri, M; Regmi, K; Rocca, CH; Shrestha, P, 2018
)
0.48
"Early mifepristone-misoprostol abortion was as effective and safe when provided by trained auxiliary nurse-midwives at pharmacies as at government-certified health facilities."( Effectiveness and safety of early medication abortion provided in pharmacies by auxiliary nurse-midwives: A non-inferiority study in Nepal.
Blum, M; Darney, PD; Grossman, D; Harper, CC; Maharjan, D; Puri, M; Regmi, K; Rocca, CH; Shrestha, P, 2018
)
0.96
" We aimed to estimate the costs and cost effectiveness of providing three safe second-trimester abortion services (dilation and evacuation (D&E)), medical induction with mifepristone and misoprostol (MI-combined), or medical induction with misoprostol alone (MI-misoprostol)) in Western Cape Province, South Africa to aid policymakers with planning for service provision in South Africa and similar settings."( The costs and cost effectiveness of providing second-trimester medical and surgical safe abortion services in Western Cape Province, South Africa.
Blanchard, K; Constant, D; Grossman, D; Harries, J; Kluge, J; Lince-Deroche, N; Sinanovic, E, 2018
)
0.68
" Abdominal cramping was the most common side effect (95."( Safety, Efficacy and Acceptability of Early First Trimester Abortion using Oral Mifepristone and Sublingual Misoprostol.
Aryal, S; Sharma, B; Shrestha, D, 2018
)
0.71
"The results of the study suggest that oral administration of 200 mg mifepristone in term patients is an effective method of labor induction; and is more convenient and equally safe as compared to intravaginal instillation of dinoprostone."( Safety and efficacy of mifepristone versus dinoprostone gel in induction of labor: A randomized controlled trial.
Dhiman, B; Jamwal, A; Jindal, N; Kandoria, M; Rao, R, 2019
)
1.06
"After years of the worsening burden of unsafe abortion and attendant morbidities and mortalities in Nigeria, a National Guideline on the Safe termination of pregnancy for legal indications was enunciated."( The Benefits of a Guideline on Safe Termination of Pregnancy for Legal Indications: An Illustrative Case Report of a Hydranencephaly.
Abdullahi, ZG; Bello, N; Igashi, JB; Koledade, AK; Maikudi, HA; Mohammed, U; Shittu, OS, 2019
)
0.51
"At the conference "Developing an Advocacy Agenda for Abortion in the 21st Century and Making Change Happen" held on 5-7 September 2018, Lisbon, Portugal, organized by the International Campaign for Women's Right to Safe Abortion, it was argued that abortion services not only need to be treated as a bona fide form of health care but also completely reconceptualized, particularly because of the influence of medical abortion pills."( Reconceptualizing safe abortion and abortion services in the age of abortion pills: A discussion paper.
Berer, M, 2020
)
0.56
"Primary: Analyze the Adverse Events (AEs) reported to the Food and Drug Administration (FDA) after use of mifepristone as an abortifacient."( Deaths and Severe Adverse Events after the use of Mifepristone as an Abortifacient from September 2000 to February 2019.
Aultman, K; Beran, BD; Cirucci, CA; Harrison, DJ; Lockwood, MD; Seiler, S, 2021
)
1.09
"Adverse Event Reports (AERs) for mifepristone used as an abortifacient, submitted to the FDA from September 2000 to February 2019, were analyzed using the National Cancer Institute's Common Terminology Criteria for Adverse Events (CTCAEv3)."( Deaths and Severe Adverse Events after the use of Mifepristone as an Abortifacient from September 2000 to February 2019.
Aultman, K; Beran, BD; Cirucci, CA; Harrison, DJ; Lockwood, MD; Seiler, S, 2021
)
1.16
" The FDA AER system is inadequate and significantly underestimates the adverse events from mifepristone."( Deaths and Severe Adverse Events after the use of Mifepristone as an Abortifacient from September 2000 to February 2019.
Aultman, K; Beran, BD; Cirucci, CA; Harrison, DJ; Lockwood, MD; Seiler, S, 2021
)
1.1
"For this prospective, observational cohort study, we recruited callers from two safe abortion accompaniment groups in Argentina and Nigeria who requested information on self-managed medication abortion."( Effectiveness of self-managed medication abortion with accompaniment support in Argentina and Nigeria (SAFE): a prospective, observational cohort study and non-inferiority analysis with historical controls.
Bercu, C; Carbone, S; Egwuatu, I; Gerdts, C; Grosso, B; Jayaweera, R; Kristianingrum, IA; Moseson, H; Motana, R; Nmezi, S; Zurbriggen, R, 2022
)
0.72
" There were no material changes between the period before mifepristone was available and the nonrestricted period in the incidence of severe adverse events (0."( Abortion Safety and Use with Normally Prescribed Mifepristone in Canada.
Darling, EK; Dunn, S; Gayowsky, A; Kaczorowski, J; Laba, TL; Law, MR; McGrail, K; Norman, WV; Schummers, L, 2022
)
1.22
"After mifepristone became available as a normal prescription, the abortion rate remained relatively stable, the proportion of abortions provided by medication increased rapidly, and adverse events and complications remained stable, as compared with the period when mifepristone was unavailable."( Abortion Safety and Use with Normally Prescribed Mifepristone in Canada.
Darling, EK; Dunn, S; Gayowsky, A; Kaczorowski, J; Laba, TL; Law, MR; McGrail, K; Norman, WV; Schummers, L, 2022
)
1.46
"Effectiveness, defined as complete abortion after 200 μg of mifepristone and up to 1600 μg of misoprostol without additional intervention, and major abortion-related adverse events, defined as hospital admission, major surgery, or blood transfusion."( Outcomes and Safety of History-Based Screening for Medication Abortion: A Retrospective Multicenter Cohort Study.
Boraas, CM; Coplon, L; Gold, M; Kaneshiro, B; Koenig, LR; Raymond, EG; Upadhyay, UD; Winikoff, B, 2022
)
0.96
"90%) were followed by major abortion-related adverse events, and 4 patients (0."( Outcomes and Safety of History-Based Screening for Medication Abortion: A Retrospective Multicenter Cohort Study.
Boraas, CM; Coplon, L; Gold, M; Kaneshiro, B; Koenig, LR; Raymond, EG; Upadhyay, UD; Winikoff, B, 2022
)
0.72
"In this cohort study, screening for medication abortion eligibility by history alone was effective and safe with either in-person dispensing or mailing of medications, resulting in outcomes similar to published rates of models involving ultrasonography or pelvic examination."( Outcomes and Safety of History-Based Screening for Medication Abortion: A Retrospective Multicenter Cohort Study.
Boraas, CM; Coplon, L; Gold, M; Kaneshiro, B; Koenig, LR; Raymond, EG; Upadhyay, UD; Winikoff, B, 2022
)
0.72
"Mifepristone and misoprostol are extremely safe medications with many applications."( Mifepristone: A Safe Method of Medical Abortion and Self-Managed Medical Abortion in the Post-Roe Era.
Katz, A; Schmidt, EO; Stein, RA,
)
3.02
" Each of these medications has a unique adverse effect and toxicity profile."( Toxicity of abortifacients: A review for physicians in the post roe era.
Mazer-Amirshahi, M; Ye, P, 2022
)
0.72
"Agents used for medication abortion have unique contraindications and adverse effects."( Toxicity of abortifacients: A review for physicians in the post roe era.
Mazer-Amirshahi, M; Ye, P, 2022
)
0.72
" No adverse events related to EA occurred during hospitalization, only 3 patients showed mild lumbago and back pain after follow-up to three months postpartum, which was significantly relieved after proper rest."( Evaluation efficacy and safety of epidural analgesia in second-trimester induced labor: A single-center, prospective, non-randomized, controlled study.
Chen, KM; He, WR; Jiang, T; Liu, ZR; Wang, L; Wang, XW; Wei, H; Yi, C; Zeng, Y; Zhang, XF; Zheng, YH, 2022
)
0.72
"EA can significantly reduce the pain of parturients, which may be effective and safe in the second-trimester induced labor."( Evaluation efficacy and safety of epidural analgesia in second-trimester induced labor: A single-center, prospective, non-randomized, controlled study.
Chen, KM; He, WR; Jiang, T; Liu, ZR; Wang, L; Wang, XW; Wei, H; Yi, C; Zeng, Y; Zhang, XF; Zheng, YH, 2022
)
0.72
" This review will rather focus specifically on adverse events associated with these drugs (ketoconazole, levoketoconazole, metyrapone, osilodrostat, pasireotide, cabergoline and mifepristone), and the way in which to monitor and treat them, based on retrospective studies and the most recently published prospective studies."( How best to monitor the specific side effects of medical treatments of Cushing's disease.
Castinetti, F, 2022
)
0.91
"Judging from our case, long-term, ultra-low-dose mifepristone for uterine fibroids treatment was safe and more effective than conventional therapy."( Long-term use of ultra-low-dose mifepristone for uterine leiomyoma control and safety discussion: A case report.
Li, Q; Zhou, G, 2022
)
1.26
" Meanwhile, GZFL combined with low-dose MFP did not significantly increase the incidence of adverse drug reactions compared with low-dose MFP alone (p = 0."( The efficacy and safety of Chinese herbal medicine Guizhi Fuling capsule combined with low dose mifepristone in the treatment of uterine fibroids: a systematic review and meta-analysis of 28 randomized controlled trials.
Bai, Y; Dong, T; Gao, F; Lei, Y; Li, M; Ou, L; Wei, P; Yang, H; Yang, L, 2023
)
1.13
"This study suggests that GZFL combined with low-dose MFP is more effective and safe in the treatment of UFs, and it is a potential treatment for UFs."( The efficacy and safety of Chinese herbal medicine Guizhi Fuling capsule combined with low dose mifepristone in the treatment of uterine fibroids: a systematic review and meta-analysis of 28 randomized controlled trials.
Bai, Y; Dong, T; Gao, F; Lei, Y; Li, M; Ou, L; Wei, P; Yang, H; Yang, L, 2023
)
1.13
"Although some studies in this updated review were adjudicated to have a high risk of bias, the results continue to support the key conclusion of our 2019 analysis: misoprostol-only is effective and safe for the termination of first-trimester intrauterine pregnancy."( Effectiveness and safety of misoprostol-only for first-trimester medication abortion: An updated systematic review and meta-analysis.
Raymond, EG; Shochet, T; Weaver, MA, 2023
)
0.91
"Misoprostol-only is a safe and effective option for medication abortion in the first trimester if mifepristone is unavailable or inaccessible."( Effectiveness and safety of misoprostol-only for first-trimester medication abortion: An updated systematic review and meta-analysis.
Raymond, EG; Shochet, T; Weaver, MA, 2023
)
1.13
" After literature screening, data extraction and quality evaluation, effective rate, recurrence rate, pregnancy rate and adverse reaction rate were used as outcome indicators to evaluate the efficacy and safety of drugs."( Efficacy and safety of different subsequent therapies after fertility preserving surgery for endometriosis: A systematic review and network meta-analysis.
Ma, R; Mao, H; Wang, L; Xu, H; Zhang, L; Zhao, R; Zheng, Y, 2023
)
0.91
" Adverse reaction rate: the application of dienogest, leuprolide, danazol, gestrinone, mifepristone and LNG-IUS after EMT fertility preservation surgery was higher than that of placebo."( Efficacy and safety of different subsequent therapies after fertility preserving surgery for endometriosis: A systematic review and network meta-analysis.
Ma, R; Mao, H; Wang, L; Xu, H; Zhang, L; Zhao, R; Zheng, Y, 2023
)
1.13
"For this prospective observational cohort study of callers to safe abortion hotlines and accompaniment groups in Argentina, Nigeria, and Southeast Asia, participants were recruited between July 31, 2019, and October 1, 2020, prior to starting their medication abortion."( Medication Abortion Safety and Effectiveness With Misoprostol Alone.
Bercu, C; Egwuatu, I; Gerdts, C; Grosso, B; Jayaweera, R; Kristianingrum, IA; Moseson, H; Nmezi, S; Zurbriggen, R, 2023
)
0.91
" Secondary outcomes included method safety, measured by self-report of experiencing warning signs (eg, heavy bleeding, pain, fever, discharge) indicative of a potential complication and by medical treatment (eg, blood transfusion, intravenous fluids, overnight hospital stay) indicative of a potential adverse event."( Medication Abortion Safety and Effectiveness With Misoprostol Alone.
Bercu, C; Egwuatu, I; Gerdts, C; Grosso, B; Jayaweera, R; Kristianingrum, IA; Moseson, H; Nmezi, S; Zurbriggen, R, 2023
)
0.91
" Potential adverse events were reported by 6 participants (0."( Medication Abortion Safety and Effectiveness With Misoprostol Alone.
Bercu, C; Egwuatu, I; Gerdts, C; Grosso, B; Jayaweera, R; Kristianingrum, IA; Moseson, H; Nmezi, S; Zurbriggen, R, 2023
)
0.91

Pharmacokinetics

The pharmacokinetics of mifepristone are characterised by rapid absorption, a long half-life of 25 to 30 hours and micromolar serum concentrations following ingestion of doses currently in clinical use. This validated HPLC method was successfully applied to pharmacokinetic study of m ifepriston in human plasma samples collected from volunteers.

ExcerptReferenceRelevance
" The plasma concentrations fitted the equation for a two-compartment open model from which the pharmacokinetic parameters were calculated."( Pharmacokinetic study of orally administered RU 486 in non-pregnant women.
Fotherby, K; He, CH; Jiang, NX; Shi, YE; Van Look, PF; Ye, ZH; Zhang, GG, 1989
)
0.28
"The pharmacokinetic characteristics of RU486 and its acute effects on anterior pituitary hormone secretion after oral administration were examined in six normal women."( Pharmacodynamics of the antiprogesterone RU486 in women after oral administration.
Garzo, VG; Liu, JH; Yen, SS, 1988
)
0.27
" The pharmacokinetic behaviour of RU 486 during the treatment period was similar between the study subjects, whereas the elimination phase pharmacokinetics showed wide individual variation."( Pharmacokinetics of the antiprogesterone RU 486 in women during multiple dose administration.
Heikinheimo, O, 1989
)
0.28
" The authors studied the pharmacokinetic properties of this drug in normal volunteers and patients with Cushing's syndrome using a rat progesterone radioreceptor assay."( Pharmacokinetic properties of the antiglucocorticoid and antiprogesterone steroid RU 486 in man.
Brandon, DD; Chrousos, GP; Kawai, S; Loriaux, DL; Nieman, LK; Udelsman, R, 1987
)
0.27
" The pharmacokinetic parameters were calculated by MEDUSA computer programme."( [Pharmacokinetics of RU 486 and its active metabolites in humans].
Falkay, G; Földesi, I; Kovács, L, 1994
)
0.29
" 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
"A human progesterone receptor assay has been developed for the measurement of the biologically active molecular fraction of RU486 (RU486 binding equivalent) for studying its pharmacokinetic properties."( Determination of RU486 (mifepristone) in blood by radioreceptorassay; a pharmacokinetic study.
Falkay, G; Földesi, I; Kovács, L, 1996
)
0.6
" The pharmacokinetics of mifepristone are characterised by rapid absorption, a long half-life of 25 to 30 hours and micromolar serum concentrations following ingestion of doses currently in clinical use."( Clinical pharmacokinetics of mifepristone.
Heikinheimo, O, 1997
)
0.89
" Whether LIL and ONA share these latter two characteristics with MIF has not yet been determined but they illustrate properties that, in addition to diminished antiglucocorticoid activities and altered pharmacokinetic characteristics, warrant consideration during the development of these and never antiprogestational agents."( Antiprogestin pharmacodynamics, pharmacokinetics, and metabolism: implications for their long-term use.
Benet, LZ; Jang, GR, 1997
)
0.3
"The potentiality of mifepristone as an abortifacient and contraceptive drug along with its pharmacokinetic parameters is reviewed."( Mifepristone: bioavailability, pharmacokinetics and use-effectiveness.
Sarkar, NN, 2002
)
2.08
" The results showed that absorption and initiation of metabolism of RU 486 were rapid in both groups, as indicated by the fact that RU 486 and its 3 metabolites could be measured in plasma 20 minutes after administration and that Tmax of RU 486 was between 1 and 2 hours."( [Pharmacokinetic study on RU 486 and its metabolites after oral administration of various doses in pregnant and non-pregnant women].
He, CH; Shi, YE; Ye, ZH; Zhang, GQ, 1992
)
0.28
"The pharmacokinetics of mifepristone is characterized by rapid absorption, a long half-life of 25-30 h, and high micromolar serum concentrations following ingestion of doses of >/=100 mg of the drug."( The pharmacokinetics of mifepristone in humans reveal insights into differential mechanisms of antiprogestin action.
Heikinheimo, O; Kekkonen, R; Lähteenmäki, P, 2003
)
0.93
" The pharmacokinetic data on 10 mg mifepristone are in line with previous pharmacokinetic and clinical data, and encourage further development of the 10-mg dose in emergency contraception."( Pharmacokinetics of 10 mg of mifepristone.
Heikinheimo, O; Leminen, R; Oehler, J; Ranta, S; von Hertzen, H, 2003
)
0.89
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
" This validated HPLC method was successfully applied to pharmacokinetic study of mifepristone in human plasma samples collected from volunteers after oral administration of 10 mg mifepristone."( Development of a high-performance liquid chromatographic method for the determination of mifepristone in human plasma using norethisterone as an internal standard: application to pharmacokinetic study.
Guo, Z; Wang, S; Wei, D; Zhai, J, 2007
)
0.79
" The validated LC-MS/MS method was successfully used in a pharmacokinetic study in healthy female volunteers after oral administration of 25 mg mifepristone tablet."( Simultaneous determination of mifepristone and monodemethyl-mifepristone in human plasma by liquid chromatography-tandem mass spectrometry method using levonorgestrel as an internal standard: application to a pharmacokinetic study.
Bi, HC; Chen, X; Huang, M; Huang, ZY; Tang, C; Zhong, GP, 2009
)
0.84
"The aim of this study is to establish an HPLC method for simultaneous determinations of mifepristone and its metabolites, mono-demethylated mifepristone, di-demethylated mifepristone and C-hydroxylated mifepristone in plasma and to evaluate the pharmacokinetic characteristics of mifepristone tablet."( Determinations of mifepristone and its metabolites and their pharmacokinetics in healthy female Chinese subjects.
Dong, RQ; Guo, RC; Jiang, ZM; Liu, HJ; Liu, XY; Teng, YN; Wang, BJ; Wei, CM; Yuan, GY; Zhang, R, 2011
)
0.93

Compound-Compound Interactions

Oral or vaginal misoprostol combined with mifepristone, is effective and safe for termination of pregnancy between 8 and 16 weeks of gestation. However, the efficacy and safety of GZFL in combination with low-dose mifEPristone (MFP) remains controversial.

ExcerptReferenceRelevance
" A randomised study was carried out to determine the efficacy of mifepristone and dilapan in combination with gemeprost for second trimester termination between 12-18 weeks' gestation."( A study of gemeprost alone, dilapan or mifepristone in combination with gemeprost for the termination of second trimester pregnancy.
Baird, DT; Thong, KJ, 1992
)
0.79
"The availability of a medical mode of termination of early pregnancy by the administration of RU486, an antiprogesterone alone, or in combination with one of the PG analogues significantly reduces the maternal morbidity and mortality associated with the classical surgical abortion."( Mifepristone (RU486) alone or in combination with a prostaglandin analogue for termination of early pregnancy: a review.
Avrech, OM; Bukovsky, I; Caspi, E; Golan, A; Weinraub, Z, 1991
)
1.72
"Abortion was attempted in 316 healthy women in early pregnancy within 7 weeks with the RU486 alone (600mg in a single oral dose) or in combination with a PG (15-dl-methyl-PGF2 alpha-methyl-ester) 1 mg suppository."( [Termination of early pregnancy using RU 486 alone or in combination with prostaglandin. The RU 486 Collaboration Group].
, 1990
)
0.28
"5 mg/kg combined with anordrin 2 mg/kg when given on d 6-8 of pregnancy."( [Antifertility effects of RU-486 in combination with anordrin in rats].
Lin, ZM; Liu, GM; Qian, YX; Shen, PJ; Shen, QC; Xu, RY, 1989
)
0.28
"A progesterone antagonist (RU 486), combined with oxytocin, was effective in achieving cervical dilation, labor induction, and early delivery in near-term monkeys."( Progesterone antagonist (RU 486) for cervical dilation, labor induction, and delivery in monkeys: effectiveness in combination with oxytocin.
Anderson, TL; Baulieu, EE; Hodgen, GD; Sinosich, M; Ulmann, A; Wolf, JP, 1989
)
0.28
"Abortion was attempted in 39 women in early pregnancy (less than 56 days amenorrhea) with the progesterone antagonist RU486 alone (150 mg per day for 4 days) or in combination with a PG analogue, 16,16-dimethyl-trans-delta 2-PGE1 (Gemeprost) in the form of a 1 mg vaginal pessary."( Therapeutic abortion in early pregnancy with antiprogestogen RU486 alone or in combination with prostaglandin analogue (gemeprost).
Baird, DT; Cameron, IT; Michie, AF, 1986
)
0.27
"Abortion was attempted in 39 women in early pregnancy (less than 56 days amenorrhea) with the progesterone antagonist RU486 alone (150 mg per day for 4 days) or in combination with a PG analogue, 16,16-dimethyl-trans-delta2-PGE1 (Gemeprost) in the form of a 1 mg vaginal pessary."( Therapeutic abortion in early pregnancy with antiprogestogen RU486 alone or in combination with prostaglandin analogue (gemeprost).
Baird, DT; Cameron, IT; Michie, AF, 1986
)
0.27
"Mifepristone (600 mg) in combination with a prostaglandin has been demonstrated to be a safe, acceptable alternative to vacuum aspiration for induction of abortion in the first 9 weeks of pregnancy."( Randomized trial of misoprostol and cervagem in combination with a reduced dose of mifepristone for induction of abortion.
Baird, DT; Sukcharoen, N; Thong, KJ, 1995
)
1.96
" The authors' previous research had indicated there is no difference in clinical efficacy between 200 mg and 600 mg (standard dose) of mifepristone in combination with 600 mcg of misoprostol."( Randomized trial of misoprostol and cervagem in combination with a reduced dose of mifepristone for induction of abortion.
Baird, DT; Sukcharoen, N; Thong, KJ, 1995
)
0.72
"In view of the unexpected ability of anordrin to synergize with RU 486 in terminating pregnancy, it was pertinent to examine the actions of the dihydroxylated metabolite of anordrin, anordiol, alone and in combination with RU 486."( Anordiol is more potent than anordrin for terminating pregnancy when administered with RU 486.
Bardin, CW; Chang, CC; Wang, WC, 1993
)
0.29
"The effects of RU 486 combined with tamoxifen and tamoxifen alone on hormonal parameters and endometrial development at the time of implantation were studied."( Effect of tamoxifen alone and in combination with RU 486 on the endometrium in the mid-luteal phase.
Bygdeman, M; Cekan, S; Johannisson, E; Seppälä, M; Swahn, ML, 1993
)
0.29
"A prospective randomized study was conducted to compare the efficacy of misoprostol with gemeprost when combined with mifepristone for termination of second trimester pregnancy."( Misoprostol is as effective as gemeprost in termination of second trimester pregnancy when combined with mifepristone: a randomised comparative trial.
Chan, YF; Ho, PC; Lau, W, 1996
)
0.72
"Findings are presented from a prospective randomized study conducted to compare the efficacy of misoprostol with gemeprost when combined with mifepristone to terminate second trimester pregnancy."( Misoprostol is as effective as gemeprost in termination of second trimester pregnancy when combined with mifepristone: a randomised comparative trial.
Chan, YF; Ho, PC; Lau, W, 1996
)
0.71
"Two regimens of the prostaglandin E1 analogue, gemeprost, in combination with mifepristone were compared in a randomised trial for termination of pregnancy between 12-19 weeks."( A randomised study of two doses of gemeprost in combination with mifepristone for induction of abortion in the second trimester of pregnancy.
Baird, DT; Lynch, P; Thong, KJ, 1996
)
0.76
"Two regimens of prostaglandin E1 analogue, gemeprost, in combination with mifepristone were compared in a randomized trial for termination of pregnancy at 12-19 weeks."( A randomised study of two doses of gemeprost in combination with mifepristone for induction of abortion in the second trimester of pregnancy.
Baird, DT; Lynch, P; Thong, KJ, 1996
)
0.76
"The effectiveness of mifepristone, onapristone, and ORG 31806 alone or in combination with anordiol to terminate pregnancy in the rat was evaluated."( Comparative effectiveness of three antiprogestins alone and in combination with anordiol in terminating pregnancy in the rat.
Bardin, CW; Dao, B; Koide, SS; Li, XJ; Vanage, G, 1997
)
0.62
"The pregnancy termination potency of varying doses of mifepristone, onapristone, and ORG 3806--alone and in combination with the estrogenic/antiestrogenic compound anordiol--was evaluated in adult rats."( Comparative effectiveness of three antiprogestins alone and in combination with anordiol in terminating pregnancy in the rat.
Bardin, CW; Dao, B; Koide, SS; Li, XJ; Vanage, G, 1997
)
0.55
" These findings provide a molecular explanation for the ability of disparate chemicals to induce CYP3A4 levels and, furthermore, provide a basis for developing in vitro assays to aid in predicting whether drugs will interact in humans."( The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
Kliewer, SA; Lehmann, JM; McKee, DD; Moore, JT; Watson, MA; Willson, TM, 1998
)
0.3
" injection of 50 mg/m2 methotrexate alone or a single dose of 600 mg oral mifepristone in combination with the same dose of methotrexate."( Mifepristone in combination with methotrexate for the medical treatment of tubal pregnancy: a randomized, controlled trial.
Alfirevic, Z; Baruah, DN; Emery, SJ; Gazvani, MR, 1998
)
1.97
"To clarify the role of DL111-IT when combined with mifepristone (Mif) on termination of early pregnancy."( Synergistic effects on pregnancy-termination activity of DL111-IT in combination with mifepristone.
Fang, RY; Yang, B, 1996
)
0.77
"Mifepristone in combination with prostaglandin has been used since 1988 for induction of early abortion."( Interruption of early pregnancy with mifepristone in combination with gemeprost.
Brooks, L; Grinsted, J; Grinsted, L; Jacobsen, JD; Nielsen, SP; Sandstrøm, O; Schantz, A, 1999
)
2.02
" Oral misoprostol (400 microg) given every 3 h up to five doses, when combined with mifepristone, was as effective as the vaginal (200 microg) route in second trimester termination of pregnancy."( Randomized comparison of vaginal (200 microg every 3 h) and oral (400 microg every 3 h) misoprostol when combined with mifepristone in termination of second trimester pregnancy.
Ho, PC; Ngai, SW; Tang, OS, 2000
)
0.74
"The objectives of this study were to determine the synergistic effects of DL111-IT in combination with mifepristone (RU486) on termination of early pregnancy in rhesus monkeys."( Synergistic effects of DL111-IT combined with mifepristone on termination of early pregnancy in rhesus monkeys.
Fang, RY; He, QJ; Yang, B; Ying, Y, 2000
)
0.78
"To investigate the effectiveness and side-effects of different doses of mifepristone alone or in combination with anordrin given orally within 96 hours after unprotected intercourse as an emergency contraceptive."( [A randomized multicentre clinical trial on different doses of mifepristone alone and in combination with anordrin as emergency contraception].
Sang, G; Shao, Q; Zhang, L, 1999
)
0.78
" Two groups received mifepristone in combination with anordrin showed significant lower incidence of withdrawal bleeding than those in mifepristone alone groups."( [A randomized multicentre clinical trial on different doses of mifepristone alone and in combination with anordrin as emergency contraception].
Sang, G; Shao, Q; Zhang, L, 1999
)
0.86
"DL111-IT, a non-hormonal contragestional agent, revealed synergistic effects in combination with mifepristone (RU486) in some species."( Effects of DL111-IT or combined with RU486 on uterine polyamines biosynthesis in rats during early gestation.
Fang, R; He, Q; Shentu, J; Wang, L; Zhou, H, 2001
)
0.53
"Gemeprost and misoprostol are two of the most widely used prostaglandins in combination with mifepristone for medical abortion in early pregnancy."( Double-blind randomized trial of mifepristone in combination with vaginal gemeprost or misoprostol for induction of abortion up to 63 days gestation.
Baird, DT; Bartley, J; Brown, A; Elton, R, 2001
)
0.81
" Tyrosine combined with RU486 was shown to have a synergistic effect to terminate early pregnancy."( [Effects of tyrosine alone and tyrosine in combination with RU486 on early pregnancy in mice and the mechanism of action].
Duan, H; Wang, NG, 1997
)
0.3
" Further studies should be conducted to determine whether tamoxifen combined with mifepristone for emergency contraception is more effective as compared with mifepristone alone."( A randomized comparative study on mifepristone alone and in combination with tamoxifen for emergency contraception.
Bingshun, W; Changhai, H; Ersheng, G; Exiang, Z; Jie, Y; Mauck, C; Youlun, G, 2002
)
0.82
"To compare the effectiveness of gemeprost and misoprostol as prostaglandins used in combination with mifepristone for induction of mid-trimester termination."( A randomised study of misoprostol and gemeprost in combination with mifepristone for induction of abortion in the second trimester of pregnancy.
Baird, DT; Bartley, J, 2002
)
0.77
" For drugs with narrow therapeutic windows, such as digoxin, an understanding of the potential mechanisms by which drugs might interact is essential to clinical practice."( From bench to bedside: utilization of an in vitro model to predict potential drug-drug interactions in the kidney: the digoxin-mifepristone example.
Ito, S; Koren, G; Woodland, C, 2003
)
0.52
"This study evaluated the effectiveness and acute toxicity of DL111-IT combined with mifepristone (RU486) and misoprostol (MISO) on early pregnancy termination."( Synergistic effects of DL111-IT in combination with mifepristone and misoprostol on termination of early pregnancy in preclinical studies.
Fang, RY; He, QJ; Wang, WF; Wu, HH; Yang, B, 2003
)
0.79
"To assess the safety of mifepristone in combination with misoprotol for medical abortion."( [Side effect of mifepristone in combination with misoprostol for medical abortion].
Jiang, S; Lei, ZW; Li, Q; Li, YP; Lü, L; Zou, Y, 2004
)
0.98
"To observe the effects of mifepristone combined with methotrexate for conservative treatment of tubal ectopic pregnancy."( [Mifepristone combined with methotrexate for conservative treatment of tubal ectopic pregnancy].
Li, ZH; Quan, S, 2004
)
1.53
"20%) receiving oral mifepristone combined with calcium leucovorin and methotrexate were cured, a curative rate significantly higher than that in the control group, where 70 cases (81."( [Mifepristone combined with methotrexate for conservative treatment of tubal ectopic pregnancy].
Li, ZH; Quan, S, 2004
)
1.56
"Mefepristone combined with methotrexate is safe and effective in the treatment of tubal ectopic pregnancy, without obvious side effects."( [Mifepristone combined with methotrexate for conservative treatment of tubal ectopic pregnancy].
Li, ZH; Quan, S, 2004
)
1.23
"Sublingual misoprostol, when combined with mifepristone, is effective for medical abortion in the second trimester."( A prospective randomized comparison of sublingual and oral misoprostol when combined with mifepristone for medical abortion at 12-20 weeks gestation.
Chan, CC; Ho, PC; Kan, AS; Tang, OS, 2005
)
0.81
"To assess women's acceptability, the efficacy and side effects of sublingual versus vaginal administration of misoprostol in combination with mifepristone for medical abortion up to 13 weeks of gestation."( A randomised controlled trial of mifepristone in combination with misoprostol administered sublingually or vaginally for medical abortion up to 13 weeks of gestation.
Ashok, PW; Flett, GM; Hamoda, H; Templeton, A, 2005
)
0.81
"A high-capacity ('gutless') adenoviral vector carrying a liver-specific, mifepristone (Mif)-inducible system for the expression of IL-12 (HC-Ad/RUmIL-12) was used in combination with chemotherapy."( Oxaliplatin in combination with liver-specific expression of interleukin 12 reduces the immunosuppressive microenvironment of tumours and eradicates metastatic colorectal cancer in mice.
Alzuguren, P; Berraondo, P; Crettaz, J; Gonzalez-Aparicio, M; Gonzalez-Aseguinolaza, G; Hernandez-Alcoceba, R; Hervas-Stubbs, S; Mancheno, U; Mauleon, I; Medina-Echeverz, J; Prieto, J, 2011
)
0.6
"Long-term controlled expression of IL-12 using an HC-Ad vector in combination with oxaliplatin is effective and clinically applicable against hepatic colon cancer metastases."( Oxaliplatin in combination with liver-specific expression of interleukin 12 reduces the immunosuppressive microenvironment of tumours and eradicates metastatic colorectal cancer in mice.
Alzuguren, P; Berraondo, P; Crettaz, J; Gonzalez-Aparicio, M; Gonzalez-Aseguinolaza, G; Hernandez-Alcoceba, R; Hervas-Stubbs, S; Mancheno, U; Mauleon, I; Medina-Echeverz, J; Prieto, J, 2011
)
0.37
"Medical regimens using mifepristone in combination with prostaglandins have been widely available for women undergoing termination of pregnancy (TOP) at 10-16 weeks' gestation in China."( Mifepristone in combination with prostaglandins for termination of 10-16 weeks' gestation: a systematic review.
Chen, QJ; Cheng, LN; Hong, QQ; Hou, SP; Huang, YM; Meads, C; Zhu, HP, 2011
)
2.12
"Mifepristone combined with misoprostol for second-trimester abortion (MM) and intra-amniotic injection of ethacridine lactate (EL; Rivanol®) are the common methods for termination of second-trimester pregnancy in China."( Termination of second-trimester pregnancy by mifepristone combined with misoprostol versus intra-amniotic injection of ethacridine lactate (Rivanol®): a systematic review of Chinese trials.
Chen, OJ; Chen, QF; Cheng, LN; Fang, AH; Hou, SP; Huang, YM, 2011
)
2.07
"To compare the efficacy and safety of misoprostol and mifepristone combination with misoprostol alone in management of intrauterine death."( Comparison of mifepristone combination with misoprostol and misoprostol alone in the management of intrauterine death: condensation - misoprostol and mifepristone combination is more effective than misoprostol alone in the management of intrauterine death
Paul, A; Sharma, D; Singhal, SR, 2011
)
0.98
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
"Methotrexate-mifepristone, either alone or in combination with other minimally invasive strategies, could be considered an option for the treatment of both cervical and interstitial ectopic pregnancy."( Medical therapy (methotrexate and mifepristone) alone or in combination with another type of therapy for the management of cervical or interstitial ectopic pregnancy.
Aguarón Benitez, G; Barberá Belda, B; Callejón Rodríguez, C; Gómez García, MT; González Merlo, G, 2012
)
1.03
"Mifepristone in combination with ethacridine lactate may significantly improve the outcomes of second trimester pregnancy termination compared with ethacridine lactate alone, without increasing complications and side effects apart from nausea."( Effectiveness of mifepristone in combination with ethacridine lactate for second trimester pregnancy termination.
Li, X; Liu, H; Mei, Q; Zhou, H, 2014
)
2.18
"This study aimed to investigate the effectiveness and safety of lower doses of mifepristone combined with misoprostol for the termination of ultra-early pregnancy."( Effectiveness and Safety of Lower Doses of Mifepristone Combined With Misoprostol for the Termination of Ultra-Early Pregnancy: A Dose-Ranging Randomized Controlled Trial.
Chen, DJ; Chen, WL; Li, CL; Liu, MX; Song, LP; Wang, Y; Zhang, ZF, 2015
)
0.91
"To assess the efficacy and safety of mifepristone combined with oral or vaginal misoprostol for termination of pregnancy between 8 and 16 weeks of gestation."( [Efficacy and safety of mifepristone combined with misoprostol for termination of pregnancy between 8 and 16 weeks of gestation].
Chang, Q; Di, W; Dong, B; Huang, Z; Jing, X; Li, Y; Qian, J; Ren, M; Shen, H; Shi, H; Song, W; Wu, S; Yao, C; Zheng, S, 2015
)
1
"Oral or vaginal misoprostol combined with mifepristone, is effective and safe for termination of pregnancy between 8 and 16 weeks of gestation."( [Efficacy and safety of mifepristone combined with misoprostol for termination of pregnancy between 8 and 16 weeks of gestation].
Chang, Q; Di, W; Dong, B; Huang, Z; Jing, X; Li, Y; Qian, J; Ren, M; Shen, H; Shi, H; Song, W; Wu, S; Yao, C; Zheng, S, 2015
)
0.99
" Lastly, doses of proteasome inhibitors that are inadequate to block the activity of the proteasomes, caused cell death when combined with mifepristone; this phenotype was accompanied by accumulation of poly-ubiquitinated proteins denoting proteasome inhibition."( Mifepristone increases mRNA translation rate, triggers the unfolded protein response, increases autophagic flux, and kills ovarian cancer cells in combination with proteasome or lysosome inhibitors.
Callegari, EA; Chien, J; Drappeau, DD; Eyster, KM; Gamarra-Luques, CD; Goyeneche, AA; Hapon, MB; Knapp, JR; Pan, B; Srinivasan, R; Telleria, CM; Terpstra, EJ; Wang, X; Zhang, L, 2016
)
2.08
"Mifepristone combined with ethacridine lactate is safe and effective for patients with low placentation or/and prior cesarean in the second-trimester pregnancy termination."( Mifepristone combined with ethacridine lactate for the second-trimester pregnancy termination in women with placenta previa and/or prior cesarean deliveries.
Chen, C; Jiang, Y; Lin, F; Wang, X; Wu, S, 2017
)
3.34
" In this paper, we analyzed the effect of laparoscopy combined with mifepristone in the treatment of endometriosis."( Effect of laparoscopy combined with mifepristone in the treatment of endometriosis and drug reaction analysis.
Li, J; Song, J; Yang, H, 2018
)
0.99
"The aim of the present study was to investigate the safety and efficacy of low-dose mifepristone combined with self-administered misoprostol for termination of early pregnancy."( Early medical abortion with self-administered low-dose mifepristone in combination with misoprostol.
Li, CL; Mo, XT; Song, LP; Tang, SY; Zhou, LJ, 2018
)
0.95
"Highly Active Metastasis Preventing Therapy (HAMPT) is a quardruple drug combination consisting of mifepristone, aspirin, lysine and doxycycline."( HAMPT, A Novel Quadruple Drug Combination Designed for Cancer Metastatic Chemoprevention: From Hypothesis to Proof-of-concept.
Jia, L; Liu, J; Wan, L; Xu, H; Xu, J; Zheng, N, 2019
)
0.73
"The present study demonstrated that HAMPT is a novel quadruple drug combination that can safely and effectively prevent cancer metastasis."( HAMPT, A Novel Quadruple Drug Combination Designed for Cancer Metastatic Chemoprevention: From Hypothesis to Proof-of-concept.
Jia, L; Liu, J; Wan, L; Xu, H; Xu, J; Zheng, N, 2019
)
0.51
"To evaluate the clinical outcomes of transvaginal ultrasound-guided (US-guided) radiofrequency ablation (RFA) combined with mifepristone for the treatment of large uterine fibroids."( Comparison between radiofrequency ablation combined with mifepristone and radiofrequency ablation for large uterine fibroids.
Dong, X; Guo, R; Hai, N; Hou, Q, 2021
)
1.07
"Between June 2016 and December 2018, a total of 30 patients with symptomatic uterine fibroids (≥5cm) who underwent transvaginal US-guided RFA combined with mifepristone were included in this retrospective study."( Comparison between radiofrequency ablation combined with mifepristone and radiofrequency ablation for large uterine fibroids.
Dong, X; Guo, R; Hai, N; Hou, Q, 2021
)
1.06
"US-guided RFA combined with mifepristone might be a simple, safe and effective alternative for the treatment of large uterine fibroids."( Comparison between radiofrequency ablation combined with mifepristone and radiofrequency ablation for large uterine fibroids.
Dong, X; Guo, R; Hai, N; Hou, Q, 2021
)
1.16
" In China, Xuefu Zhuyu Decoction (XFZYD), combined with Mifepristone, is widely used in the treatment of UL."( The efficacy and safety of Xuefu Zhuyu Decoction combined with Mifepristone in the treatment of uterine leiomyoma: A systematic review and meta-analysis.
Peng, F; Shi, S; Ye, Q; Yu, C, 2021
)
1.11
"This systematic review aims to evaluate the effectiveness and safety of XFZYD combined with Mifepristone as a method of treatment for UL."( The efficacy and safety of Xuefu Zhuyu Decoction combined with Mifepristone in the treatment of uterine leiomyoma: A systematic review and meta-analysis.
Peng, F; Shi, S; Ye, Q; Yu, C, 2021
)
1.08
" The primary outcome was the effect of XFZYD combined with Mifepristone on the effective rate, uterine leiomyoma volume (ULV), and uterine volume (UV) of uterine leiomyoma."( The efficacy and safety of Xuefu Zhuyu Decoction combined with Mifepristone in the treatment of uterine leiomyoma: A systematic review and meta-analysis.
Peng, F; Shi, S; Ye, Q; Yu, C, 2021
)
1.1
" In the past decade, a large number of clinical randomized controlled trials have proven that Chinese patent medicine combined with mifepristone in the treatment of uterine fibroids has a better curative effect, fewer adverse reactions, and higher safety than mifepristone alone."( Network meta-analysis of 6 kinds of Chinese patent medicines combined with mifepristone in the treatment of uterine fibroids: A protocol for systematic review and network meta-analysis.
Bi, C; Jia, Y; Qiao, M; Wang, H, 2021
)
1.06
" Clinical randomized controlled trials of 6 Chinese patent medicines combined with mifepristone for the treatment of uterine fibroids, including Guizhi Fuling Capsule, Gongliuxiao Capsule, Gongliuqing Capsule, Danbie Capsule, Gongliuning Capsule, and Xiaojiean Capsule were retrieved."( Network meta-analysis of 6 kinds of Chinese patent medicines combined with mifepristone in the treatment of uterine fibroids: A protocol for systematic review and network meta-analysis.
Bi, C; Jia, Y; Qiao, M; Wang, H, 2021
)
1.08
"This study provides the clinical efficacy and safety of network meta-analysis of 6 kinds of Chinese patent medicines combined with mifepristone in the treatment of uterine fibroids will be systematically evaluated or descriptively analyzed."( Network meta-analysis of 6 kinds of Chinese patent medicines combined with mifepristone in the treatment of uterine fibroids: A protocol for systematic review and network meta-analysis.
Bi, C; Jia, Y; Qiao, M; Wang, H, 2021
)
1.06
"To review and analyze the efficacy and safety of mifepristone combined with ethacridine lactate for induction of stillbirth in the third trimester."( Mifepristone combined with ethacridine lactate for third-trimester stillbirth induction: a 5-year experience from Shanghai.
Huang, RJ; Li, J; Ma, J; Xue, RH; Yao, YL; Zhang, L, 2022
)
2.42
"Mifepristone combined with ethacridine lactate is a safe and low-risk induction method for patients with stillbirth in the third trimester."( Mifepristone combined with ethacridine lactate for third-trimester stillbirth induction: a 5-year experience from Shanghai.
Huang, RJ; Li, J; Ma, J; Xue, RH; Yao, YL; Zhang, L, 2022
)
3.61
"Systematically evaluate the clinical efficacy of mifepristone combined with methotrexate therapy for ectopic pregnancy (EP), analyze the experimental designs, put forward improvement ideas."( The efficacy of mifepristone combined with methotrexate for the treatment of ectopic pregnancy: a systematic review and meta-analysis.
Feng, H; Li, X; Li, Y; Liao, X; Su, Q; Tian, T, 2022
)
1.32
"RCTs of mifepristone combined with mifepristone for EP until January 2022 in six databases were searched."( The efficacy of mifepristone combined with methotrexate for the treatment of ectopic pregnancy: a systematic review and meta-analysis.
Feng, H; Li, X; Li, Y; Liao, X; Su, Q; Tian, T, 2022
)
1.5
"The mifepristone combined with methotrexate therapy for EP has better curative effects on improving the cure rate, lowering β-HCG level, reducing the mass, and alleviating symptoms of abdominal pain and bleeding, without amplifying the toxic side effects."( The efficacy of mifepristone combined with methotrexate for the treatment of ectopic pregnancy: a systematic review and meta-analysis.
Feng, H; Li, X; Li, Y; Liao, X; Su, Q; Tian, T, 2022
)
1.63
" In the control group, 34 patients were treated with HIFU alone, 29 patients with HIFU combined with mifepristone, 10 patients with HIFU combined with LNG-IUS."( Clinical evaluation of high-intensity focused ultrasound ablation combined with mifepristone and levonorgestrel-releasing intrauterine system to treat symptomatic adenomyosis.
Dong, G; Li, Y; Ma, Q; Mu, Y; Song, S; Yang, L; Zhu, H, 2023
)
1.35
" This combination therapy demonstrates superior efficacy to treatment with HIFU alone, HIFU combined with mifepristone, and HIFU combined with LNG-IUS."( Clinical evaluation of high-intensity focused ultrasound ablation combined with mifepristone and levonorgestrel-releasing intrauterine system to treat symptomatic adenomyosis.
Dong, G; Li, Y; Ma, Q; Mu, Y; Song, S; Yang, L; Zhu, H, 2023
)
1.35
" However, the efficacy and safety of GZFL in combination with low-dose mifepristone (MFP) remains controversial."( The efficacy and safety of Chinese herbal medicine Guizhi Fuling capsule combined with low dose mifepristone in the treatment of uterine fibroids: a systematic review and meta-analysis of 28 randomized controlled trials.
Bai, Y; Dong, T; Gao, F; Lei, Y; Li, M; Ou, L; Wei, P; Yang, H; Yang, L, 2023
)
1.36
"We searched eight literature databases and two clinical trial registries for randomized controlled trials (RCTs) of the efficacy and safety of GZFL combined with low-dose MFP in the treatment of UFs from database inception to April 24, 2022."( The efficacy and safety of Chinese herbal medicine Guizhi Fuling capsule combined with low dose mifepristone in the treatment of uterine fibroids: a systematic review and meta-analysis of 28 randomized controlled trials.
Bai, Y; Dong, T; Gao, F; Lei, Y; Li, M; Ou, L; Wei, P; Yang, H; Yang, L, 2023
)
1.13
" The meta-analysis showed that compared with low-dose MFP alone, GZFL combined with low-dose MFP significantly reduced follicle stimulating hormone (p < 0."( The efficacy and safety of Chinese herbal medicine Guizhi Fuling capsule combined with low dose mifepristone in the treatment of uterine fibroids: a systematic review and meta-analysis of 28 randomized controlled trials.
Bai, Y; Dong, T; Gao, F; Lei, Y; Li, M; Ou, L; Wei, P; Yang, H; Yang, L, 2023
)
1.13
"This study suggests that GZFL combined with low-dose MFP is more effective and safe in the treatment of UFs, and it is a potential treatment for UFs."( The efficacy and safety of Chinese herbal medicine Guizhi Fuling capsule combined with low dose mifepristone in the treatment of uterine fibroids: a systematic review and meta-analysis of 28 randomized controlled trials.
Bai, Y; Dong, T; Gao, F; Lei, Y; Li, M; Ou, L; Wei, P; Yang, H; Yang, L, 2023
)
1.13
"To analyze the efficacy and influencing factors of Mifepristone combined with estrogen-progesterone sequential therapy (Femoston) in the treatment of incomplete abortion."( The efficacy and influence factors analysis of Mifepristone combined with estrogen-progesterone in the treatment of incomplete abortion.
Luo, ZY; Shen, HL; Su, RD; Wang, K; Wang, WR; Zhuang, LL, 2023
)
1.42

Bioavailability

The study was conducted to assess the bioavailability of two formulations of mifepristone in capsule and tablet forms at a single dose of 75 mg (half the registered dose in China) Mifepristsone is an orally active compound with nearly 40% bioavailability after first pass effect.

ExcerptReferenceRelevance
" bioavailability of CDB-2914 in intact female rhesus monkeys, and to compare the serum concentrations of CDB-2914 with that of mifepristone following oral administration."( Circulating concentrations of the antiprogestins CDB-2914 and mifepristone in the female rhesus monkey following various routes of administration.
Blye, RP; Larner, JM; Reel, JR, 2000
)
0.75
" It is an orally active compound with nearly 70% absorption rate but its bioavailability is reduced to around 40% because of the first-pass effect."( Mifepristone: bioavailability, pharmacokinetics and use-effectiveness.
Sarkar, NN, 2002
)
1.76
" Mifepristone is an orally active compound with nearly 40% bioavailability after first pass effect."( The potential of mifepristone (RU486) as a female contraceptive drug.
Sarkar, NN, 2002
)
1.56
" Upon administration to Sprague-Dawley rats, both compounds were found to be orally bioavailable and to inhibit transactivation of liver GR."( Glucocorticoid receptor antagonism by cyproterone acetate and RU486.
Chatelain, RE; Cornell, W; Fink, C; Honer, C; Ksander, G; Marshall, P; Nam, K; Schumacher, C; Schweitzer, R; Steele, R, 2003
)
0.32
"The objective of this study was to prepare an oral dosage formulation of mifepristone that will improve the oral bioavailability of mifepristone and sustain the release of mifepristone for at least 3 days to effectively control reproduction, especially in coyotes."( Improved bioavailability of orally administered mifepristone from PLGA nanoparticles.
He, W; Horn, SW; Hussain, MD, 2007
)
0.83
" One compound 4a, with high oral bioavailability (59%) in rat, exhibited functional antagonism of GR in oral glucose tolerance test (OGTT)."( Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
Allan, G; Demarest, K; Fiordeliso, JJ; Gunnet, J; Jiang, W; Linton, O; Lundeen, S; Sui, Z; Tannenbaum, P; Xu, J; Zhu, P, 2007
)
0.34
" Analogues 43 and 45 had >50% oral bioavailability in the dog."( 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
Belanoff, J; Blaney, P; Bright, CP; Clark, DE; Clark, RD; Crackett, PH; Devos, R; Dyke, HJ; Hurley, C; Jenkins, RE; Lockey, P; Porres, SS; Ray, NC; Ward, S; Williams, K; Wong, M, 2008
)
0.35
"The study was conducted to assess the bioavailability of two formulations of mifepristone in capsule and tablet forms at a single dose of 75 mg (half the registered dose in China)."( Bioavailability of mifepristone in capsule versus tablet form in healthy nonpregnant women.
Li, H; Liao, A; Pang, X; Wu, X; Xiong, Z, 2008
)
0.9
" Relative bioavailability (capsule/tablet) was derived from AUC(0-96 h)."( Bioavailability of mifepristone in capsule versus tablet form in healthy nonpregnant women.
Li, H; Liao, A; Pang, X; Wu, X; Xiong, Z, 2008
)
0.67
" The relative bioavailability was 109."( Bioavailability of mifepristone in capsule versus tablet form in healthy nonpregnant women.
Li, H; Liao, A; Pang, X; Wu, X; Xiong, Z, 2008
)
0.67
" Optimization of the sulfonamide substituent has provided compounds with a very desirable overall profile, including minimal hERG activity, good bioavailability and in vivo efficacy."( 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.
Belanoff, JK; Golding, E; Gourdet, B; Hunt, HJ; Phillips, T; Swift, D; Thomas, J; Unitt, JF; Walters, I, 2015
)
0.42
" We studied whether glucocorticoid receptor (GR) silencing or inhibition in human epileptic brain endothelial cells (EPI-ECs) functionally impacts drug bioavailability across an in vitro model of the blood-brain barrier (BBB) by CYP-multidrug transporter (multidrug resistance protein 1, MDR1) mechanisms."( Modulation of glucocorticoid receptor in human epileptic endothelial cells impacts drug biotransformation in an in vitro blood-brain barrier model.
Bingaman, W; Ghosh, C; Gonzalez-Martinez, J; Hossain, M; Janigro, D; Khan, S; Marchi, N; Mishra, S; Najm, I, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Until now, there are a lot of research focusing on enhancing the solubility and oral bioavailability of Mifepristone."( Mifepristone polymorph with enhanced solubility, dissolution and oral bioavailability.
Chen, XF; Gong, XF; Li, P; Ning, LF; Wang, HP; Xu, J, 2020
)
2.21
" The established UHPLC-QqQ-MS/MS method is suitable for forensic toxicological analysis as well as in terms of clinical toxicology in future investigations (examination of pharmacokinetics, bioavailability and metabolism of RU-486)."( Determination of Mifepristone (RU-486) and Its Metabolites in Maternal Blood Sample after Pharmacological Abortion.
Jurek, T; Szpot, P; Wachełko, O; Zawadzki, M, 2022
)
1.06

Dosage Studied

Mifepristone is an effective means of early pregnancy termination, but the type and dosage of the prostaglandin require further definition. Expulsion of the ovum was difficult to date when mifepristsone was used alone; it occurred within 24 hours of prostaglandsin dosing in more than 80 per cent of the women.

ExcerptRelevanceReference
" Further studies on dosage and treatment protocols would be justified."( The efficacy of oral Mifepristone (RU 38,486) with a prostaglandin E1 analog vaginal pessary for the termination of early pregnancy: complications and patient acceptability.
Ferguson, J; Hill, NC; MacKenzie, IZ, 1990
)
0.6
" An appropriate dose of mifepristone at an appropriate gestational age in combination with a prostaglandin is an effective means of early pregnancy termination, but the type and dosage of the prostaglandin require further definition."( Abortion.
Blumenthal, PD, 1991
)
0.58
" The stimulation of fibrinogen mRNA levels appears to be mediated by the glucocorticoid receptor, because 1) the dose-response relationship parallels the reported affinity of dexamethasone for the Xenopus glucocorticoid receptor; and 2) the induction is blocked by RU 486, a potent antiglucocorticoid."( Coordinate regulation of fibrinogen subunit messenger RNA levels by glucocorticoids in primary cultures of Xenopus liver parenchymal cells.
Bhattacharya, A; Holland, LJ, 1991
)
0.28
" 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
)
0.87
" However, P at a dosage of 10 and 20,mg/kg had no effect on ovarian 3 beta-HSD activities."( [The effect of progesterone and RU486 on progesterone production in the ovulatory process of rats].
Iwamasa, J, 1991
)
0.28
" Dose-response studies with estrogen and R5020 revealed that the extent of progestin activity was only partially dependent upon the R5020 dose with the major determining factor being the dose of estrogen."( Progesterone action in normal mouse mammary gland.
Counterman, LJ; Haslam, SZ; Wang, S, 1990
)
0.28
" Dexamethasone administration led to a sigmoidal dose-response curve in the case of alpha 2-APG whereas a biphasic sinusoidal-like dose-response curve was obtained for CRP."( Modulation of rat C-reactive protein serum level by dexamethasone and adrenaline--comparison with the response of alpha 2-acute phase globulin.
Bürger, W; Göhler, K; Hirschelmann, R; Schade, R, 1987
)
0.27
" Expulsion of the ovum was difficult to date when mifepristone was used alone; it occurred within 24 hours of prostaglandin dosing in more than 80 per cent of the other women."( [Use of mifepristone in the termination of early pregnancy. The experience in France].
Dubois, C; Silvestre, L; Ulmann, A, 1989
)
0.96
"Six pregnant women (below 49 days of amenorrhea) desiring pregnancy termination received 600 mg RU486 orally in a single dosage and 1 mg PG-05 or ONO-802 as vaginal suppository 48 h afterward."( Functional status of the pituitary-adrenal axis during treatment of RU486 for termination of early pregnancy in combination with PGs in Chinese women.
Wu, XR; Yang, XL, 1989
)
0.28
"Mifepristone was used in a dosage of 400 mg/d in a double-blind study to induce labour in patients with intra-uterine fetal death in late pregnancy."( Termination of pregnancy with mifepristone after intra-uterine death. Clinical and hormonal effects.
Heyns, A; Moodley, J; Norman, RJ; Padayachi, T, 1989
)
2.01
" The human dosage is 200 mg/day."( [RU-486: clinical application in gynecology].
Menashe, Y; Serr, DM; Shalev, J, 1989
)
0.28
" Mifepristone in the dosage administered has shown nearly no clinical side effects."( [The antiprogesterone action of mifepristone].
Haspels, AA, 1989
)
1.28
" Depending upon the dosing regime employed microgram quantities of the steroid were sufficient to significantly inhibit the clinical development of EAE and milligram doses of the drug completely suppressed the emergence of disease."( The effects of the anti-glucocorticoid RU 38486 on steroid-mediated suppression of experimental allergic encephalomyelitis (EAE) in the Lewis rat.
Bolton, C; Flower, RJ, 1989
)
0.28
" Longitudinal studies with daily dosing and frequent blood sampling were conducted during three consecutive cycles (control/treatment/recovery)."( Luteal contraception.
Garzo, G; Liu, J; Yen, S, 1987
)
0.27
" 4) The lack of antiglucocorticosteroid activity, at the dosage of 100 mg/day, suggests that RU 486 may be useful for fertility control."( Effects of the antiprogesterone steroid RU 486 during midluteal phase in normal women.
Baulieu, EE; George, M; Lestrat, N; Reinberg, A; Schaison, G, 1985
)
0.27
" 4) The lack of antiglucocorticosteroid activity, at a dosage of 100 mg/day, suggests that RU 486 may be useful for fertility control."( Effects of the antiprogesterone steroid RU 486 during midluteal phase in normal women.
Baulieu, EE; George, M; Lestrat, N; Reinberg, A; Schaison, G, 1985
)
0.27
" The antiglucocorticoid RU 38486 administered subcutaneously (1 and 10 mg/kg) inhibited the dexamethasone effect and caused a parallel shift in the dose-response curve of dexamethasone."( Antiglucocorticoid RU 38486 attenuates retention of a behaviour and disinhibits the hypothalamic-pituitary adrenal axis at different brain sites.
De Kloet, ER; De Kock, S; Schild, V; Veldhuis, HD, 1988
)
0.27
" In order to determine the optimal dosage of this drug to terminate early pregnancy, we treated 106 healthy women with normal pregnancies by real time ultrasound examination whose gestational duration was less than 49 days from onset of last menses with either a medium or low dose treatment regimen."( Termination of early gestation with the anti-progestin steroid RU 486: medium versus low dose.
Brenner, PF; Horenstein, J; Lacarra, M; Lahteenmaki, P; Mishell, DR; Shoupe, D; Spitz, IM, 1987
)
0.27
" The dose-response and time-response characteristics of the behavior facilitating actions of both progesterone and R 5020 were measured."( Actions of progestins on estrous behaviour in female rats.
Barfield, RJ; Etgen, AM; Vathy, IU, 1987
)
0.27
" The percentage of women with complete abortion was similar in all dosage groups."( Termination of early pregnancy by the progesterone antagonist RU 486 (Mifepristone).
Baulieu, EE; Couzinet, B; Le Strat, N; Schaison, G; Ulmann, A, 1986
)
0.5
" Thus, the fact of adding on the 4th day of the RU 486 treatment a weak dosage of synthetic prostaglandin equal to 1/6 of that used alone when inducing abortions made a clear improvement in the results possible."( Fertility control in women: results with RU 486 by the end of 1985.
Baulieu, E, 1986
)
0.27
" Cortisol concentrations increased during treatment with all 3 dosage regimens but the levels remained within the normal range."( Termination of very early pregnancy by RU 486--an antiprogestational compound.
Bygdeman, M; Kovacs, L; Resch, BA; Rowe, PJ; Sas, M; Swahn, ML; Ugocsai, G, 1984
)
0.27
" Cortisol concentrations increased during treatment with all 3 dosage regimens but the levels remained within the normal range."( Termination of very early pregnancy by RU 486--an antiprogestational compound.
Bygdeman, M; Kovacs, L; Resch, BA; Rowe, PJ; Sas, M; Swahn, ML; Ugocsai, G, 1984
)
0.27
" However, differences in dose-response patterns for suppression of cytokine gene expression and suppression of the AFC response suggest the involvement of additional factors."( Mechanisms of ethanol-induced suppression of a primary antibody response in a mouse model for binge drinking.
Han, YC; Pruett, SB, 1995
)
0.29
" Early trials to determine dosage are now being followed by larger studies of efficacy and side-effects."( Non-surgical abortion: who's for methotrexate?
Potts, M, 1995
)
0.29
" Most of the clinical trials have studied its efficacy in the termination of early pregnancy when used in conjunction with a low dosage of a prostaglandin analogue."( Mifepristone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential.
Brogden, RN; Faulds, D; Goa, KL, 1993
)
1.73
" When the latter dosage of mifepristone (50 microM) was added 4h after LH+IBMX, no inhibitory effect was seen (17."( Inhibitory effect of mifepristone (RU 486) on ovulation in the isolated perfused rat ovary.
Brännström, M, 1993
)
0.9
" Mifepristone at the dosage of 4 mg/100 g body weight completely suppressed the growth of PC-3 tumors for 21 days, although this was followed by a growth rate similar to that of the control tumor."( Growth inhibition of androgen-insensitive human prostate carcinoma cells by a 19-norsteroid derivative agent, mifepristone.
Grunberg, SM; Kawachi, MH; Lin, FF; Lin, MF; Stallcup, MR, 1995
)
1.41
" To rule out any differences in end-organ sensitivity to glucocorticoids between the two strains, we evaluated dose-response relations of whole body, thymus, spleen, and adrenal weights after 1 week daily administration of graded doses of dexamethasone."( Glucocorticoid and/or glucocorticoid antagonist effects in inflammatory disease-susceptible Lewis rats and inflammatory disease-resistant Fischer rats.
Chrousos, GP; Crofford, L; Karalis, K; Wilder, RL, 1995
)
0.29
" These situations call for aggressive dosing of uterine stimulants (e."( Drug therapy during labor and delivery.
Kelsey, JJ; Prevost, RR, 1994
)
0.29
" So, the duration of termination, and the PG dosage are reduced by half."( [Methods of second trimester pregnancy termination and evacuation of in utero dead fetuses. Value of mifepristone].
Maria, B; Matheron, I, 1994
)
0.5
" Time-course and dose-response studies showed that maximal enhancement occurred at a 1-microM dexamethasone concentration after 48 h of treatment."( Dexamethasone potentiates IGF-I actions in porcine granulosa cells.
Bodenburg, YH; Nagamani, M; Peirce, J; Urban, RJ, 1994
)
0.29
" The dosage of RU 486 used is significantly lower than that required for antagonizing progesterone action."( A regulatory system for use in gene transfer.
O'Malley, BW; Tsai, SY; Wang, Y, 1994
)
0.29
" The effects of hydrocortisone were clearly confirmed through the dose-response study of both DMN and hydrocortisone."( Role of hydrocortisone in dimethylnitrosamine-induced suppression of antibody response in the mixed culture of murine hepatocytes and splenocytes.
Holsapple, MP; Jeong, TC; Jordan, SD; Stevens, WD; Yang, KH, 1994
)
0.29
" There were no significant differences between the 2 dosage groups in serum estradiol, progesterone, and human chorionic gonadotropin."( Dose and time dependent rise of plasma cortisol following administration of mifepristone in early pregnancy.
Baird, DT; Brooks, AN; Thong, KJ, 1993
)
0.52
" ATtempts have been made to shorten the induction-abortion interval and to lower dosage of the prostaglandins in order to reduce the incidence of side effects."( Termination of second trimester pregnancy with sulprostone and mifepristone: a randomized double-blind placebo-controlled trial.
Ho, PC; Ma, HK, 1993
)
0.53
" Three dosage schedules were used: single oral dose of 40 mg tamoxifen alone and in combination with 200 mg RU 486, and 40 mg tamoxifen for three consecutive days starting on the first day after the luteinizing hormone (LH) surge."( Effect of tamoxifen alone and in combination with RU 486 on the endometrium in the mid-luteal phase.
Bygdeman, M; Cekan, S; Johannisson, E; Seppälä, M; Swahn, ML, 1993
)
0.29
" In need of further investigation is the RU-486 dosage that can treat pathophysiologic states while minimizing the endometrial effects."( Mifepristone: clinical application in general gynecology.
Kettel, LM; Morales, AJ; Murphy, AA, 1996
)
1.74
" Titration of RU-486 dosing remains imprecise due to the lack of an acceptable rapid biochemical measurement to monitor glucocorticoid action."( Mifepristone: treatment of Cushing's syndrome.
Cutler, GB; Sartor, O, 1996
)
1.74
" and high dose oral dosing regimens, with little or no activity with the oral low dose; and (3) infants resulting from surviving pregnancies were not affected by early gestation exposure."( Effects of two antiprogestins on early pregnancy in the long-tailed macaque (Macaca fascicularis).
Gu, QQ; Hendrickx, AG; Lasley, BL; Matlin, SA; Tarantal, AF; Thomas, CA; Van Look, PF; Vince, PM, 1996
)
0.29
" Results of these studies suggest: 1) both antiprogestins are roughly comparable in terminating early pregnancy, although HRP 2000 may be more efficacious when administered im, whereas mifepristone may be more effective when administered orally; 2) similar levels of biological activity are seen with the im and high-dose oral dosing regimens, with little or no activity with the oral low dose; and 3) infants resulting from surviving pregnancies were not affected by early gestation exposure."( Effects of two antiprogestins on early pregnancy in the long-tailed macaque (Macaca fascicularis).
Gu, QQ; Hendrickx, AG; Lasley, BL; Matlin, SA; Tarantal, AF; Thomas, CA; Van Look, PF; Vince, PM, 1996
)
0.49
" These increases were relatively insensitive to the concentration of reporter gene, suggesting the titration of some transcription factor(s) involved in regulating the position of the glucocorticoid dose-response curve and the agonist activity of an antiglucocorticoid."( Induction properties of a transiently transfected glucocorticoid-responsive gene vary with glucocorticoid receptor concentration.
Simons, SS; Szapary, D; Xu, M, 1996
)
0.29
" From detailed dose-response curves, corticosterone in vivo shows approximately 3% the apparent affinity of aldosterone for MR in colon and kidney, approximately 30% for those in the heart, and approximately 300% in the hippocampus."( Exclusion of corticosterone from epithelial mineralocorticoid receptors is insufficient for selectivity of aldosterone action: in vivo binding studies.
Funder, J; Myles, K, 1996
)
0.29
"Mifepristone of 10mg daily is considered to be a more ideal dosage for treatment."( [Treatment of uterine leiomyoma by two different doses of mifepristone].
Li, K; Yang, Y; Zheng, S, 1996
)
1.98
" Whole blood T-cell trafficking was determined indirectly by using the glucocorticoid receptor antagonist RU-40555 (250 ng/mL) added to ex vivo cultures of whole blood from animals dosed with prednisolone."( Influence of gender on prednisolone effects on whole blood T-cell deactivation and trafficking in rats.
Gobburu, JV; Jusko, WJ; Meno-Tetang, GM, 1999
)
0.3
" Treatment of cumulus-enclosed or denuded oocytes with increasing concentrations of cortisol or DEX for 48 h resulted in a dose-response inhibition of germinal vesicle breakdown (GVB)."( Effects of glucocorticoids on maturation of pig oocytes and their subsequent fertilizing capacity in vitro.
Chen, WY; Li, PS; Yang, JG, 1999
)
0.3
"0 ng] into the NTS did not significantly affect retention performance, but shifted the dose-response effects of post-training systemic injections of the synthetic glucocorticoid dexamethasone to the right."( Glucocorticoid receptor activation in the rat nucleus of the solitary tract facilitates memory consolidation: involvement of the basolateral amygdala.
McGaugh, JL; Roozendaal, B; Williams, CL, 1999
)
0.3
" Transfected cells were dosed with several known inducers of CYP3A4 and the levels of SPAP were measured."( A reporter gene assay to assess the molecular mechanisms of xenobiotic-dependent induction of the human CYP3A4 gene in vitro.
Gibson, GG; Goldfarb, PS; Gray, TJ; Ogg, MS; Tarbit, M; Williams, JM, 1999
)
0.3
"High dosage of mifepristone in treating ectopic pregnancy is convenient, safe, and has no side-effects."( [Mifepristone in the treatment of 47 ectopic pregnancy patients].
Liu, F; Liu, Y; Tao, G; Wu, Y; Xu, L; Zhang, H, 1998
)
1.56
" The effects of corticosterone were evaluated by administration of a glucocorticoid antagonist (RU 486) or a dosage of corticosterone previously shown to induce similar blood levels as treatment with EtOH."( Ethanol suppresses NK cell activation by polyinosinic-polycytidylic acid (poly I:C) in female B6C3F1 mice: role of endogenous corticosterone.
Collier, SD; Pruett, SB; Wu, WJ, 2000
)
0.31
"EtOH at 5-7 g/kg suppressed poly I:C-induced increases in NK cell lytic activity, and at least the lower end of this dosage range yields blood EtOH levels that are relevant for humans (0."( Ethanol suppresses NK cell activation by polyinosinic-polycytidylic acid (poly I:C) in female B6C3F1 mice: role of endogenous corticosterone.
Collier, SD; Pruett, SB; Wu, WJ, 2000
)
0.31
" Dose-response experiments indicated that the lowest stimulatory concentration of 17 beta-estradiol, DHT, and norgestrel is 10(-11) M, 10(-10) M, and 10(-10) M, respectively."( The normal epithelial cell-specific 1 (NES1) gene is up-regulated by steroid hormones in the breast carcinoma cell line BT-474.
Diamandis, EP; Grass, L; Luo, LY,
)
0.13
" We further evaluated the dose-response of ICI 182,780 and RU-486 (mifepristone) on PR and estrogen receptors (ER) in the presence of either progesterone, norgestrel or estradiol."( Is ICI 182,780 an antiprogestin in addition to being an antiestrogen?
Diamandis, EP; Grass, L; Jenkins, DJ; Magklara, A; Rosenberg Zand, RS, 2000
)
0.54
" Dose-response studies in fibroblasts indicated that the majority of the suppressive effect required concentrations characteristic of cell-surface GC receptors, a point confirmed by persistent DEX-induced suppression in the presence of RU486, an antagonist of classic cytosolic steroid hormone receptors."( Glucocorticoids induce a near-total suppression of hyaluronan synthase mRNA in dermal fibroblasts and in osteoblasts: a molecular mechanism contributing to organ atrophy.
Liu, C; Watson, CE; Werth, VP; Williams, KJ; Zhang, W, 2000
)
0.31
" The dose-response and time-response curves were bell-shaped with maximal activation at 10(-9) M and at 15 min."( Corticosterone-induced rapid phosphorylation of p38 and JNK mitogen-activated protein kinases in PC12 cells.
Chen, Y; Li, X; Qiu, J; Wang, J; Zhong, Y; Zhu, J, 2001
)
0.31
" The patients took mifepristone at a dosage 2 times anti-early pregnancy dosage."( Mifepristone in treating ectopic pregnancy.
Wang, L; Zhang, W, 1999
)
2.07
"Treatment with tyrosine at the dosage of 85 mg."( [Effects of tyrosine alone and tyrosine in combination with RU486 on early pregnancy in mice and the mechanism of action].
Duan, H; Wang, NG, 1997
)
0.3
" District Court, Eastern District of New York, ordered the FDA to return an individual dosage of RU-486 to a pregnant woman who had imported the drug from London two weeks earlier."( Benten v. Kessler.
, 1992
)
0.28
" Administration of the ligand mifepristone (MFP) up-regulated GHRH expression, as shown by elevations of IGF-I levels, and when MFP dosing was withdrawn, IGF-I returned to baseline levels."( Enhanced animal growth via ligand-regulated GHRH myogenic-injectable vectors.
Draghia-Akli, R; Ellis, KM; Hill, LA; Malone, PB; Nordstrom, JL; Schwartz, RJ, 2002
)
0.6
" In particular, the method used to deliver the transgenes and adjustment of ligand dosage are critical for in vivo gene expression."( Ligand-inducible transgene regulation for gene therapy.
Burcin, MM; O'Malley, BW; Schillinger, K; Tsai, SY; Ye, X, 2002
)
0.31
" Treatment with MTX at a dosage of 24 mg."( [Effects of methotrexate on early pregnancy in mice].
Guan, M; Wang, N; Zheng, W, 1998
)
0.3
" Treatment of transformants with various concentrations of rifampicin produced a dose-response curve with maximal induction at 10 microM (5."( A cell-based reporter gene assay for determining induction of CYP3A4 in a high-volume system.
Allen, SW; Raucy, J; Warfe, L; Yueh, MF, 2002
)
0.31
" The trial aims to identify the optimal dosage of RU-486 for preventing pregnancy and to learn whether lower doses produce fewer side effects (e."( News in contraception.
, 1994
)
0.29
" 48 hours later she must return to have a dosage of prostaglandins which cause the uterus to contract."( RU-486 hits snags in U.K.
Diconsiglio, JM,
)
0.13
"The plasma concentration of RU486 and its metabolites were studied to achieve a systematic comparison of different dosages, and to investigate the pharmacokinetics of different dosages in order to determine the optimum dosage and means of administration of RU486 in clinical applications."( [HPLC of RU 486 and its metabolites in human blood].
Bai, XM; He, CH; Shi, YE; Xu, JQ; Ye, ZH; Zhang, GQ, 1991
)
0.28
" The trials are evaluating the effectiveness of a 200 mg dosage of the drug and will continue until there is a commercial product."( Medical abortion options may advance in 1998.
, 1997
)
0.3
" This pilot study suggests that mifepristone 200 mg, followed on the same day by misoprostol 800 microg vaginally, effects abortion in women 50 to 63 days' gestation at rates comparable to regimens using longer dosing intervals between medications."( Mifepristone and vaginal misoprostol on the same day for abortion from 50 to 63 days' gestation.
Creinin, MD; Fox, MC; Harwood, B, 2002
)
2.04
" Both markers co-varied with a similar dose-response and time course after the nicotine-treatment."( Nicotine-induced inflammatory decreasing effect on passive skin arthus reaction in paraventricular nucleus-lesioned wistar rats.
Kita, T; Kubo, K; Nakashima, T; Nakatani, T; Narushima, I; Tanaka, T, 2003
)
0.32
" In this study, we show that the selective inactivation of the GR gene in the brains of mice profoundly flattened the dose-response function for cocaine intravenous self-administration and suppressed sensitization, two experimental procedures considered relevant models of addiction."( The glucocorticoid receptor as a potential target to reduce cocaine abuse.
Aouizerate, B; Deroche-Gamonet, V; Ghozland, S; Izawa, R; Jaber, M; Kellendonk, C; Le Moal, M; Piazza, PV; Schütz, G; Sillaber, I; Spanagel, R; Tronche, F, 2003
)
0.32
" In view of the pharmacokinetic data, it may be speculated that dosing of mifepristone for pregnancy termination and for emergency contraception could be reduced to approximately 100 mg and 2-5 mg, respectively."( The pharmacokinetics of mifepristone in humans reveal insights into differential mechanisms of antiprogestin action.
Heikinheimo, O; Kekkonen, R; Lähteenmäki, P, 2003
)
0.86
"Mifepristone 200 mg followed 6 to 8 hours later by misoprostol 800 microg vaginally is as effective for abortion and has significantly fewer side effects as compared with regimens using a 24-hour dosing interval."( A randomized comparison of misoprostol 6 to 8 hours versus 24 hours after mifepristone for abortion.
Chen, A; Creinin, MD; Fox, MC; Meyn, LA; Schaff, EA; Teal, S, 2004
)
2
" After a change in dosage and route of administration, a further 20 women were managed with oral mifepristone and vaginal misoprostol (group two)."( Management of late intrauterine death using a combination of mifepristone and misoprostol--experience of two regimens.
Fairley, TE; Mackenzie, F; Mackenzie, M; Owen, P, 2005
)
0.79
" Issues related to its optimal dosing and to prediction of response are discussed, as are the implications of lack of a placebo group and the use of nonblinded ratings in the present study."( An 8-week open-label trial of a 6-day course of mifepristone for the treatment of psychotic depression.
El Sheshai, A; Fawzy, W; Fayek, M; Kingsbury, SJ; Loza, N; Rady, A; Simpson, GM, 2005
)
0.58
" We believe that the observed reduction in the number of bleeding days by almost 50% compared to placebo in both the mifepristone combination group and the doxycycline group demonstrates a clinically significant improvement in bleeding patterns and that further trials are needed to compare different combinations of therapy as well as multiple dosing regimens in order to establish which is the most effective treatment option."( A pilot study to assess the effect of three short-term treatments on frequent and/or prolonged bleeding compared to placebo in women using Implanon.
Findlay, JK; Fraser, IS; Hickey, M; O'Connor, V; Palmer, D; Salamonsen, LA; Weisberg, E, 2006
)
0.54
" Chemists knew mifepristone and misoprostol were prescription drugs but less about dosage and side effects."( Availability of medical abortion pills and the role of chemists: a study from Bihar and Jharkhand, India.
Ganatra, B; Manning, V; Pallipamulla, SP, 2005
)
0.68
"This study examines bleeding pattern following medication-induced termination of pregnancy, comparing two different dosing schedules of mifepristone and misoprostol."( Bleeding after medication-induced termination of pregnancy with two dosing schedules of mifepristone and misoprostol.
Borgatta, L; Chen, AY; Mottl-Santiago, J; Vragovic, O; Wasserman, S, 2006
)
0.76
"One thousand eighty women with pregnancies up to 63 days' gestation were recruited for the study; 540 were randomized to the 6- to 8-h dosing schedule, and 540 were randomized to the 24-h dosing schedule."( Bleeding after medication-induced termination of pregnancy with two dosing schedules of mifepristone and misoprostol.
Borgatta, L; Chen, AY; Mottl-Santiago, J; Vragovic, O; Wasserman, S, 2006
)
0.56
" In addition, simultaneous dosing was highly acceptable."( Simultaneous very low dose mifepristone and vaginal misoprostol for medical abortion.
Borgatta, L; Ellis, SC; Kapp, N; Stubblefield, P, 2006
)
0.63
" 36, 52, and 60 have anti-inflammatory activity in a mouse model of inflammation after topical dosing with 52 and 60, having an effect similar to that of dexamethasone."( Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
Barker, M; Clackers, M; Copley, R; Demaine, DA; Haase, MV; House, D; Humphreys, D; Inglis, GG; Johnston, MJ; Jones, HT; Loiseau, R; Macdonald, SJ; McLay, IM; Nisbet, L; Pacquet, F; Shanahan, SE; Skone, PA; Tape, D; Uings, I; Upton, R; Vinader, VM; Washington, M, 2006
)
0.33
" A high throughput pharmacokinetic selection strategy that employs the cassette dosing of MP-Acids was developed to identify liver-targeting compounds."( Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
Backes, BJ; Fung, S; Goos-Nilsson, A; Grynfarb, M; Hamilton, GL; Jacobson, PB; Nguyen, P; von Geldern, TW; Wang, J; Wilcox, D, 2007
)
0.34
"As medical abortion with mifepristone and misoprostol becomes more prevalent, more studies are necessary to establish the dosage and regimens for multiple pregnancies associated with uterine anomalies."( Mifepristone-induced abortion in one horn and a growing fetus in another horn in a patient with a twin pregnancy in a bicornuate uterus.
Chao, A; Chao, AS; Wang, ST; Wang, TH, 2006
)
2.08
"The objective of this study was to prepare an oral dosage formulation of mifepristone that will improve the oral bioavailability of mifepristone and sustain the release of mifepristone for at least 3 days to effectively control reproduction, especially in coyotes."( Improved bioavailability of orally administered mifepristone from PLGA nanoparticles.
He, W; Horn, SW; Hussain, MD, 2007
)
0.83
"Mifepristone 200 mg and misoprostol 800 mcg vaginally used simultaneously is as effective for abortion as compared with regimens using a 24-hour dosing interval."( Mifepristone and misoprostol administered simultaneously versus 24 hours apart for abortion: a randomized controlled trial.
Bednarek, P; Creinin, MD; Lintu, H; Meyn, LA; Schreiber, CA; Wagner, MS, 2007
)
3.23
" From September 2001, a flexible dosing interval of 1, 2 or 3 days between mifepristone and misoprostol was adopted."( Termination of early pregnancy using flexible, low-dose mifepristone-misoprostol regimens.
Heikinheimo, O; Leminen, R; Suhonen, S, 2007
)
0.82
"A flexible dosing protocol of mifepristone and misoprostol is effective; thus, its use is encouraged."( Termination of early pregnancy using flexible, low-dose mifepristone-misoprostol regimens.
Heikinheimo, O; Leminen, R; Suhonen, S, 2007
)
0.87
"This study suggests that the two formulations of mifepristone are bioequivalent, which provides pharmacokinetic evidence for further reducing the dosage of mifepristone in clinical use."( Bioavailability of mifepristone in capsule versus tablet form in healthy nonpregnant women.
Li, H; Liao, A; Pang, X; Wu, X; Xiong, Z, 2008
)
0.93
" In this in vivo model, compounds 10j and 10u were active at 3 mg/kg when dosed orally."( 7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
Berrodin, TJ; Cohen, J; Fensome, A; Kern, JC; Terefenko, EA; Unwalla, R; Winneker, RC; Wrobel, J; Yudt, MR; Zhang, P; Zhang, Z, 2008
)
0.35
" However, many studies of medical management may underestimate success rates due to inconsistent inclusion criteria, different dosing regimens, and varying definitions of failed treatment."( Medical management of early pregnancy failure: efficacy.
Chen, BA; Creinin, MD, 2008
)
0.35
"Simultaneous use of mifepristone and misoprostol for second trimester medical abortion is not as effective as the regimen using a 36-38 h dosing interval."( A randomized trial to compare two dosing intervals of misoprostol following mifepristone administration in second trimester medical abortion.
Chai, J; Chen, QF; Cheng, LN; Ho, PC; Hong, QQ; Ng, E; Tang, OS, 2009
)
0.91
" All of the animals were completely infertile when dosed with 20 mg/kg during the post-coital period."( Collaborative work on evaluation of ovarian toxicity. 2) Two- or four-week repeated dose studies and fertility study of mifepristone in female rats.
Harada, C; Hayashi, M; Kobayashi, K; Kuroda, J; Kusama, H; Nagasawa, T; Okuhara, Y; Onozato, T; Tamura, T; Terashima, Y; Yokoi, R, 2009
)
0.56
" This choice should not be made lightly, as guinea pigs have many disadvantages compared to the traditional species, including limited historical control data, variability in pregnancy rates, small and variable litter size, long gestation, relative maturity at birth, and difficulty in dosing and breeding."( The guinea pig as an animal model for developmental and reproductive toxicology studies.
Rocca, MS; Wehner, NG, 2009
)
0.35
" PCOS induced rats were administered varying dosing regimens of noscapine and were further compared with flutamide, the conventional drug for PCOS."( Relevance of an opioid, noscapine in reducing cystogeneses in rat experimental model of polycystic ovary syndrome.
Priyadarshani, A, 2009
)
0.35
" The present findings suggest that glucocorticoid-regulated oscillation in the hepatic MGMT expression is the underlying cause of dosing time-dependent changes in DTIC-induced hepatotoxicity."( Glucocorticoid-dependent expression of O(6)-methylguanine-DNA methyltransferase gene modulates dacarbazine-induced hepatotoxicity in mice.
Egawa, T; Horiguchi, M; Kaji, H; Kim, J; Koyanagi, S; Makino, K; Matsunaga, N; Ohdo, S, 2010
)
0.36
" Dose-response LHR using patient basophils was observed for different hormones but after 3 months persisted only for 5β-pregnanediol."( A case of progesterone-induced anaphylaxis, cyclic urticaria/angioedema, and autoimmune dermatitis.
Bernstein, DI; Bernstein, IL; Bernstein, JA; Lummus, ZL, 2011
)
0.37
" The LUC and the Dsred expression assumes the dosage dependence along with RU486 to increase; after the Ad-RUNrf2 infects the H460 cell, through RTPCR and Western the Blot result demonstrated that the expression of Nrf2 increases along with the RU486 dosage increases, after removing RU486, the Nrf2 expression is weaken."( [In vitro construction and confirmation of adenovirus containing a mifepristone (RU486)-inducible regulation system for NRF2 gene].
Cai, QQ; Hong, GL; Li, LF; Liang, H; Lu, ZQ; Qiu, QM; Wang, DM; Wu, HP, 2011
)
0.61
" Future research should prioritize misoprostol-only regimens with shorter dosing intervals."( Comparing two early medical abortion regimens: mifepristone+misoprostol vs. misoprostol alone.
Blum, J; Dabash, R; Diop, A; Nga, NT; Ngoc, NT; Raghavan, S; Winikoff, B, 2011
)
0.63
" Dosing every 3 h is superior to less frequent dosing, although intervals of up to 12 h are effective when using higher doses (600 or 800 mcg) of misoprostol."( Clinical guidelines. Labor induction abortion in the second trimester.
Borgatta, L; Kapp, N, 2011
)
0.37
"Both one- and two-day dosing intervals seem to be suitable for second trimester medical TOP, but women with no previous deliveries and those whose gestation exceeds 16 weeks may benefit from the longer interval."( One- and two-day dosing intervals between mifepristone and misoprostol in second trimester medical termination of pregnancy--a randomized trial.
Heikinheimo, O; Mentula, M; Suhonen, S, 2011
)
0.63
" These data were used to underwrite a clinical assessment of PF-02413873 in a randomized, double-blinded, third-party open, placebo-controlled, dose-escalation study in healthy female volunteers with dosing for 14 days."( The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human.
Apfeldorfer, C; Bess, K; Brown, A; Bungay, P; Gibson, KR; Hawcock, T; Howe, DC; Jones, G; McLeod, A; Mount, NM; Pullen, N; Ramsey, S; Richard, J; Tweedy, S; Walley, R, 2011
)
0.37
" Efficacy was evaluated 15 hours after misoprostol dosing began and the procedure was considered complete if uterine evacuation was achieved without recourse to surgical evacuation."( Mifepristone and misoprostol compared with misoprostol alone for second-trimester abortion: a randomized controlled trial.
Blum, J; Minh, NTH; Nga, NTB; Ngoc, NTN; Phan, VQ; Raghavan, S; Shochet, T; Winikoff, B, 2011
)
1.81
" Treatment of cerebellar granule neuron cultures with both GCs significantly reduced the percentage of proliferating-cell nuclear antigen (PCNA) positive neurons and increased NeuN positive neurons, with similar dose-response relationship as in vivo."( Glucocorticoids dexamethasone and hydrocortisone inhibit proliferation and accelerate maturation of chicken cerebellar granule neurons.
Aden, P; Goverud, IL; Liestøl, K; Løberg, EM; Lømo, J; Mæhlen, J; Paulsen, RE, 2011
)
0.37
" After transsphenoidal surgery, Cyberknife radiosurgery, ketoconazole, and metyrapone did not control her disease, and she was prescribed mifepristone, which was titrated to a maximal dosage of 1200 mg daily with subsequent symptom improvement."( Successful long-term treatment of Cushing disease with mifepristone (RU486).
Basina, M; Feldman, D; Hoffman, AR; Liu, H,
)
0.58
"The Caspase-3 protein expression was observed in granulosa cells of developing follicles, while the positive expression level and integrated optical density (IOD) value were increased along with the dosage of mifepristone increasing."( [The expression of Caspase-3 in granulosa cells of endometriosis treated with mifepristone].
Cai, LR; Chen, B; Qiao, L; Xiong, Y; Xu, KH, 2012
)
0.79
" The aim of this work is to develop a semi-mechanistic model to characterize the relationship between IL12 and IFNγ in wild-type and knock-out mice for the IFNγ receptor treated with HC-Ad/RUmIL12 under different dosing regimens in order to better understand the key mechanisms controlling the system."( Target-mediated disposition model describing the dynamics of IL12 and IFNγ after administration of a mifepristone-inducible adenoviral vector for IL-12 expression in mice.
Alzuguren, P; Berraondo, P; Hernandez-Alcoceba, R; Janda, A; Parra-Guillen, ZP; Troconiz, IF, 2013
)
0.61
"To explore the lowest effective dosage of mifepristone combined with misoprostol in terminating ultra-early pregnancy."( [The lowest dosages of mifepristone and misoprostol to terminate ultra-early pregnancy].
Chen, DJ; Du, PL; Li, CL; Liu, MX; Liu, Q; Sheng, XJ; Wei, M; Weng, HN, 2012
)
0.95
" The recommended starting dosage of mifepristone is 300 mg/day."( Mifepristone for management of Cushing's syndrome.
Laufgraben, MJ; Morgan, FH, 2013
)
2.11
"The pharmacological dosage of dehydroepiandrosterone (DHEA) protects against chemically induced carcinogenesis."( Dehydroepiandrosterone post-transcriptionally modifies CYP1A2 induction involving androgen receptor.
Belic, A; Dvorak, Z; Monostory, K; Orbán, E; Porrogi, P; Rozman, D; Temesvári, M; Tóth, K; Vrzal, R, 2013
)
0.39
"To compare the efficacy of a shorter interval (24hours) between misoprostol and mifepristone administration with that of the conventional dosing interval (48hours) for second-trimester termination of pregnancy (TOP)."( Dosing interval of 24hours versus 48hours between mifepristone and misoprostol administration for mid-trimester termination of pregnancy.
Chaudhuri, P; Das, C; Mandal, A; Mazumdar, A, 2014
)
0.88
"The rate of successful abortions was similar with the 24-hour and 48-hour dosing intervals (95."( Dosing interval of 24hours versus 48hours between mifepristone and misoprostol administration for mid-trimester termination of pregnancy.
Chaudhuri, P; Das, C; Mandal, A; Mazumdar, A, 2014
)
0.66
"The 24-hour dosing interval between misoprostol and mifepristone administration seems to be as effective as the 48-hour dosing interval for second trimester TOP."( Dosing interval of 24hours versus 48hours between mifepristone and misoprostol administration for mid-trimester termination of pregnancy.
Chaudhuri, P; Das, C; Mandal, A; Mazumdar, A, 2014
)
0.91
"46 ng/mL progesterone activity in a dose-response manner."( Molecular screening of Chinese medicinal plants for progestogenic and anti-progestogenic activity.
Ahmed, HM; Cheng, WT; Ou, BR; Tang, YC; Yeh, JY, 2014
)
0.4
" Standardised evaluation of pain is needed and the correlation between the dosage of misoprostol and the intensity of pain must be assessed in future studies."( Pain during medical abortion, the impact of the regimen: a neglected issue? A review.
Bombas, T; Cameron, S; Fiala, C; Gemzell-Danielsson, K; Parachini, M; Saya, L, 2014
)
0.4
" Five candidate positive regulators of life span were identified, including dosage compensation regulator Unr and three X-linked genes: multi sex combs (PcG gene), Dopamine 2-like receptor and CG14215."( The progesterone antagonist mifepristone/RU486 blocks the negative effect on life span caused by mating in female Drosophila.
Brookes, N; Keroles, D; Landis, GN; Salomon, MP; Sekimura, T; Tower, J, 2015
)
0.71
" While good profiles of contraceptive use are available for many countries and we have good technical data on the MA drugs' efficacy, dosages and regimens such as home dosage of misoprostol versus clinic dosage, we have very little information about the quantities of MA drugs sold, how they are used, where they are used, and, in the case of misoprostol, for what purposes."( Medical abortion: the hidden revolution.
Harvey, P, 2015
)
0.42
" The propofol self-administration model was established by a fixed ratio 1 (FR1) schedule of reinforced dosing over successive 14days in rats."( Glucocorticoid receptor mediated the propofol self-administration by dopamine D1 receptor in nucleus accumbens.
Chen, Z; Dong, Z; Ge, RS; Lian, Q; Liang, Y; Lin, W; Wang, B; Wang, S; Wu, B; Zhang, G, 2016
)
0.43
" Median misoprostol dosing time was shorter in the 24-hour interval arm (7."( Simultaneous Administration Compared With a 24-Hour Mifepristone-Misoprostol Interval in Second-Trimester Abortion: A Randomized Controlled Trial.
Abbas, DF; Blum, J; Chi, HT; Martin, R; Nga, NT; Ngoc, NT; Winikoff, B, 2016
)
0.68
" Simultaneous dosing results in less total time from the first clinical contact to complete abortion."( Simultaneous Administration Compared With a 24-Hour Mifepristone-Misoprostol Interval in Second-Trimester Abortion: A Randomized Controlled Trial.
Abbas, DF; Blum, J; Chi, HT; Martin, R; Nga, NT; Ngoc, NT; Winikoff, B, 2016
)
0.68
"The aim of the study was to assess the efficacy and acceptability of a regimen using mifepristone and buccal misoprostol with unlimited dosing for second trimester abortion in Armenia."( Second trimester medical abortion with mifepristone followed by unlimited dosing of buccal misoprostol in Armenia.
Abrahamyan, R; Avagyan, G; Chong, E; Louie, KS; Tsereteli, T; Winikoff, B, 2017
)
0.95
" Recent studies on the continuous dosing of misoprostol have produced critical evidence to support continued dosing until expulsion."( Update on second trimester medical abortion.
Lerma, K; Shaw, KA, 2017
)
0.46
" Further research is needed to refine second trimester medical abortion methods, specific to the mifepristone, misoprostol dosing interval."( Update on second trimester medical abortion.
Lerma, K; Shaw, KA, 2017
)
0.67
"The addition of mifepristone to medical treatment regimens for first trimester miscarriage significantly decreased the need for repeat medical dosing and surgical curettage."( Combination therapy with mifepristone and misoprostol for the management of first trimester miscarriage: Improved success.
Dunford, A; Fyfe, R, 2018
)
1.13
"The survey found that 99% of pharmacy workers visited had knowledge of MR procedures but only two-thirds (67%) could state the legal time limit correctly; they mentioned misoprostol (86%) over mifepristone-misoprostol combination (78%) as a procedure of MR with medication (MRM); 36% reported knowing the recommended dosage of mifepristone-misoprostol combination; 70% reported providing information on effectiveness of the medicines; 50% reported recommending at least one follow-up visit to them; 63% reported explaining possible complications of using the medications; and 47% reported offering any post-MR contraception to their clients."( Provision of menstrual regulation with medication among pharmacies in three municipal districts of Bangladesh: a situation analysis.
Ahmed, A; Ahmmed, F; Al Haque, N; Alam, A; Huda, FA; Karim, F; Mahmood, HR; Sarker, BK, 2018
)
0.67
"We found knowledge gaps regarding recommended dosage for MRM and inconsistent practice in informing women on effectiveness, follow-up visits, possible complications and provision of post-MR contraceptives among the pharmacy workers, particularly during the mystery client visits."( Provision of menstrual regulation with medication among pharmacies in three municipal districts of Bangladesh: a situation analysis.
Ahmed, A; Ahmmed, F; Al Haque, N; Alam, A; Huda, FA; Karim, F; Mahmood, HR; Sarker, BK, 2018
)
0.48
" This led to the discovery of AZD9567 (15) with excellent in vivo efficacy when dosed orally in a rat model of joint inflammation."( Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Berger, M; Bird, J; Chang, HF; Chapman, D; Dearman, M; Drmota, T; Edenro, G; Edman, K; Geschwindner, S; Harrison, R; Hegelund-Myrbäck, T; Hendrickx, R; Köhler, C; Lawitz, K; Lepistö, M; Llinas, A; Malmberg, J; Nikitidis, A; Olsson, RI; Ripa, L; Svanberg, P; Thorne, P; Ullah, V; Wissler, L, 2018
)
0.48
" High-dose progestins may inhibit brain tumor growth by downregulating PR-B, yet the dosage thresholds may differ between glial and meningeal tumors due to higher total PR expression in meningiomas."( Reproductive epidemiology of glial tumors may reveal novel treatments: high-dose progestins or progesterone antagonists as endocrino-immune modifiers against glioma.
Altinoz, MA; Elmaci, I; Ozpinar, A, 2019
)
0.51
" Our primary outcome was treatment success with simultaneous dosing compared with a regimen with a 24- to 48-hour interval between medications."( Simultaneous Compared With Interval Medical Abortion Regimens Where Home Use Is Restricted.
Aiken, ARA; Lohr, PA; Scott, JG; Starling, JE, 2018
)
0.48
" Overall success rates were high with both regimens but lower with simultaneous than with interval dosing (94."( Simultaneous Compared With Interval Medical Abortion Regimens Where Home Use Is Restricted.
Aiken, ARA; Lohr, PA; Scott, JG; Starling, JE, 2018
)
0.48
" Pragmatic use of simultaneous dosing is reasonable given the small difference in effectiveness."( Simultaneous Compared With Interval Medical Abortion Regimens Where Home Use Is Restricted.
Aiken, ARA; Lohr, PA; Scott, JG; Starling, JE, 2018
)
0.48
" Dose-response results further suggest that effects of contraceptives containing MPA on HIV-1 acquisition and disease progression may be critically dependent on dose, time after injection and intrinsic factors that affect serum concentrations in women."( Medroxyprogesterone acetate, unlike norethisterone, increases HIV-1 replication in human peripheral blood mononuclear cells and an indicator cell line, via mechanisms involving the glucocorticoid receptor, increased CD4/CD8 ratios and CCR5 levels.
Avenant, C; Bick, AJ; Govender, Y; Hapgood, JP; Maritz, MF; Ray, RM; Tomasicchio, M; Woodland, JG, 2018
)
0.48
"PAEC features may be explained by the altered genes and their networks affecting tissue architecture although not involved in endometrial cancer signaling pathways, and thus, treatment with mifepristone at this dosage does not show any adverse effect at endometrial level."( Molecular characterization of PRM-associated endometrial changes, PAEC, following mifepristone treatment.
Berger, C; Boggavarapu, N; Engman, M; Falk, A; Gemzell-Danielsson, K; Hörnaeus, K; Lalitkumar, PGL; Norlin, E; Queckbörner, S; Ramström, M, 2018
)
0.9
" Structure-based modification of mifepristone led to the discovery of ORIC-101 (28), a highly potent steroidal GR antagonist with reduced androgen receptor (AR) agonistic activity amenable for dosing in androgen receptor positive tumors and with improved CYP2C8 and CYP2C9 inhibition profile to minimize drug-drug interaction potential."( Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Chen, C; Du, X; Eksterowicz, J; Fantin, VR; Huang, E; Huang, T; Jackson, E; Jahchan, N; Kawai, H; McGee, LR; Medina, JC; Rew, Y; Sun, D; Sutimantanapi, D; Waszczuk, J; Yan, X; Ye, Q; Zavorotinskaya, T; Zhou, H; Zhu, L, 2018
)
0.76
" To avoid unintended pregnancy in the pretreatment period, the dosage used should, ideally, also be effective for contraception and the pretreatment period should be kept as short as possible."( Mifepristone treatment prior to insertion of a levonorgestrel releasing intrauterine system for improved bleeding control - a randomized controlled trial.
Gemzell-Danielsson, K; Kopp Kallner, H; Papaikonomou, K; Söderdahl, F, 2018
)
1.92
" Initial dose-response assessments on sperm hyperactivation determined the optimum concentration of P4 (10 nM), mibefradil (a non-specific Ca2+ channel antagonist; 5µM), NNC 55-0396 dihydrochloride (NNC; a CatSper antagonist; 2µM), mifepristone (a classical and membrane P4 receptor antagonist; 400nM) and AG205 (a membrane P4 receptor antagonist; 10μM)."( Progesterone induces the release of bull spermatozoa from oviductal epithelial cells.
Cronin, S; Donnellan, E; Fair, S; Romero-Aguirregomezcorta, J, 2019
)
0.7
" In accordance with the misoprostol dosing recommendations by the International Federation of Gynecology and Obstetrics (FIGO), the incidences of uterine rupture and cervical laceration are relatively high in Chinese pregnant women."( Clinical application of low-dose misoprostol in the induced labor of 16 to 28 weeks pathological pregnancies (a STROBE-compliant article).
Du, X; Duan, J; Huang, YM; Wang, Y; Yang, Y, 2019
)
0.51
" Some evidence shows the feasibility of same-day cervical preparation before D&E at 20-24 weeks using Dilapan-S® with adjunctive misoprostol or serial repeat dosing of misoprostol, but same-day preparation should be limited to providers with significant experience with these regimens."( Society of Family Planning clinical recommendations: Cervical preparation for dilation and evacuation at 20-24 weeks' gestation.
Diedrich, JT; Drey, EA; Newmann, SJ, 2020
)
0.56
" A common evidence-based medical regimen for early pregnancy loss uses misoprostol, a prostaglandin E1 analog, with a dosage of 800 μg, self-administered vaginally."( Management of early pregnancy loss with mifepristone and misoprostol: clinical predictors of treatment success from a randomized trial.
Atrio, JM; Creinin, MD; Koelper, N; McAllister, A; Sammel, MD; Schreiber, CA; Sonalkar, S, 2020
)
0.83
" Tailored dosing of CORT125281 may allow tissue-specific inhibition of GR transcriptional activity."( The selective glucocorticoid receptor antagonist CORT125281 has tissue-specific activity.
Heckmans, KML; Hoekstra, M; Houtman, R; Hunt, H; Koorneef, LL; Kroon, J; Meijer, OC; van Dorst, MMAR; Viho, EMG; Wahl, LF, 2020
)
0.56
" There was no significant difference in dosing intervals between mifepristone and misoprostol and routes of misoprostol administration in combination or misoprostol alone regimens."( Medical termination for pregnancy in early first trimester (≤ 63 days) using combination of mifepristone and misoprostol or misoprostol alone: a systematic review.
Abubeker, FA; Kim, C; Lavelanet, A; Rodriguez, MI, 2020
)
1.02
"A dose-response study was made of the broad-spectrum gonadal steroid agonist tibolone (TBL) on lordosis behavior in estradiol benzoate (EB: 5 µg) primed rats."( Tibolone facilitates lordosis behavior through estrogen, progestin, and GnRH-1 receptors in estrogen-primed rats.
Domínguez-Ordoñez, R; García-Juárez, M; González-Flores, O; Lima-Hernández, FJ; Montes-Narváez, O; Pfaus, JG, 2020
)
0.56
"Both 1- and 2-day dosing intervals between mifepristone and misoprostol are suitable for clinical use for second-trimester medical termination of pregnancy."( Different dosing intervals of mifepristone-misoprostol for second-trimester termination of pregnancy: A meta-analysis and systematic review.
Chen, M; Song, L; Wei, T; Wu, L; Xiong, W; Yan, A; Zeng, M; Zhang, J; Zu, Q, 2021
)
1.17
"The results indicated that mifepristone promoted the expressions of CD80, CD86, and ICAM-1 in a dosage dependent manner."( Mifepristone regulates Tregs function mediated by dendritic cells through suppressing the expression of TGF-β.
Cao, L; Guo, Q; Huang, L; Li, Y; Niu, X; Qian, Z, 2021
)
2.36
" The optimal dosing of ibuprofen is unclear, but a single dose of ibuprofen 1600 mg was shown to be effective, and it was less certain whether 800 mg was effective."( Pain management for medical abortion before 14 weeks' gestation.
Cameron, S; Morroni, C; Reynolds-Wright, JJ; Woldetsadik, MA, 2022
)
0.72
" To assess label comprehension, we developed 11 primary and 13 secondary communication objectives related to indications for use, eligibility, dosing regimen, contraindications, warning signs, side effects, and recognizing the risk of treatment failure, with corresponding target performance thresholds (80-90% accuracy)."( Comprehension of an Over-the-Counter Drug Facts Label Prototype for a Mifepristone and Misoprostol Medication Abortion Product.
Biggs, MA; Blanchard, K; Bustamante, CK; Choimorrow, SY; Ehrenreich, K; Grossman, D; Hauser, D; Hernandez, Y; Kapp, N; Kromenaker, T; Moayedi, G; Morris, N; Perritt, JB; Ralph, L; Raymond, EG; Valladares, ES; White, K, 2022
)
0.96
" The overall sample met performance criteria for 10 of the 11 primary communication objectives (93-99% correct) related to indications for use, eligibility for use, the dosing regimen, and contraindications; young people met nine and people with limited literacy met eight of the 11 performance criteria."( Comprehension of an Over-the-Counter Drug Facts Label Prototype for a Mifepristone and Misoprostol Medication Abortion Product.
Biggs, MA; Blanchard, K; Bustamante, CK; Choimorrow, SY; Ehrenreich, K; Grossman, D; Hauser, D; Hernandez, Y; Kapp, N; Kromenaker, T; Moayedi, G; Morris, N; Perritt, JB; Ralph, L; Raymond, EG; Valladares, ES; White, K, 2022
)
0.96
" The optimal dosing of ibuprofen is unclear, but a single dose of ibuprofen 1600mg was shown to be effective and it was less certain whether 800mg was effective."( Pain management for medical abortion before 14 weeks' gestation: A systematic review.
Cameron, ST; Morroni, C; Reynolds-Wright, JJ; Woldetsadik, MA, 2022
)
0.72
" Subsequently in a dose-response study, CAFs showed an average of ∼20% higher cell viability when compared to BAFs, indicative of drug resistance to MPA."( Aberrant upregulation of CDK1 contributes to medroxyprogesterone acetate (MPA) resistance in cancer-associated fibroblasts of the endometrium.
Chung, I; Godoy, A; Gunasagran, Y; Mat Adenan, NA; Omar, IS; Teo, IH, 2022
)
0.72
" The cumulative dose-response of fludrocortisone (FLU) and dexamethasone (DEX) was measured alone or in the presence of steroid receptor antagonist mifepristone (MIF) or spironolactone (SPR)."( Non-genomic uterorelaxant actions of corticosteroid hormones in rats: An in vitro and in vivo study.
Barna, T; Benyhe, S; Gáspár, R; Mirdamadi, M; Samavati, R; Schaffer, A; Szécsi, M; Szűcs, E; Szűcs, KF, 2022
)
0.92
" No statistical difference was observed in induction failure rate between ethacridine dosage groups of < 75mg and ≥ 75mg (0/25, vs."( Mifepristone combined with ethacridine lactate for third-trimester stillbirth induction: a 5-year experience from Shanghai.
Huang, RJ; Li, J; Ma, J; Xue, RH; Yao, YL; Zhang, L, 2022
)
2.16
" In the low dosage used, mifepristone likely acts as an agonist for PGRMC-1 protein."( The role of progesterone and the progesterone receptor in cancer: progress in the last 5 years.
Check, DL; Check, JH, 2023
)
1.21
" Lowering of the misoprostol dosage with prior CS may reduce uterine rupture, although this hypothesis requires ongoing research."( Mifepristone priming and subsequent misoprostol for second trimester medical abortion in women with previous caesarean delivery.
Dickinson, JE; Doherty, DA, 2023
)
2.35
" The optimal dosing of prostaglandin to achieve the highest efficacy with the lowest proportion of complications remains to be established."( Medical abortion in the second trimester - an update.
Kopp Kallner, H, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
abortifacientA chemical substance that interrupts pregnancy after implantation.
contraceptive drugA chemical substance that prevents or reduces the probability of conception.
synthetic oral contraceptiveAn oral contraceptive which owes its effectiveness to synthetic preparation.
hormone antagonistA chemical substance which inhibits the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
3-oxo-Delta(4) steroidA 3-oxo steroid conjugated to a C=C double bond at the alpha,beta position.
acetylenic compoundAny organic molecule containing a C#C bond.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (125)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency28.18380.004023.8416100.0000AID485290
Chain A, Beta-lactamaseEscherichia coli K-12Potency25.11890.044717.8581100.0000AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency15.84890.631035.7641100.0000AID504339
Chain A, Ferritin light chainEquus caballus (horse)Potency14.12545.623417.292931.6228AID485281
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
dopamine D1 receptorHomo sapiens (human)Potency0.01030.00521.30228.1995AID624455
glp-1 receptor, partialHomo sapiens (human)Potency11.22020.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency12.38070.100020.879379.4328AID588453; AID588456
pregnane X receptorRattus norvegicus (Norway rat)Potency7.94330.025127.9203501.1870AID651751
RAR-related orphan receptor gammaMus musculus (house mouse)Potency25.61980.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency34.61670.173734.304761.8120AID1346859; AID1346924
ATAD5 protein, partialHomo sapiens (human)Potency21.92630.004110.890331.5287AID493106; AID493107
Fumarate hydrataseHomo sapiens (human)Potency33.17340.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency50.11870.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency10.00000.35487.935539.8107AID624146
SMAD family member 3Homo sapiens (human)Potency34.61670.173734.304761.8120AID1346859; AID1346924
TDP1 proteinHomo sapiens (human)Potency25.85800.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency38.33670.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency5.96050.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID588515; AID588516; AID743035; AID743040; AID743042; AID743053; AID743054; AID743063
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency14.12540.707912.194339.8107AID720542
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency2.72250.000657.913322,387.1992AID1259378
hypothetical protein, conservedTrypanosoma bruceiPotency19.83840.223911.245135.4813AID624147; AID624173
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency76.95880.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency0.00380.000417.946075.1148AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency15.00300.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.23020.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency0.28280.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency14.12540.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency6.71670.000214.376460.0339AID588533; AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency28.64780.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency13.10700.000817.505159.3239AID1159527; AID1159531; AID588544
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.41310.001530.607315,848.9004AID1224819; AID1224820; AID1224821; AID1224823; AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency36.30630.375827.485161.6524AID588526; AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency24.61760.005428.02631,258.9301AID1346982; AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.09250.000229.305416,493.5996AID1259244; AID1259248; AID588513; AID588514; AID743069; AID743075; AID743078; AID743079; AID743080; AID743091
GVesicular stomatitis virusPotency1.73770.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency7.76190.00108.379861.1304AID1645840
polyproteinZika virusPotency33.17340.00308.794948.0869AID1347053
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency12.58930.707936.904389.1251AID504333
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency16.77770.001024.504861.6448AID588534; AID588535; AID743212; AID743215; AID743227
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency11.23810.001019.414170.9645AID588536; AID588537; AID743094; AID743140; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency28.49780.023723.228263.5986AID588541; AID743222; AID743223; AID743241
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency8.01690.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency21.26050.001723.839378.1014AID743083
activating transcription factor 6Homo sapiens (human)Potency26.83250.143427.612159.8106AID1159516
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency10.00000.10009.191631.6228AID1346983
Histone H2A.xCricetulus griseus (Chinese hamster)Potency77.95570.039147.5451146.8240AID1224845
D(1A) dopamine receptorHomo sapiens (human)Potency2.31080.02245.944922.3872AID488982
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.23410.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency19.62210.006026.168889.1251AID488953; AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency23.10930.00419.984825.9290AID504444
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency14.39040.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency1.67840.042027.378961.6448AID743210
huntingtin isoform 2Homo sapiens (human)Potency35.48130.000618.41981,122.0200AID1688
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency23.28090.00669.809418.4927AID1347050
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency17.47450.00378.618923.2809AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency10.86640.000627.21521,122.0200AID651741; AID743202; AID743219
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency31.62280.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency8.91250.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency8.91250.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency8.91250.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency8.91250.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency18.58160.004611.374133.4983AID624296
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.12540.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency17.78280.125912.234435.4813AID1458
M-phase phosphoprotein 8Homo sapiens (human)Potency11.91730.177824.735279.4328AID488949
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency17.78280.891312.067628.1838AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.58930.015812.3113615.5000AID1461
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency43.86690.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency1.73770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.73770.01238.964839.8107AID1645842
Glucocorticoid receptorHomo sapiens (human)Potency0.00080.00080.01390.0270AID74238
Cellular tumor antigen p53Homo sapiens (human)Potency41.60760.002319.595674.0614AID651631; AID720552
Androgen receptorHomo sapiens (human)Potency0.00500.00500.13700.2690AID39151
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency43.86690.001551.739315,848.9004AID1259244
D(1A) dopamine receptorSus scrofa (pig)Potency11.66810.00378.108123.2809AID2667
Guanine nucleotide-binding protein GHomo sapiens (human)Potency35.48131.995325.532750.1187AID624288
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.73770.01238.964839.8107AID1645842
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency18.13480.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency22.54670.011912.222168.7989AID588378; AID651632
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.73770.01238.964839.8107AID1645842
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.00600.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, PROGESTERONE RECEPTORHomo sapiens (human)Ki0.00080.00080.00080.0008AID977610
Glucocorticoid receptor Canis lupus familiaris (dog)IC50 (µMol)0.02640.02020.02640.0326AID1356945; AID1356946
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)2.02000.11007.190310.0000AID1473738
Estrogen receptorHomo sapiens (human)IC50 (µMol)6.61030.00000.723732.7000AID387088; AID405939; AID487148; AID494981; AID625258; AID68745; AID68887; AID68891
Estrogen receptorHomo sapiens (human)Ki6.73850.00000.42297.9070AID238475; AID487139; AID625258; AID68900
Glucocorticoid receptorHomo sapiens (human)IC50 (µMol)0.25870.00000.495310.0000AID1240576; AID1356349; AID1356893; AID1356941; AID1356942; AID1356952; AID1380129; AID1380132; AID1607932; AID1607943; AID1607944; AID1797837; AID1833848; AID241310; AID241689; AID242105; AID248130; AID248634; AID248679; AID267771; AID267772; AID267774; AID276767; AID276768; AID290022; AID294499; AID300612; AID300613; AID300615; AID304379; AID304380; AID304384; AID309725; AID326404; AID387090; AID405942; AID426410; AID469718; AID483896; AID483897; AID483900; AID487151; AID494984; AID625263; AID73765; AID73929; AID74075; AID74076; AID74080; AID74091; AID74213
Glucocorticoid receptorHomo sapiens (human)Ki0.01490.00010.38637.0010AID1228843; AID1240570; AID1482036; AID1482037; AID238476; AID238669; AID244578; AID289551; AID289552; AID289553; AID306213; AID309452; AID309453; AID309461; AID318132; AID318133; AID473409; AID487141; AID625263; AID74220; AID74223
Prostaglandin G/H synthase 1Ovis aries (sheep)IC50 (µMol)0.00030.00032.177410.0000AID162121
Tyrosine-protein kinase FynHomo sapiens (human)IC50 (µMol)21.35700.00021.67898.6800AID625185
Progesterone receptorHomo sapiens (human)IC50 (µMol)0.13470.00000.580710.0000AID1356323; AID1356328; AID1356348; AID1356934; AID147646; AID147649; AID1607929; AID162117; AID162121; AID162124; AID162129; AID162131; AID162273; AID162436; AID162593; AID162600; AID162608; AID1797838; AID208687; AID226104; AID226106; AID240495; AID242073; AID266611; AID290021; AID294498; AID306214; AID309724; AID326396; AID326397; AID32841; AID345893; AID345895; AID387086; AID405937; AID426409; AID461850; AID47382; AID483899; AID487138; AID494980; AID638167
Progesterone receptorHomo sapiens (human)Ki0.00450.00030.03160.3997AID1228844; AID1240574; AID162283; AID162284; AID162286; AID162290; AID162293; AID162467; AID162470; AID238443; AID239976; AID245862; AID266610
Glucocorticoid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.77400.00010.39756.0000AID1240577; AID1797838; AID213399; AID242045; AID242414; AID242415
Glucocorticoid receptorMus musculus (house mouse)IC50 (µMol)0.00220.00220.20610.6000AID147648
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.00220.00150.76005.0740AID625263
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.00100.00070.76537.0010AID625263
Mineralocorticoid receptor Homo sapiens (human)IC50 (µMol)2.53370.00030.748410.0000AID126269; AID126275; AID126279; AID126443; AID1797838; AID242171; AID387091; AID405943; AID487152; AID494986
Mineralocorticoid receptor Homo sapiens (human)Ki3.83030.00030.17380.8510AID1240572; AID238538; AID487142
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)9.50000.00011.753610.0000AID1356930; AID1607941
Cytochrome P450 3A4Homo sapiens (human)Ki4.70000.00011.41629.9000AID1657019; AID589138
Coagulation factor VIIHomo sapiens (human)IC50 (µMol)0.00030.00020.83363.3000AID266611
Androgen receptorHomo sapiens (human)IC50 (µMol)0.29880.00000.875310.0000AID1356347; AID147647; AID1797838; AID241977; AID242094; AID242138; AID248487; AID326402; AID387089; AID38975; AID38979; AID38980; AID38990; AID38993; AID405941; AID483898; AID487150; AID494983
Androgen receptorHomo sapiens (human)Ki0.00870.00020.42407.2000AID1240573; AID238359; AID39009; AID39138; AID39147; AID487132
Cytochrome P450 2C8Homo sapiens (human)IC50 (µMol)1.50000.00081.88487.9000AID1356931; AID1607942
Thyroid hormone receptor alphaHomo sapiens (human)Ki1.25000.00020.00390.0096AID238621
Thyroid hormone receptor betaHomo sapiens (human)Ki2.25000.00010.00070.0023AID238598
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)4.90000.00002.800510.0000AID1356932
Steroid 17-alpha-hydroxylase/17,20 lyase Rattus norvegicus (Norway rat)IC50 (µMol)0.00160.00161.67077.6700AID294499
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC50 (µMol)0.55500.11003.26419.0330AID625146
Tissue factorHomo sapiens (human)IC50 (µMol)0.00030.00010.734410.0000AID266611
Androgen receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00830.00101.979414.1600AID625228
Androgen receptorRattus norvegicus (Norway rat)Ki0.00560.00031.21858.9270AID625228
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)26.46000.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki12.08200.00020.725710.0000AID625202
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.00140.00031.38338.4000AID294498
Glycine receptor subunit betaRattus norvegicus (Norway rat)IC50 (µMol)0.00220.00150.76005.0740AID625263
Glycine receptor subunit betaRattus norvegicus (Norway rat)Ki0.00100.00070.78467.0010AID625263
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00220.00150.80445.0740AID625263
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.00100.00070.78467.0010AID625263
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)0.00780.00021.557410.0000AID242094
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.00220.00150.76005.0740AID625263
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.00100.00070.78467.0010AID625263
Substance-P receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00150.00002.751810.0000AID290021; AID290022
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)2.45700.00010.813310.0000AID625163
Mu-type opioid receptorHomo sapiens (human)Ki0.99700.00000.419710.0000AID625163
Kappa-type opioid receptorHomo sapiens (human)IC50 (µMol)20.09600.00001.201110.0000AID625162
Kappa-type opioid receptorHomo sapiens (human)Ki8.03800.00000.362410.0000AID625162
Mitogen-activated protein kinase 14Homo sapiens (human)IC50 (µMol)83.06100.00010.72667.8000AID625182
Estrogen receptor betaHomo sapiens (human)IC50 (µMol)3.51400.00010.529432.7000AID487149; AID68745; AID68887; AID68891
Estrogen receptor betaHomo sapiens (human)Ki4.54200.00000.12512.8760AID238468; AID487140; AID68900
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)26.28000.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki11.04700.00000.490110.0000AID625223
Glucocorticoid receptorSus scrofa (pig)IC50 (µMol)0.01530.01090.01530.0197AID1356949; AID1356950
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)EC50 (µMol)10.00000.00000.53054.4000AID487143
Glucocorticoid receptorHomo sapiens (human)EC50 (µMol)0.72920.00040.05401.0000AID1356894; AID1797746; AID254646; AID297856; AID300614; AID487146
Glucocorticoid receptorHomo sapiens (human)Kd0.01500.01500.02200.0290AID1544123
Progesterone receptorHomo sapiens (human)EC50 (µMol)5.00020.00010.40478.2000AID161798; AID487137
Tegument protein VP16Human alphaherpesvirus 1 strain 17EC50 (µMol)0.00070.00070.13660.2726AID240092
Glucocorticoid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00250.00080.00760.0196AID307857
Mineralocorticoid receptor Homo sapiens (human)EC50 (µMol)10.00000.00000.01260.1000AID487147
Androgen receptorHomo sapiens (human)EC50 (µMol)0.01130.00000.20794.3000AID1356896; AID1607931; AID487145
ATP-dependent translocase ABCB1Mus musculus (house mouse)Kd20.00002.20005.18336.8000AID150738
Adenosine receptor A1Rattus norvegicus (Norway rat)EC50 (µMol)0.00920.00161.04608.2000AID307857; AID307858
Adenosine receptor A2aRattus norvegicus (Norway rat)EC50 (µMol)0.01590.00000.11560.7200AID307858
Progesterone receptorRattus norvegicus (Norway rat)EC50 (µMol)0.01590.01590.01590.0159AID307858
Estrogen receptor betaHomo sapiens (human)EC50 (µMol)10.00000.00000.47954.8900AID487144
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glucocorticoid receptorHomo sapiens (human)Kif0.00200.00200.00200.0020AID74235
Progesterone receptorHomo sapiens (human)Activity0.00130.00130.00130.0013AID318134
Progesterone receptorHomo sapiens (human)Kif0.01180.01180.01180.0118AID162301
Glucocorticoid receptorRattus norvegicus (Norway rat)Activity0.27000.27000.27000.2700AID243325
Mineralocorticoid receptor Homo sapiens (human)Kif0.01000.01000.01000.0100AID105813
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (563)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
antral ovarian follicle growthEstrogen receptorHomo sapiens (human)
epithelial cell developmentEstrogen receptorHomo sapiens (human)
chromatin remodelingEstrogen receptorHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
signal transductionEstrogen receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEstrogen receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEstrogen receptorHomo sapiens (human)
androgen metabolic processEstrogen receptorHomo sapiens (human)
male gonad developmentEstrogen receptorHomo sapiens (human)
negative regulation of gene expressionEstrogen receptorHomo sapiens (human)
positive regulation of phospholipase C activityEstrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptorHomo sapiens (human)
response to estradiolEstrogen receptorHomo sapiens (human)
regulation of toll-like receptor signaling pathwayEstrogen receptorHomo sapiens (human)
negative regulation of smooth muscle cell apoptotic processEstrogen receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionEstrogen receptorHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
response to estrogenEstrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
fibroblast proliferationEstrogen receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEstrogen receptorHomo sapiens (human)
stem cell differentiationEstrogen receptorHomo sapiens (human)
regulation of inflammatory responseEstrogen receptorHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
RNA polymerase II preinitiation complex assemblyEstrogen receptorHomo sapiens (human)
uterus developmentEstrogen receptorHomo sapiens (human)
vagina developmentEstrogen receptorHomo sapiens (human)
prostate epithelial cord elongationEstrogen receptorHomo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesisEstrogen receptorHomo sapiens (human)
regulation of branching involved in prostate gland morphogenesisEstrogen receptorHomo sapiens (human)
mammary gland branching involved in pregnancyEstrogen receptorHomo sapiens (human)
mammary gland alveolus developmentEstrogen receptorHomo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongationEstrogen receptorHomo sapiens (human)
protein localization to chromatinEstrogen receptorHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptorHomo sapiens (human)
negative regulation of miRNA transcriptionEstrogen receptorHomo sapiens (human)
regulation of epithelial cell apoptotic processEstrogen receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
regulation of gluconeogenesisGlucocorticoid receptorHomo sapiens (human)
chromatin organizationGlucocorticoid receptorHomo sapiens (human)
regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
apoptotic processGlucocorticoid receptorHomo sapiens (human)
chromosome segregationGlucocorticoid receptorHomo sapiens (human)
signal transductionGlucocorticoid receptorHomo sapiens (human)
glucocorticoid metabolic processGlucocorticoid receptorHomo sapiens (human)
gene expressionGlucocorticoid receptorHomo sapiens (human)
microglia differentiationGlucocorticoid receptorHomo sapiens (human)
adrenal gland developmentGlucocorticoid receptorHomo sapiens (human)
regulation of glucocorticoid biosynthetic processGlucocorticoid receptorHomo sapiens (human)
synaptic transmission, glutamatergicGlucocorticoid receptorHomo sapiens (human)
maternal behaviorGlucocorticoid receptorHomo sapiens (human)
intracellular glucocorticoid receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
glucocorticoid mediated signaling pathwayGlucocorticoid receptorHomo sapiens (human)
positive regulation of neuron apoptotic processGlucocorticoid receptorHomo sapiens (human)
negative regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
astrocyte differentiationGlucocorticoid receptorHomo sapiens (human)
cell divisionGlucocorticoid receptorHomo sapiens (human)
mammary gland duct morphogenesisGlucocorticoid receptorHomo sapiens (human)
motor behaviorGlucocorticoid receptorHomo sapiens (human)
cellular response to steroid hormone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to glucocorticoid stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to dexamethasone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to transforming growth factor beta stimulusGlucocorticoid receptorHomo sapiens (human)
neuroinflammatory responseGlucocorticoid receptorHomo sapiens (human)
positive regulation of miRNA transcriptionGlucocorticoid receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
response to singlet oxygenTyrosine-protein kinase FynHomo sapiens (human)
neuron migrationTyrosine-protein kinase FynHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusTyrosine-protein kinase FynHomo sapiens (human)
heart processTyrosine-protein kinase FynHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
calcium ion transportTyrosine-protein kinase FynHomo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
axon guidanceTyrosine-protein kinase FynHomo sapiens (human)
learningTyrosine-protein kinase FynHomo sapiens (human)
feeding behaviorTyrosine-protein kinase FynHomo sapiens (human)
regulation of cell shapeTyrosine-protein kinase FynHomo sapiens (human)
gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of hydrogen peroxide biosynthetic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of neuron projection developmentTyrosine-protein kinase FynHomo sapiens (human)
protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
forebrain developmentTyrosine-protein kinase FynHomo sapiens (human)
T cell costimulationTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase FynHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusTyrosine-protein kinase FynHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase FynHomo sapiens (human)
response to ethanolTyrosine-protein kinase FynHomo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
dendrite morphogenesisTyrosine-protein kinase FynHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
activated T cell proliferationTyrosine-protein kinase FynHomo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase FynHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase FynHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTyrosine-protein kinase FynHomo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase FynHomo sapiens (human)
cellular response to transforming growth factor beta stimulusTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein targeting to membraneTyrosine-protein kinase FynHomo sapiens (human)
dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to nucleusTyrosine-protein kinase FynHomo sapiens (human)
regulation of glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to L-glutamateTyrosine-protein kinase FynHomo sapiens (human)
cellular response to glycineTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to membraneTyrosine-protein kinase FynHomo sapiens (human)
regulation of calcium ion import across plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activityTyrosine-protein kinase FynHomo sapiens (human)
innate immune responseTyrosine-protein kinase FynHomo sapiens (human)
cell differentiationTyrosine-protein kinase FynHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
ovulation from ovarian follicleProgesterone receptorHomo sapiens (human)
glandular epithelial cell maturationProgesterone receptorHomo sapiens (human)
regulation of DNA-templated transcriptionProgesterone receptorHomo sapiens (human)
signal transductionProgesterone receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProgesterone receptorHomo sapiens (human)
cell-cell signalingProgesterone receptorHomo sapiens (human)
positive regulation of gene expressionProgesterone receptorHomo sapiens (human)
negative regulation of gene expressionProgesterone receptorHomo sapiens (human)
paracrine signalingProgesterone receptorHomo sapiens (human)
negative regulation of phosphorylationProgesterone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
lung alveolus developmentProgesterone receptorHomo sapiens (human)
regulation of epithelial cell proliferationProgesterone receptorHomo sapiens (human)
progesterone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
maintenance of protein location in nucleusProgesterone receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisProgesterone receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
signal transductionMineralocorticoid receptor Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionMineralocorticoid receptor Homo sapiens (human)
regulation of transcription by RNA polymerase IIMineralocorticoid receptor Homo sapiens (human)
intracellular steroid hormone receptor signaling pathwayMineralocorticoid receptor Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
response to hypoxiaCoagulation factor VIIHomo sapiens (human)
positive regulation of leukocyte chemotaxisCoagulation factor VIIHomo sapiens (human)
blood coagulationCoagulation factor VIIHomo sapiens (human)
circadian rhythmCoagulation factor VIIHomo sapiens (human)
response to carbon dioxideCoagulation factor VIIHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayCoagulation factor VIIHomo sapiens (human)
protein processingCoagulation factor VIIHomo sapiens (human)
positive regulation of blood coagulationCoagulation factor VIIHomo sapiens (human)
positive regulation of cell migrationCoagulation factor VIIHomo sapiens (human)
animal organ regenerationCoagulation factor VIIHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor VIIHomo sapiens (human)
response to estradiolCoagulation factor VIIHomo sapiens (human)
response to vitamin KCoagulation factor VIIHomo sapiens (human)
response to genisteinCoagulation factor VIIHomo sapiens (human)
response to estrogenCoagulation factor VIIHomo sapiens (human)
positive regulation of positive chemotaxisCoagulation factor VIIHomo sapiens (human)
response to growth hormoneCoagulation factor VIIHomo sapiens (human)
response to cholesterolCoagulation factor VIIHomo sapiens (human)
response to thyroxineCoagulation factor VIIHomo sapiens (human)
response to Thyroid stimulating hormoneCoagulation factor VIIHomo sapiens (human)
response to 2,3,7,8-tetrachlorodibenzodioxineCoagulation factor VIIHomo sapiens (human)
response to astaxanthinCoagulation factor VIIHomo sapiens (human)
response to thyrotropin-releasing hormoneCoagulation factor VIIHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
MAPK cascadeAndrogen receptorHomo sapiens (human)
in utero embryonic developmentAndrogen receptorHomo sapiens (human)
regulation of systemic arterial blood pressureAndrogen receptorHomo sapiens (human)
epithelial cell morphogenesisAndrogen receptorHomo sapiens (human)
transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
signal transductionAndrogen receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAndrogen receptorHomo sapiens (human)
cell-cell signalingAndrogen receptorHomo sapiens (human)
spermatogenesisAndrogen receptorHomo sapiens (human)
single fertilizationAndrogen receptorHomo sapiens (human)
positive regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
negative regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
positive regulation of gene expressionAndrogen receptorHomo sapiens (human)
male somatic sex determinationAndrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
intracellular receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
Leydig cell differentiationAndrogen receptorHomo sapiens (human)
multicellular organism growthAndrogen receptorHomo sapiens (human)
positive regulation of phosphorylationAndrogen receptorHomo sapiens (human)
positive regulation of MAPK cascadeAndrogen receptorHomo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of cell differentiationAndrogen receptorHomo sapiens (human)
negative regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIIAndrogen receptorHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
regulation of developmental growthAndrogen receptorHomo sapiens (human)
animal organ formationAndrogen receptorHomo sapiens (human)
male genitalia morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell proliferationAndrogen receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationAndrogen receptorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityAndrogen receptorHomo sapiens (human)
activation of prostate induction by androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
morphogenesis of an epithelial foldAndrogen receptorHomo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
prostate gland growthAndrogen receptorHomo sapiens (human)
prostate gland epithelium morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell differentiation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
mammary gland alveolus developmentAndrogen receptorHomo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
cellular response to steroid hormone stimulusAndrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusAndrogen receptorHomo sapiens (human)
cellular response to testosterone stimulusAndrogen receptorHomo sapiens (human)
seminiferous tubule developmentAndrogen receptorHomo sapiens (human)
non-membrane-bounded organelle assemblyAndrogen receptorHomo sapiens (human)
positive regulation of miRNA transcriptionAndrogen receptorHomo sapiens (human)
regulation of protein localization to plasma membraneAndrogen receptorHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayAndrogen receptorHomo sapiens (human)
male gonad developmentAndrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayAndrogen receptorHomo sapiens (human)
lipid hydroxylationCytochrome P450 2C8Homo sapiens (human)
organic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C8Homo sapiens (human)
steroid metabolic processCytochrome P450 2C8Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C8Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C8Homo sapiens (human)
retinol metabolic processCytochrome P450 2C8Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
oxidative demethylationCytochrome P450 2C8Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
cartilage condensationThyroid hormone receptor alphaHomo sapiens (human)
ossificationThyroid hormone receptor alphaHomo sapiens (human)
regulation of thyroid hormone mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
learning or memoryThyroid hormone receptor alphaHomo sapiens (human)
regulation of heart contractionThyroid hormone receptor alphaHomo sapiens (human)
female courtship behaviorThyroid hormone receptor alphaHomo sapiens (human)
response to coldThyroid hormone receptor alphaHomo sapiens (human)
hormone-mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of RNA polymerase II transcription preinitiation complex assemblyThyroid hormone receptor alphaHomo sapiens (human)
erythrocyte differentiationThyroid hormone receptor alphaHomo sapiens (human)
thyroid gland developmentThyroid hormone receptor alphaHomo sapiens (human)
regulation of myeloid cell apoptotic processThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of DNA-templated transcriptionThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of female receptivityThyroid hormone receptor alphaHomo sapiens (human)
regulation of lipid catabolic processThyroid hormone receptor alphaHomo sapiens (human)
type I pneumocyte differentiationThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of cold-induced thermogenesisThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of DNA-templated transcription initiationThyroid hormone receptor alphaHomo sapiens (human)
thyroid hormone mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
cell differentiationThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
retinoic acid receptor signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of thyroid hormone mediated signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
DNA-templated transcriptionThyroid hormone receptor betaHomo sapiens (human)
sensory perception of soundThyroid hormone receptor betaHomo sapiens (human)
negative regulation of female receptivityThyroid hormone receptor betaHomo sapiens (human)
regulation of heart contractionThyroid hormone receptor betaHomo sapiens (human)
female courtship behaviorThyroid hormone receptor betaHomo sapiens (human)
mRNA transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
retinal cone cell developmentThyroid hormone receptor betaHomo sapiens (human)
type I pneumocyte differentiationThyroid hormone receptor betaHomo sapiens (human)
cellular response to thyroid hormone stimulusThyroid hormone receptor betaHomo sapiens (human)
retinal cone cell apoptotic processThyroid hormone receptor betaHomo sapiens (human)
retinoic acid receptor signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
cell differentiationThyroid hormone receptor betaHomo sapiens (human)
thyroid hormone mediated signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
positive regulation of gene expressionTissue factorHomo sapiens (human)
positive regulation of interleukin-8 productionTissue factorHomo sapiens (human)
positive regulation of endothelial cell proliferationTissue factorHomo sapiens (human)
activation of plasma proteins involved in acute inflammatory responseTissue factorHomo sapiens (human)
activation of blood coagulation via clotting cascadeTissue factorHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTissue factorHomo sapiens (human)
blood coagulationTissue factorHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayTissue factorHomo sapiens (human)
protein processingTissue factorHomo sapiens (human)
positive regulation of cell migrationTissue factorHomo sapiens (human)
positive regulation of TOR signalingTissue factorHomo sapiens (human)
positive regulation of angiogenesisTissue factorHomo sapiens (human)
positive regulation of positive chemotaxisTissue factorHomo sapiens (human)
cytokine-mediated signaling pathwayTissue factorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipopolysaccharideMitogen-activated protein kinase 14Homo sapiens (human)
DNA damage checkpoint signalingMitogen-activated protein kinase 14Homo sapiens (human)
cell morphogenesisMitogen-activated protein kinase 14Homo sapiens (human)
cartilage condensationMitogen-activated protein kinase 14Homo sapiens (human)
angiogenesisMitogen-activated protein kinase 14Homo sapiens (human)
osteoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
placenta developmentMitogen-activated protein kinase 14Homo sapiens (human)
response to dietary excessMitogen-activated protein kinase 14Homo sapiens (human)
chondrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusMitogen-activated protein kinase 14Homo sapiens (human)
glucose metabolic processMitogen-activated protein kinase 14Homo sapiens (human)
regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 14Homo sapiens (human)
chemotaxisMitogen-activated protein kinase 14Homo sapiens (human)
signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor protein serine/threonine kinase signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
skeletal muscle tissue developmentMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of gene expressionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myotube differentiationMitogen-activated protein kinase 14Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 14Homo sapiens (human)
fatty acid oxidationMitogen-activated protein kinase 14Homo sapiens (human)
platelet activationMitogen-activated protein kinase 14Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 14Homo sapiens (human)
osteoclast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated protein kinase signaling cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cyclase activityMitogen-activated protein kinase 14Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
response to muramyl dipeptideMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of interleukin-12 productionMitogen-activated protein kinase 14Homo sapiens (human)
response to insulinMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of hippo signalingMitogen-activated protein kinase 14Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusMitogen-activated protein kinase 14Homo sapiens (human)
response to muscle stretchMitogen-activated protein kinase 14Homo sapiens (human)
p38MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of protein import into nucleusMitogen-activated protein kinase 14Homo sapiens (human)
signal transduction in response to DNA damageMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of erythrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
glucose importMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of glucose importMitogen-activated protein kinase 14Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
stem cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
striated muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationMitogen-activated protein kinase 14Homo sapiens (human)
bone developmentMitogen-activated protein kinase 14Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipoteichoic acidMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to ionizing radiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to UV-BMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of brown fat cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular senescenceMitogen-activated protein kinase 14Homo sapiens (human)
stress-induced premature senescenceMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to virusMitogen-activated protein kinase 14Homo sapiens (human)
regulation of synaptic membrane adhesionMitogen-activated protein kinase 14Homo sapiens (human)
regulation of cytokine production involved in inflammatory responseMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast fusionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processMitogen-activated protein kinase 14Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
signal transductionEstrogen receptor betaHomo sapiens (human)
cell-cell signalingEstrogen receptor betaHomo sapiens (human)
negative regulation of cell growthEstrogen receptor betaHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptor betaHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptor betaHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptor betaHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (176)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
TFIIB-class transcription factor bindingEstrogen receptorHomo sapiens (human)
transcription coregulator bindingEstrogen receptorHomo sapiens (human)
transcription corepressor bindingEstrogen receptorHomo sapiens (human)
transcription coactivator bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
chromatin bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
nuclear receptor activityEstrogen receptorHomo sapiens (human)
steroid bindingEstrogen receptorHomo sapiens (human)
protein bindingEstrogen receptorHomo sapiens (human)
calmodulin bindingEstrogen receptorHomo sapiens (human)
beta-catenin bindingEstrogen receptorHomo sapiens (human)
zinc ion bindingEstrogen receptorHomo sapiens (human)
TBP-class protein bindingEstrogen receptorHomo sapiens (human)
enzyme bindingEstrogen receptorHomo sapiens (human)
protein kinase bindingEstrogen receptorHomo sapiens (human)
nitric-oxide synthase regulator activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor bindingEstrogen receptorHomo sapiens (human)
estrogen response element bindingEstrogen receptorHomo sapiens (human)
identical protein bindingEstrogen receptorHomo sapiens (human)
ATPase bindingEstrogen receptorHomo sapiens (human)
14-3-3 protein bindingEstrogen receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen receptorHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
core promoter sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activityGlucocorticoid receptorHomo sapiens (human)
RNA bindingGlucocorticoid receptorHomo sapiens (human)
nuclear receptor activityGlucocorticoid receptorHomo sapiens (human)
nuclear glucocorticoid receptor activityGlucocorticoid receptorHomo sapiens (human)
steroid bindingGlucocorticoid receptorHomo sapiens (human)
protein bindingGlucocorticoid receptorHomo sapiens (human)
zinc ion bindingGlucocorticoid receptorHomo sapiens (human)
TBP-class protein bindingGlucocorticoid receptorHomo sapiens (human)
protein kinase bindingGlucocorticoid receptorHomo sapiens (human)
identical protein bindingGlucocorticoid receptorHomo sapiens (human)
Hsp90 protein bindingGlucocorticoid receptorHomo sapiens (human)
steroid hormone bindingGlucocorticoid receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingGlucocorticoid receptorHomo sapiens (human)
estrogen response element bindingGlucocorticoid receptorHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
protein bindingTyrosine-protein kinase FynHomo sapiens (human)
ATP bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase FynHomo sapiens (human)
enzyme bindingTyrosine-protein kinase FynHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
identical protein bindingTyrosine-protein kinase FynHomo sapiens (human)
alpha-tubulin bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase FynHomo sapiens (human)
transmembrane transporter bindingTyrosine-protein kinase FynHomo sapiens (human)
metal ion bindingTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
tau protein bindingTyrosine-protein kinase FynHomo sapiens (human)
tau-protein kinase activityTyrosine-protein kinase FynHomo sapiens (human)
growth factor receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
scaffold protein bindingTyrosine-protein kinase FynHomo sapiens (human)
disordered domain specific bindingTyrosine-protein kinase FynHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
transcription coactivator bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
DNA bindingProgesterone receptorHomo sapiens (human)
nuclear steroid receptor activityProgesterone receptorHomo sapiens (human)
G protein-coupled receptor activityProgesterone receptorHomo sapiens (human)
steroid bindingProgesterone receptorHomo sapiens (human)
protein bindingProgesterone receptorHomo sapiens (human)
zinc ion bindingProgesterone receptorHomo sapiens (human)
enzyme bindingProgesterone receptorHomo sapiens (human)
identical protein bindingProgesterone receptorHomo sapiens (human)
ATPase bindingProgesterone receptorHomo sapiens (human)
estrogen response element bindingProgesterone receptorHomo sapiens (human)
nuclear receptor activityProgesterone receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificMineralocorticoid receptor Homo sapiens (human)
DNA-binding transcription factor activityMineralocorticoid receptor Homo sapiens (human)
nuclear steroid receptor activityMineralocorticoid receptor Homo sapiens (human)
steroid bindingMineralocorticoid receptor Homo sapiens (human)
protein bindingMineralocorticoid receptor Homo sapiens (human)
zinc ion bindingMineralocorticoid receptor Homo sapiens (human)
TBP-class protein bindingMineralocorticoid receptor Homo sapiens (human)
sequence-specific double-stranded DNA bindingMineralocorticoid receptor Homo sapiens (human)
nuclear receptor activityMineralocorticoid receptor Homo sapiens (human)
estrogen response element bindingMineralocorticoid receptor Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
serine-type endopeptidase activityCoagulation factor VIIHomo sapiens (human)
signaling receptor bindingCoagulation factor VIIHomo sapiens (human)
calcium ion bindingCoagulation factor VIIHomo sapiens (human)
protein bindingCoagulation factor VIIHomo sapiens (human)
serine-type peptidase activityCoagulation factor VIIHomo sapiens (human)
transcription cis-regulatory region bindingAndrogen receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
RNA polymerase II general transcription initiation factor bindingAndrogen receptorHomo sapiens (human)
transcription coactivator bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
chromatin bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityAndrogen receptorHomo sapiens (human)
nuclear receptor activityAndrogen receptorHomo sapiens (human)
G protein-coupled receptor activityAndrogen receptorHomo sapiens (human)
signaling receptor bindingAndrogen receptorHomo sapiens (human)
steroid bindingAndrogen receptorHomo sapiens (human)
androgen bindingAndrogen receptorHomo sapiens (human)
protein bindingAndrogen receptorHomo sapiens (human)
beta-catenin bindingAndrogen receptorHomo sapiens (human)
zinc ion bindingAndrogen receptorHomo sapiens (human)
enzyme bindingAndrogen receptorHomo sapiens (human)
ATPase bindingAndrogen receptorHomo sapiens (human)
molecular adaptor activityAndrogen receptorHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingAndrogen receptorHomo sapiens (human)
POU domain bindingAndrogen receptorHomo sapiens (human)
molecular condensate scaffold activityAndrogen receptorHomo sapiens (human)
estrogen response element bindingAndrogen receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2C8Homo sapiens (human)
iron ion bindingCytochrome P450 2C8Homo sapiens (human)
protein bindingCytochrome P450 2C8Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C8Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C8Homo sapiens (human)
aromatase activityCytochrome P450 2C8Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
heme bindingCytochrome P450 2C8Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C8Homo sapiens (human)
transcription cis-regulatory region bindingThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activityThyroid hormone receptor alphaHomo sapiens (human)
nuclear receptor activityThyroid hormone receptor alphaHomo sapiens (human)
protein bindingThyroid hormone receptor alphaHomo sapiens (human)
zinc ion bindingThyroid hormone receptor alphaHomo sapiens (human)
TBP-class protein bindingThyroid hormone receptor alphaHomo sapiens (human)
protein domain specific bindingThyroid hormone receptor alphaHomo sapiens (human)
chromatin DNA bindingThyroid hormone receptor alphaHomo sapiens (human)
thyroid hormone bindingThyroid hormone receptor alphaHomo sapiens (human)
general transcription initiation factor bindingThyroid hormone receptor alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificThyroid hormone receptor betaHomo sapiens (human)
transcription coactivator bindingThyroid hormone receptor betaHomo sapiens (human)
DNA bindingThyroid hormone receptor betaHomo sapiens (human)
DNA-binding transcription factor activityThyroid hormone receptor betaHomo sapiens (human)
nuclear receptor activityThyroid hormone receptor betaHomo sapiens (human)
protein bindingThyroid hormone receptor betaHomo sapiens (human)
zinc ion bindingThyroid hormone receptor betaHomo sapiens (human)
enzyme bindingThyroid hormone receptor betaHomo sapiens (human)
chromatin DNA bindingThyroid hormone receptor betaHomo sapiens (human)
thyroid hormone bindingThyroid hormone receptor betaHomo sapiens (human)
sequence-specific double-stranded DNA bindingThyroid hormone receptor betaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingThyroid hormone receptor betaHomo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
serine-type endopeptidase activityTissue factorHomo sapiens (human)
protease bindingTissue factorHomo sapiens (human)
protein bindingTissue factorHomo sapiens (human)
phospholipid bindingTissue factorHomo sapiens (human)
cytokine receptor activityTissue factorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Mus musculus (house mouse)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 14Homo sapiens (human)
enzyme bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein phosphatase bindingMitogen-activated protein kinase 14Homo sapiens (human)
mitogen-activated protein kinase p38 bindingMitogen-activated protein kinase 14Homo sapiens (human)
NFAT protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptor betaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptor betaHomo sapiens (human)
DNA bindingEstrogen receptor betaHomo sapiens (human)
nuclear steroid receptor activityEstrogen receptor betaHomo sapiens (human)
nuclear receptor activityEstrogen receptor betaHomo sapiens (human)
steroid bindingEstrogen receptor betaHomo sapiens (human)
protein bindingEstrogen receptor betaHomo sapiens (human)
zinc ion bindingEstrogen receptor betaHomo sapiens (human)
enzyme bindingEstrogen receptor betaHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptor betaHomo sapiens (human)
estrogen response element bindingEstrogen receptor betaHomo sapiens (human)
receptor antagonist activityEstrogen receptor betaHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (94)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
nucleoplasmEstrogen receptorHomo sapiens (human)
transcription regulator complexEstrogen receptorHomo sapiens (human)
cytoplasmEstrogen receptorHomo sapiens (human)
Golgi apparatusEstrogen receptorHomo sapiens (human)
cytosolEstrogen receptorHomo sapiens (human)
plasma membraneEstrogen receptorHomo sapiens (human)
membraneEstrogen receptorHomo sapiens (human)
chromatinEstrogen receptorHomo sapiens (human)
euchromatinEstrogen receptorHomo sapiens (human)
protein-containing complexEstrogen receptorHomo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleoplasmGlucocorticoid receptorHomo sapiens (human)
cytoplasmGlucocorticoid receptorHomo sapiens (human)
mitochondrial matrixGlucocorticoid receptorHomo sapiens (human)
centrosomeGlucocorticoid receptorHomo sapiens (human)
spindleGlucocorticoid receptorHomo sapiens (human)
cytosolGlucocorticoid receptorHomo sapiens (human)
membraneGlucocorticoid receptorHomo sapiens (human)
nuclear speckGlucocorticoid receptorHomo sapiens (human)
synapseGlucocorticoid receptorHomo sapiens (human)
chromatinGlucocorticoid receptorHomo sapiens (human)
protein-containing complexGlucocorticoid receptorHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
nucleusTyrosine-protein kinase FynHomo sapiens (human)
mitochondrionTyrosine-protein kinase FynHomo sapiens (human)
endosomeTyrosine-protein kinase FynHomo sapiens (human)
cytosolTyrosine-protein kinase FynHomo sapiens (human)
actin filamentTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
postsynaptic densityTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
perikaryonTyrosine-protein kinase FynHomo sapiens (human)
cell bodyTyrosine-protein kinase FynHomo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase FynHomo sapiens (human)
perinuclear endoplasmic reticulumTyrosine-protein kinase FynHomo sapiens (human)
glial cell projectionTyrosine-protein kinase FynHomo sapiens (human)
Schaffer collateral - CA1 synapseTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneProgesterone receptorHomo sapiens (human)
nucleoplasmProgesterone receptorHomo sapiens (human)
mitochondrial outer membraneProgesterone receptorHomo sapiens (human)
cytosolProgesterone receptorHomo sapiens (human)
chromatinProgesterone receptorHomo sapiens (human)
nucleusProgesterone receptorHomo sapiens (human)
nucleoplasmGlucocorticoid receptorMus musculus (house mouse)
nucleoplasmMineralocorticoid receptor Homo sapiens (human)
endoplasmic reticulum membraneMineralocorticoid receptor Homo sapiens (human)
cytosolMineralocorticoid receptor Homo sapiens (human)
chromatinMineralocorticoid receptor Homo sapiens (human)
receptor complexMineralocorticoid receptor Homo sapiens (human)
nucleusMineralocorticoid receptor Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
extracellular regionCoagulation factor VIIHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor VIIHomo sapiens (human)
Golgi lumenCoagulation factor VIIHomo sapiens (human)
plasma membraneCoagulation factor VIIHomo sapiens (human)
vesicleCoagulation factor VIIHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor VIIHomo sapiens (human)
serine-type peptidase complexCoagulation factor VIIHomo sapiens (human)
extracellular spaceCoagulation factor VIIHomo sapiens (human)
plasma membraneAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
nucleoplasmAndrogen receptorHomo sapiens (human)
cytoplasmAndrogen receptorHomo sapiens (human)
cytosolAndrogen receptorHomo sapiens (human)
nuclear speckAndrogen receptorHomo sapiens (human)
chromatinAndrogen receptorHomo sapiens (human)
protein-containing complexAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C8Homo sapiens (human)
plasma membraneCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
cytoplasmCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
nucleusThyroid hormone receptor alphaHomo sapiens (human)
nucleoplasmThyroid hormone receptor alphaHomo sapiens (human)
cytosolThyroid hormone receptor alphaHomo sapiens (human)
chromatinThyroid hormone receptor alphaHomo sapiens (human)
nucleusThyroid hormone receptor alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexThyroid hormone receptor alphaHomo sapiens (human)
nucleoplasmThyroid hormone receptor betaHomo sapiens (human)
nuclear bodyThyroid hormone receptor betaHomo sapiens (human)
RNA polymerase II transcription regulator complexThyroid hormone receptor betaHomo sapiens (human)
chromatinThyroid hormone receptor betaHomo sapiens (human)
nucleusThyroid hormone receptor betaHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
extracellular spaceTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
external side of plasma membraneTissue factorHomo sapiens (human)
cell surfaceTissue factorHomo sapiens (human)
membraneTissue factorHomo sapiens (human)
collagen-containing extracellular matrixTissue factorHomo sapiens (human)
serine-type peptidase complexTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
plasma membraneGlycine receptor subunit betaRattus norvegicus (Norway rat)
plasma membraneATP-dependent translocase ABCB1Mus musculus (house mouse)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
spindle poleMitogen-activated protein kinase 14Homo sapiens (human)
extracellular regionMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 14Homo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
nuclear speckMitogen-activated protein kinase 14Homo sapiens (human)
secretory granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
glutamatergic synapseMitogen-activated protein kinase 14Homo sapiens (human)
ficolin-1-rich granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
nucleoplasmEstrogen receptor betaHomo sapiens (human)
mitochondrionEstrogen receptor betaHomo sapiens (human)
intracellular membrane-bounded organelleEstrogen receptor betaHomo sapiens (human)
chromatinEstrogen receptor betaHomo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (668)

Assay IDTitleYearJournalArticle
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID494980Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1356934Antagonist activity at human PR expressed in CHO-K1 cells assessed as reduction in progesterone-induced response incubated for 20 hrs by luciferase reporter gene assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID161969Antagonistic efficacy towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
AID1386833Antagonist activity at PR-b (unknown origin) expressed in Ishikawa cells assessed as inhibition of progesterone-induced PRE activity after 24 hrs by luciferase reporter gene based luminescence assay2018Journal of natural products, 09-28, Volume: 81, Issue:9
Irilone from Red Clover ( Trifolium pratense) Potentiates Progesterone Signaling.
AID240495Inhibition of human progesterone receptor2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
AID1380186Induction of PRGC1 recruitment in N-terminal thrombin cleavable 6-His-tagged glucocorticoid receptor (unknown origin) at 50 uM by SPR method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID249804Initial weight of the ob/ob mice before oral treatment at 100 mpk b.i.d. for 13 days2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1474136Drug concentration at steady state in human at 600 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1381666Toxicity in Balb/C nude mouse implanted with human UM1 cells assessed as loss of body weight at 1 mg, ip qd for 4 weeks2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID304379Displacement of fluorescent labeled Dexamethasone from glucocorticoid receptor2007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
AID326401Agonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID1815652Effect on P4 induced GR expression in CD-1 mouse uterine luminal epithelium at 10 mg/kg, ip for 7 days by immunohistochemical analysis
AID679792TP_TRANSPORTER: increase in Doxorubicin intracellular accumulation (Doxorubicin: 10 ug/mL, RU486: 10 uM) in RHC1 cells1994FEBS letters, Nov-28, Volume: 355, Issue:2
The antiprogestatin drug RU 486 potentiates doxorubicin cytotoxicity in multidrug resistant cells through inhibition of P-glycoprotein function.
AID226106Antagonist activity against progesterone receptor (PR) using PRE-luciferase plasmid co-transfected CV-1 cells2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID161974Efficacy as a function of maximal inhibition against human progesterone receptor B (hPR-B).1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
AID1607929Antagonist activity at human progesterone receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1657020Inactivation of CYP3A4 (unknown origin) assessed as Kinact2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID237139Half life period of the compound in rat hepatocytes was determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID326402Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1381652Antiproliferative activity against human SUM149PT cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID74376Relative binding affinity to glucocorticoid receptor on cytosol from liver at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID309454Displacement of [3H]estradiol from estrogen receptor alpha at 10 uM2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
AID1671596Antagonist activity at recombinant glucocorticoid receptor (unknown origin) transfected in human PC-3 cells co-transfected with MMTV and luciferase at 1 uM incubated for 24 hrs by dual luciferase reporter gene assay2019European journal of medicinal chemistry, Mar-15, Volume: 166Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist.
AID343784Antiprogestin activity against ovariectomized Sprague-Dawley rat assessed as effect on ethinyl estradiol-induced C3 expression at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID1410424Transrepression of GCR in human HeLa cells assessed as suppression of DEX-induced GILZ mRNA expression at 0.4 uM after 24 hrs by Taqman-based real-time PCR analysis2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Imidazo[2,1-
AID47382Inhibitory concentration against progesterone induced PRE-luciferase activity in CV-cells2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.
AID483898Binding affinity to AR2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
AID162592Antagonist activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
AID1356942Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID326447Selectivity for human AR over human PR2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID276775Inhibition of prednisilone-induced lymphopenia in Sprague-Dawley rat at 100 mg/kg, po2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID161798Antagonistic activity at human progesterone receptor in CV-1 cells.2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID306214Antagonist activity at progesterone receptor expressed in human T47 cells assessed as blockade of progesterone-induced alkaline phosphatase activity2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID326396Antagonist activity at human PR expressed in human T47D cells assessed as inhibition of progesterone induced alkaline phosphatase2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID241689Inhibition of CHO-K1 cells expressing glucocorticoid receptor2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
AID1607950AUC in rat at 5 mg/kg, po2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID306215Selectivity index, Ratio of IC50 for glucocorticoid receptor expressed in human A549 cells to IC50 for progesterone receptor expressed in human T47 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID115684Effect on pregnancy in mice as implantation at 0.5 mg/mouse dose with simultaneous 0.5 mg RU-486 dose1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.
AID307857Binding affinity to rat glucocorticoid receptor2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.
AID276095Lowering of plasma glucose level in DIO C57BL/6J mouse at 30 mg/kg, po after 4 hr fasting2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID306229AUC in mouse at 2 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID38827Efficacy as a function of maximal inhibition against human androgen receptor.1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
AID1381670Cell cycle arrest in human SUM149PT cells assessed as decrease in cells at S phase at 20 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID251622Inhibitory activity against human lymphocytes2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID1482058In vivo antagonist activity at glucocorticoid receptor in Sprague-Dawley rat assessed as reduction in cortisone-induced plasma glucose levels at 30 mg/kg, po bid via gavage for 6 days pretreated for 12 hrs followed by cortisone 21-acetate treatment measur2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor
AID1356347Antagonist activity at human AR assessed as reduction in DHT-induced transactivation2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
AID1607963Solubility of compound in fasted state simulated gastric fluid at pH 1.22019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1356949Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1240589Reduction in LDL level in high fat and high cholesterol diet fed Syrian golden hamster at 30 mg/kg, po qd for 14 days2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID1356910Clearance in rat at 0.5 mg/kg, iv2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID245862Inhibition of 4 nM progesterone-stimulated transactivation of MMTV-Luc reporter in CV-1 cells expressing PR-B2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
AID162436Antagonist activity against the Progesterone Receptor (PR)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1356913Oral bioavailability in rat at 5 mg/kg2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID118296Effect on pregnancy in mice as percent pregnant at 0.5 mg/mouse dose with simultaneous 0.5 mg RU-486 dose1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.
AID1380183Induction of NCOA2 recruitment in N-terminal thrombin cleavable 6-His-tagged glucocorticoid receptor (unknown origin) at 50 uM by SPR method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID162283Binding affinity against Baculovirus-Expressed hPR-A1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1482039AUC in Sprague-Dawley CD-1 rat plasma at 3 mg/kg, po administered as cassette dose via gavage measured up to 24 hrs by LC/MS analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor
AID461850Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity2010Bioorganic & 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.
AID237156Half life period of the compound in rat liver microsomes was determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID38979Displacement of [3H]mibolerone from human Androgen receptor2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
AID309455Displacement of [3H]dihydrotestosterone from androgen receptor at 10 uM2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
AID242105Inhibition of [3H]dexamethasone binding to human glucocorticoid receptor2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID161801Effective concentration for agonist activity towards human progesterone receptor (hPR) expressed in CV-1 cells; Not active2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
AID394847Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISA relative to Dexamethasone in presence of RU-4862009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.
AID529376Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells assessed as a reduction in 16S rRNA transcript at 2 uM after 72 hrs by RT-PCR2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID276771Plasma concentration in Sprague-Dawley rat after 7 hrs at 100 mg/kg, po2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID343787Tmax in rat at 30 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID405941Antagonist activity at cloned androgen receptor-ligand binding domain expressed in african green monkey COS7 cells by two hybrid luciferase assay2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
AID276773Inhibition of prednisilone-stimulated TAT production in Sprague-Dawley rat at 100 mg/kg, po2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID1607931Agonist activity at human androgen receptor in human LNCAP cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID387086Antagonist activity at progesterone receptor assessed as progesterone-induced alkaline phosphatase activity in human T47D cells2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
AID162464Displacement of [3H]progesterone at progesterone receptor of T47D cells2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Novel pyrrole-containing progesterone receptor modulators.
AID162593Antagonist activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
AID529378Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells assessed as a reduction in 16S rRNA transcript at 2 uM after 72 hrs by RT-PCR in presence of cycloheximide2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID1240573Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID494983Antagonist activity at androgen receptor ligand binding domain by two hybrid assay2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
AID208687Inhibitory concentration against progesterone stimulated alkaline phosphatase activity in T47D human breast carcinoma cell line2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.
AID494986Antagonist activity at mineralocorticoid receptor ligand binding domain by two hybrid assay2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
AID309724Antagonist activity at progesterone receptor expressed in human T47D cells assessed as inhibition of promegestone-induced alkaline phosphatase activity2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1240590Increase in HDL level in high fat and high cholesterol diet fed Syrian golden hamster at 30 mg/kg, po qd for 14 days2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID1356897Agonist activity at AR (unknown origin) expressed in human LNCaP cells incubated for 20 hrs by luciferase reporter gene assay relative to mifepristone2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1607964Solubility of compound in PBS at pH 7.42019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1607936Agonist activity at human androgen receptor in human LNCAP cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay relative to control2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID162597Agonistic efficacy relative to progesterone (100%) on Human Progesterone receptor B isoform in co-transfected CV-1 cell lines.1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID239976Displacement of fluorescent ligand from binding domain of progesterone receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
AID529379Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells assessed as growth inhibition at 2 uM pretreated for 1 hr before infection2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID1381657Inhibition of KLF5 expression levels in human HCC1937 cells after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID276769Stability in rat liver microsomes after 20 mins2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID1228844Displacement of [3H]-progesterone from cytosolic fraction of human recombinant progesterone-B receptor by scintillation counting analysis2015Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
AID1179648Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HepG2 cells assessed as relative luciferase activity at 1 uM by MMTV promoter-driven luciferase reporter gene assay relative to dexamethasone2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Triterpenes from Alisma orientalis act as androgen receptor agonists, progesterone receptor antagonists, and glucocorticoid receptor antagonists.
AID1199781Inhibition of p-gp (unknown origin) in doxorubicin-resistant human K562/R7 cells assessed as increase in daunorubicin accumulation measured as fluorescence ratio at 10 uM incubated for 1 hr with 10 uM daunorubicin by flow cytometry relative to control2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells.
AID304381Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay2007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
AID483896Displacement of fluorescent-labeled Dexamethasone from GR by fluorescent polarization assay2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
AID300612Binding affinity to glucocorticoid receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
AID68891Inhibition of antagonist activity towards estrogen(hER) receptor2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID248634Inhibition of glucocorticoid receptor Dexamethasone response in reporter gene assay2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
AID32843Antagonistic efficacy to the progesterone receptor measured in the T-47D alkaline phosphatase assay1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID147654In vitro agonist potency in transactivation assay of CV-1 cells stably transfected with human androgen receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID105811Antagonist activity against human mineralocorticoid receptor as displacement of radioligand, percent inhibition at 10 nM2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID237394Free fatty acid (FFA) levels in ob/ob mice after 14 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID405937Inhibition of progesterone receptor mediated progesterone-induced alkaline phosphatase activity in human T47D cells2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
AID237393Free fatty acid (FFA) levels in ob/ob mice after 13 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID290022Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced GRE-linked luciferase reporter gene activity2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.
AID318133Antagonist activity at GR in SW1353/MMTV5 cells assessed as inhibition of dexamethasone-induced luciferase expression2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID74217Antagonist activity as displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor, percent inhibition at 1 uM2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID306223Cmax in mouse at 10 mg/kg, po2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID405943Antagonist activity at cloned mineralocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
AID147647In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID74080Effect on human Glucocorticoid receptor (GR) in a whole cell assay to measure functional cellular GR-antagonism (GRAF)2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
AID326407Agonist activity at human ER ligand binding domain expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID405939Antagonist activity at cloned estrogen receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
AID226104Antagonist activity against progesterone receptor (PR) in an alkaline phosphatase assay in the T47D human breast carcinoma cell line2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID73765Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.
AID1240576Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID1687196Lipid lowering activity in mouse 3T3-L1 cells assessed as reduction in adipogenic cocktail induced triglyceride levels at 1 uM incubated for 6 days by GPO-POD assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Tigliane Diterpenoids as a New Type of Antiadipogenic Agents Inhibit GRα-Dexras1 Axis in Adipocytes.
AID1240577Antagonist activity against glucocorticoid receptor in rat H4-IIE cells assessed as inhibition of dexamethasone-induced receptor transactivation pre-incubated for 1 hr before dexamethasone addition and measured 24 hrs post dexamethasone stimulation by tyr2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID249797Final weight of the ob/ob mice after 13 days of oral treatment at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1356908Agonist activity at AR in human MDA-MB-453 cells assessed as increase in CYPGF8 gene expression at 111 to 333 nM incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID266612Efficacy against PR beta-mediated transactivation of MMTV luciferase reporter gene in BacMam transduced progesterone-stimulated CV1 cells relative to RU4862006Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.
AID1356911Volume of distribution at steady state in rat at 0.5 mg/kg, iv2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID238468Inhibition of human Estrogen receptor beta2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID1381660Cmax in Sprague-Dawley rat at 30 mg/kg administered via oral gavage by HPLC analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID249805Initial weight of the ob/ob mice before oral treatment at 100 mpk b.i.d. for 14 days2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID237151Half life period of the compound in human hepatocytes; Not determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID309461Binding affinity to glucocorticoid receptor in SW1353 cells by whole-cell binding assay2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
AID162131Antagonistic activity against Progesterone receptor (PR) in transcriptional activation assay in human T47D breast carcinoma cell line2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.
AID242414Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytes2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
AID276091Effect on body weight in DIO C57BL/6J mouse at 30 mg/kg, po2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID487151Antagonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID38990Inhibitory activity against human Androgen receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID487150Antagonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID238538Inhibition of human Mineralocorticoid receptor2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID1381658Induction of PARP cleavage in human SUM149PT cells after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1381653Antiproliferative activity against human HCC1937 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID244403Agonistic activity against VP-16 GR transcriptional activation assay in human Huh-7 cells2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID487144Agonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID487147Agonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID487349Decidulization activity in ovariectomized BALB/c mouse assessed as inhibition of sesame oil-induced uterine wet weight gain at 0.1 mg/day administered intralbuminally2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1356930Inhibition of CYP3A4 (unknown origin) using midazolam as substrate2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1327819Antagonist activity at progesterone receptor in human T47D cells assessed as suppression of P4-induced Na/K-ATPase-beta1 expression level at 30 nM measured after 16 hrs by Western blot analysis2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Development of
AID1687195Inhibition of adipogenic cocktail-induced GR-alpha nuclear translocation in mouse 3T3-L1 cells at 10 uM after 8 hrs by Western blot analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Tigliane Diterpenoids as a New Type of Antiadipogenic Agents Inhibit GRα-Dexras1 Axis in Adipocytes.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1607933Agonist activity at human glucocorticoid receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID237400Aspartate aminotransferase (AST) levels in ob/ob mice after 13 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID487132Displacement of [3H]DHT from human androgen receptor after 16 hrs by scintillation counting2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1671605Binding affinity to recombinant human untagged full length glucocorticoid receptor expressed in baculovirus expression system assessed as apparent binding affinity measured for 1 min by biolayer interferometry2019European journal of medicinal chemistry, Mar-15, Volume: 166Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID289553Inhibition of human GR transcriptional activation by HepTAT cells2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
AID1544123Binding affinity to GR (unknown origin)2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Profiling withanolide A for therapeutic targets in neurodegenerative diseases.
AID238598Inhibition of human Thyroid hormone receptor beta2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID248058Inhibition of [3H]taurocholate uptake in rat hepatocytes; Not determined2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
AID473409Displacement of [3H]DEX from human glucocorticoid receptor2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID39147Binding affinity for human androgen receptor in transiently-transfected COS-1 cells.1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
AID326450Antagonist activity in rat uterus assessed as progesterone-induced decidualization response in stromal cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID529373Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells at 2 uM after 72 hrs2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID529380Cmax in pregnant women at 800 mg, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID487149Antagonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1815667Toxicity in P4 induced CD-1 mouse assessed as effect on body weight at 10 mg/kg, ip for 7 days (Rvb= 30g)
AID309456Displacement of [3H]aldosterone from recombinant mineralocorticoid receptor in Sf9 cells at 10 uM2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
AID1380140Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced transactivation incubated for 24 hrs by beta-galactosidase reporter gene assay relative to mifepristone2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID38826Efficacy as percent inhibition of Androgen receptor with DHT EC501998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID126435Relative binding affinity for mineralocorticoid receptor of rat kidney at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID70201Displacement of [3H]-estradiol from human estrogen receptor alpha; ND means Not determined2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
AID1356935Selectivity index, ratio of IC50 for antagonist activity at human PR expressed in CHO-K1 cells to IC50 for antagonist activity at human GR expressed in CHO-K1 cells a2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID74091Inhibitory activity against human glucocorticoid receptor (hGR)1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID161962Efficacy at human progesterone receptor in T47D human breast cancer cell.2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID1607949Cmax in rat at 5 mg/kg, po2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1356950Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID39151Antagonist activity against steroid Androgen receptor1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID304380Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay2007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
AID487153Agonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay relative to control2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1356909Agonist activity at AR in human MDA-MB-453 cells assessed as increase in SEC14L2 gene expression at 111 to 333 nM incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1356349Antagonist activity at human GR assessed as reduction in dexamethasone-induced transactivation2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID162117Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells.1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
AID570062Agonist activity at progesterone receptor in sc dosed estrogen-primed immature New Zealand White rabbit assessed as stimulation of progesterone-induced endometrial transformation by McPhail assay2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
AID1380129Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID1482036Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor
AID74378Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID487138Antagonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc assessed as effect on progesterone-induced activity by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID326423Induction of early menses in cynomolgus monkey at 5 mg/kg, po2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID326408Antagonist activity at human ER ligand binding domain expressed in african green monkey COS7 cells in presence of 17-beta-estradiol by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID1356893Antagonist activity at human GR expressed in CHO-K1 cells assessed as reduction in dexamethasone-induced response incubated for 20 hrs by luciferase reporter gene assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID266610Binding affinity at PR by fluorescence binding assay2006Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.
AID73929Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR)2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
AID494984Antagonist activity at glucocorticoid receptor ligand binding domain by two hybrid assay2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
AID126443Displacement of [3H]aldosterone from human Mineralocorticoid receptor2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
AID1199783Intrinsic cytotoxicity against human K562 cells assessed as cell survival at 10 uM after 24 hrs by MTT assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1694381Antiproliferative activity against human A549 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers.
AID242045Inhibition of [3H]dexamethasone binding to rat glucocorticoid receptor2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID251371Reduction of progesterone levels in pregnant rats after q.d. oral dosing at 3 mpk2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID405942Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
AID1815669Toxicity in P4 induced CD-1 mouse assessed as effect on MG weight at 10 mg/kg, ip for 7 days (Rvb= 0.22g)
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID487137Agonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID309726Ratio of IC50 for glucocorticoid receptor to IC50 for progesterone receptor2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.
AID237164Half life period of the compound in human liver microsomes; Not determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID162602Antagonistic efficacy relative to progesterone on Human Progesterone receptor B isoform expressed in CV-1 cells1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID267771Inhibition of fluorescent-labeled Dexamethasone binding to GR2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
AID1380132Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced transactivation incubated for 24 hrs by beta-galactosidase reporter gene assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID38980Antagonist activity against the Androgen Receptor (AR)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID1228871Antidepressant-like activity in Wistar rat assessed as decrease in immobility time at 10 mg/kg, po administered at 1, 5, 23.5 hrs prior to testing measured for 5 mins by forced swimming test relative to vehicle-treated control2015Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
AID238621Inhibition of human Thyroid hormone receptor alpha2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID294499Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.
AID147651In vitro agonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor; NE=no effect2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID681167TP_TRANSPORTER: Northern blot from LS174T cell2001The Journal of biological chemistry, May-04, Volume: 276, Issue:18
Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin.
AID387088Antagonist activity at estrogen receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
AID1356894Agonist activity at human GR expressed in CHO-K1 cells incubated for 20 hrs by luciferase reporter gene assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1607944Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of glucocorticoid receptor-dexamethasone coactivator protein-protein interaction incubated for 24 hrs by bioluminescence assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID181260inhibitory activity against progesterone receptor (PR) in ovariectomized mature female rat complement C3 model2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID1694383Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers.
AID1482038Cmax in Sprague-Dawley CD-1 rat plasma at 3 mg/kg, po administered as cassette dose via gavage measured up to 24 hrs by LC/MS analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor
AID529381Cytotoxicity against human Hep2 cells at >2 uM2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID343789Half life in rat at 30 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID1356905Agonist activity at AR in human LNAR cells assessed as increase in PSA gene expression at 100 nM incubated for 24 hrs in presence of 1 uM enzalutamide by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID74373Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID248487Inhibition of human lymph node carcinoma of prostate (LNCaP) cell proliferation2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
AID266611Antagonist activity against PR beta-mediated transactivation of MMTV luciferase reporter gene in BacMam transduced progesterone-stimulated CV1 cells2006Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.
AID290021Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.
AID300615Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
AID487145Agonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1607947Half-life in rat at 0.5 mg/kg, iv2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID68116Displacement of radioligand from human Estrogen receptor beta, percent inhibition at 10 uM2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID1380139Aqueous solubility of the compound2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID237377Glycogen levels in ob/ob mice after 14 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1356912Half life in rat at 0.5 mg/kg, iv2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID238476Inhibition of human glucocorticoid receptor2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID178999Inhibitory activity against progesterone receptor (PR) in ovariectomized mature female rat decidualization model2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID300613Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
AID38820Antagonist efficacy as percent inhibition of DHT (EC50) binding to Androgen receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID1607946Volume of distribution at steady state in rat at 0.5 mg/kg, iv2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID469718Antagonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay2009Journal of natural products, Nov, Volume: 72, Issue:11
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.
AID1381665Antitumor activity against human UM1 cells implanted in Balb/C nude mouse at 1 mg, ip qd for 4 weeks2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID162124Inhibitory concentration for antagonistic activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
AID487140Displacement of [3H]E2 from human ERbeta after 16 hrs by scintillation counting2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1179643Agonist activity at progesterone receptor (unknown origin) expressed in human HepG2 cells assessed as relative luciferase activity at 1 uM by MMTV promoter-driven luciferase reporter gene assay relative to progesterone2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Triterpenes from Alisma orientalis act as androgen receptor agonists, progesterone receptor antagonists, and glucocorticoid receptor antagonists.
AID1694387Selectivity index, ratio of IC50 for human MCF-10A cells to IC50 for human MCF-7 cells2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers.
AID1356932Inhibition of CYP2C9 (unknown origin) using midazolam as substrate2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1607965Solubility of compound in fasted state simulated intestinal fluid at pH 6.52019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID126269Antagonist activity against the Mineralocorticoid Receptor (MR)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID237372Glucose levels in ob/ob mice after 13 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID162293Binding affinity at human progesterone receptor.2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID570061Antagonist activity at progesterone receptor in estrogen-primed immature New Zealand White rabbit assessed as inhibition of progesterone-induced endometrial transformation at 1 mg/kg, sc by McPhail assay2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
AID70343Displacement of radioligand from human Estrogen receptor alpha, percent inhibition at 10 uM2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID254646Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
AID126275Inhibitory activity against human mineralocorticoid receptor (hMR)1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID74076Antagonist activity against the Glucocorticoid Receptor (GR)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID426410Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay2009Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID68729Antagonist efficacy as percent inhibition of estradiol (EC50) binding to human Estrogen Receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID294500Selectivity of human progesterone receptor over human glucocorticoid receptor2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.
AID306231Oral bioavailability in mouse at 10 mg/kg2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID238443Inhibition of human progesterone receptor2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID426411Blockade of progesterone-dependent inhibition of ethinyl estradiol-induced complement C3 expression in po dosed ovariectomized Sprague-Dawley rat uterus2009Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.
AID126137Antagonist efficacy for mineralocorticoid receptor (hMR)2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID68745Antagonist activity against the Estrogen Receptor (ER)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
AID1474135AUC in human at 600 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID242094Inhibition of AR-dimerization in CHO-K1 cells expressing human androgen receptor2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
AID248679Inhibition of dexamethasone-induced glucocorticoid receptor mediated alkaline phosphatase activity2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
AID1381659Induction of PARP cleavage in human HCC1937 cells after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID1815645Effect on P4 induced PR protein level in CD-1 mouse uterus at 10 mg/kg, ip for 7 days by immunohistochemical staining method
AID74238Antagonist activity against Glucocorticoid receptor1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID304384Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation2007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
AID326403Agonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID1262373Reduction in cortisone-induced insulin level in rat at 30 mg/kg, po bid2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.
AID1356945Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID147649In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-B progesterone receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID162121In vitro antagonist activity against human progesterone receptor isoform B(hPR-B) in mammalian(CV-1) cells1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID1410419Non-competitive transrepression of GCR (unknown origin) expressed in human fibrosarcoma cells assessed as inhibition of DEX-induced GCR activation after 6 hrs by luciferase reporter gene assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Imidazo[2,1-
AID147650In vitro agonist potency in transactivation assay in neuroblastoma cells expressing human PR-A progesterone receptor; NE=no effect2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID1381663AUC (0 to t) in Sprague-Dawley rat at 30 mg/kg administered via oral gavage by HPLC analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID1240574Displacement of [3H]-progesterone from human progesterone receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID330358Agonist activity at human glucocorticoid receptor expressed in CV1 cells assessed as transcriptional activity by MMTV luciferase reporter gene assay relative to Dexamethasone2007Proceedings of the National Academy of Sciences of the United States of America, Dec-04, Volume: 104, Issue:49
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID237373Glucose levels in ob/ob mice after 14 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID162286Displacement of radioligand from human Progesterone receptor2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID483897Activity at GR in human A549 cells by NF-kappaB transrepression assay2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
AID309725Antagonist activity at glucocorticoid receptor expressed in A549 cells assessed as inhibition of corticoid-induced gene transcription by luciferase reporter gene assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.
AID1607941Inhibition of CYP3A4 (unknown origin) using midazolam as substrate2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1228843Displacement of [3H]-dexamethasone from cytosolic fraction of human recombinant glucocorticoid receptor by scintillation counting analysis2015Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
AID1694386Cytotoxicity against human MCF-10A cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers.
AID1607948Oral bioavailability in rat at 5 mg/kg2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID161807Effective concentration for human progesterone receptor in T47D human breast cancer cell; not active (<20% efficacy and/or >10 mM potency)2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID73911Antagonist efficacy as percent inhibition of Dexamethasone (EC50) binding to Glucocorticoid receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID1356324Agonist activity at PR in human T47D cells at 10 uM2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
AID343785Cmax in rat at 30 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID242073Inhibition of human progesterone receptor2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1520522Time dependent inhibition of CYP3A4 (unknown origin) assessed as Ki/Kinact ratio using testosterone as substrate2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
AID162290Binding affinity to human progesterone receptor2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
AID1356328Displacement of [1,2,6,7-3H]progesterone from recombinant human GST-tagged PGR LBD (678 to 933 residues) expressed in baculovirus-infected insect cells measured after 24 hrs by liquid scintillation counting method2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
AID1356327Antagonist activity at PR in human T47D cells assessed as inhibition of progesterone-induced beta1-Na/K-ATPase expression at 0.3 uM measured after 24 hrs by Western blot analysis2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
AID1380184Induction of NROB1 recruitment in N-terminal thrombin cleavable 6-His-tagged glucocorticoid receptor (unknown origin) at 50 uM by SPR method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID74075Inhibition of Dexamethasone binding to Glucocorticoid receptor2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.
AID529375Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells assessed as a reduction in 16S rRNA transcript at 2 uM after 24 hrs by RT-PCR2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID147648In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID1240575Binding affinity to human estrogen receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID1694385Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers.
AID74223Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID162600Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines.1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID276772Liver concentration in Sprague-Dawley rat after 7 hrs at 100 mg/kg, po2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID487139Displacement of [3H]E2 from human ERalpha after 16 hrs by scintillation counting2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1657019Inactivation of CYP3A4 (unknown origin)2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID300614Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
AID318132Displacement of [3H]dexamethasone from human recombinant GR2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
AID1687202Inhibition of GR-alpha in mouse 3T3-L1 cells assessed as reduction in adipogenic cocktail-induced Dexras1 mRNA expression at 10 uM incubated for 4 hrs by RT-qPCR analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Tigliane Diterpenoids as a New Type of Antiadipogenic Agents Inhibit GRα-Dexras1 Axis in Adipocytes.
AID162470Binding affinity determined for human Progesterone receptor A isoform1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID589138Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1356941Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1381662Tmax in Sprague-Dawley rat at 30 mg/kg administered via oral gavage by HPLC analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID487155Agonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay relative to control2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID267773Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells relative to Dexamethasone2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
AID162301Antagonist activity against human Progesterone receptor by displacement of radioligand2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID276093Lowering of plasma insulin level in DIO C57BL/6J mouse at 30 mg/kg, po after 4hrs fasting2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1356899Agonist activity at AR in human LNAR cells assessed as increase in PSA gene expression at 100 nM incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID243469Inhibition of glucocorticoid receptor mediated glycogen deposition2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID68734Efficacy as percent inhibition of Estrogen receptor with estradiol EC501998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1356947Antagonist activity at GR in monkey PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID326406Antagonist activity at human MR ligand binding domain expressed in african green monkey COS7 cells in presence of aldosterone by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID126284Antagonist activity against Mineralocorticoid receptor1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID487156Agonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay relative to control2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID483899Binding affinity to PR2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID242415Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
AID147646In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-A progesterone receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID679989TP_TRANSPORTER: increase in Calcein intracellular accumulation (Calcein: 0.5 uM, RU486: 50 uM) in GLC4/Sb30 cells1999Biochemical and biophysical research communications, May-19, Volume: 258, Issue:3
Reversal of MRP-mediated multidrug resistance in human lung cancer cells by the antiprogestatin drug RU486.
AID238359Inhibition of human androgen receptor2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID1356896Agonist activity at AR (unknown origin) expressed in human LNCaP cells incubated for 20 hrs by luciferase reporter gene assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID494981Antagonist activity at estrogen receptor ligand binding domain by two hybrid assay2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
AID394846Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISA in presence of RU-4862009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.
AID297856Antagonist activity at human GR expressed in CV1 cells by GRE activation assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
AID1356323Antagonist activity at PR in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity measured after 24 hrs2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
AID300619Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay relative to Dexamethasone2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
AID73916Efficacy as percent inhibition of glucocorticoid receptor with EC50 Dexamethasone1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID1356931Inhibition of CYP2C8 (unknown origin) using midazolam as substrate2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1356914Cmax in rat at 5 mg/kg, po2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID181268Antiglucocorticoid activity in adrenalectomized young male rats after oral administration2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID483900Antagonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of dexamethasone-induced luciferase transactivation activity after 24 hrs2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
AID1815636Inhibition of P4 induced antiproliferative activity against CD-1 mouse uterine epithelial cell at 10 mg/kg, ip for 7 days by immunohistochemistry method
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1228869Antidepressant-like activity in Wistar rat assessed as immobility time at 30 mg/kg, po administered at 1, 5, 23.5 hrs prior to testing measured for 5 mins by forced swimming test (Rvb = 211.3 to 232.2 secs)2015Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
AID1380185Induction of NRIP1 recruitment in N-terminal thrombin cleavable 6-His-tagged glucocorticoid receptor (unknown origin) at 50 uM by SPR method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID267775Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID276768Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID162129Inhibition of human progesterone receptor activation in T47D human breast cancer cell.2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID1694384Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers.
AID1815668Toxicity in P4 induced CD-1 mouse assessed as effect on uterus weight at 10 mg/kg,ip for 7 days (Rvb= 0.033g)
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID306224Clearance in mouse at 2 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID38993Inhibition of antagonist activity towards Androgen receptor2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID237375Insulin levels in ob/ob mice after 13 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1356900Agonist activity at AR in human LNAR cells assessed as increase in TMPRSS2 gene expression at 100 nM incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID147652In vitro agonist potency in transactivation assay of neuroblastoma cells expressing human PR-B progesterone receptor; NE=no effect2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID1687197Inhibition of adipogenic cocktail-induced PPARgamma mRNA expression in mouse 3T3-L1 cells at 1 uM by RT-qPCR analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Tigliane Diterpenoids as a New Type of Antiadipogenic Agents Inhibit GRα-Dexras1 Axis in Adipocytes.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID426409Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity2009Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.
AID290023Selectivity for human progesterone receptor over human glucocorticoid receptor2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.
AID1544148Induction of neurite outgrowth in human SH-SY5Y cells assessed as increase in neurite length of more than 50 micrometer by measuring cell differentiation at 1 uM incubated for 6 days by Giemsa staining based phase contrast microscopic analysis relative to2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Profiling withanolide A for therapeutic targets in neurodegenerative diseases.
AID1356933In-vivo inhibition of CYP2C8 in mouse assessed as increase in paclitaxel plasma concentration after 2 to 26 hrs2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID237376Insulin levels in ob/ob mice after 14 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID162467Binding affinity against human progesterone receptor-A (hPR-A)1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
AID1607932Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1381664AUC (0 to infinity) in Sprague-Dawley rat at 30 mg/kg administered via oral gavage by HPLC analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID161953Agonist efficacy towards human progesterone receptor (hPR) expressed in CV-1 cells; Not active2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
AID483901Antagonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of dexamethasone-induced luciferase transactivation activity after 24 hrs relative to RU4862010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1815638Upregulation of P4 induced HAND2 expression in CD-1 mouse uterus at 10 mg/kg, ip for 7 days by immunohistochemical staining method
AID289555Inhibition of prednisilone-induced glycogen depostion in Sprague-Dawley rats at 100 mg/kg, po2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
AID74375Relative binding affinity to glucocorticoid receptor on cytosol from liver at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID243325Activity against dexamethasone-induced GR-mediated TAT activity in rat hepatocytes2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID38975Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells.1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
AID242138Inhibition of human androgen receptor expressed in Escherichia coli2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
AID162608Displacement of [3H]progesterone from human Progesterone receptor2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
AID309452Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in recombinant baculovirus2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
AID306213Antagonist activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of corticoid-induced transcription by glucocorticoid response element-linked luciferase reporter gene assay2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID529368Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells 0.02 to 2 uM after 72 hrs2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID326397Displacement of [3H]R5020 from human PR in human T47D cells by whole cell assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID1607942Inhibition of CYP2C8 (unknown origin) using paclitaxel as substrate2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1228868Antidepressant-like activity in Wistar rat assessed as immobility time at 10 mg/kg, po administered at 1, 5, 23.5 hrs prior to testing measured for 5 mins by forced swimming test (Rvb = 211.3 to 232.2 secs)2015Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
AID345895Antagonist 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 hrs2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Syntheses and antigestagenic activity of mifepristone derivatives.
AID289552Inhibition of human GR expressed in hGRAF cells2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
AID306227Half life in mouse at 2 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID32841Antagonistic potency to the human progesterone receptor measured in the T-47D alkaline phosphatase assay1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID181267Antiandrogenic activity in orchidectomized young male rats after oral administration2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1228872Antidepressant-like activity in Wistar rat assessed as decrease in immobility time at 30 mg/kg, po administered at 1, 5, 23.5 hrs prior to testing measured for 5 mins by forced swimming test relative to vehicle-treated control2015Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
AID238475Inhibition of human Estrogen receptor alpha2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID1815670Toxicity in P4 induced CD-1 mouse assessed as effect on liver weight at 10 mg/kg, ip for 7 days (Rvb= 1.3 g)
AID1607943Displacement of fluormone tracer from full length human recombinant glucocorticoid receptor expressed in baculovirus expression system incubated for 2 hrs by competitive fluorescence polarization binding assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID487142Displacement of [3H]aldosterone from human mineralocorticoid receptor after 16 hrs by scintillation counting2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID318134Displacement of [3H]dihydrotesterone from PR2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID638166Intrinsic clearance in liver microsomes2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.
AID162284Binding affinity towards progesterone receptor was measured2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.
AID487141Displacement of [3H]dexamethasone from human glucocorticoid receptor after 16 hrs by scintillation counting2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID529374Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells at 2 uM after 72 hrs in presence of cycloheximide2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID309457Displacement of [3H]progesterone from progesterone receptor at 10 uM2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
AID297855Antagonist efficacy at human GR expressed in CV1 cells by GRE activation assay relative to Dexamethasone2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID529369Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID74213Inhibition of antagonist activity towards glucocorticoid receptor2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID237367Liver levels in ob/ob mice after 14 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1607945Clearance in rat at 0.5 mg/kg, iv2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID1815671Toxicity in P4 induced CD-1 mouse assessed as effect on glucose level at 10 mg/kg, ip for 7 days (Rvb=231.6 mg/dL)
AID74220Binding affinity was determined for human glucocorticoid receptor(hGR).1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID162282Antagonist activity against human Progesterone receptor as displacement of radioligand, percent inhibition at 1 uM2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID529377Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells assessed as a reduction in 16S rRNA transcript at 2 uM after 24 hrs by RT-PCR in presence of cycloheximide2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID289556Inhibition of prednisilone-induced lymphopenia in Sprague-Dawley rats at 100 mg/kg, po2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID243517Inhibition of glucocorticoid receptor mediated tyrosine aminotransferase activity2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID68725Antagonist efficacy for Estrogen receptor2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1380187Induction of PRGC2 recruitment in N-terminal thrombin cleavable 6-His-tagged glucocorticoid receptor (unknown origin) at 50 uM by SPR method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
AID242171Inhibition of human mineralocorticoid receptor2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1155483Neuroprotective activity against rat PC12 cells assessed as protection against corticosterone- induced lesion at 1.25 uM after 1 day by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Synthesis and biological evaluation of novel naphthalene compounds as potential antidepressant agents.
AID487819Agonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay relative to control2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID68887Inhibitory activity against human estrogen receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID1607934Agonist activity at human progesterone receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID237398Alanine aminotransferase (ALT) levels in ob/ob mice after 13 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1210949Ratio of Kinact to Ki for CYP3A4 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug.
AID343795AUC (0 to infinity) in rat at 30 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID119318Effect on pregnancy in mice as number pregnant/mated at 0.5 mg/mouse dose with simultaneous 0.5 mg RU-486 dose; out of 161998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.
AID276774Inhibition of prednisilone-induced glycogen deposition in Sprague-Dawley rat at 100 mg/kg, po2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID110453Effect on pregnancy in mice as corpora lutea at 0.5 mg/mouse dose with simultaneous 0.5 mg RU-486 dose1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.
AID644976Selectivity ratio of IC50 for progesterone receptor in human T47D cells to IC50 for glucocorticoid receptor in human A549 cells2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihormonal properties of novel 11β-benzoxazole-substituted steroids.
AID267774Activity at GR assessed as ability to antagonize dexamethasone-induced MMTV luciferase reporter gene transactivation in human A549 cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
AID387090Antagonist activity at glucocorticoid receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
AID276770Protein binding in rat plasma2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID39138Displacement of [3H]DHT from human Androgen receptor2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID256204Percent efficacy for transcriptional repression of IL-6 production in IL-1 stimulated human foreskin fibroblasts at 2 uM2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
AID238669Inhibition of glucocorticoid receptor mediated tyrosine amino transferase activity2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID1356943Antagonist activity at GR in rat PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID161960Efficacy at human progesterone receptor in CV-1 cells.2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID105813Antagonist activity against human mineralocorticoid receptor as displacement of radioligand2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID680146TP_TRANSPORTER: increase in Doxorubicin intracellular accumulation (Doxorubicin: 10 ug/mL, RU486: 10 uM) in K562 R7 cells1994FEBS letters, Nov-28, Volume: 355, Issue:2
The antiprogestatin drug RU 486 potentiates doxorubicin cytotoxicity in multidrug resistant cells through inhibition of P-glycoprotein function.
AID1356906Agonist activity at AR in human LNAR cells assessed as increase in TMPRSS2 gene expression at 100 nM incubated for 24 hrs in presence of 1 uM enzalutamide by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID306222Cmax in mouse at 2 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID1356348Antagonist activity at human PRB expressed in African green monkey CV1 cells2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
AID39009Binding affinity determined against human Androgen receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID1356946Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID289554Inhibition of prednisilone-induced TAT level in Sprague-Dawley rats at 100 mg/kg, po2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
AID1381669Cell cycle arrest in human SUM149PT cells assessed as increase in cells at G1 phase at 20 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID1356944Antagonist activity at GR in rat PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID343783Antiprogestin activity against ovariectomized po dosed Sprague-Dawley rat assessed as effect on ethinyl estradiol-induced C3 expression2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID487152Antagonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID326405Agonist activity at human MR ligand binding domain receptor expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID185802Ability to block progesterone induced stimulation of rat uterine luminal cells at 3 mg/kg peroral dose in rat decidualisation assay2002Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.
AID276097Effect on plasma triglyceride level in DIO C57BL/6J mouse at 30 mg/kg, po after 4 hr fasting2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID68900Binding affinity for human estrogen receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID267772Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
AID1474137Ratio of drug concentration at steady state in human at 600 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID182657Ability to block progesterone induced stimulation of rat uterine luminal cells at 3 mg/kg peroral dose in rat decidualisation assay2002Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.
AID126140Antagonist efficacy as percent inhibition of aldosterone (EC50) binding to Mineralocorticoid receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
AID487146Agonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1240570Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID1423422Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate assessed as testosterone 6beta-hydroxylation rate at 50 uM preincubated for 30 mins followed by substrate/NADPH addition measured after 10 mins by LC-MS/MS analy2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.
AID39320Relative binding affinity for androgen receptor of prostate of rat at 2 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID306230AUC in mouse at 10 mg/kg, po2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID1694382Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID150738Compound was tested for the binding affinity towards recombinant NBD2 C-terminal cytotoxic nucleotide-binding domain of mouse P-Glycoprotein2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
The flavanolignan silybin and its hemisynthetic derivatives, a novel series of potential modulators of P-glycoprotein.
AID306225Tmax in mouse at 2 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID1356907Agonist activity at AR in human MDA-MB-453 cells assessed as increase in CLDN8 gene expression at 111 to 333 nM incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID330907Displacement of quinaldine red from human AAG by fluorescence method2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1815651Effect on P4 induced GR expression in CD-1 mouse uterine stroma at 10 mg/kg, ip for 7 days by immunohistochemical analysis
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID294498Antagonist activity at human progesterone receptor assessed as inhibition of alkaline phosphatase activity in human T47D cells2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID529371Cytotoxicity against human Hep2 cells at 20 uM2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID387091Antagonist activity at mineralocorticoid receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
AID161976In vitro antagonist activity against human progesterone receptor isoform B(hPR-B) in mammalian(CV-1) cells as percent inhibition1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID74235Antagonist activity as displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
AID306234Decrease in plasma glucose level in po dosed ob/ob mouse after 15 days by OGTT2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID1356948Antagonist activity at GR in monkey PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1356915AUC in rat at 5 mg/kg, po2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID73783Antagonist efficacy for glucocorticoid receptor2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID638167Antagonist activity at progesterone receptor2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.
AID1833848Antagonist activity at glucocorticoid receptor in human HeLa cells assessed as reduction in dexamethasone-induced luciferase activity by dual-Glo luciferase assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Discovery of a Novel Androgen Receptor Antagonist Manifesting Evidence to Disrupt the Dimerization of the Ligand-Binding Domain via Attenuating the Hydrogen-Bonding Network Between the Two Monomers.
AID487148Antagonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID309453Antagonist activity at human glucocorticoid receptor in SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression by MMTV5 reporter gene assay2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
AID213399Inhibition of prednisilone-induced tyrosine aminotransferase (TAT) activity in rat hepatocytes2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.
AID289551Displacement of radiolabeled Dexamethasone from human GR2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
AID306226Tmax in mouse at 10 mg/kg, po2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1381656Inhibition of KLF5 expression levels in human SUM149PT cells after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID161951Agonist efficacy for human progesterone receptor in T47D human breast cancer cell; not active (<20% efficacy and/or >10 mM potency)2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID387089Antagonist activity at androgen receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
AID248130Antagonistic activity against 5 nM Dexamethasone induced glucocorticoid receptor mediated alkaline phosphatase activity2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID345893Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Syntheses and antigestagenic activity of mifepristone derivatives.
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID529370Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells at 20 uM2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID38818Antagonist efficacy for human Androgen receptor2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID1262372Reduction in cortisone-induced glucose level in rat at 30 mg/kg, po bid2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.
AID1423418Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate assessed as testosterone 6beta-hydroxylation rate at 10 uM preincubated for 30 mins followed by substrate/NADPH addition measured after 10 mins by LC-MS/MS analy2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID1199782Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID343793AUC (last) in rat at 30 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID343791Mean retention time in rat at 30 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids.
AID241310Inhibition of [3H]dexamethasone binding to human glucocorticoid receptor2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
AID487143Agonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID240092Antagonistic activity against VP-16 transcriptional activation domain protein2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID244578Inhibition of glucocorticoid receptor dependent alkaline phosphatase activity2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID255347Percentage inhibition of dexamethasone-induced glucocorticoid receptor transactivation of the mouse mammary tumor virus(MMTV) luciferase gene in HeLa cells at a concentration of 100 nM2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
AID306228Half life in mouse at 10 mg/kg, po2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
AID1356895Agonist activity at human GR expressed in CHO-K1 cells incubated for 20 hrs by luciferase reporter gene assay relative to dexamethasone2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID326404Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID1482037Antagonist activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor
AID162273Progesterone receptor antagonist activity based on its ability to block progesterone induced alkaline phosphatase in the human breast cancer cell line T47D2002Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.
AID1815641Inhibition of PR induced ZBTB16 expression in CD-1 mouse uterus at 10 mg/kg, ip for 7 days by Immunohistochemical staining method
AID241977Inhibition of human androgen receptor2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID237381Cholesterol levels in ob/ob mice after 14 days of oral dose at 100 mpk b.i.d.2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID276767Binding affinity to human GR2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
AID1381661Elimination half life in Sprague-Dawley rat at 30 mg/kg administered via oral gavage by HPLC analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer.
AID162613Relative binding affinity for progestin receptor of uterus of rabbit at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID251370Reduction of uterine weight in pregnant rats after q.d. oral dosing at 3 mpk2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID307858Binding affinity to progesterone receptor2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.
AID126143Efficacy as percent inhibition of Mineralocorticoid receptor with aldosterone EC501998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID74377Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID126279Inhibition of antagonist activity towards mineralocorticoid receptor (hMR)2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
AID1240572Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
AID1482059In vivo antagonist activity at glucocorticoid receptor in Sprague-Dawley rat cortisone model of exogenous Cushing's syndrome assessed as inhibition of plasma insulin levels at 30 mg/kg, po bid via gavage for 6 days pretreated for 12 hrs followed by cortis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor
AID529372Antimicrobial activity against Chlamydia pneumoniae infected in HEp-2 cells assessed as inhibition of bacterial replication at 2 uM after 24 hrs2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Chlamydia pneumoniae growth inhibition in cells by the steroid receptor antagonist RU486 (mifepristone).
AID68912Antagonist activity against Estrogen receptor1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
AID1356952Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1797838Competitive Receptor Binding Assay from Article 10.1021/jm050205o: \\Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.\\2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID1797746GR-Mediated Antagonist Activity Assay and IL-6 Repression Assay from Article 10.1021/jm070370z: \\Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.\\2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
AID1797837GR Binding Assay and GRAF Assay from Article 10.1021/jm050205o: \\Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.\\2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1346741Human Pregnane X receptor (1I. Vitamin D receptor-like receptors)1998The Journal of clinical investigation, Sep-01, Volume: 102, Issue:5
The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
AID1346849Human Glucocorticoid receptor (3C. 3-Ketosteroid receptors)1987Journal of steroid biochemistry, Feb, Volume: 26, Issue:2
Plasma concentrations and receptor binding of RU 486 and its metabolites in humans.
AID1346851Human Progesterone receptor (3C. 3-Ketosteroid receptors)2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
AID1346849Human Glucocorticoid receptor (3C. 3-Ketosteroid receptors)1993European journal of pharmacology, Oct-15, Volume: 247, Issue:2
Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
AID1346888Human Androgen receptor (3C. 3-Ketosteroid receptors)2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2009The Journal of biological chemistry, Jul-17, Volume: 284, Issue:29
The X-ray structure of RU486 bound to the progesterone receptor in a destabilized agonistic conformation.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,308)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990544 (8.62)18.7374
1990's1908 (30.25)18.2507
2000's1911 (30.29)29.6817
2010's1482 (23.49)24.3611
2020's463 (7.34)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 120.72

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.

MetricThis Compound (vs All)
Research Demand Index120.72 (24.57)
Research Supply Index8.87 (2.92)
Research Growth Index4.90 (4.65)
Search Engine Demand Index228.83 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (120.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials595 (9.10%)5.53%
Reviews567 (8.68%)6.00%
Case Studies129 (1.97%)4.05%
Observational29 (0.44%)0.25%
Other5,216 (79.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (167)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Evaluation of the Efficacy, Tolerance of the Treatment, and Patient Satisfaction During the Management of an Arrested Pregnancy in the First Trimester According to the New Toulouse University Hospital Protocol [NCT05049980]52 participants (Actual)Interventional2021-11-01Completed
Phase II Study of Pembrolizumab and Mifepristone in Patients With Advanced HER2-negative Breast Cancer [NCT03225547]Phase 274 participants (Anticipated)Interventional2018-02-12Active, not recruiting
An Open Label Study of 400 mcg Sublingual Misoprostol Following Mifepristone 200 mg for Abortion up to 63 Days LMP [NCT01173003]688 participants (Actual)Interventional2009-06-30Completed
A RANDOMIZED, PHASE II STUDY OF ENZALUTAMIDE, ENZALUTAMIDE WITH MIFEPRISTONE, and TREATMENT OF PHYSICIAN'S CHOICE IN PATIENTS WITH AR+ METASTATIC TRIPLE-NEGATIVE OR ER-LOW BREAST CANCER [NCT06099769]Phase 2201 participants (Anticipated)Interventional2023-10-18Recruiting
Short-Term Oral Mifepristone for Central Serous Chorioretinopathy. A Placebo-controlled Dose Ranging Study of Mifepristone in the Treatment of CSC (STOMP-CSC) [NCT02354170]Phase 216 participants (Actual)Interventional2015-01-31Completed
Mifepristone and Misoprostol Versus Misoprostol Alone for Missed Abortion: A Randomized-controlled Trial [NCT02342002]Phase 4416 participants (Anticipated)Interventional2015-01-31Terminated(stopped due to lack of funding)
Alternative Provision of Medication Abortion Via Pharmacy Dispensing [NCT03320057]Phase 4326 participants (Actual)Interventional2018-06-01Completed
An Outpatient Medical Abortion Regimen With Mifepristone and Two Doses of Misoprostol at 71-77 and 78-84 Days of Pregnancy [NCT05119439]Phase 423 participants (Actual)Interventional2022-10-07Terminated(stopped due to Enrollment)
Improving Access to Abortion in the Republic of Georgia [NCT04458558]Phase 4120 participants (Anticipated)Interventional2020-06-30Recruiting
A Phase I Adaptive Dose, Double-Blind, Placebo-Controlled, SAD and MAD Study to Measure the Safety, Tolerability, Pharmacokinetics and Pharmacological Effects of Orally Administered CORT125134 in Healthy Subjects [NCT03508635]Phase 1130 participants (Actual)Interventional2014-09-30Completed
Acceptability and Feasibility of a Simplified Medical Abortion Regimen in Georgia: A Study of 400 mcg Buccal Misoprostol Following 200 mg Mifepristone for Abortion up to 63 Days Gestation [NCT02398838]622 participants (Actual)Interventional2009-12-31Completed
A Randomized, Placebo-Controlled, Double-Blind, Phase II Trial of Nanoparticle Albumin-Bound Paclitaxel (Nab-Paclitaxel, Abraxane®) With or Without Mifepristone for Advanced, Glucocorticoid Receptor-Positive, Triple-Negative Breast Cancer [NCT02788981]Phase 264 participants (Anticipated)Interventional2017-03-28Active, not recruiting
A Pilot Study on the Safety and Efficacy of Mifepristone for the Prevention of Relapses of Alcohol Drinking [NCT02243709]Phase 1/Phase 232 participants (Actual)Interventional2014-09-30Completed
Outpatient Medical Abortion With Mifepristone and Misoprostol Through 77 Days of Gestation: A Non-inferiority Trial [NCT02314754]Phase 4719 participants (Actual)Interventional2014-12-31Completed
Study of Hypercortisolism in Patients With Difficult to Control Type 2 Diabetes Despite Receiving Standard-of-Care Therapies: Prevalence and Treatment With Korlym® (Mifepristone) (CATALYST) [NCT05772169]Phase 41,000 participants (Anticipated)Interventional2023-03-31Recruiting
Randomized Controlled Trial of Mifepristone Versus Laminaria for Cervical Ripening In Midtrimester Induction [NCT00383032]72 participants Interventional2004-01-31Completed
A Multicenter Randomized Clinical Trial of Mifepristone Versus GnRHa for the Treatment of Adenomyosis [NCT05151016]Early Phase 1140 participants (Anticipated)Interventional2021-12-01Not yet recruiting
The Effect of a Progesterone Receptor Modulator on Breast Tissue in Women With BRCA-1 and -2 Mutations - a Placebo Controlled RCT. [NCT01898312]Phase 245 participants (Actual)Interventional2013-09-30Completed
Cervical Prostaglandin EP3 Receptor mRNA Expression 48 Hours After Administration of Mifepristone [NCT01224509]18 participants (Actual)Interventional2004-09-30Terminated(stopped due to Longer than expected recruitment period.)
A Biomarker Study of Mifepristone in Early Stage Breast Cancer [NCT01138553]Early Phase 14 participants (Actual)Interventional2010-06-30Terminated(stopped due to Inadequate subject accrual)
Comparison Between Misopristol and Pitocin After Mifepristone Preparation for Second Trimeter Abortion [NCT00784797]Phase 4145 participants (Actual)Interventional2009-01-31Completed
Efficacy of Mifepristone in Males With Type 2 Diabetes Mellitus [NCT03052400]Phase 28 participants (Actual)Interventional2017-02-03Terminated(stopped due to End of Funding)
Evaluation of Efficacy of Two Therapeutic Strategies for Cervical Maturation Before Medical Termination: Mechanical Plus Medicinal Maturation vs Medicinal Maturation Alone [NCT03194126]120 participants (Actual)Interventional2018-02-11Completed
A Pilot Study of the Effect of a Glucocorticoid Receptor Antagonist in Patients With Subclinical Cushings [NCT00721201]Phase 1/Phase 26 participants (Anticipated)Interventional2008-11-30Completed
"Evaluating the Safety, Acceptability and Feasibility of an Outpatient Day Procedure Service Documenting the Roles of Health Workers in the Provision of Medical Abortion at 13-18 Weeks Gestation" [NCT03346629]Phase 4230 participants (Actual)Interventional2017-12-01Completed
Comparison of Efficacy and Safety of Sequential Use of Mifepristone and Misoprostol vs Misoprostol Alone in Women With Early Pregnancy Loss: Randomized Controlled Trial [NCT05124314]Phase 4220 participants (Anticipated)Interventional2021-10-27Recruiting
Compassionate Use Protocol for the Administration of CORLUX® (Mifepristone) in the Treatment of the Signs and Symptoms of Endogenous Cushing's Syndrome [NCT01371565]Phase 34 participants (Actual)Interventional2010-11-30Completed
RESET-medication: Glucocorticoid Receptor (GR) Blockade as Diseasemodifying Treatment for Depression With Childhood Trauma [NCT05217758]Phase 2158 participants (Anticipated)Interventional2021-12-09Recruiting
A Randomised Placebo-controlled Trial of Mifepristone and Misoprostol Versus Misoprostol Alone in the Medical Management of Missed Miscarriage [NCT03065660]Phase 3711 participants (Actual)Interventional2017-09-20Completed
Mifepristone 5 mg Versus 10 mg for the Treatment of Uterine Leiomyomata. A Randomized, Double Blinded Clinical Trial. [NCT00712595]Phase 2/Phase 3200 participants (Actual)Interventional2007-01-31Completed
A Phase I, Open-Label, Fixed-Sequence Study to Determine the Effect of Single and Multiple Oral Doses of CORLUX (TM) (Mifepristone) on the Pharmacokinetics of a Single Oral Dose of Fluvastatin (a CYP2C9 Probe) in Healthy Volunteers [NCT00752843]Phase 120 participants (Actual)Interventional2008-09-30Completed
Uptake and Acceptability of Home-use of Mifepristone for Medical Abortion [NCT00994734]615 participants (Actual)Interventional2009-05-31Completed
Mifepristone 5 mg Versus 10 mg During 6 Months for the Treatment of Uterine Leiomyomata. A Randomized, Double Blinded Clinical Trial. [NCT00886873]Phase 2/Phase 3100 participants (Actual)Interventional2008-05-31Completed
Mifepristone Versus Osmotic Dilators in Conjunction With Misoprostol for Cervical Preparation Prior to D&E at 14-19 Weeks [NCT02679092]0 participants (Actual)Interventional2016-04-30Withdrawn(stopped due to Funding changes.)
Comparing Two Regimens for Medical Abortion: Mifepristone+Misoprostol Versus Misoprostol Alone [NCT00680394]440 participants (Actual)Interventional2007-07-31Completed
Novel Therapeutics in PTSD: A Randomized Clinical Trial of Mifepristone [NCT00833339]Phase 280 participants (Anticipated)Interventional2008-05-31Recruiting
A Phase II Study of Treatment With Oral Mifepristone as Salvage Therapy in Patients With Advanced or Metastatic Non-Small Cell Lung Cancer Who Have Failed Two or More Previous Chemotherapy Regimens [NCT02642939]Phase 23 participants (Actual)Interventional2015-12-31Terminated(stopped due to Lack of enrollment)
Glucocorticoid Antagonists in Heavy Drinkers: Effects on fMRI Connectivity, Withdrawal and Drinking [NCT02989662]150 participants (Anticipated)Interventional2016-02-29Recruiting
A Randomized, Double-blind Placebo-controlled Crossover Trial of Mifepristone in Gulf War Veterans With Chronic Multisymptom Illness [NCT00691067]Phase 465 participants (Actual)Interventional2008-05-31Completed
Mifepristone and Misoprostol Versus Misoprostol Alone for Mid-trimester Termination of Pregnancy (14 - 21 Weeks LMP): A Randomized-controlled Double-blinded Trial [NCT00784186]120 participants (Actual)Interventional2008-08-31Completed
Pilot Study of an Ambulatory Medical Abortion Service at 13-18 Weeks of Gestation in Colombia [NCT04063904]Phase 416 participants (Actual)Interventional2019-10-16Terminated(stopped due to Difficulties with recruitment, COVID 19 pandemic)
The Effect of Vaginal Mifepristone on Reduction of Uterine Fibroids Size and the Symptoms Associated With the Fibroids - Pilot Study (Phase IIa) [NCT00881140]Phase 230 participants (Actual)Interventional2009-04-30Completed
A Randomized Controlled Trial to Compare Sublingual and Buccal Misoprostol Regimens After Mifepristone for Termination of Pregnancy 13 - 21 Weeks From Last Menstrual Period (LMP) [NCT02708446]Phase 4320 participants (Anticipated)Interventional2014-05-31Recruiting
Mifepristone and Misoprostol Versus Misoprostol Alone for Mid-trimester Termination of Pregnancy (14-21 Weeks LMP): A Randomized-controlled Double-blinded Trial [NCT00957346]Phase 320 participants (Anticipated)Interventional2011-02-28Terminated
Mifepristone and Misoprostol Versus Misoprostol Alone for Mid-trimester Termination of Pregnancy (14 - 21 Weeks LMP): A Randomized-controlled Double-blinded Trial [NCT00969982]238 participants (Actual)Interventional2009-06-30Completed
Comparison of the Effectiveness of Abortive Measures From the Administration of Mifegyne and Cytotec at One and Two Visits [NCT00920465]Phase 3200 participants (Anticipated)Interventional2009-06-30Recruiting
A Randomized, Double-Blind, Placebo-Controlled Study of Safety and Efficacy of CORLUX™ (Mifepristone) in the Treatment of Psychotic Symptoms in Patients With Major Depressive Disorder With Psychotic Features [NCT00130676]Phase 3257 participants (Actual)Interventional2004-09-30Completed
The Effectiveness, Safety, and Acceptability of Home-administered Medical Abortion at Gestational Age of 8 to ≤9 Weeks Versus >9 to ≤12 Weeks: A Prospective Cohort Study in Mexico City [NCT02745093]Phase 4648 participants (Anticipated)Interventional2016-09-30Not yet recruiting
A Pilot Study of the Acceptability and Feasibility of an Out-patient Regimen of Medical Abortion With Mifepristone and 400 mcg Sublingual Misoprostol at 71-77 and 78-84 Days Gestation [NCT02720991]Phase 450 participants (Actual)Interventional2014-07-31Completed
Carboplatin, Gemcitabine, and Mifepristone for Advanced Breast Cancer and Recurrent or Persistent Epithelial Ovarian Cancer [NCT02046421]Phase 131 participants (Actual)Interventional2013-11-30Completed
An Open-label Study of the Efficacy and Safety of CORLUX (Mifepristone) in the Treatment of the Signs and Symptoms of Endogenous Cushing's Syndrome [NCT00569582]Phase 350 participants (Actual)Interventional2007-12-31Completed
A Phase II Evaluation of Mifepristone in the Treatment of Recurrent or Persistent Epithelial Ovarian or Primary Peritoneal Carcinoma [NCT00459290]Phase 224 participants (Actual)Interventional2007-05-31Completed
Assessing Acceptability and Use of Medical Menstrual Regulation in the United States [NCT03972358]Phase 2284 participants (Anticipated)Interventional2020-02-12Recruiting
Treatment of Early Pregnancy Failure [NCT00468299]16 participants (Actual)Interventional2007-04-30Terminated(stopped due to poor enrollment)
A Double-blind, Placebo-controlled Study of Mifepristone in Patients With Non-psychotic Major Depressive Disorder Referred for Bilateral Electroconvulsive Therapy (ECT) [NCT00285818]11 participants (Actual)Interventional2003-01-31Completed
A Randomized, Placebo-Controlled, Phase I/II Trial of the Anti-HIV Activity and Safety of VGX-410 (Mifepristone) at Three Dose Levels in HIV-1 Infected Subjects [NCT00099645]Phase 1/Phase 248 participants InterventionalCompleted
Early Versus Delayed Insertion of Nexplanon® at Medical Abortion - a Randomized Controlled Equivalence Trial. [NCT01920022]Phase 4551 participants (Actual)Interventional2013-10-31Completed
Pre-treatment With Mifepristone in Patients With Mirena for Optimizing Bleeding Pattern in Pre-menopausal Women [NCT01931657]Phase 260 participants (Anticipated)Interventional2013-08-31Completed
Cervical Preparation With Mifepristone Prior to Osmotic Dilators: A Randomized, Double-blind, Placebo-controlled Pilot Study [NCT03714880]Phase 244 participants (Actual)Interventional2019-04-26Terminated(stopped due to Slow recruitment compounded by COVID-19)
Effects of Mifepristone on Biomarkers of Metabolic Function and Neuropsychological Performance Among Middle-Aged and Older Individuals [NCT01988610]Phase 123 participants (Actual)Interventional2013-10-31Completed
Phase 1 Study of Mifepristone in Combination With Eribulin in Patients With Locally Advanced/Metastatic Breast or Other Specified Solid Tumors, With a Dose Expansion Cohort in Patients With Triple Negative Breast Cancer. [NCT02014337]Phase 137 participants (Actual)Interventional2014-01-31Completed
Acceptability and Feasibility of a Simplified Medical Abortion Regimen in Kazakhstan: A Study of 600 µg Sublingual Misoprostol Following 200 mg Mifepristone for Abortion up to 70 Days Gestation [NCT02018796]290 participants (Actual)Observational2013-10-31Completed
Acceptability and Feasibility of a Demedicalized Medical Abortion Regimen in the Caucasus [NCT02219100]613 participants (Actual)Interventional2010-11-30Completed
A Pilot Study of Mifepristone Followed by Misoprostol in Women Undergoing Second Trimester Abortion [NCT00592215]Phase 10 participants (Actual)Interventional2008-03-31Withdrawn
Hypothalamic-Pituitary-Adrenal (HPA)/Dopamine Axis in Psychotic Depression [NCT00867360]Phase 310 participants (Actual)Interventional2005-08-31Terminated(stopped due to Insufficient recruitment.)
Non-surgical Alternatives to Treatment of Failed Medical Abortion: A Randomized Controlled Double-blind Trial [NCT02704481]Phase 416 participants (Actual)Interventional2016-06-01Terminated(stopped due to Funding mechanism compromised)
Understanding Gulf War Illness: An Integrative Modeling Approach [NCT04255498]Phase 120 participants (Anticipated)Interventional2017-10-30Recruiting
Mifepristone and Misoprostol Versus Misoprostol Alone for Treatment of Fetal Death at 14-28 Weeks of Pregnancy: A Randomized, Placebo-controlled Double-blinded Trial [NCT02633761]Phase 3200 participants (Anticipated)Interventional2015-04-01Terminated(stopped due to Lack of funding)
Medical Termination of Pregnancy Due to Emergency Contraception Failure: A Randomized Trial Comparing Mifepristone Combined Misoprostol and Misoprostol Alone. [NCT00677755]394 participants (Actual)Interventional2004-10-31Completed
Mifepristone Treatment for Breast Cancer Patients Expressing Levels of Progesterone Receptor Isoform A (PRA) Higher Than Those of Isoform B (PRB): Neoadjuvant Therapy. [NCT02651844]20 participants (Actual)Interventional2016-04-30Completed
Glucocorticoid Antagonist Treatment for Tobacco Use Disorder [NCT03248713]Early Phase 18 participants (Actual)Interventional2017-11-29Terminated(stopped due to Lack of recruitment)
Mifepristone and Misoprostol for the Treatment of Early Pregnancy Failure: a Pilot Clinical Trial [NCT00177372]Phase 430 participants (Actual)Interventional2005-01-31Completed
Feasibility and Acceptability of Dispensing Mifepristone Via Mail Order Pharmacy [NCT03913104]Phase 4538 participants (Actual)Interventional2020-01-05Active, not recruiting
The Extended Gestational Age Medical Abortion Study: The Effectiveness of Medical Abortion With Mifepristone and Misoprostol at 57-63 Days Versus 64-70 Days Gestation [NCT00997347]Phase 41,400 participants (Actual)Interventional2009-07-31Completed
"Assessing Use Of Mifepristone After Progestin Priming For Use As Missed Period Pills" [NCT04676776]Phase 2139 participants (Anticipated)Interventional2021-01-25Recruiting
[NCT00206193]0 participants ObservationalRecruiting
The Effect of Preoperative Treatment With Mifepristone on Uterine Fibroids and Breast Tissue [NCT00579475]Phase 130 participants (Actual)Interventional2004-11-30Completed
The Acceptability of an Out-patient Regimen of Medical Abortion With Mifepristone and 800 Mcg Misoprostol Administered Buccally or Sublingually at 78-84 Days Gestation: Two Pilot Studies [NCT01856985]Phase 450 participants (Actual)Interventional2013-04-30Completed
A Randomized Phase I Trial of Nanoparticle Albumin Bound Paclitaxel (Nab-paclitaxel, Abraxane) With or Without Mifepristone for Advanced Breast Cancer [NCT01493310]Phase 19 participants (Actual)Interventional2011-11-30Completed
A Two-Week, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Mifepristone in the Prevention of Olanzapine-Induced Weight Gain in Healthy Male Volunteers [NCT00455442]Phase 257 participants (Actual)Interventional2007-03-31Completed
Phase II Study of Mifepristone (RU-486) in the Treatment of PR Positive Advanced/Recurrent Endometrioid Adenocarcinoma and Low Grade Endometrial Stromal Sarcoma (LGESS) [NCT00505739]Phase 213 participants (Actual)Interventional2001-09-30Completed
Mifepristone and Misoprostol for Undesired Pregnancy of Unknown Location: A Randomized Pilot Study of Misoprostol Dosing [NCT05839899]Phase 350 participants (Anticipated)Interventional2023-08-30Recruiting
COMPARATIVE STUDY OF EFFECTS BETWEEN LETROZOLE PLUS MISOPROSTOL AND MIFEPRISTONE PLUS MISOPROSTOL IN TERMINATING NON-VIABLE FIRST TRIMESTER PREGNANCIES [NCT05304273]Phase 3120 participants (Anticipated)Interventional2022-05-05Recruiting
Mifepristone Outpatient Labour Induction [NCT05177510]Phase 3400 participants (Anticipated)Interventional2023-08-25Recruiting
Mifepristone After Trauma to Enhance Resilience [NCT00554177]Phase 15 participants (Actual)Interventional2007-09-30Completed
The Use of Letrozole or Mifepristone for Pretreatment of Medical Termination of Pregnancy: a Randomized, Non-inferiority Trial [NCT05341817]Phase 4144 participants (Anticipated)Interventional2022-11-22Recruiting
Cervical Rippening With Antiprogesterone in Midtrimester Abortions [NCT00410345]Phase 4145 participants (Actual)Interventional2004-08-31Completed
An Open Label Extension Study of the Efficacy and Safety of CORLUX® (Mifepristone) in the Treatment of the Signs and Symptoms of Endogenous Cushing's Syndrome [NCT00936741]Phase 330 participants (Actual)Interventional2009-07-31Completed
Mifepristone Tablets in the Treatment of Symptomatic Uterine Fibroids With Safety and Efficacy in Open, Multicenter Phase IV Clinical Studies [NCT03210324]Phase 4434 participants (Actual)Interventional2017-06-01Terminated(stopped due to It is difficult to recruit enough participants)
A Pilot Study on the Combined Use of Letrozole, Miferpristone and Misoprostol in Termination of First Trimester Pregnancy up to 63 Days Gestation [NCT01475318]50 participants (Anticipated)Interventional2011-10-31Recruiting
A Double-blind, Placebo-controlled Trial of the Safety and Efficacy of C-1073 (Mifepristone) as Adjunctive Therapy in Alzheimer's Disease [NCT00105105]Phase 2160 participants Interventional2003-04-30Terminated
Medication Enhanced Rapid Therapy [NCT02099825]Phase 115 participants (Actual)Interventional2014-01-13Terminated(stopped due to COVID and staffing issues)
[NCT00482209]1,220 participants (Anticipated)Interventional2007-05-31Completed
An International, Double-Blind, Placebo-Controlled, Study of the Efficacy and Safety of CORLUX™ (Mifepristone) vs. Placebo in the Treatment of Psychotic Symptoms in Patients With Psychotic Major Depression (PMD) [NCT00146523]Phase 3247 participants (Actual)Interventional2005-05-31Completed
A Phase II Study of Mifepristone (RU-486) in Androgen Independent Prostate Cancer With Correlative Assessment of Androgen Receptor Co-Repressor Proteins [NCT00140478]Phase 248 participants (Anticipated)Interventional2005-02-28Completed
A Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Mifepristone vs. Placebo in the Treatment of Psychotic Symptoms in Patients With Major Depressive Disorder With Psychotic Features [NCT00637494]Phase 3292 participants (Actual)Interventional2008-03-31Terminated(stopped due to DRC recommended stopping study as it had missed its primary endpoint)
Investigation of the Effects of Mifepristone (RU486) on Stress Sensitivity and Relapse Prevention in Cocaine Dependent Patients [NCT01134198]Phase 2/Phase 358 participants (Actual)Interventional2010-05-31Completed
Antiglucocorticoid Therapy for Cognitive Impairment in Late-life Anxiety Disorders [NCT01333098]Phase 1/Phase 215 participants (Actual)Interventional2012-09-30Completed
Preliminary, Double Blind, Placebo Controlled Trial of the Effect of Glucocorticoid Receptor Antagonist Treatment on Biologic and Symptom Outcomes in Patients With Borderline Personality Disorder and Histories of Childhood Abuse [NCT01212588]Phase 222 participants (Actual)Interventional2010-09-30Terminated(stopped due to Funding ended)
Mifepristone vs. Laminaria Insertion for Cervical Preparation Prior to Surgical Abortion at 14-16 Weeks [NCT00986921]50 participants (Actual)Interventional2009-10-31Completed
Randomized Control Trial Of Mifepristone for Fibroids [NCT00133705]Phase 370 participants (Actual)Interventional2003-07-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study of the Safety and Efficacy of Three Dose Levels of CORLUX™ (Mifepristone) Plus an Antidepressant vs. Placebo Plus an Antidepressant in the Treatment of Psychotic Symptoms in Patients Wit [NCT00128479]Phase 3443 participants (Actual)Interventional2004-09-30Completed
Antiglucocorticoid Therapy in Bipolar Depression With Mifepristone (RU486) [NCT00043654]Phase 2110 participants Interventional2002-08-07Completed
An International, Open-Label Extension Study of the Safety and Tolerability of CORLUX™ (Mifepristone) for Recurrent Psychotic Symptoms in Patients With Major Depressive Disorder With Psychotic Features [NCT00128505]Phase 3104 participants (Actual)Interventional2005-08-31Completed
An Open-Label Extension Study of the Safety and Tolerability of CORLUX™ (Mifepristone) for Recurrent Psychotic Symptoms in Patients With Major Depressive Disorder With Psychotic Features [NCT00208156]Phase 387 participants (Actual)Interventional2005-05-31Completed
A Placebo Controlled Study on the Efficacy of 10 mg Oral Mifepristone for the Treatment of Symptomatic Uterine Leiomyomas [NCT00219778]Phase 220 participants (Anticipated)Interventional2004-12-31Terminated
Glucocorticoid and Mineralocorticoid Receptor Function in Post Traumatic Stress Disorder [NCT00046553]97 participants Observational2002-09-30Completed
Comparison Expectant With Immediate Medical Management for the Evacuation of the no Evolutionary Pregnancies Before 13 GW [NCT00190294]Phase 4200 participants (Actual)Interventional2003-04-30Completed
Prospective, Open-Label, Multicenter, International Study of Mifepristone for Symptomatic Treatment of Cushing's Syndrome Caused by Ectopic Adrenal Corticotrophin Hormone (ACTH) Secretion [NCT00422201]Phase 218 participants (Actual)Interventional2007-05-15Terminated
Mifepristone Dynamic Testing for Diagnosis for Central Adrenal Insufficiency [NCT04588688]Phase 23 participants (Actual)Interventional2021-05-05Terminated(stopped due to low recruitment)
Mifepristone Versus Placebo to Treat Adenomyosis: a Double-blind, Multicentre,Randomized Clinical Trial [NCT03520439]Phase 2/Phase 3134 participants (Actual)Interventional2018-05-19Completed
INST 0817: Compassionate Use of Mifepristone [NCT00832871]4 participants (Actual)Interventional2008-11-30Terminated(stopped due to Low accrual; 4 patients enrolled between 2008-2015)
Psychophysiology of Delayed Extinction and Reconsolidation in Humans [NCT01631682]Phase 4186 participants (Actual)Interventional2010-11-30Completed
A Multicenter, Randomized Comparison of Mifepristone and Misoprostol Administered Simultaneously Versus 24 Hours Apart for Abortion Through 63 Days [NCT00269568]Phase 41,128 participants (Actual)Interventional2004-06-30Completed
Mifepristone 2.5, 5, 10 mg Versus Placebo in the Treatment of Endometriosis [NCT02271958]Phase 2/Phase 3360 participants (Actual)Interventional2010-11-30Completed
A Randomized Study of Sublingual Versus Oral Misoprostol Administration Following Mifepristone 200 mg for Abortion up to 63 Days Gestation [NCT00286208]1,443 participants (Actual)Interventional2005-08-31Completed
Oral Mifepristone and Buccal Misoprostol Administered Simultaneously for Abortion Through 63 Days Gestation [NCT00330993]Phase 2120 participants Interventional2006-03-31Completed
Cervical Preparation for Surgical Abortion at 12-14 Weeks: a Prospective, Randomized, Evaluator-blinded, Multicenter, Controlled Comparison Between Mifepristone, Misoprostol and Their Combination [NCT01795599]Phase 3198 participants (Anticipated)Interventional2013-05-31Recruiting
Medical Abortion With Mifepristone + Misoprostol (13 - 22 Weeks): A Double-blind Randomized-controlled Trial [NCT01768299]Phase 4504 participants (Actual)Interventional2013-02-28Completed
Treatment of Uterine Myoma With 2.5 or 5 mg Mifepristone Daily During 3 Months With 9 Months Post-treatment Follow-up. Randomized Clinical Trial. [NCT01786226]Phase 2/Phase 3220 participants (Actual)Interventional2010-03-31Terminated
Exploring a Patient-centered Approach to Mifepristone Administration in Medical Abortion [NCT01811056]401 participants (Actual)Interventional2013-04-30Completed
Acceptability and Feasibility of a Simplified Medical Abortion Service Delivery in Western Ukraine: A Demonstration Study of 800 mcg Buccal Misoprostol Following 200 mg Mifepristone for Abortion up to 70 Days Gestation [NCT02981030]Phase 4102 participants (Actual)Interventional2016-11-23Completed
Mifepristone Versus Misoprostol for Cervical Preparation Prior to Surgical Abortion Between 11 to 15 Weeks [NCT01636063]42 participants (Actual)Interventional2012-06-30Terminated(stopped due to Poor subject enrollment)
Double Blind Randomized Trial of the Anti-Progestational Agent Mifepristone In The Treatment of Unresectable Meningioma [NCT03015701]Phase 3193 participants (Actual)Interventional1992-08-31Completed
Value of Mifepristone in Eliminating the Need for a Second Set of Osmotic Dilators Prior to Dilation and Evacuation Between 19-24 Weeks: A Randomized Trial [NCT01615731]50 participants (Actual)Interventional2012-05-31Completed
A Randomized, Open-label Phase II Trial of the Anti-HCV Activity and Safety of VGX-410 (Mifepristone) at 3 Dose Levels in HCV Infected Patients [NCT00255177]Phase 244 participants (Actual)Interventional2005-11-30Completed
Mifepristone Versus Osmotic Dilator Insertion for Cervical Preparation Prior to Surgical Abortion at 15-18 Weeks [NCT01436279]Phase 350 participants (Actual)Interventional2011-07-31Completed
Glucocorticoid Antagonist Treatment of Alcohol Use Disorder [NCT02179749]Phase 2103 participants (Actual)Interventional2014-09-30Completed
Cervical Preparation of Abortions Under Paracervical Block in the First Trimester: A Randomized Clinical Trial [NCT03043014]110 participants (Actual)Interventional2017-06-01Completed
A Randomized Trial of Mifepristone Antagonization With High-Dose Progesterone to Prevent Medical Abortion [NCT03774745]Phase 1/Phase 212 participants (Actual)Interventional2019-02-11Terminated(stopped due to Safety)
A Randomized, Placebo-Controlled, Double-Blinded Study of Mifepristone in Midtrimester Termination of Pregnancy [NCT00382538]64 participants Interventional2005-03-31Completed
Acceptability and Feasibility of Medical Abortion in Mexico, Puerto Rico, Armenia and Azerbaijan: A Study of Buccal Misoprostol Administration Following Mifepristone 200 mg for Abortion up to 63 Days' Gestation [NCT00386282]1,250 participants (Actual)Interventional2006-09-30Completed
Glucocorticoid Receptor Blockade With Mifepristone in Patients With Mild Adrenal Hypercortisolism [NCT01990560]Phase 48 participants (Actual)Interventional2013-11-30Completed
Prospective Non Interventional Phase IV Multi-centre Canadian Study on the Effectiveness and Safety of Combination Mifepristone/Misoprostol for Medical Abortion Under 63 Days Gestation [NCT04905251]3,000 participants (Anticipated)Observational2022-02-22Recruiting
The HYsteroscopic Miscarriage MaNagement (HYMMN) Trial [NCT04751500]149 participants (Actual)Interventional2021-01-31Completed
Efficacy of Mifepristone (RU-486) in the Treatment of Bipolar Depression. [NCT00359125]Phase 20 participants (Actual)Interventional2006-07-31Withdrawn
Mifepristone Induction for Fetal Demise, a Randomized Control Trial [NCT02620904]Phase 49 participants (Actual)Interventional2016-07-14Terminated(stopped due to unable to recruit. Projected completion was 2018 however, enrollment and recruitment were difficult. The study was terminated due to inability to enroll.)
Simultaneous Mifepristone and Misoprostol Versus Misoprostol Alone for Induction of Labor of Nonviable Second Trimester Pregnancy: a Pilot Randomized Controlled Trial [NCT05322252]Phase 430 participants (Anticipated)Interventional2022-07-01Recruiting
A Randomized, Placebo-controlled, Dose Escalating, Phase II Trial of the Anti -HIV-Activity and Safety of VGX-410 (Mifepristone) in HIV-1 Infected Subjects [NCT00352911]Phase 219 participants (Actual)Interventional2006-07-31Completed
Acceptability and Feasibility of Medical Abortion in Singapore: A Study of 800 μg Buccal Misoprostol Following 200 mg Mifepristone for Abortion Through 70 Days Gestation [NCT02985229]Phase 3130 participants (Actual)Interventional2016-10-31Completed
Mifepristone and Misoprostol for 2nd Trimester Termination of Pregnancy (13-22 Weeks LMP) in Burkina Faso [NCT03269279]Phase 3100 participants (Anticipated)Interventional2017-05-20Recruiting
A Phase I/II Trial of Enzalutamide Plus the Glucocorticoid Receptor Antagonist Mifepristone for Patients With Metastatic Castration Resistant Prostate Cancer (CRPC) [NCT02012296]Phase 1/Phase 288 participants (Actual)Interventional2013-12-13Completed
A Multicenter,Prospective Clinical Trial for Reducing Remaining Submucous Fibroids Volume and Preventing Recurrence by Treating With GnRH Analogues or Mifepristone After Transcervical Resection of Type I-II Myoma [NCT05898321]294 participants (Anticipated)Interventional2023-06-01Not yet recruiting
"A Study of Acceptability and Feasibility of an Outpatient Day Procedure for Medical Abortion at 13-18 Weeks Gestation in Two Public Sector Hospitals in Nepal" [NCT05046041]Phase 4120 participants (Actual)Interventional2020-11-25Completed
Introducing Mifepristone-Misoprostol for Menstrual Regulation in Public Sector Facilities in Bangladesh [NCT01798017]Phase 41,738 participants (Actual)Interventional2012-11-30Completed
Effects of the Glucocorticoid Antagonist, Mifepristone, on Glucose Intolerance in Obese and Overweight Individuals [NCT01419535]Phase 1/Phase 219 participants (Actual)Interventional2011-11-29Completed
Mifepristone in Refractory Depression [NCT00186056]31 participants (Actual)Interventional2003-01-31Completed
A Randomized Comparison of Same-Day Oral Mifepristone-Misoprostol to Misoprostol Only for Cervical Preparation in Second Trimester Surgical Abortion [NCT02412618]Phase 4100 participants (Actual)Interventional2012-09-30Completed
Medication Development in Alcoholism: Investigating Glucocorticoid Antagonists [NCT01548417]Phase 256 participants (Actual)Interventional2012-03-31Completed
An Open-label Study of the Safety, Pharmacokinetics and Pharmacodynamics of Mifepristone in Children With Refractory Cushing's Disease [NCT01925092]Phase 30 participants (Actual)Interventional2013-08-31Withdrawn(stopped due to Lack of enrollment)
Alternative Provision of Medication Abortion Via Advance Provision [NCT03829696]Phase 40 participants (Actual)Interventional2020-01-31Withdrawn(stopped due to The study is not proceeding at this time.)
Mifepristone as an Adjunct to Transcervical Balloon for Labor Induction (MiLI): A Randomized Clinical Trial [NCT05097326]Phase 330 participants (Actual)Interventional2022-06-27Completed
Developing Memory Reconsolidation Blockers as Novel PTSD Treatments [NCT01490697]Phase 434 participants (Actual)Interventional2009-03-31Completed
Novel Therapeutics in PTSD: A Randomized Clinical Trial of Mifepristone [NCT01739335]Phase 281 participants (Actual)Interventional2012-11-19Completed
Mifepristone and Misoprostol Compared With Misoprostol Alone for Second Trimester Abortion [NCT03044093]Phase 4200 participants (Anticipated)Interventional2017-01-31Recruiting
Why Antiprogestrone (Mifepristone) and Cyp 26 Inhibitor Must be Combined With Tamoxifen or ( Tamoxifen and Retinoic Acid) for Treating Early Breast Cancer [NCT05016349]Phase 3160 participants (Anticipated)Interventional2021-08-31Not yet recruiting
Evaluation of Cortisol Resistance in Young Sedentary and Endurance-trained Men and Elderly Sedentary Men [NCT01294319]Phase 251 participants (Actual)Interventional2011-01-24Completed
Treatment of Schizoaffective Disorder Using Mifepristone [NCT00725270]Phase 2/Phase 312 participants (Actual)Interventional1998-04-30Terminated(stopped due to Lack of funding.)
Cervical Preparation Before Dilation and Evacuation in the Second Trimester: A Multicenter Randomized Trial Comparing Osmotic Dilators Alone to Dilators Plus Adjunctive Misoprostol or Adjunctive Mifepristone. [NCT01751087]300 participants (Actual)Interventional2013-01-31Completed
A Phase 1, Open-Label, Drug-Drug Interaction Study in Healthy Subjects to Determine the Effects of a Strong Inhibitor (Itraconazole) of Cytochrome P450 3A on Exposure to Mifepristone and Its Metabolites [NCT03259542]Phase 133 participants (Actual)Interventional2017-08-09Completed
A Phase 1, Open-Label, Fixed-Sequence, Crossover Drug-Drug Interaction Study in Healthy Subjects to Determine the Effects of a Strong Inducer of Cytochrome P450 3A on Exposure to Mifepristone and Its Metabolites [NCT03258372]Phase 148 participants (Actual)Interventional2017-08-16Completed
Targeting Progesterone Signaling for Breast Cancer Prevention in BRCA1 Carriers: a Pilot Study [NCT05062174]0 participants (Actual)Observational2021-11-01Withdrawn(stopped due to PI decision to cancel research)
A 4-week, Double-blind, Placebo-controlled Study of the Efficacy and Safety of Mifepristone in the Prevention of Risperidone-induced Weight Gain in Healthy Male Volunteers [NCT00698022]Phase 176 participants (Actual)Interventional2008-11-30Completed
Protocol Title: Reducing Complications and Patient Barriers in Second Trimester Abortion: Pre-Operative Effects of Mifepristone (POEM) on Dilatation and Evacuation Services [NCT01862991]80 participants (Actual)Interventional2013-07-31Completed
Tumor Necrosis Factor (TNF) and Glucocorticoid Antagonist for Gulf War Illness (GWI)-Associated Multi-symptom Disease Homeostasis Reset [NCT04254627]Phase 120 participants (Anticipated)Interventional2021-09-24Recruiting
Comparative Effectiveness of Pregnancy Failure Management Regimens [NCT02012491]Phase 3300 participants (Actual)Interventional2014-01-31Completed
Mifepristone and Misoprostol Versus Misoprostol Alone for Uterine Evacuation After Early Pregnancy Failure: a Randomized Double Blind Placebo-controlled Comparison (Triple M Trial) [NCT03212352]Phase 4342 participants (Actual)Interventional2018-06-27Terminated(stopped due to Advised by DSMB based on interim-analysis, highly significant difference.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00133705 (1) [back to overview]Uterine Volume
NCT00186056 (1) [back to overview]Hamilton Depression Rating Scale
NCT00255177 (1) [back to overview]Mean Log Change in Viral Load From Baseline (Day 1) to Day 28
NCT00285818 (1) [back to overview]Hamilton Depression Rating Scale Score
NCT00352911 (1) [back to overview]Mean Log Change in Viral Load From Baseline (Day 1) to Day 56
NCT00422201 (2) [back to overview]Features of Cushing's Syndrome
NCT00422201 (2) [back to overview]Glycemic Disorders Improved or Normalized
NCT00459290 (8) [back to overview]Number of Participants With Adverse Effects (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0
NCT00459290 (8) [back to overview]Proportion of Patients With Objective Tumor Response
NCT00459290 (8) [back to overview]Progression-free Survival by Platinum Sensitivity
NCT00459290 (8) [back to overview]Overall Survival
NCT00459290 (8) [back to overview]Progression-free Survival
NCT00459290 (8) [back to overview]Progression-free Survival at 6 Months
NCT00459290 (8) [back to overview]Progression-free Survival by Age (y)
NCT00459290 (8) [back to overview]Progression-free Survival by Performance Status
NCT00468299 (2) [back to overview]Number of Women With Complete Abortion 24-48hrs After Receiving Medical Treatment for Early Pregnancy Failure.
NCT00468299 (2) [back to overview]Complete Abortion at One Week
NCT00569582 (2) [back to overview]Decrease in Diastolic Blood Pressure.
NCT00569582 (2) [back to overview]Improvement in Diabetes and/or Glucose Intolerance.
NCT00637494 (2) [back to overview]Proportion of Mifepristone vs. Placebo Treated Patients With at Least a 50% Reduction From Baseline in Brief Psychiatric Rating Scale-Positive Symptom Subscale (BPRS-PSS) at Days 7 and 56
NCT00637494 (2) [back to overview]Proportion of Mifepristone Treated Patients With Plasma Drug Concentrations Equal to or Above 1637 ng/mL vs. Placebo Treated Patients Who Achieve a ≤ 50% Reduction in BPRS-PSS at Days 7 and 56
NCT00698022 (4) [back to overview]Percentage of Participants With <5% and <7% Increase From Baseline in Body Weight
NCT00698022 (4) [back to overview]Percentage of Participants With One or More Adverse Events
NCT00698022 (4) [back to overview]Percentage of Participants Discontinued From the Study Due to an Adverse Event
NCT00698022 (4) [back to overview]Change From Baseline in Body Weight
NCT00725270 (2) [back to overview]Change in Mood Symptoms
NCT00725270 (2) [back to overview]Change in Positive Psychotic Symptoms Over the Course of Treatment
NCT00832871 (3) [back to overview]Toxicity Associated With Adrenal Insufficiency
NCT00832871 (3) [back to overview]Duration of Response
NCT00832871 (3) [back to overview]Overall Survival
NCT00867360 (3) [back to overview]Change in Mean Cortisol Level
NCT00867360 (3) [back to overview]% Change in Mean Evening Pre- and Post- Florinef Cortisol After Treatment With Either Mifepristone or Placebo
NCT00867360 (3) [back to overview]Change in Psychotic Symptoms Subscale (PSS) of the Brief Psychiatric Rating Scale (BPRS)
NCT00936741 (2) [back to overview]Number of Participants With Adverse Events
NCT00936741 (2) [back to overview]The Long-term Benefit of Mifepristone Treatment in Cushing's Syndrome as Measured by Changes in the Score on the Physician's Global Assessment of Disease Severity
NCT00986921 (3) [back to overview]Time for Completion of Procedure
NCT00986921 (3) [back to overview]Moderate or Severe Pain Overnight
NCT00986921 (3) [back to overview]Assessment of Ease of Procedure by Operator
NCT01134198 (1) [back to overview]Number of Participants With Relapse by Days 10 and 28
NCT01212588 (15) [back to overview]Symptom Change - SCL-90-R
NCT01212588 (15) [back to overview]Symptom Change - SCL-90-R
NCT01212588 (15) [back to overview]Symptom Change - CGI-S
NCT01212588 (15) [back to overview]Symptom Change - CGI-I
NCT01212588 (15) [back to overview]Symptom Change - BPRS
NCT01212588 (15) [back to overview]Symptom Change - BPDSI Subscales
NCT01212588 (15) [back to overview]Symptom Change - SCL-90-R
NCT01212588 (15) [back to overview]Symptom Change - BPDSI Subscales
NCT01212588 (15) [back to overview]Symptom Change - BPDSI Subscales
NCT01212588 (15) [back to overview]Symptom Change - Borderline Checklist
NCT01212588 (15) [back to overview]Durable Symptom Change
NCT01212588 (15) [back to overview]Levels of Cortisol
NCT01212588 (15) [back to overview]Metacognitive Capacity
NCT01212588 (15) [back to overview]Number of Participants With Possibly and Probably Related Adverse Events
NCT01212588 (15) [back to overview]Rapid Symptom Change
NCT01294319 (2) [back to overview]Proportion of Suppressors After Dexamethasone
NCT01294319 (2) [back to overview]Post-dexamethasone Cortisol Level
NCT01333098 (4) [back to overview]Drug Acceptability, as Measured by Number of Participants With Dose-limiting Side Effects
NCT01333098 (4) [back to overview]Anxiety Symptoms
NCT01333098 (4) [back to overview]Number of Participants With Self-reported Side Effects
NCT01333098 (4) [back to overview]Cognitive Changes Over Time, as Measured by Between Group and Within-subjects Comparison of Neuropsychological Measures.
NCT01371565 (1) [back to overview]Number of Participants With Adverse Events
NCT01419535 (6) [back to overview]Adipose-tissue Insulin Sensitivity Index (Adipo-SI)
NCT01419535 (6) [back to overview]Change in Fasting Insulin Levels
NCT01419535 (6) [back to overview]Change in Fasting Plasma Glucose
NCT01419535 (6) [back to overview]Change in Insulin Sensitivity Index
NCT01419535 (6) [back to overview]Homeostatic Model Assessment of Insulin Resistance (HOMA-IR)
NCT01419535 (6) [back to overview]Adipose-tissue Insulin Resistance Index (Adipo-IR)
NCT01436279 (8) [back to overview]Cervical Dilation Achieved
NCT01436279 (8) [back to overview]Difficulty of Procedure
NCT01436279 (8) [back to overview]Pain Medication (Midazolam) During the Abortion
NCT01436279 (8) [back to overview]Pain Medication (Fentanyl) During the Abortion
NCT01436279 (8) [back to overview]Operative Time
NCT01436279 (8) [back to overview]Acceptability to Patient
NCT01436279 (8) [back to overview]Length of Procedure
NCT01436279 (8) [back to overview]Subject Discomfort Before the Abortion
NCT01490697 (2) [back to overview]Physiological Posttraumatic Stress Disorder (PTSD) Probability as Determined From Psychophysiologic Responses to Traumatic Recollection
NCT01490697 (2) [back to overview]Change From Baseline in the Impact of Event Scale-Revised (IES-R) Total Score
NCT01548417 (2) [back to overview]Drinking
NCT01548417 (2) [back to overview]Craving to Drink
NCT01615731 (8) [back to overview]Procedure Time
NCT01615731 (8) [back to overview]Pain Perceived by Patient
NCT01615731 (8) [back to overview]Maximum Cervical Dilation
NCT01615731 (8) [back to overview]Adverse Events
NCT01615731 (8) [back to overview]Total Procedure Time
NCT01615731 (8) [back to overview]Overall Patient Experience
NCT01615731 (8) [back to overview]Adverse Events (EBL)
NCT01615731 (8) [back to overview]Ease of Procedure by Blinded Surgeon
NCT01631682 (1) [back to overview]Change From Baseline Skin Conductance Response
NCT01636063 (1) [back to overview]Initial Cervical Dilation at the Time of Surgical Abortion
NCT01739335 (12) [back to overview]Change in CAPS Avoidance Symptom Scores From Baseline to 4-Week and 12-Week
NCT01739335 (12) [back to overview]Change in Plasma Cortisol From Baseline to 4-Week
NCT01739335 (12) [back to overview]Change in Plasma Cortisol From Baseline to 1-Week
NCT01739335 (12) [back to overview]Change in Adrenocorticotropic Hormone (ACTH) From Baseline to 4-week
NCT01739335 (12) [back to overview]Change in Anger Level (Measured by the STAXI Total Score) From Baseline to 4-Week and 12-Week
NCT01739335 (12) [back to overview]Change in CAPS Intrusive Symptom Scores From Baseline to 4-Week and 12-Week
NCT01739335 (12) [back to overview]Change in CAPS Hyperarousal Symptom Scores From Baseline to 4-Week and 12-Week
NCT01739335 (12) [back to overview]Change in Adrenocorticotropic Hormone (ACTH) From Baseline to 1-week
NCT01739335 (12) [back to overview]Change in Depression (Measured by the BDI Total Score) From Baseline to 4-Week and 12-Week
NCT01739335 (12) [back to overview]Change in Sleep Quality (Measured by the PSQI Total Score) From Baseline to 4-Week and 12-Week
NCT01739335 (12) [back to overview]Changes in PTSD Symptom Severity (Measured by the Stressful Life Total Score From the PTSD Checklist) From Baseline to 4-Week and 12-Week
NCT01739335 (12) [back to overview]Change in CAPS Total Score From Baseline to 4-week and 12-week
NCT01751087 (9) [back to overview]Chills (Any) After Day 2 Medication Administration
NCT01751087 (9) [back to overview]Ability to Complete the D&E on the First Attempt
NCT01751087 (9) [back to overview]Operative Time
NCT01751087 (9) [back to overview]Complications From Procedure
NCT01751087 (9) [back to overview]Physician Satisfaction With Cervical Preparation
NCT01751087 (9) [back to overview]Patient Satisfaction With Cervical Prep
NCT01751087 (9) [back to overview]Need for Mechanical Dilation
NCT01751087 (9) [back to overview]Initial Cervical Dilation
NCT01751087 (9) [back to overview]Ease of Mechanical Dilation
NCT01862991 (2) [back to overview]Procedure Time
NCT01862991 (2) [back to overview]Adverse Events
NCT01990560 (11) [back to overview]Body Mass Index (BMI)
NCT01990560 (11) [back to overview]CushingQoL
NCT01990560 (11) [back to overview]Fasting Lipid Profile
NCT01990560 (11) [back to overview]HOMA-IR
NCT01990560 (11) [back to overview]Hospital Anxiety and Depression Scale (HADS)
NCT01990560 (11) [back to overview]Quality of Life
NCT01990560 (11) [back to overview]State Trait Anxiety Inventory (STAI)
NCT01990560 (11) [back to overview]Waist Circumference
NCT01990560 (11) [back to overview]Weight
NCT01990560 (11) [back to overview]A1C Level
NCT01990560 (11) [back to overview]Nottingham Health Profile (NHP)
NCT02012296 (7) [back to overview]Number of Participants With Positive AR Expression Within Circulating Tumor Cells (CTCs)
NCT02012296 (7) [back to overview]Number of Participants With Positive GR Expression Within Circulating Tumor Cells (CTCs)
NCT02012296 (7) [back to overview]PSA Progression-free Survival
NCT02012296 (7) [back to overview]Radiographic PFS
NCT02012296 (7) [back to overview]Testosterone
NCT02012296 (7) [back to overview]Thyroid Stimulating Hormone
NCT02012296 (7) [back to overview]Cortisol
NCT02012491 (6) [back to overview]Uterine Asperation
NCT02012491 (6) [back to overview]Gestational Sac Expulsion With One Treatment Dose on Day 3 (Visit 2) and no Need for Additional Medical or Surgical Intervention Within 30 Days of Treatment.
NCT02012491 (6) [back to overview]Gestational Sac Expulsion by the Second Follow-up Visit at Day 8
NCT02012491 (6) [back to overview]Gestational Sac Expulsion by the 30-day Telephone Call
NCT02012491 (6) [back to overview]Frequency of Serious Adverse Events Between Study Arms.
NCT02012491 (6) [back to overview]Adverse Event Reported by Participants
NCT02179749 (2) [back to overview]Drinking Quantity Per Day
NCT02179749 (2) [back to overview]Craving
NCT02243709 (3) [back to overview]Alcohol Craving Score on the Alcohol Craving Questionnaire in the Mifepristone Versus Placebo Group
NCT02243709 (3) [back to overview]Drinking Consumption in the Mifepristone Verses Placebo Group
NCT02243709 (3) [back to overview]Number of Participants Experiencing Adverse Events in the Mifepristone Versus Placebo Group as a Measure of Safety and Tolerability
NCT02412618 (2) [back to overview]Initial Cervical Dilation
NCT02412618 (2) [back to overview]Patient Acceptability and Assessment of Pain and Side Effects (5-point Likert Scale)
NCT02620904 (1) [back to overview]Time to Delivery of Fetus
NCT03052400 (13) [back to overview]Adverse Events
NCT03052400 (13) [back to overview]ACTH
NCT03052400 (13) [back to overview]Cortisol
NCT03052400 (13) [back to overview]Hemoglobin A1c
NCT03052400 (13) [back to overview]Weight
NCT03052400 (13) [back to overview]Systolic BP
NCT03052400 (13) [back to overview]PSA
NCT03052400 (13) [back to overview]LDL-cholesterol
NCT03052400 (13) [back to overview]Hypoglycemic Events
NCT03052400 (13) [back to overview]Diastolic BP
NCT03052400 (13) [back to overview]Uric Acid
NCT03052400 (13) [back to overview]Body Mass Index
NCT03052400 (13) [back to overview]Basal Insulin Dose
NCT03320057 (6) [back to overview]Difference in Pharmacists' Mean Knowledge Score Related to Medication Abortion
NCT03320057 (6) [back to overview]Number of Pharmacists Who Report Being Satisfied With Pharmacy Dispensing of Mifeprex
NCT03320057 (6) [back to overview]Number of Participants Who Report Being Satisfied With Obtaining Mifeprex in the Pharmacy
NCT03320057 (6) [back to overview]Number of Participants With an Adverse Event
NCT03320057 (6) [back to overview]Number of Participants With a Complete Abortion With Medication Alone and Who do Not Require a Surgical Procedure to Complete the Abortion
NCT03320057 (6) [back to overview]Number of Pharmacists Who Objected to Participate in Dispensing Mifeprex
NCT03714880 (7) [back to overview]"Provider Assessment of Procedure as Very Easy or Easy"
NCT03714880 (7) [back to overview]Cervical Dilation
NCT03714880 (7) [back to overview]Number of Participants That Experienced Complications
NCT03714880 (7) [back to overview]Number of Participants That Required Mechanical Dilation
NCT03714880 (7) [back to overview]Number of Participants That Had Placement of Expected Dilators or More
NCT03714880 (7) [back to overview]Number of Participants That Required Mechanical Dilation
NCT03714880 (7) [back to overview]Pain Dilator Placement Using Visual Analog Scale
NCT03774745 (5) [back to overview]Number of Participants With Adverse Events During Follow-up Evaluation
NCT03774745 (5) [back to overview]Medical Safety During Treatment and Follow-up
NCT03774745 (5) [back to overview]Expulsion During Follow-up Evaluation
NCT03774745 (5) [back to overview]Continuing Pregnancy Based on Ultrasound Examination
NCT03774745 (5) [back to overview]Number of Participants With Change in Serum Progesterone and hCG During Follow-up
NCT04588688 (4) [back to overview]Peak Cortisol Measured After Mifepristone
NCT04588688 (4) [back to overview]Number of Study Participants With Complete Study Data Captured
NCT04588688 (4) [back to overview]Number of Study Participants Recruited
NCT04588688 (4) [back to overview]Absolute ACTH After Mifepristone

Uterine Volume

Uterine volume is measured in mLs (NCT00133705)
Timeframe: 6 months

InterventionmL (Mean)
Treatment Group719
Placebo Group449

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Hamilton Depression Rating Scale

"Hamilton Depression Rating Scale. Minimum score of 0 (no depressive symptoms) to maximum of 68 (very severely depressed).~Outcome Measure is reporting a Change from Baseline in HAMD scores, i.e., scores at Day 35 minus scores at Baseline." (NCT00186056)
Timeframe: Baseline and Day 35 HAMD scores

Interventionunits on a scale (Mean)
Mifepristone18.75
Placebo19.68

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Mean Log Change in Viral Load From Baseline (Day 1) to Day 28

Mean log change in HCV RNA viral load (significant reduction is considered >0.5 log 10) from baseline (Day 1) following once or twice daily dosing for 28 days at the 28 day timepoint (NCT00255177)
Timeframe: Baseline (Day 1) to Day 28

Interventioncopies/mL on log scale (Log Mean)
Placebo0.30
VGX-410 150mg Daily0.00
VGX-410 300mg Daily0.18
VGX-410 300mg Twice Daily0.04

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Hamilton Depression Rating Scale Score

The Hamilton Depression Scale measures the severity of depression. There are 17 items rated 0 to 4. A total score of 0 indicates that the patient does not endorse any symptoms of depression. The maximum score (the most severe depression) is 68. The outcome measure is the difference between Visit 1 and Visit 4 Hamilton Depression Rating Scale scores of the mifepristone and placebo groups. (NCT00285818)
Timeframe: Screening to Final Visit

,
Interventionunits on a scale (Mean)
BaselineVisit 4; 4 weeks
Mifepristone28.520.5
Placebo23.019.0

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Mean Log Change in Viral Load From Baseline (Day 1) to Day 56

Mean log change in HIV RNA viral load (significant reduction is considered >0.5 log 10) from baseline (Day 1) to Day 56 following 150mg twice daily for 14 days, dose escalation to 300mg twice daily for 14 days and then 28 days off treatment. (NCT00352911)
Timeframe: Baseline (Day 1) to Day 56

Interventioncopies/mL on log scale (Log Mean)
VGX-410 (Mifepristone)0.18
Placebo for VGX-410 (Mifepristone)0.42

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Features of Cushing's Syndrome

"Criteria for secondary glycemic disorder improvement of clinical symptoms attributable to the Cushing's syndrome A. For diabetic patients~Improvement of the following parameters: glycemic profile, fasting blood glucose, fructosamine, 2-hour OGTT (for diabetics diagnosed at screening)~Number of anti-diabetics treatment or dose of anti-diabetics treatment for diabetic patients already on diabetes treatment at inclusion~Doses of insulin for insulin-treated patients B. For patients with IGT~HbA1c~Fructosamine C. For patients with IFG~HbA1c~Fructosamine D. For all patients~Fasting plasma insulin~Area Under the Curve of OGTT results when OGTT performed~HOMA index" (NCT00422201)
Timeframe: 8 weeks at steady dose

Interventionparticipants (Number)
Prospective, Open-label, Study of Mifepristone2

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Glycemic Disorders Improved or Normalized

"Criteria for improvement or normalization of glycemic disorders:~A. For diabetic patients (known or diagnosed at pre-inclusion visit)~Decrease in HbA1c > 0.3% B. For patients with IGT~Normalization of OGTT (2-hour glucose plasma level after 75 g OGTT < 7.8 mmol/L (140 mg/dL) D. For patients with IFG~If impaired fasting glucose is also associated with impaired glucose tolerance during OGTT at pre-inclusion:~- Normalization of OGTT (2-hour glucose plasma level after 75 g OGTT < 7.8 mmol/L (140 mg/dL)~If impaired fasting glycemia is associated with normal OGTT at pre-inclusion (except at T0):~- Normalization of fasting plasma glucose (fasting plasma glucose < 5.5 mmol/L (100 mg/dL)" (NCT00422201)
Timeframe: 8 weeks at steady dose

Interventionparticipants (Number)
Mifepristone2

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Number of Participants With Adverse Effects (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0

(NCT00459290)
Timeframe: Every cycle, during treatment (average of 3 months).

InterventionParticipants (Count of Participants)
AnemiaCoagulationDermatologicGastrointestinalHemorrhage
Mifepristone12111

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Proportion of Patients With Objective Tumor Response

"Complete and Partial Tumor Response by Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0). Per RECIST v1.0 for target lesions and assessed by MRIor CT scan: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest dimensions (LD) of all target measurable lesions taking as reference the baseline sum of LD.~CT scan or MRI is used to follow lesion for measurable disease every other cycle for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels. Responses must be confirmed by repeat imaging 4 weeks following documentation of response." (NCT00459290)
Timeframe: Every other cycle, for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels.

Interventionpercentage of participants (Number)
Mifepristone4.5

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Progression-free Survival by Platinum Sensitivity

Platinum Senstive defined as treatment free interval >6 months on most recent platinum (NCT00459290)
Timeframe: Every other cycle, for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels.

Interventionmonths (Median)
Not Platinum Sensitive1.7
Platinum Sensitive1.9

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Overall Survival

(NCT00459290)
Timeframe: Five years

Interventionmonths (Median)
MifepristoneNA

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Progression-free Survival

"Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter (LD) of target lesions taking as reference the smallest sum LD recorded since study entry, or unequivocal progression of existing non-target lesions, or the appearance of one or more new lesions.~CT scan or MRI is used to follow lesion for measurable disease every other cycle for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels. Responses must be confirmed by repeat imaging 4 weeks following documentation of response." (NCT00459290)
Timeframe: Every other cycle, for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels.

Interventionmonths (Median)
Mifepristone1.8

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Progression-free Survival at 6 Months

"Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter (LD) of target lesions taking as reference the smallest sum LD recorded since study entry, or unequivocal progression of existing non-target lesions, or the appearance of one or more new lesions.~CT scan or MRI is used to follow lesion for measurable disease every other cycle for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels. Responses must be confirmed by repeat imaging 4 weeks following documentation of response." (NCT00459290)
Timeframe: Every other cycle, for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels.

Interventionpercentage of participants (Number)
Mifepristone13.6

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Progression-free Survival by Age (y)

"Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter (LD) of target lesions taking as reference the smallest sum LD recorded since study entry, or unequivocal progression of existing non-target lesions, or the appearance of one or more new lesions.~CT scan or MRI is used to follow lesion for measurable disease every other cycle for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels. Responses must be confirmed by repeat imaging 4 weeks following documentation of response." (NCT00459290)
Timeframe: Every other cycle, for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels.

Interventionmonths (Median)
< 601.7
60 <704.0
>=701.7

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Progression-free Survival by Performance Status

(NCT00459290)
Timeframe: Every other cycle, for the first 6 months; every three months thereafter; and at any time if clinically indicated based on symptoms or physical signs suggestive of progressive disease or rising serum tumor marker levels.

Interventionmonths (Median)
GOG Performance Status 01.8
GOG Performance Status 11.7

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Number of Women With Complete Abortion 24-48hrs After Receiving Medical Treatment for Early Pregnancy Failure.

(NCT00468299)
Timeframe: 24-48 hrs

Interventionparticipants (Number)
Misoprostol and Placebo5
Mifepristone and Misoprostol5

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Complete Abortion at One Week

Complete abortion at one week; uterus demonstrated to be empty on transvaginal ultrasound (NCT00468299)
Timeframe: 3 weeks

Interventionparticipants (Number)
Misoprostol and Placebo6
Mifepristone and Misoprostol7

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Decrease in Diastolic Blood Pressure.

Responder is defined as subject with a decrease greater than or equal to 5mm Hg in diastolic blood pressure from baseline to week 24 or last visit. (NCT00569582)
Timeframe: Baseline to Week 24

Interventionparticipants (Number)
Mifepristone8

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Improvement in Diabetes and/or Glucose Intolerance.

Responder is defined as subject with a decrease greater than or equal to 25% in area under the curve for glucose on 2-hour oral glucose test from baseline to week 24 or last visit, for Cushing's patients with type-2 diabetes mellitus/impaired glucose tolerance. (NCT00569582)
Timeframe: Baseline to Week 24

Interventionparticipants (Number)
Mifepristone15

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Proportion of Mifepristone vs. Placebo Treated Patients With at Least a 50% Reduction From Baseline in Brief Psychiatric Rating Scale-Positive Symptom Subscale (BPRS-PSS) at Days 7 and 56

Response as measured by 50% reduction in psychosis at Days 7 and 56 was compared between the group administered placebo and the group administered mifepristone (NCT00637494)
Timeframe: 56 days

Interventionparticipants (Number)
Active51
Placebo48

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Proportion of Mifepristone Treated Patients With Plasma Drug Concentrations Equal to or Above 1637 ng/mL vs. Placebo Treated Patients Who Achieve a ≤ 50% Reduction in BPRS-PSS at Days 7 and 56

Response as measured by 50% reduction in psychosis at Days 7 and 56 was compared between the group administered placebo and the group who achieved a sufficiently high plasma level of mifepristone (NCT00637494)
Timeframe: 56 days

Interventionparticipants (Number)
Active37
Placebo48

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Percentage of Participants With <5% and <7% Increase From Baseline in Body Weight

(NCT00698022)
Timeframe: Baseline and 28 days

,,
InterventionParticipants (Count of Participants)
<5% increase in body weight<7% increase in body weight
Mifepristone Plus Risperidone913
Risperidone Plus Mifepristone-matched Placebo310
Risperidone-matched Placebo Plus Mifepristone811

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Percentage of Participants With One or More Adverse Events

(NCT00698022)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Mifepristone Plus Risperidone29
Risperidone Plus Mifepristone-matched Placebo27
Risperidone-matched Placebo Plus Mifepristone13

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Percentage of Participants Discontinued From the Study Due to an Adverse Event

(NCT00698022)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Mifepristone Plus Risperidone5
Risperidone Plus Mifepristone-matched Placebo4
Risperidone-matched Placebo Plus Mifepristone1

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Change From Baseline in Body Weight

(NCT00698022)
Timeframe: Baseline and 28 days

Interventionkilograms (Mean)
Mifepristone Plus Risperidone2.32
Risperidone Plus Mifepristone-matched Placebo4.23
Risperidone-matched Placebo Plus Mifepristone2.87

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Change in Mood Symptoms

Utilized the Hamilton Depression Rating Scale, 21-item version to assess depressive symptoms, with a range of 0-63, with higher scores indicating greater levels of depression. (NCT00725270)
Timeframe: Baseline and Day 9

,
Interventionunits on a scale (Mean)
BaselineDay 9
Mifepristone24.8613.57
Placebo26.219.0

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Change in Positive Psychotic Symptoms Over the Course of Treatment

Utilized the Positive Symptoms Subscale of the Brief Psychiatric Rating Scale is assess psychotic symptoms. Range for the subscale is 4-28, with 4 = no positive symptoms (NCT00725270)
Timeframe: 8 days

,
Interventionunits on a scale (Mean)
Baseline PSS ScoresDay 9 PSS scores
Mifepristone7.576.0
Placebo12.011.0

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Toxicity Associated With Adrenal Insufficiency

Toxicity will be evaluated per National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE), version 3.0. Frequency and severity of adverse events will be tabulated using counts the following events of interest, which are related to possible adrenal insufficiency: nausea, vomiting, lethargy, dizziness, fatigue, anorexia, and skin rash. Any grade of these events that are self-reported by patients as well as events identified by physician assessment (e.g. physical exam) will be included. (NCT00832871)
Timeframe: Up to 8 weeks after the end of study treatment or until any adverse events are resolved (whichever is longest)

Interventionpercentage of participants (Number)
NauseaVomitingLethargyDizzinessFatigueAnorexiaSkin Rash
Mifepristone0000000

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Duration of Response

The time from the date of response (not the beginning of treatment unless there is stable disease) to disease progression. Response and progression are evaluated according to Response Evaluation Criteria in Solid Tumors (RECIST) (version 1.0). Target lesions are assessed by computerized tomography (CT) or magnetic resonance imaging (MRI): Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Stable Disease (SD), neither sufficient decrease in the sum of the longest diameter of target lesions to qualify for PR nor sufficient increase in the sum of the longest diameter of target lesions to qualify for Progressive Disease; Progressive Disease (PD), 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions (NCT00832871)
Timeframe: 5 years

Interventiondays (Median)
Mifepristone44

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Overall Survival

The time from patient entry into the protocol to death by any cause. (NCT00832871)
Timeframe: 5 years

InterventionMonths (Median)
Mifepristone24.2

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Change in Mean Cortisol Level

The reported value is the difference in mean evening cortisol from baseline to Day 9 The mean evening cortisol is calculated from the hourly cortisol value taken from 1800 hrs to 0100 hrs for both time points. The outcome measure is the difference of mean evening cortisol from Day 9 less the mean evening cortrisol from baseline. Negative values indicate a reduction in cortisol levels at Day 9, whereas positive values indicate an increase in cortisol at Day 9. Serum cortisol levels are reported in ug/dL (NCT00867360)
Timeframe: Day 1 to Day 9 difference

Interventionug/dL (Mean)
Mifepristone-3.96
Placebo.285

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% Change in Mean Evening Pre- and Post- Florinef Cortisol After Treatment With Either Mifepristone or Placebo

"Time 1 (baseline) = Difference in cortisol level from Day 1 (pre-florinef mean evening cortisol) at Baseline less Day 2 (post-florinef mean evening cortisol) at baseline~Time 2 (post- mife or placebo treatment) = Difference in cortisol level from Day 22 (pre-florinef mean evening cortisol) and Day 23 (post-florinef mean evening cortisol level).~All measurements were the percent change in mean cortisol level from 6 pm to 10 pm. Cortisol levels are expressed as ug/dL~Percent change in cortisol decrease between Time 2 and Time 1 post florinef should be greater with mifepristone than placebo, reflecting enhanced mineralocorticoid receptor activity." (NCT00867360)
Timeframe: Day 23

Interventionpercentage change (Mean)
Mifepristone14
Placebo-.04

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Change in Psychotic Symptoms Subscale (PSS) of the Brief Psychiatric Rating Scale (BPRS)

"The BRPS is a rating scale of various psychiatric symptoms. Each item is rated on a scale of 1 to 7, with 1 being not present. The PSS is the sum of 4 items from the BPRS, which indicates the level of positive psychotic symptoms.. Thus, the range for the PSS is 4 to 28, with higher scores indicating greater levels of positive psychotic symptoms.~For ease of interpretation, the sum of the PSS then has 4 items subtracted so that a score of 0 (instead of 4) indicates that there are no psychotic symptoms. In doing this, the range for the PSS becomes 0 to 24), with larger values indicating more positive psychotic symptoms.~The measure is the change score of PSS total day 1 less PSS total Day 9. 0 indicates no change, where as positive numbers indicate a decrease in psychotic symptoms." (NCT00867360)
Timeframe: baseline to day 9

Interventionunits on a scale (Mean)
Mifepristone.000
Placebo1.00

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Number of Participants With Adverse Events

Subjects who received at least one dose of mifepristone were included in the safety analysis. (NCT00936741)
Timeframe: Up to three years.

Interventionparticipants (Number)
Open-label30

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The Long-term Benefit of Mifepristone Treatment in Cushing's Syndrome as Measured by Changes in the Score on the Physician's Global Assessment of Disease Severity

"The mean Investigator's rating of the change in subject's signs and symptoms of Cushing's syndrome from Baseline (Entry into C1073-415) to Endpoint on the Physician's Global Assessment of Disease Severity was ranked on a 9-point scale (9 = much worse, 7 = worse, 5 = no change, 3 = better, 1 = much better). Higher scores indicate more severe illness. Scoring was done at all visits except the 6 Week Follow-up visit; the final visit result (Endpoint) is reported here.~The instruction was Rate the change in the subject's signs and symptoms of Cushing's from Baseline (1 = much better to 9 = much worse)." (NCT00936741)
Timeframe: Up to three years.

Interventionunits on a scale (Mean)
Open-label3.3

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Time for Completion of Procedure

Minutes, from the time of the start of the procedure (speculum insertion) to the conclusion of the procedure (speculum removal) (NCT00986921)
Timeframe: Performance and completion of the abortion procedure takes 10-20 minutes. The length of the procedure is measured. The procedure occurs approximately 24 hours after enrollment.

InterventionMinutes (Mean)
Standard Osmotic Dilators8.0
Mifepristone9.87

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Moderate or Severe Pain Overnight

Women wer asked to rank their amount of pain on a catergorical scale. The outcome measure is the number of women experiencing moderate or severe pain overnight (after mifepristone or osmotic dilators, and before the abortions procedure) (NCT00986921)
Timeframe: Overnight

Interventionpercentage of participants (Number)
Standard Osmotic Dilators52
Mifepristone8

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Assessment of Ease of Procedure by Operator

"The operator for each procedure rated the ease of procedure on a categorical scale. The categories were collapsed into two: easy or very easy and average or difficult." (NCT00986921)
Timeframe: It is administered shortly after the primary outcome, which is one day after enrollment. The study is complete at that point.

Interventionpercentage of participants (Number)
Standard Osmotic Dilators46
Mifepristone36

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Number of Participants With Relapse by Days 10 and 28

assessed percent of sample with documented cocaine use by days 10 and 28 based on self reported use and urine toxicology. Those with documented use were considered to have relapsed. (NCT01134198)
Timeframe: assessed during 8 weeks of trial, but reported for days 10 and 28 of trial

InterventionParticipants (Count of Participants)
Day 1072243148Day 1072243149Day 2872243148Day 2872243149
relapsedabstinent
Mifepristone3
Mifepristone6
Mifepristone5
Placebo8
Mifepristone4
Placebo3

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Symptom Change - SCL-90-R

The Symptom Checklist-90-Revised (SCL-90-R) instrument helps evaluate a broad range of psychological problems and symptoms of psychopathology. The instrument is also useful in measuring patient progress or treatment outcomes. The SCL-90-R contains 90 items on a 5-point rating scale, with a higher score indicating more severity. The items are categorized into 12 domains (9 scores along primary symptom dimensions and 3 scores among global distress indices). A t-score for each domain is then obtained by norming by sex and ranges between 19-81, with a higher score indicating more severity. (NCT01212588)
Timeframe: Baseline (Visit 2)

,
InterventionScores on a scale (Mean)
SCl-90-R - SomatizationSCL-90-R - Obsessive-ComplusiveSCL-90-R - Interpersonal SensitivitySCL-90-R - DepressionSCL-90-R - AnxietySCL-90-R - HostilitySCL-90-R - Phobic AnxietySCL-90-R - Paranoid IdeationSCL-90-R - PsychoticismSCL-90-R - Global Severity IndexSCL-90-R - Positive Symptom TotalSCL-90-R - Positive Symptom Distress Index
Mifepristone55.8056.2056.5054.4052.6053.7050.0056.4052.2055.2055.9054.50
Placebo50.2551.5051.5849.7547.1753.0054.5848.4547.6750.0049.0052.25

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Symptom Change - SCL-90-R

The Symptom Checklist-90-Revised (SCL-90-R) instrument helps evaluate a broad range of psychological problems and symptoms of psychopathology. The instrument is also useful in measuring patient progress or treatment outcomes. The SCL-90-R contains 90 items on a 5-point rating scale, with a higher score indicating more severity. The items are categorized into 12 domains (9 scores along primary symptom dimensions and 3 scores among global distress indices). A t-score for each domain is then obtained by norming by sex and ranges between 19-81, with a higher score indicating more severity. (NCT01212588)
Timeframe: 7 days of study medication (Visit 4)

,
InterventionScores on a scale (Mean)
SCl-90-R - SomatizationSCL-90-R - Obsessive-ComplusiveSCL-90-R - Interpersonal SensitivitySCL-90-R - DepressionSCL-90-R - AnxietySCL-90-R - HostilitySCL-90-R - Phobic AnxietySCL-90-R - Paranoid IdeationSCL-90-R - PsychoticismSCL-90-R - Global Severity IndexSCL-90-R - Positive Symptom TotalSCL-90-R - Positive Symptom Distress Index
Mifepristone53.0054.3053.0052.6049.1052.8049.6053.8048.8052.3053.4054.20
Placebo46.2747.9148.4547.8243.0952.0049.5547.9147.2745.8246.9151.91

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Symptom Change - CGI-S

The Clinical Global Impressions Severity Scale (CGI-S) is used for repeated evaluations of global psychopathology. The CGI-S scale is widely used in schizophrenia research and is a single 7-point Likert scale rating severity of psychopathology on a scale of 1 (normal, not ill) to 7 (very severely ill), with a higher score indicating more severity. (NCT01212588)
Timeframe: Baseline, 7 days of study medication (Visit 4), 21 days after discontinuation of study medication (Visit 6)

,
InterventionScores on a scale (Mean)
CGI-S - BaselineCGI-S - 7 days of study medCGI-S - 21 days after disc of study med
Mifepristone4.304.203.89
Placebo4.424.093.70

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Symptom Change - CGI-I

The Clinical Global Impressions Improvement (CGI-I) scale is used to assess the clinical change as compared to symptoms at baseline using a 7-point Likert scale, ranging from very much improved (1) to very much worse (7), with a higher score indicating more severity. (NCT01212588)
Timeframe: 7 days of study medication (Visit 4), 21 days after discontinuation of study medication (Visit 6)

,
InterventionScores on a scale (Mean)
CGI-I - 7 days of study medCGI-I - 21 days after disc of study med
Mifepristone3.303.44
Placebo3.362.80

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Symptom Change - BPRS

The Brief Psychiatric Rating Scale (BPRS) is an 19-item scale measuring positive symptoms, general psychopathology and affective symptoms during the last 7 days. The BPRS measures symptoms with scores ranging from 0-7, with a higher score indicating more severity. A total score is then calculated by adding all the item scores, ranging from 0-133, with a higher score indicating more severity. (NCT01212588)
Timeframe: Baseline (Visit 2), 7 days of study medication (Visit 4), 7 days after discontinuation of study medication (Visit 5), 21 days after discontinuation of study medication (Visit 6)

,
InterventionScores on a scale (Mean)
BPRS - BaselineBPRS - 7 days of study medicationBPRS - 7 days after disc of study medBPRS - 21 days after disc study med
Mifepristone37.7033.9035.7835.22
Placebo37.5033.3633.5030.50

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Symptom Change - BPDSI Subscales

Borderline Personality Disorder Severity Index (BPDSI) symptom domain subscales scores. The BPDSI is a semi-structured clinical interview assessing the frequency and severity of manifestations of Borderline Personality Disorder (BPD) during a circumscribed period of the previous 7 days. The BPDSI measures 9 symptoms associated with BPD on a Likert scale ranging from 0-7 (0 = never; 7 = daily). Each symptom measure produces a mean score ranging from 0-7, with a higher score indicating more prevalent symptoms. (NCT01212588)
Timeframe: Baseline (Visit 2)

,
InterventionScores on a scale (Mean)
BPDSI Subscale Score - AbandonmentBPDSI Subscale Score - Interpersonal RelationshipsBPDSI Subscale Score - IdentityBPDSI Subscale Score - ImpulsivityBPDSI Subscale Score - Parasuicidal BehaviorBPDSI Subscale Score - Affective InstabilityBPDSI Subscale Score - EmptinessBPDSI Subscale Score - Outbursts of AngerBPDSI Sub. Score-Dissociation & Paranoid Ideation
Mifepristone1.461.342.760.780.484.403.961.451.45
Placebo1.360.701.490.320.304.482.351.531.14

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Symptom Change - SCL-90-R

The Symptom Checklist-90-Revised (SCL-90-R) instrument helps evaluate a broad range of psychological problems and symptoms of psychopathology. The instrument is also useful in measuring patient progress or treatment outcomes. The SCL-90-R contains 90 items on a 5-point rating scale, with a higher score indicating more severity. The items are categorized into 12 domains (9 scores along primary symptom dimensions and 3 scores among global distress indices). A t-score for each domain is then obtained by norming by sex and ranges between 19-81, with a higher score indicating more severity. (NCT01212588)
Timeframe: 21 days after discontinuation of study medication (Visit 6)

,
InterventionScores on a scale (Mean)
SCl-90-R - SomatizationSCL-90-R - Obsessive-ComplusiveSCL-90-R - Interpersonal SensitivitySCL-90-R - DepressionSCL-90-R - AnxietySCL-90-R - HostilitySCL-90-R - Phobic AnxietySCL-90-R - Paranoid IdeationSCL-90-R - PsychoticismSCL-90-R - Global Severity IndexSCL-90-R - Positive Symptom TotalSCL-90-R - Positive Symptom Distress Index
Mifepristone49.7851.3348.8949.0048.4450.1146.0050.3345.4449.0049.5651.67
Placebo47.6044.6045.3044.0042.7048.8050.1046.8045.7045.1044.8046.60

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Symptom Change - BPDSI Subscales

Borderline Personality Disorder Severity Index (BPDSI) symptom domain subscales scores. The BPDSI is a semi-structured clinical interview assessing the frequency and severity of manifestations of Borderline Personality Disorder (BPD) during a circumscribed period of the previous 7 days. The BPDSI measures 9 symptoms associated with BPD on a Likert scale ranging from 0-7 (0 = never; 7 = daily). Each symptom measure produces a mean score ranging from 0-7, with a higher score indicating more prevalent symptoms. (NCT01212588)
Timeframe: 7 days of study medication (Visit 4)

,
InterventionScores on a scale (Mean)
BPDSI Subscale Score - AbandonmentBPDSI Subscale Score - Interpersonal RelationshipsBPDSI Subscale Score - IdentityBPDSI Subscale Score - ImpulsivityBPDSI Subscale Score - Parasuicidal BehaviorBPDSI Subscale Score - Affective InstabilityBPDSI Subscale Score - EmptinessBPDSI Subscale Score - Outbursts of AngerBPDSI Sub. Score-Dissociation & Paranoid Ideation
Mifepristone0.900.801.640.660.373.672.761.081.63
Placebo1.270.581.340.110.192.891.510.790.77

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Symptom Change - BPDSI Subscales

Borderline Personality Disorder Severity Index (BPDSI) symptom domain subscales scores. The BPDSI is a semi-structured clinical interview assessing the frequency and severity of manifestations of Borderline Personality Disorder (BPD) during a circumscribed period of the previous 7 days. The BPDSI measures 9 symptoms associated with BPD on a Likert scale ranging from 0-7 (0 = never; 7 = daily). Each symptom measure produces a mean score ranging from 0-7, with a higher score indicating more prevalent symptoms. (NCT01212588)
Timeframe: 21 days after discontinuation of study medication (Visit 6)

,
InterventionScores on a scale (Mean)
BPDSI Subscale Score - AbandonmentBPDSI Subscale Score - Interpersonal RelationshipsBPDSI Subscale Score - IdentityBPDSI Subscale Score - ImpulsivityBPDSI Subscale Score - Parasuicidal BehaviorBPDSI Subscale Score - Affective InstabilityBPDSI Subscale Score - EmptinessBPDSI Subscale Score - Outbursts of AngerBPDSI Sub. Score-Dissociation & Paranoid Ideation
Mifepristone1.060.841.920.530.433.272.940.971.62
Placebo0.630.640.630.110.252.961.790.620.56

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Symptom Change - Borderline Checklist

The Borderline Personality Checklist (BPD Checklist) is a 47-item DSM-IV based self-report questionnaire, designed to assess the experienced burden of specific BPD symptoms during the previous week. The BPD Checklist measures symptoms with scores ranging from 1-5, with a higher score indicating more severity. A total score is then calculated by adding all the item scores, ranging from 47-235, with a higher score indicating more severity. (NCT01212588)
Timeframe: Baseline (Visit 2), 7 days of study medication (Visit 4), 7 days after discontinuation of study medication (Visit 5), 21 days after discontinuation of study medication (Visit 6)

,
InterventionScores on a scale (Mean)
BPD Checklist - BaselineBPD Checklist - 7 days of study medBPD Checklist - 7 days after disc of study medBPD Checklist - 21 days after disc study med
Mifepristone103.6098.1091.5687.89
Placebo96.9288.3682.8078.80

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Durable Symptom Change

To evaluate whether seven days of mifepristone treatment will result in a durable change in symptoms persisting after active treatment discontinuation, as measured by Borderline Personality Disorder Severity Index (BPDSI) total score. The BPDSI is a semi-structured clinical interview assessing the frequency and severity of manifestations of Borderline Personality Disorder (BPD) during a circumscribed period of the previous 7 days. The BPDSI measures 9 symptoms associated with BPD on a Likert scale ranging from 0-7 (0 = never; 7 = daily). Each symptom measure produces a mean score ranging from 0-7, with a higher score indicating more prevalent symptoms. A total score is then calculated using the summed symptom mean scores, ranging from 0-63, with a higher score indicating more prevalent symptoms. (NCT01212588)
Timeframe: 7 days of study medication to 21 days after discontinuation of study medication

,
InterventionScores on a scale (Mean)
BPDSI Total Score after 7 days of medicationBPDSI Total Score 21 days after discont. study med
Mifepristone13.5013.58
Placebo9.458.17

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Levels of Cortisol

To assess cortisol levels as a potential biomarker of hypothalamic-pituitary-adrenal (HPA)-axis engagement (NCT01212588)
Timeframe: Baseline (Visit 2), 7 days of study medication (Visit 4), 7 days after discontinuation of study medication (Visit 5), 21 days after discontinuation of study medication (Visit 6)

,
Interventionmcg/dL (Mean)
Cortisol Level - BaselineCortisol Level - 7 days of study medCortisol Level - 7 days after disc of study medCortisol Level - 21 days after disc study med
Mifepristone13.8835.0120.9111.90
Placebo14.3816.3314.3015.73

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Metacognitive Capacity

The Indiana Psychiatric Illness Interview (IPII) is a semi-structured interview developed to assess illness narratives. Responses are audio taped and later transcribed. It is scored using the Metacognition Assessment Scale- Abbreviated (MAS-A), which has four domains of metacognition: i) Self-Reflectivity ranging from 0-9; ii) Understanding the Mind of Other ranging from 0-7; iii) Decentration ranging from 0-3; and iv) Mastery ranging from 0-9. Lower scores indicate metacognitive deficits, higher scores indicate more integrated and nuanced metacognition. MAS-A total score is the sum of the scores on each of the domains of metacognition, ranging from 0-28, with a lower score indicating metacognitive deficits and a higher score indicating more integrated and nuanced metacognition. (NCT01212588)
Timeframe: Baseline, 21 days after discontinuation of study medication

,
InterventionScores on a scale (Mean)
IIPI - Self-Reflectivity - BaselineIIPI-Self-Reflectivity-21 days after dis study medIIPI - Understanding Others - BaselineIIPI-Understanding Others-21 days after dis medsIIPI - Decentration - BaselineIIPI-Decentration-21 days after dis medsIIPI - Mastery - BaselineIIPI-Mastery-21 days after dis medsIIPI - Total - BaselineIIPI-Total-21 days after dis meds
Mifepristone5.085.253.252.750.500.382.672.7511.5011.13
Placebo4.633.902.882.500.380.203.882.8011.759.40

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Rapid Symptom Change

To evaluate whether mifepristone will produce rapid symptom change after seven days of active treatment, as measured by Borderline Personality Disorder Severity Index (BPDSI) total score. The BPDSI is a semi-structured clinical interview assessing the frequency and severity of manifestations of Borderline Personality Disorder (BPD) during a circumscribed period of the previous 7 days. The BPDSI measures 9 symptoms associated with BPD on a Likert scale ranging from 0-7 (0 = never; 7 = daily). Each symptom measure produces a mean score ranging from 0-7, with a higher score indicating more prevalent symptoms. A total score is then calculated using the summed symptom mean scores, ranging from 0-63, with a higher score indicating more prevalent symptoms. (NCT01212588)
Timeframe: Baseline to 7 days of study medication

,
InterventionScores on a scale (Mean)
BPDSI Total Score after 7 days of medicationBPDSI Total Score at Baseline
Mifepristone13.517.99
Placebo9.4513.66

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Proportion of Suppressors After Dexamethasone

"All subjects will take 0.25mg dexamethasone as an outpatient between 2300 and 2400h and will then report to the clinic by 0800h next day for the final visit.~At the final visit, cortisol response to dexamethasone suppression was assessed. The cortisol response was dichotomized (suppression vs. non-suppression, using 1.8 ug/dL as the cutoff point) and compared between the two groups,Sedentary Young Adults and Endurance-trained Young Athletes." (NCT01294319)
Timeframe: cortisol measured between 8 and 9 after dexamethasone was taken between 11 PM and midnight

InterventionParticipants (Count of Participants)
Endurance-trained Young Athletes0
Sedentary Young Adults1

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Post-dexamethasone Cortisol Level

(NCT01294319)
Timeframe: Cortisol obtained at 8-9 AM after dexamethasone taken between 11 pm and midnight

Interventionmcg/dL (Mean)
Endurance-trained Young Athletes11.98
Sedentary Young Adults9.98

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Drug Acceptability, as Measured by Number of Participants With Dose-limiting Side Effects

number of participants with dose-limiting side effects (NCT01333098)
Timeframe: Baseline, Week 2, Week 4

InterventionParticipants (Count of Participants)
Mifepristone1

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Anxiety Symptoms

Self-report assessment of worry using Penn State Worry Questionnaire- Abbreviated, an 8-item measure (range 8-40 with high scores indicating higher levels of anxiety and worry symptoms.The average score for older adults with generalized anxiety disorder is 22, while the mean score for healthy older adults is 15. (NCT01333098)
Timeframe: baseline, week 4, week 12

,
InterventionScores on a scale (Mean)
BaselineWeek 4Week 12
High Baseline Cortisol30.8022.4023.0
Without High Baseline Corisol27.8827.0025.29

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Number of Participants With Self-reported Side Effects

(NCT01333098)
Timeframe: 4 weeks

Interventionparticipants with reported side effects (Number)
dizzinessfatiguenausea
Mifepristone532

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Cognitive Changes Over Time, as Measured by Between Group and Within-subjects Comparison of Neuropsychological Measures.

Memory composite z-score: The two memory measures were a 16-word list recall similar to the Rey auditory verbal learning test, which has been used by the Washington University Alzheimer's Disease Research Center; and two paragraphs from a set of paragraph recall tests validated as sensitive to effects of stress-level glucocorticoids. For each memory variable, a z score was computed for each participant, where z score = (participant score mean)/standard deviation. Then a single composite memory variable was created by summing up these z scores. Summed Z-scores range from -6 to 6, with scores above 0 being higher than the mean. (NCT01333098)
Timeframe: Baseline, Week 4, Week 12

,
Interventionz-score (Mean)
BaselineWeek 4Week 12
High Baseline Cortisol0.931.853.00
Without High Baseline Corisol-0.59-0.45-0.26

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Number of Participants With Adverse Events

Safety was assessed at all visits and adverse events were recorded. (NCT01371565)
Timeframe: 6 months

Interventionparticipants (Number)
Mifepristone4

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Adipose-tissue Insulin Sensitivity Index (Adipo-SI)

The Adipo-SI was calculated as ratio of the slope of the linear decrease in natural log transformed FFA [Ln (FFA) slope] during the first 90 minutes of the FSIVGTT and the area under the curve (AUC) of insulin during that 90-minute period (AUC Insulin 0-90 min). (NCT01419535)
Timeframe: 9 days

Interventionln(mmol /uU/mL*min)*10^8 (Mean)
Post-mifepristone61.7
Post-placebo42.8

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Change in Fasting Insulin Levels

Fasting insulin after study agent administration compared to baseline (NCT01419535)
Timeframe: 9 days

Interventionpmol/L (Mean)
Post-mifepristone95.6
Post-placebo142.8

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Change in Fasting Plasma Glucose

fasting plasma glucose after study agent compared to baseline (NCT01419535)
Timeframe: Nine days

Interventionmg/dL (Mean)
Post-mifepristone100.4
Post-placebo107.8

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Change in Insulin Sensitivity Index

insulin sensitivity index based on the effect of insulin on glucose during frequently sampled intravenous glucose tolerance test (FSIVGTT) (NCT01419535)
Timeframe: Nine days

Interventionmin-1·μU·ml-1 (Mean)
Post-mifepristone1.49
Post-placebo1.41

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Homeostatic Model Assessment of Insulin Resistance (HOMA-IR)

HOMA-IR is an index of insulin resistance, measured as glucose in mmol/L x insulin in mIU/mL)/22.5. HOMA-IR > 2.5 indicates insulin resistance. (NCT01419535)
Timeframe: 9 days

Interventionunits on a scale (Mean)
Post-mifepristone3.58
Post-placebo5.78

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Adipose-tissue Insulin Resistance Index (Adipo-IR)

The adipose tissue insulin resistance index (Adipo-IR), a surrogate measure for fasting adipose-tissue insulin resistance, was calculated as the product of fasting insulin and fasting free fatty acids (FFA) (NCT01419535)
Timeframe: 9 days

Interventionmmol/l·μU/l (Mean)
Post-mifepristone49.9
Post-placebo65.5

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Cervical Dilation Achieved

Cervical dilation at start of procedure (NCT01436279)
Timeframe: At time of abortion

Interventionmm (Mean)
Mifepristone + Misoprostol42
Osmotic Dilators56

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Difficulty of Procedure

"Outcome measure is the number and percentage of participants where the provider rated the procedure as difficult or very difficult. Provider assessment of difficulty of procedure categories were: very easy, easy, moderate, difficult, or very difficult." (NCT01436279)
Timeframe: After completion of procedure

InterventionParticipants (Count of Participants)
Mifepristone + Misoprostol5
Osmotic Dilators3

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Pain Medication (Midazolam) During the Abortion

Amount of pain medication used during the procedure: reported as milligrams of midazolam (NCT01436279)
Timeframe: Subjects will be followed from the administration of mifepristone/misoprostol, or laminaria, until the end of their procedure, a total of two days.

Interventionmg (Mean)
Mifepristone + Misoprostol104
Osmotic Dilators105

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Pain Medication (Fentanyl) During the Abortion

Amount of pain medication used during the procedure: reported as micrograms of fentanyl (NCT01436279)
Timeframe: Subjects will be followed from the administration of mifepristone/misoprostol, or laminaria, until the end of their procedure, a total of two days.

Interventionmcg (Mean)
Mifepristone + Misoprostol3.1
Osmotic Dilators2.9

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Operative Time

Interval from initiation of vacuum aspiration to speculum removal (NCT01436279)
Timeframe: Subjects will be followed from the administration of mifepristone/misoprostol, or laminaria, until the end of their procedure, a total of two days.

Interventionminutes (Median)
Mifepristone + Misoprostol9
Osmotic Dilators8.5

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Acceptability to Patient

"Patient was asked whether they would choose to be in the same group again if they had a similar procedure again. The number of participants whose response was yes is being reported." (NCT01436279)
Timeframe: After procedure completion

InterventionParticipants (Count of Participants)
Mifepristone + Misoprostol26
Osmotic Dilators11

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Length of Procedure

Interval from speculum insertion to speculum removal (NCT01436279)
Timeframe: Subjects will be followed from the administration of mifepristone/misoprostol or laminaria, until the end of their procedure, a total of two days.

Interventionminutes (Mean)
Mifepristone + Misoprostol14
Osmotic Dilators13.5

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Subject Discomfort Before the Abortion

Pain was subjectively described by the subjects as : None, Mild, Moderate, Severe (NCT01436279)
Timeframe: Subjects will be followed from the administration of mifepristone/misoprostol, or laminaria, until the end of their procedure, a total of two days.

,
Interventionparticipants (Number)
NoneMildModerateSevere
Mifepristone + Misoprostol18750
Osmotic Dilators7634

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Physiological Posttraumatic Stress Disorder (PTSD) Probability as Determined From Psychophysiologic Responses to Traumatic Recollection

The posterior probability of developing PTSD was determined for each participant from a composite of psychophysiological responses to script-driven imagery of traumatic events that included assessments of heart rate response in beats per minute, skin conductance response in microSiemens, and corrugator electromyogram (EMG) responses of the left lateral frontalis facial muscle in microVolts. Responses for the traumatic scripts were averaged and square-root transformed for analysis. Responses during personal traumatic imagery of previously studied individuals with and without current PTSD was used to calculate each participant's posterior probability of being classified as PTSD. (NCT01490697)
Timeframe: 1 week following treatment (Day 14)

Interventionpercent probability (Mean)
Placebo Plus Placebo44
Mifepristone Plus d-Cycloserine (DCS)45

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Change From Baseline in the Impact of Event Scale-Revised (IES-R) Total Score

IES-R is a 22-item patient reported measure of PTSD symptoms. Each question is answered using a 5-point scale where 0=not at all to 4=extremely for a total possible score of 0 to 88. Lower scores represent less severe symptoms and higher scores representing more severe symptoms. IES-R change scores were calculated by subtracting the Day 14 IES-R total score from the Day 7 IES-R total score. A negative change from Baseline indicates improvement of symptoms and a positive change from Baseline indicates a worsening of symptoms. (NCT01490697)
Timeframe: Day 7 (Baseline) and Day 14

,
Interventionscore on a scale (Mean)
BaselineChange from Baseline at Day 14
Mifepristone Plus d-Cycloserine (DCS)52.4-8.9
Placebo Plus Placebo55.3-5.0

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Drinking

Number of standard drinks per week using the Timeline Followback Interview. Total number of alcoholic drinks consumed per week with a minimum value of 0 and a maximum value of 70. (NCT01548417)
Timeframe: 2 weeks

Interventionalcoholic drinks per week (Mean)
Korlym (Mifepristone)27.661
Sugar Pill38.175

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Craving to Drink

Visual Analog Scale (VAS) scores of craving severity in response to in vivo alcohol cues. Higher scores indicate greater craving severity with a minimum score of 0 and a maximum score of 80. (NCT01548417)
Timeframe: 1 week

Interventionunits on a scale (Mean)
Korlym (Mifepristone)36.5
Sugar Pill42.9

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Procedure Time

Measured as time from speculum insertion to removal (NCT01615731)
Timeframe: Intraoperative Time

Interventionminutes (Mean)
Two Sets of Dilators10.9
Mifepristone Plus One Set of Dilators11.8

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Pain Perceived by Patient

Used a Visual Analogue Scale to determine the pain perceived by the patient pre-operatively (after misoprostol, immediately before transport to OR) and post-operatively (in recovery room, on average 1.5 hours post-operatively). The VAS ranges from 0-100. 0 being no pain felt by the patient and 100 being the worst pain imaginable felt by the patient. (NCT01615731)
Timeframe: Measured pre-operatively (after misoprostol, immediately before transport to OR) and post-operatively (in recovery room, on average 1.5 hours post-operatively)

,
Interventionunits on a scale (Median)
Subject Pain Pre-OpSubject Pain Post-Op
Mifepristone Plus One Set of Dilators6316
Two Sets of Dilators133

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Maximum Cervical Dilation

Measured by estimate with bimanual exam and passage of largest dilator immediately prior to procedure. (NCT01615731)
Timeframe: Measured intra-operatively

,
Interventionparticipants (Number)
Pre-op Cervical Dilation 2 cmPre-op Cervical Dilation 3 cmPre-Op Cervical Dilation 4 cmPre-Op Cervical Dilation 5 cm
Mifepristone Plus One Set of Dilators31451
Two Sets of Dilators2982

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Adverse Events

uterine perforation, uterine injury, etc. (NCT01615731)
Timeframe: Intraoperatively and 2 weeks post operatively

,
Interventionparticipants (Number)
Pre-Procedure DeliveryCervical InjuryRUpture of Membranes with Subsequent Fever
Mifepristone Plus One Set of Dilators110
Two Sets of Dilators201

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Total Procedure Time

(NCT01615731)
Timeframe: Measured at clinic visits and on OR day, over a 3 day period

Interventionhours (Mean)
Two Sets of Dilators165
Mifepristone Plus One Set of Dilators86

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Overall Patient Experience

Used a Visual Analogue Scale to determine the patient's overall satisfaction with her experience. The VAS ranges from 0-100. 0 being a worse than expected experience, 50 being what the patient expected and 100 being a better than expected experience. (NCT01615731)
Timeframe: Measured post operatively (at least 30 minutes, on average 1.5 hours) prior to discharge

Interventionunits on a scale (Median)
Two Sets of Dilators72
Mifepristone Plus One Set of Dilators79

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Adverse Events (EBL)

One adverse event: Estimated Blood Loss (NCT01615731)
Timeframe: Intraoperatively

InterventionmL (Mean)
Two Sets of Dilators57
Mifepristone Plus One Set of Dilators63

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Ease of Procedure by Blinded Surgeon

Used a Visual Analogue Scale to determine the ease of procedure by blinded surgeon. The VAS ranges from 0-100. 0 being the easiest procedure the surgeon felt they had every performed and 100 being the most difficult procedure imaginable by the surgeon. (NCT01615731)
Timeframe: Measured Immediately after procedure

Interventionunits on a scale (Median)
Two Sets of Dilators29
Mifepristone Plus One Set of Dilators30

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Change From Baseline Skin Conductance Response

Skin conductance response (SCR) is the change in skin conductance level in response to a stimulus. We compared the SCR to a non-treated conditioned stimulus (CS+N) with the SCR to a treated conditioned stimulus (CS+R) by creating a difference score (CS+R - CS+N) for the day 3 data. Day 3 is 48 hours after the fear-conditioning procedure and serves as the primary measure of whether the treatment had an effect. SCR was measured in microSiemens; the SCR difference score reflects a change in microSiemens. (NCT01631682)
Timeframe: 48hrs

InterventionmicroSiemens (Mean)
Propranolol.06
Reactivation With Time Delay.17
Mifepristone-1.27
Intranasal Oxytocin-.04

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Initial Cervical Dilation at the Time of Surgical Abortion

Initial cervical dilation as measured in French units by a Pratt cervical dilator prior to surgical abortion. The dilation was measured in French units with each French unit being equivalent to 0.33 mm. (NCT01636063)
Timeframe: 24 to 48 hours after enrollment

InterventionFrench units (Mean)
Mifepristone30.8
Misoprostol31.1

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Change in CAPS Avoidance Symptom Scores From Baseline to 4-Week and 12-Week

"The Clinical Administered PTSD Scale (CAPS) was used to assess the diagnosis of PTSD symptoms. Its avoidance symptom subscale (ranges 0 - 56) is the sum of 7 PTSD symptoms (each ranges 0 - 8) in the avoidance/emotional numbing symptom subcategory. A higher avoidance symptom score indicates worse PTSD symptoms. A positive change score indicates an increased avoidance symptom score (i.e., worse PTSD symptoms) at 4-week (or 12-week) compared to its baseline value, while a negative change score indicates an opposite direction.~The higher is the avoidance/emotional numbing PTSD subscale score, the worse is the PTSD symptom." (NCT01739335)
Timeframe: baseline to 4-Week and 12-Week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone 600 mg/Day-6.24-6.30
Sugar Pill-6.81-6.22

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Change in Plasma Cortisol From Baseline to 4-Week

Mifepristone will induce acute increase in Cortisol and ACTH levels. Higher Cortisol value indicates higher magnitude of mifepristone's effects on negative feedback inhibition. Cortisol value in placebo group at follow-up visits will remain at the similar level as its baseline magnitude. A positive change value indicates an increased cortisol level at 4-week (i.e., higher magnitude on negative feedback inhibition) compared to its baseline value, while a negative change value indicates an opposite direction. (NCT01739335)
Timeframe: Baseline to 4-week

Interventionug/dl (Median)
Mifepristone (600 mg/Day)-0.6
Sugar Pill-0.4

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Change in Plasma Cortisol From Baseline to 1-Week

Mifepristone will induce acute increase in Cortisol and ACTH levels. Higher Cortisol value indicates higher magnitude of mifepristone's effects on negative feedback inhibition. Cortisol value in placebo group at follow-up visits will remain at the similar level as its baseline magnitude. A positive change value indicates increased cortisol level at 1-week (i.e., higher magnitude on negative feedback inhibition) compared to its baseline value, while a negative change value indicates an opposite direction. (NCT01739335)
Timeframe: Baseline to 1-week

Interventionug/dl (Median)
Mifepristone (600 mg/Day)22.3
Sugar Pill-0.9

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Change in Adrenocorticotropic Hormone (ACTH) From Baseline to 4-week

Mifepristone will induce acute increase in Cortisol and ACTH levels. Higher ACTH value indicates higher magnitude of mifepristone's effects on negative feedback inhibition. ACTH value in placebo group at follow-up visits will remain at the similar level as its baseline magnitude. A positive change value indicates an increased ACTH level at 4-week (i.e., higher magnitude on negative feedback inhibition) compared to its baseline value, while a negative change value indicates an opposite direction. (NCT01739335)
Timeframe: Baseline to 4-week

Interventionpg/ml (Median)
Mifepristone (600 mg/Day)-0.8
Sugar Pill1.5

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Change in Anger Level (Measured by the STAXI Total Score) From Baseline to 4-Week and 12-Week

The State-Trait Anger Expression Inventory (STAXI) total score is the sum of 10 items assessing intensity of anger as an emotional state (State Anger) and the disposition to experience angry feelings as a personality trait (Trait Anger). Each item consists of a 4-point scale (1=not at all, 4=very much) that assess intensity of anger at a particular moment and the frequency of anger experience, expression and control. The STAXI total score ranges from 10 to 40, with a higher score indicating a higher intensity of anger.The sum of the 7 component scores yields the PSQI total score (range 0-21) with a higher score indicating a worse sleep quality. A positive change score indicates an increased STAXI total score (i.e., higher intensity of anger) at 4-week (or 12-week) compared to its baseline value, while a negative change score indicates an opposite direction. (NCT01739335)
Timeframe: Baseline to 4-week and 12-week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone (600 mg/Day)-0.61-1.73
Sugar Pill-1.83-3.20

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Change in CAPS Intrusive Symptom Scores From Baseline to 4-Week and 12-Week

The Clinical Administered PTSD Scale (CAPS) was used to assess the diagnosis of PTSD symptoms. Its intrusive symptom subscale (ranges 0 - 40) is the sum of 5 PTSD symptoms (each ranges 0 - 8) in the intrusive/re-experiencing symptom subcategory. A higher intrusive symptom score indicates worse PTSD symptoms. A positive change score indicates an increased intrusive symptom score (i.e., worse PTSD symptoms) at 4-week (or 12-week) compared to its baseline value, while a negative change score indicates an opposite direction. (NCT01739335)
Timeframe: baseline to 4-Week and 12-Week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone (600 mg/Day)-4.27-4.77
Sugar Pill-5.49-7.78

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Change in CAPS Hyperarousal Symptom Scores From Baseline to 4-Week and 12-Week

The Clinical Administered PTSD Scale (CAPS) was used to assess the diagnosis of PTSD symptoms. Its hyperarousal symptom subscale (ranges 0 - 40) is the sum of 5 PTSD symptoms (each ranges 0 - 8) in the hyperarousal symptom subcategory. A higher hyperarousal symptom score indicates worse PTSD symptoms. A positive change score indicates an increased hyperarousal symptom score (i.e., worse PTSD symptoms) at 4-week (or 12-week) compared to its baseline value, while a negative change score indicates an opposite direction. (NCT01739335)
Timeframe: baseline to 4-Week and 12-Week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone (600 mg/Day)-3.35-3.22
Sugar Pill-3.49-4.15

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Change in Adrenocorticotropic Hormone (ACTH) From Baseline to 1-week

Mifepristone will induce acute increase in Cortisol and ACTH levels. Higher ACTH value indicates higher magnitude of mifepristone's effects on negative feedback inhibition. ACTH value in placebo group at follow-up visits will remain at the similar level as its baseline magnitude. A positive change value indicates an increased ACTH level at 1-week (i.e., higher magnitude on negative feedback inhibition) compared to its baseline value, while a negative change value indicates an opposite direction. (NCT01739335)
Timeframe: baseline to 1-week

Interventionpg/ml (Median)
Mifepristone (600 mg/Day)28.8
Sugar Pill-0.5

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Change in Depression (Measured by the BDI Total Score) From Baseline to 4-Week and 12-Week

The Beck Depression Inventory (BDI) total score (ranges 0-63) is the sum of 21 items (each item rated on a 4-point scale of 0 to 3) relating to symptoms of depression, cognitions, and physical symptoms. The BDI total score measures the overall severity of depression. The higher the BDI total score, the more severe the depression. A positive change score indicates an increased BDI total score (i.e., more severe depression) at 4-week (or 12-week) compared to its baseline value, while a negative change score indicates an opposite direction. (NCT01739335)
Timeframe: baseline to 4-Week and 12-Week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone (600 mg/Day)-3.50-2.25
Sugar Pill-4.52-5.07

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Change in Sleep Quality (Measured by the PSQI Total Score) From Baseline to 4-Week and 12-Week

The Pittsburgh Sleep Quality Index (PSQI) assesses self-report sleep quality and disturbances. Nineteen individual items generate 7 component scores: subjective sleep quality, sleep latency, sleep duration, habitual sleep efficiency, sleep disturbances, use of sleeping medication and daytime dysfunction. Each component is scored from 0=better to 3=worse. The sum of the 7 component scores yields the PSQI total score (range 0-21) with a higher score indicating a worse sleep quality. A positive change score indicates an increased PSQI total score (i.e., worse sleep quality) at 4-week (or 12-week) compared to its baseline value, while a negative change score indicates an opposite direction. (NCT01739335)
Timeframe: baseline to 4-Week and 12-Week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone (600 mg/Day)-1.63-0.86
Sugar Pill-1.27-2.04

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Changes in PTSD Symptom Severity (Measured by the Stressful Life Total Score From the PTSD Checklist) From Baseline to 4-Week and 12-Week

"Stressful life total score (ranges 17-85) is the sum of the severity ratings of the 17 PTSD-related symptoms (each symptom is rated on a 5-point scale of 1=not at all to 5=extremely) over the past week. It evaluates the extent to which responders have been bothered by the symptoms of PTSD. The higher stressful life score indicates more stressful life events. A positive change score indicates an increased stressful life total score (i.e., more stressful life events) at 4-week (or 12-week) compared to its baseline value, while a negative change score indicates an opposite direction." (NCT01739335)
Timeframe: baseline to 4-Week and 12-Week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone (600 mg/Day)-6.84-6.84
Sugar Pill-8.65-8.12

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Change in CAPS Total Score From Baseline to 4-week and 12-week

The Clinical Administered PTSD Scale (CAPS) was used to assess the diagnosis of PTSD symptoms. The CAPS total score ranges 0 to 136, which is the sum of 17 PTSD symptoms (each symptom is the sum of the frequency score (ranges 0-4) and the intensity score (ranges 0-4)) in the three different symptom subcategories (intrusive/re-experiencing (0-40), avoidance/numbing (0-56) and hyperarousal (0-40)). A higher CAPS total score indicates worse PTSD symptoms. A positive change score indicates an increased CAPS total score (i.e., worse PTSD symptoms) at 4-week (12-week) compared to its baseline value, while a negative change score indicates an opposite direction. (NCT01739335)
Timeframe: baseline to 4-week

,
Interventionunits on a scale (Least Squares Mean)
Change Score from Baseline to 4-weekChange Score from Baseline to 12-week
Mifepristone (600 mg/Day)-13.96-15.15
Sugar Pill-15.83-18.06

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Chills (Any) After Day 2 Medication Administration

chills (any) after Day 2 medication administration (NCT01751087)
Timeframe: assessed immediately after administration of day 2 medication

Interventionparticipants (Number)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)12
Osmotic Dilators + Placebo (Vit c) + Misoprostol39
Osmotic Dilators + Mifepristone + Placebo (Vit B12)18

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Ability to Complete the D&E on the First Attempt

Assessed on day of procedure and following day. If the procedure was unable to be completed as planned and the subject had to leave the procedure room and return for another attempt either at a time later the same day or the next day. (NCT01751087)
Timeframe: participants were assessed for the duration of the procedure, an average of 6 minutes

Interventionparticipants (Number)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)98
Osmotic Dilators + Placebo (Vit c) + Misoprostol98
Osmotic Dilators + Mifepristone + Placebo (Vit B12)98

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Operative Time

The duration of the D&E procedure was measured with a stopwatch, starting with the first instrument that passes into the uterus and ending when the last instrument is removed from the uterus upon completion of the D&E (NCT01751087)
Timeframe: participants were assessed for the duration of the procedure, an average of 6 minutes

Interventionminutes (Mean)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)6.27
Osmotic Dilators + Placebo (Vit c) + Misoprostol6.28
Osmotic Dilators + Mifepristone + Placebo (Vit B12)5.53

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Complications From Procedure

Patient having any complication, including hospitalizations transfusions additional unplanned procedures (NCT01751087)
Timeframe: assessed immediately after completion of D&E and at 1 week and 1 month post-procedure

Interventionparticipants (Number)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)10
Osmotic Dilators + Placebo (Vit c) + Misoprostol2
Osmotic Dilators + Mifepristone + Placebo (Vit B12)2

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Physician Satisfaction With Cervical Preparation

Participants for whom the operating physician reported being satisfied or very satisfied with the cervical preparation. Assessed on Day of procedure. Assessed after completion of D&E procedure. (NCT01751087)
Timeframe: physicians' satisfaction with cervical prep was evaluated over course of procedure, an average of 6 minutes

Interventionparticipants (Number)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)71
Osmotic Dilators + Placebo (Vit c) + Misoprostol78
Osmotic Dilators + Mifepristone + Placebo (Vit B12)85

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Patient Satisfaction With Cervical Prep

Patients who were very satisfied or satisfied with cervical preparation. Assessed on Day of procedure. Assessed after completion of D&E procedure and just prior to discharge home. (NCT01751087)
Timeframe: patients' satisfaction with cervical prep was evaluated over course of cervical prep and procedure, up to 3 days

Interventionparticipants (Number)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)72
Osmotic Dilators + Placebo (Vit c) + Misoprostol80
Osmotic Dilators + Mifepristone + Placebo (Vit B12)80

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Need for Mechanical Dilation

Assessed on Day of procedure. Assessed immediately after completion of D&E (NCT01751087)
Timeframe: participants were assessed for the duration of the procedure, an average of 6 minutes

Interventionparticipants (Number)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)26
Osmotic Dilators + Placebo (Vit c) + Misoprostol9
Osmotic Dilators + Mifepristone + Placebo (Vit B12)16

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Initial Cervical Dilation

Measured at the time of procedure (immediately before the start of D&E) (NCT01751087)
Timeframe: participants were assessed during cervical dilation process, average time of 1 minute

Interventioncentimeters (Mean)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)2.2
Osmotic Dilators + Placebo (Vit c) + Misoprostol2.5
Osmotic Dilators + Mifepristone + Placebo (Vit B12)2.4

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Ease of Mechanical Dilation

Number of participants for whom, if additional mechanical dilation was required, it was difficult or very difficult. Assessed on day of procedure. Assessed after completion of D&E (NCT01751087)
Timeframe: participants were assessed for the duration of the procedure, an average of 6 minutes

Interventionparticipants (Number)
Osmotic Dilators + Placebo (Vit c) + Placebo (Vit B12)6
Osmotic Dilators + Placebo (Vit c) + Misoprostol4
Osmotic Dilators + Mifepristone + Placebo (Vit B12)1

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Procedure Time

Measured as time from speculum insertion to removal (NCT01862991)
Timeframe: Intraoperative Time, Collected immediately within procedure

Interventionminutes (Median)
Dilapan-Placebo13
Dilapan-Mifepristone12
Mifepristone18.5

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Adverse Events

Uterine perforation (NCT01862991)
Timeframe: Intraoperatively and 2 weeks post operatively

InterventionParticipants (Count of Participants)
Dilapan-Placebo0
Dilapan-Mifepristone1
Mifepristone2

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Body Mass Index (BMI)

Change in metabolic syndrome as assessed by BMI (NCT01990560)
Timeframe: Baseline and 6 months

Interventionkg/m2 (Mean)
Baseline6 months
Mifepristone35.153834.5463

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CushingQoL

Change in Quality of Life - as assessed by the Cushing's Quality of Life questionnaire (CushingQoL). Patient completed questionnaire, 12 items, each scored on a 5 point score, resulting in a score of 12 (worst) to 60 (best) where higher scores indicate more favorable QOL. (NCT01990560)
Timeframe: Baseline and 6 months

Interventionunits on a scale (Mean)
Baseline6 months
Mifepristone37.285738.7857

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Fasting Lipid Profile

Change in metabolic syndrome as assessed by fasting lipid profile which includes Low-density lipoproteins ( LDL), High-density lipoproteins (HDL), and Triglycerides (Trigs) levels, and total cholesterol which is the sum of HDL plus LDL and 20% of trigs. (NCT01990560)
Timeframe: Baseline and 6 months

Interventionmg/dL (Mean)
Total Cholesterol BaselineTotal Cholesterol 6 monthsLDL baselineLDL 6 monthsHDL BaselineHDL 6 monthsTrigs BaselineTrigs 6 months
Mifepristone178.63171.4397.88104.3759.1346.86107.88100.29

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HOMA-IR

Change in hyperglycemia assessed by Homeostatic Model Assessment of Insulin Resistance, HOMA-IR (a validated assessment of insulin resistance). HOMA-IR = fasting insulin (microU/L) x fasting glucose (nmol/L)/22.5. (NCT01990560)
Timeframe: Baseline and 6 months

InterventionHOMA-IR score (Mean)
Baseline6 months
Mifepristone2.4181.465

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Hospital Anxiety and Depression Scale (HADS)

Change in Quality of Life as assessed by the Hospital Anxiety and Depression Scale (HADS). Questionnaire with 7 items for anxiety and 7 items for depression, each item is scored on a 4 point response 0 - 3, with full range from 0 to 42, with higher score indicating more severe anxiety or depression (NCT01990560)
Timeframe: Baseline and 6 months

Interventionunits on a scale (Mean)
Baseline6 months
Mifepristone16.285711.1667

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Quality of Life

Change in Quality of Life as assessed by the Beck Depression Inventory. a 21-question multiple choice, self-report inventory that is used for measuring the severity of anxiety. Scoring is from a 0 (not at all) to 3 (severe) with a total score range of 0-63. Higher total scores indicate more severe anxiety symptoms. (NCT01990560)
Timeframe: Baseline and 6 months

Interventionunits on a scale (Mean)
Baseline6 months
Mifepristone16.142911.7143

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State Trait Anxiety Inventory (STAI)

Change in Quality of Life - as assessed by the State Trait Anxiety Inventory (STAI). The State-Trait Anxiety Inventory both state and trait anxiety separately. Each type of anxiety has its own scale of 20 different questions that are scored and averaged. Total scores range from 20 to 80, with higher scores correlating with greater anxiety. (NCT01990560)
Timeframe: Baseline and 6 months

Interventionunits on a scale (Mean)
Baseline6 months
Mifepristone25.428628.8571

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Waist Circumference

Change in metabolic syndrome as assessed by waist circumference (NCT01990560)
Timeframe: Baseline and 6 months

Interventioncm (Mean)
Baseline6 months
Mifepristone103.2599.3125

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Weight

Change in metabolic syndrome as assessed by weight (NCT01990560)
Timeframe: Baseline and 6 months

Interventionkg (Mean)
Baseline6 months
Mifepristone99.5797.75

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A1C Level

Change in hyperglycemia assessed by HbA1c, also known as glycated hemoglobin (NCT01990560)
Timeframe: Baseline, 3 months, and 6 months

Interventionpercentage of red blood cells (Mean)
Baseline3 months6 months
Mifepristone6.26.13756.125

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Nottingham Health Profile (NHP)

Change in Quality of Life as assessed by the Nottingham Health Profile (NHP) which is a patient reported questionnaire to measure a patient's view of their own health status. There are 6 sections (Energy level, Pain, Emotional Reaction, Sleep, Social Isolation, and Physical Abilities. All questions have only yes/no answer options and each section score is weighted so that the possible score range for any section is 0-100. The higher the score, the greater the number and severity of problems. (NCT01990560)
Timeframe: Baseline and 6 months

Interventionunits on a scale (Mean)
Energy Level (EL) BaselineEL 6 monthsPain (P) BaselineP 6 monthsEmotional Reaction (ER) BaselineER 6 monthsSleep (S) BaselineS 6 monthsSocial Isolation (SI) BaselineSI 6 monthsPhysical Abilities (PA) BaselinePA 6 months
Mifepristone32.6045.4024.8832.0827.0335.0924.8731.1520.0931.1523.0627.49

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Number of Participants With Positive AR Expression Within Circulating Tumor Cells (CTCs)

Positive/negative classification with positive defined as a cytokeratin cell for whom there was an androgen receptor > 0 (NCT02012296)
Timeframe: Week 12 (randomization)

InterventionParticipants (Count of Participants)
Treatment (Enzalutamide)16
Treatment (Enzalutamide, Mifepristone)8
Not Randomized5

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Number of Participants With Positive GR Expression Within Circulating Tumor Cells (CTCs)

Positive/negative classification with positive defined as a cytokeratin cell for whom there was an glucocorticoid receptor > 0 (NCT02012296)
Timeframe: Week 12 (randomization)

InterventionParticipants (Count of Participants)
Treatment (Enzalutamide)17
Treatment (Enzalutamide, Mifepristone)8
Not Randomized5

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PSA Progression-free Survival

PSA progression was defined as a PSA that is ≥1.25 times (25% increase) the PSA at randomization (week 12) and an absolute 5 ng/ml increase. PSA progression-free survival is PSA progression or death from any cause. (NCT02012296)
Timeframe: Up to 3 years, measured from randomization

InterventionMonths (Median)
Treatment (Enzalutamide)20.8
Treatment (Enzalutamide, Mifepristone)16.5

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Radiographic PFS

Radiographic progression or death from any cause. (NCT02012296)
Timeframe: Up to 3 years, measured from randomization

InterventionMonths (Median)
Treatment (Enzalutamide)NA
Treatment (Enzalutamide, Mifepristone)16.5

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Testosterone

Change from week 12 to week 16 (NCT02012296)
Timeframe: 12 to 16 weeks

Interventionng/dL (Mean)
Treatment (Enzalutamide)0.6
Treatment (Enzalutamide, Mifepristone)21.0

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Thyroid Stimulating Hormone

Change in log(TSH) from week 12 to week 16 (NCT02012296)
Timeframe: 12 to 16 weeks

Interventionlog(mcU/mL) (Mean)
Treatment (Enzalutamide)-0.121
Treatment (Enzalutamide, Mifepristone)0.306

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Cortisol

Change in log(Cortisol) from week 12 to week 16 (NCT02012296)
Timeframe: 12 to 16 weeks

Interventionlog(ug/dL) (Mean)
Treatment (Enzalutamide)0.072
Treatment (Enzalutamide, Mifepristone)0.733

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Uterine Asperation

Surgical removal of the miscarriage. (NCT02012491)
Timeframe: 30 Days

InterventionParticipants (Count of Participants)
Misoprostol35
Misoprostol Plus Mifepristone13

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Gestational Sac Expulsion With One Treatment Dose on Day 3 (Visit 2) and no Need for Additional Medical or Surgical Intervention Within 30 Days of Treatment.

(NCT02012491)
Timeframe: Day 3 (visit 2) and up to 30 days following visit (to ensure surgical measures were not done

InterventionParticipants (Count of Participants)
Misoprostol100
Misoprostol Plus Mifepristone124

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Gestational Sac Expulsion by the Second Follow-up Visit at Day 8

(NCT02012491)
Timeframe: Day 8 (visit 3) and up to 30 day to ensure additional measures were not done (surgical)

InterventionParticipants (Count of Participants)
Misoprostol111
Misoprostol Plus Mifepristone132

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Gestational Sac Expulsion by the 30-day Telephone Call

(NCT02012491)
Timeframe: 30 Days

InterventionParticipants (Count of Participants)
Misoprostol113
Misoprostol Plus Mifepristone135

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Frequency of Serious Adverse Events Between Study Arms.

(NCT02012491)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Misoprostol3
Misoprostol Plus Mifepristone5

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Adverse Event Reported by Participants

(NCT02012491)
Timeframe: 30 Days

Interventionadverse events (Mean)
Misoprostol5.6
Misoprostol Plus Mifepristone6.1

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Drinking Quantity Per Day

"Drinking quantity in standard drinks per day is measured by the Timeline Followback interview.~A standard drink contains 14 grams of alcohol, e.g., 1.5 ounces of distilled spirits, 5 ounces of wine, or 12 ounces of beer." (NCT02179749)
Timeframe: Participants will be followed for up to 12 weeks post-assignment

InterventionStandard drinks per day (Mean)
Placebo1.25
600 mg/d of Mifepristone1.38
1200 mg/d of Mifepristone1.10

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Craving

Alcohol Craving Questionnaire; minimum value equals 12, maximum value equals 84; higher scores mean greater craving for alcohol. (NCT02179749)
Timeframe: Participants will be followed for up to 12 weeks

Interventionscore on a scale (Mean)
Experimental: Mifepristone 1200 mg Daily29.02
Placebo Daily, 1-week33.66
Experimental: Mifepristone 600 mg Day28.33

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Alcohol Craving Score on the Alcohol Craving Questionnaire in the Mifepristone Versus Placebo Group

Alcohol craving will be assessed by the Alcohol Craving Questionnaire Short Form - Revised (ACQ-SF-R). The ACQ-SF-R is a 12-item self-report scale that contains items from the 47-item Alcohol Craving Questionnaire (ACQ-Now). ACQ-SF-R also produces scores for compulsivity, expectancy, purposefulness, and emotionality. To assess this outcome, at the alcohol cue reactivity procedures/visits 3 and 5 during alcohol trial 1, the 12-item total ACQ will be summed for each participant and then the total score will be averaged for a mean score. The average ACQ score in the presence of alcohol cues will be compared when participants are taking mifepristone compared to placebo. The ACQ has a total score range between 0-84. A lower score indicates less subjective alcohol craving. (NCT02243709)
Timeframe: 1 day

Interventionscore on a scale (Mean)
Mifepristone42.92
Placebo50.13

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Drinking Consumption in the Mifepristone Verses Placebo Group

Number of standard drinks desired to be consumed by participants during mifepristone administration compared to placebo administration during the open bar (free choice procedure) in the alcohol cue reactivity at visits 3 and 5. (NCT02243709)
Timeframe: 1 day

Interventiondrinks (Mean)
Mifepristone0.8
Placebo0.5

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Number of Participants Experiencing Adverse Events in the Mifepristone Versus Placebo Group as a Measure of Safety and Tolerability

Safety and tolerability was assessed by the number of participants who experienced adverse events (AEs) while taking the medication, in the mifepristone group verses the placebo group during Visit 2 through and until Visit 5. AEs were assessed at each visit and special attention was paid to any AEs experienced after administration of the oral administration of mifepristone or placebo- Visit 2 to Visit 3 (7 days total) and Visit 4 through Visit 5 (7 days total), and when it was administered with alcohol during the laboratory paradigms at visits 3 and 4. (NCT02243709)
Timeframe: 5 weeks (one week of drug administration, 3 weeks of washout, followed by one week of drug administration)

InterventionParticipants (Count of Participants)
Mifepristone0
Placebo3

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Initial Cervical Dilation

Initial cervical dilation as measured by Hegar Dilator accepted with least resistance (NCT02412618)
Timeframe: Assessed 4-6 hour following medications at time of D&E procedure

Interventionmm (Mean)
Mifepristone11.7
Placebo10.9

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Patient Acceptability and Assessment of Pain and Side Effects (5-point Likert Scale)

"5-point Likert scale given to patients following procedure once recovered from anesthesia assessing pain, side effects including nausea, vomiting, diarrhea, cramping, and if they would choose the method again or recommend to friends.~Likert scale: Strongly agree (5), Agree (4), Neutral (3), Disagree (2), Strongly Disagree (1)" (NCT02412618)
Timeframe: intraoperative

,
Interventionunits on a scale (Mean)
NauseaSevere Cramps
Mifepristone44
Placebo44

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Time to Delivery of Fetus

From the initiation of medical therapy for induction to delivery of fetus, assessed up to 36 hours (NCT02620904)
Timeframe: From the initiation of medical therapy for induction to delivery of fetus, assessed up to 36 hours

Interventionhours (Mean)
Mifepristone14
Placebo Pill20

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Adverse Events

Non-hypoglycemia-related adverse events (NCT03052400)
Timeframe: Baseline to 3 months

Interventionnumber of events (Number)
Mifepristone 600 mg Daily6
Placebo2

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ACTH

Serum adrenocorticotrophic hormone level (AM) (NCT03052400)
Timeframe: Baseline to 3 months

Interventionpg/mL, change from baseline (Mean)
Mifepristone 600 mg Daily56.0
Placebo-8.3

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Cortisol

Serum cortisol level (AM) (NCT03052400)
Timeframe: Baseline to 3 months

Interventionmg/dL, change from baseline (Mean)
Mifepristone 600 mg Daily18.8
Placebo-0.9

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Hemoglobin A1c

Glycemic lowering (NCT03052400)
Timeframe: Baseline to 3 months

InterventionPercentage of hemoglobin (Mean)
Mifepristone 600 mg Daily-2.4
Placebo-1.5

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Weight

Weight in kg (NCT03052400)
Timeframe: Baseline to 3 months

Interventionkg, change from baseline (Mean)
Mifepristone 600 mg Daily1.4
Placebo0.5

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Systolic BP

Systolic blood pressure (NCT03052400)
Timeframe: Baseline to 3 months

Interventionmm Hg, change from baseline (Mean)
Mifepristone 600 mg Daily3.0
Placebo-3.7

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PSA

Prostate-specific antigen level (NCT03052400)
Timeframe: Baseline to 3 months

Interventionng/mL, change from baseline (Mean)
Mifepristone 600 mg Daily-0.3
Placebo0.1

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LDL-cholesterol

Low-density lipoprotein cholesterol (NCT03052400)
Timeframe: Baseline to 3 months

Interventionmg/dL, change from baseline (Mean)
Mifepristone 600 mg Daily-1.3
Placebo-9.7

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Hypoglycemic Events

Symptomatic mild and severe hypoglycemic events (NCT03052400)
Timeframe: Baseline to 3 months

Interventionnumber of events (Number)
Mifepristone 600 mg Daily22
Placebo31

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Diastolic BP

Diastolic blood pressure (NCT03052400)
Timeframe: Baseline to 3 months

Interventionmm Hg, change from baseline (Mean)
Mifepristone 600 mg Daily-4.3
Placebo-3.7

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Uric Acid

Serum uric acid level (NCT03052400)
Timeframe: Baseline to 3 months

Interventionmg/dL, change from baseline (Mean)
Mifepristone 600 mg Daily-0.8
Placebo1.1

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Body Mass Index

Body mass index in kg/m^2 (NCT03052400)
Timeframe: Baseline to 3 months

Interventionkg/m^2, change from baseline (Mean)
Mifepristone 600 mg Daily0.6
Placebo0.0

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Basal Insulin Dose

Total daily basal insulin dosage (NCT03052400)
Timeframe: Baseline to 3 months

InterventionUnits of insulin per day (Mean)
Mifepristone 600 mg Daily-1.3
Placebo0.7

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Number of Pharmacists Who Report Being Satisfied With Pharmacy Dispensing of Mifeprex

"Number of pharmacists who report being somewhat satisfied or very satisfied when asked Overall, how satisfied are you with mifepristone dispensing at your pharmacy? in endline survey" (NCT03320057)
Timeframe: End of the study, month 24

InterventionParticipants (Count of Participants)
Pharmacists36

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Number of Participants Who Report Being Satisfied With Obtaining Mifeprex in the Pharmacy

"Number of participants who report being somewhat satisfied or very satisfied when asked Overall, how satisfied were you with your experience at the pharmacy when you got the abortion pill?" (NCT03320057)
Timeframe: Day 2 following initial medication abortion visit

InterventionParticipants (Count of Participants)
Medication Abortion Patients230

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Number of Participants With an Adverse Event

Number of participants who had a medical problem that required them to go to the hospital, emergency department or a doctor's office (other than regularly scheduled follow-up visit) since receiving the abortion pill (NCT03320057)
Timeframe: Up to 6 weeks after initial visit

InterventionParticipants (Count of Participants)
Medication Abortion Patients4

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Number of Participants With a Complete Abortion With Medication Alone and Who do Not Require a Surgical Procedure to Complete the Abortion

"Number of participants who report that their abortion is now complete and they are no longer pregnant and who did not end up having a suction procedure (or vacuum aspiration or dilation and curettage procedure) to complete the abortion" (NCT03320057)
Timeframe: Up to 6 weeks after initial visit

InterventionParticipants (Count of Participants)
Medication Abortion Patients243

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Number of Pharmacists Who Objected to Participate in Dispensing Mifeprex

Number of pharmacists who objected to participate in dispensing Mifeprex at least once during the study period. This includes pharmacists who declined participation in the study training on medication abortion due to discomfort as well as pharmacists who participated in the training but declined to dispense Mifeprex. (NCT03320057)
Timeframe: End of the study, month 24

InterventionParticipants (Count of Participants)
Pharmacists4

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"Provider Assessment of Procedure as Very Easy or Easy"

"Survey providers blinded to study grouping regarding overall ease of procedure based on cervical dilation Identified procedures that were categorized as Very Easy or Easy (Survey response based on Likert scale: Very Easy, Easy, Moderate, Difficult, Very Difficult)" (NCT03714880)
Timeframe: At time of ~1 hour scheduled procedure time

InterventionParticipants (Count of Participants)
Mifepristone8
Placebo9

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Cervical Dilation

Measurement of cervical dilation at time of procedure (NCT03714880)
Timeframe: At time of ~1 hour scheduled procedure time (1 minute)

Interventioncm (Median)
Mifepristone3.2
Placebo2.6

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Number of Participants That Experienced Complications

Composite of complications including cervical lacerations requiring repair, perforations, blood transfusions, ED visits, hospitalizations, infections, additional surgical procedures, or extramural deliveries (NCT03714880)
Timeframe: At time of ~1 hour scheduled procedure time (0-30 minute)

InterventionParticipants (Count of Participants)
Mifepristone3
Placebo3

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Number of Participants That Required Mechanical Dilation

A count of the number of participants that required of mechanical dilation at time of procedure (NCT03714880)
Timeframe: At time of ~1 hour scheduled procedure time (10 minute)

InterventionParticipants (Count of Participants)
Mifepristone2
Placebo4

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Number of Participants That Had Placement of Expected Dilators or More

"The number of expected dilators (Dilapan-S) is calculated based on the gestational age. Four dilators are expected to be placed at 18 weeks 0 days to 19 weeks 6 days gestation. Five dilators are expected to be placed at 20 weeks 0 days to 20 weeks 6 days gestation. Six dilators are expected to be placed at 21 weeks 0 days to 21 weeks 6 days gestation. Seven dilators are expected to be placed at 22 weeks 0 days to 23 weeks 5 days gestation. Therefore, at any given gestational age, if the expected number of dilators (or additional dilators) were placed, the participant was counted as Yes, participant had placement of expected dilators or more." (NCT03714880)
Timeframe: At time of 1 hour clinic visit (10 minutes)

InterventionParticipants (Count of Participants)
Mifepristone17
Placebo21

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Number of Participants That Required Mechanical Dilation

Number of participants that required mechanical dilation at time of procedure (NCT03714880)
Timeframe: At time of ~1 hour scheduled procedure time

InterventionParticipants (Count of Participants)
Mifepristone2
Placebo4

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Pain Dilator Placement Using Visual Analog Scale

"Title: Pain at time of dilator placement. Participants mark their associated pain score on a 10-cm visual analog scale at time of dilator placement with anchors of no pain at 0 cm and worst pain in your life at 10 cm.~Higher scores indicate worse outcome." (NCT03714880)
Timeframe: At time of 1 hour clinic visit (10 minutes)

Interventioncm (Median)
Mifepristone1.2
Placebo3.3

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Number of Participants With Adverse Events During Follow-up Evaluation

Side effects from progesterone/placebo treatment and ability to continued treatment as prescribed (NCT03774745)
Timeframe: up to 16 days after mifepristone administration

,
Interventionparticipants (Number)
NauseaVomitingMastalgiaTirednessMood changesRefluxDizzinessBleedingSpottingCramping
Placebo Oral Capsule1001000300
Progesterone2200100100

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Medical Safety During Treatment and Follow-up

Adverse events related to morbidity, e.g. hemorrhage, emergency department visits, emergent dilation and curettage procedures (NCT03774745)
Timeframe: up to 16 days after mifepristone administration

,
Interventionparticipants (Number)
HemorrhageEmergency Room VisitTransfusionEmergent D&CSide effects - request D&C
Placebo Oral Capsule22121
Progesterone11001

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Expulsion During Follow-up Evaluation

Pregnancy expulsion following mifepristone treatment (NCT03774745)
Timeframe: up to 16 days after mifepristone administration

InterventionParticipants (Count of Participants)
Progesterone1
Placebo Oral Capsule2

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Continuing Pregnancy Based on Ultrasound Examination

Pregnancy still in uterus with normal growth and gestational cardiac activity present based on ultrasound examination (NCT03774745)
Timeframe: at 14-16 days after mifepristone administration

InterventionParticipants (Count of Participants)
Progesterone4
Placebo Oral Capsule2

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Number of Participants With Change in Serum Progesterone and hCG During Follow-up

Change in serum progesterone and hCG during follow-up evaluation (NCT03774745)
Timeframe: up to 16 days after mifepristone administration

,
Interventionparticipants (Number)
Progesterone increase from baseline at FU 1Progesterone decrease from baseline at FU 1hCG increase from baseline at FU 1hCG decrease from baseline at FU 1
Placebo Oral Capsule2233
Progesterone5041

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Peak Cortisol Measured After Mifepristone

Serum cortisol was collected the day after mifepristone administration and insulin tolerance test insulin tolerance test (ITT). (NCT04588688)
Timeframe: Day 2 (day after mifepristone administration)

Interventionmicrograms per deciliter (Mean)
ITT Greater or Equal to 15 Max Cortisol13.9

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Number of Study Participants With Complete Study Data Captured

Because this was a feasibility trial, the goal was to see how many participants could be successfully recruited. The original intent was for the recruitment period to be for 36 months, with a target enrollment of 26 participants. Because of low enrollment, the decision to terminate was made after the trial had been open for recruitment for approximately 30 months (February 17, 2020 - September 7, 2022). (NCT04588688)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Mifepristone3

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Number of Study Participants Recruited

Because this was a feasibility trial, the goal was to see how many participants could be successfully recruited. The original intent was for the recruitment period to be for 36 months, with a target enrollment of 26 participants. The trial opened for recruitment on February 17, 2020. Because of low enrollment, the decision to terminate was made on September 7, 2022, approximately 30 months later. (NCT04588688)
Timeframe: Up to 88 days

InterventionParticipants (Count of Participants)
Mifepristone3

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Absolute ACTH After Mifepristone

ACTH level 8:00 am (Day 2) following administration of mifepristone the night before at 10:00 pm. (NCT04588688)
Timeframe: Day 2 (day after mifepristone administration)

InterventionPicogram per milliliter (Mean)
Greater or Equal to 15 Max Cortisol18.5

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