Rx00161 - Mifepristone


Name:
Mifepristone
Rx ID:
Rx00161
Validation Level:
Reference ID:
DB00834
Primary Indications:
Pregnancy termination
Orphan Indications:
No annotated orphan indications.
Rare Indications:
No annotated rare indications.
Common Indications:
Psychotic major depression
Pathways:
Serotonin Receptor 4-6-7 and NR3C Signaling; Regulation of Androgen receptor activity
Drug Interactions:
Buserelin; Dabigatran etexilate; Degarelix; Etravirine; Oxytocin; Pasireotide Tofacitinib;
Food Interactions:
No annotated food interactions in DrugBank.

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Rx00161
Primary Indication
Secondary Indication

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Chemical, Pharmacological and Biological Annotations


ATC Code:
G03XB01
Brands:
Corlux (Corcept Therapeutics Incorporated); Mefipil (Abbott); Mifegyne (Exelgyn Laboratories); Mifeprex (Danco Laboratories)
Categories:
Hormone Antagonists; Contraceptives, Oral, Synthetic; Abortifacient Agents, Steroidal; Contraceptives, Postcoital, Synthetic; Luteolytic Agents; Menstruation-Inducing Agents
ChEBI ID:
50692
PubChem ID:
55245
KEGG Drug ID:
D00585
SMILE:
[H][C@@]12CC[C@@](O)(C#CC)[C@@]1(C)C[C@H](C1=CC=C(C=C1)N(C)C)C1=C3CCC(=O)C=C3CC[C@@]21[H]
InChI:
1S/C29H35NO2/c1-5-15-29(32)16-14-26-24-12-8-20-17-22(31)11-13-23(20)27(24)25(18-28(26,29)2)19-6-9-21(10-7-19)30(3)4/h6-7,9-10,17,24-26,32H,8,11-14,16,18H2,1-4H3/t24-,25+,26-,28-,29-/m0/s1
Classification:
Kingdom:
Organic Compounds
Superclass:
Lipids
Class:
Steroids and Steroid Derivatives
Subclass:
Ketosteroids
Indication:
For the medical termination of intrauterine pregnancy through 49 days' pregnancy. Also indicated to control hyperglycemia secondary to hypercortisolism in adult patients with endogenous Cushing's syndrome who have type 2 diabetes mellitus o...
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Pharmacodynamics:
Mifepristone is a synthetic steroid with antiprogestational effects indicated for the medical termination of intrauterine pregnancy through 49 days' pregnancy. Doses of 1 mg/kg or greater of mifepristone have been shown to antagonize the en...
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Description:
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 glucocortico...
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Mechanism:
The anti-progestational activity of mifepristone results from competitive interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species (mouse, rat, rabbit and monkey), the ...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
+
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Inhibitor
P-glycoprotein inhibitor II:
Inhibitor
Renal organic cation transporter:
Non-inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Inhibitor
CYP450 2C19 substrate:
Inhibitor
CYP450 inhibitory promiscuity:
High CYP Inhibitory Promiscuity
Ames test:
Non AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
2.7705 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Non-inhibitor

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Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
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Manhattan, New York City, NY
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