Mifeprex: profile and news






Teva's generic Zofran gets provisional FDA approval  Feb 27, 2006
The FDA has granted tentative approval for Teva Pharmaceutical's generic version of GlaxoSmithKline's Zofran, a treatment of chemotherapy induced nausea and ... - Pharmaceutical Business Review

Teva Generic Zofran Unlikely To Hurt GSK  Feb 27, 2006
1050 GMT [Dow Jones] Teva's (TEVA) announcement that it has received a tentative approval from the FDA to sell copies of GlaxoSmithKline's (GSK) Zofran is not ... - New Ratings

SCOLR Pharma Reports Positive Ondansetron Clinical Results, New ...  Feb 16, 2006
Ondansetron hydrochloride is the active ingredient in Zofran(R), GlaxoSmithKline's tablet and injection formulations to prevent chemotherapy and radiation ... - Genetic Engineering News,

Scolr's ondansetron tablets found to outperform Glaxo rival  Feb 17, 2006
Ondansetron hydrochloride is the active ingredient in Zofran, GlaxoSmithKline's tablet and injection formulations to prevent chemotherapy and radiation related ... - Pharmaceutical Business Review

Par Pharmaceutical Reports Sales and Earnings for 2005  Feb 28, 2006
Ondansetron HCl is the generic version of the antiemetic drug Zofran(R), and risperidone is the generic equivalent of the antipsychotic medication Risperdal(R ... - MSN Money

Jagged little pills  Mar 2, 2006
...anxiety. Her psychiatrist put her on Zofran, a nausea medicine given to chemotherapy patients, and she began a long, slow recovery. ... - Silver Chips Online,

GSK says profits could fall prey to generic rivals  Feb 8, 2006
XL, an antidepressant. A third treatment, Zofran, might also fall prey to generic rivals pending an appeal, GSK said. Dr Garnier ... - Times Online,

Teva Announces Tentative Approval of Ondansetron Injection USP  Feb 27, 2006
Upon final approval, Teva's Ondansetron Injection products will be the AP-rated generic equivalent of GlaxoSmithKline's Zofran(R) Injection. ... - PharmaLive.com (press release),

Nausea and Vomiting Significant Among Very Young Pediatric ...  Feb 17, 2006
...their parents. Antiemetic therapy consisted of Zofran® (ondansetron) with or without the steroid dexamethasone. Overall, younger ... - Cancer Consultants (press release),

FDA approves generic competitor to Glaxo's Flonase  Feb 22, 2006
...its financial guidance for 2006 to 10 percent growth due in part to the likelihood of generic competition to Flonase and nausea drug Zofran reaching the market ... - Raleigh Triangle Business Journal,

FDA OKs Teva chemotherapy side effects treatment  Feb 26, 2006
Upon final approval, Teva's Ondansetron Injection products will be the AP-rated generic equivalent of GlaxoSmithKline's Zofran Injection. ... - Globes,

GSK annual results top forecast; beats hopes on 2006 guidance ...  Feb 8, 2006
Cheaper, copycat versions of products including Flonase, which generated sales of 656 mln stg last year, Zofran with 837 mln and Coreg with 573 mln could ... - Forbes

Generic Products Compete With GlaxoSmithKline  Feb 9, 2006
...with regard to the 2006 earnings as a result of low priced generic competitors for the antidepressant Wellbutrin XL, hay fever medication Flonase, and Zofran. ... - MedIndia,

Glaxo's CEO: Not ready to quit in '07  Feb 9, 2006
The company lowered its financial guidance for 2006 to 10 percent growth, based on constant exchange rates and possibly falling revenue from Zofran for nausea ... - philly.com,

GSK says profits could fall prey to generic rivals  Feb 8, 2006
XL, an antidepressant. A third treatment, Zofran, might also fall prey to generic rivals pending an appeal, GSK said. Dr Garnier ... - Times Online,

Doctors get the point  Jan 31, 2006
Last fall, researchers at Duke showed that it was far more effective for postoperative sickness in a group of subjects than Zofran, a widely used antinausea ... - Orlando Sentinel,

Hana Posts Positive Study Results  Jan 9, 2006
...a clinical trial. The study included 32 patients who received either Hana's Zensana drug or GlaxosmithKline's Zofran. Hana said ... - MSN Money

Merck Gets FDA OK for Widened Use of Emend  Jan 11, 2006
Standard therapy was defined as ondansetron, a nausea treatment marketed as Zofran by GlaxoSmithKline PLC, and dexamethasone, a synthetic steroid. - MSN Money

Emend® Approved for Prevention of Moderate Chemotherapy ...  Jan 12, 2006
The first 5-HT3-receptor antagonist, Zofran® (ondansetron), was FDA approved in January 1991 and has proved effective in controlling acute CINV (CINV that ... - Cancer Consultants (press release),

Hana Biosciences Announces Positive Results of Initial ...  Jan 9, 2006
...demonstrated Zensana(TM) (ondansetron oral spray) 8 mg dose is bioequivalent to the current commercially available 8 mg tablet (Zofran(R); GlaxoSmithKline). ... - Genetic Engineering News,

Genzyme Names New Head of Product Development for Campath and ...  Jan 13, 2006
Standard therapy was defined as ondansetron, a nausea treatment marketed as Zofran by GlaxoSmithKline PLC, and dexamethasone, a synthetic steroid. ... - Financial News USA (press release),

FLAVORx Enhances Treatment Options for Pediatric Oncology Patients  Jan 19, 2006
...most effective flavors: 1. Zofran (for nausea associated with chemotherapy)- Raspberry, Natural Orange, Bubblegum. 2. Phenergan (for ... - PR Web (press release),

Hana Biosciences Announces 2006 Corporate Goals; Key 2005 ...  Jan 7, 2006
...-- Q1 05: Zensana(TM) pilot pharmacokinetic study demonstrated pharmacokinetic profile comparable to oral Zofran(R), with multidose convenience and faster drug ... - Biotech Intelligence (press release),


Other information


Indication
For induced abortion

Pharmacology
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 endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the myometrium to the contraction-inducing activity of prostaglandins. Mifepristone also exhibits antiglucocorticoid and weak antiandrogenic activity. The activity of the glucocorticoid dexamethasone in rats was inhibited following doses of 10 to 25 mg/kg of mifepristone. Doses of 4.5 mg/kg or greater in human beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol.

Mechanism Of Action
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 compound inhibits the activity of endogenous or exogenous progesterone. The termination of pregnancy results.

Drug Category
Menstruation-Inducing Agents; Luteolytic Agents; Contraceptives, Oral, Synthetic; Contraceptives, Postcoital, Synthetic; Hormone Antagonists; Abortifacient Agents, Steroidal ATC:G03XB01

Brand Names/Synonyms
HSDB 6841; Mifegyne; Mifeprex; Mifepriston; Mifepristona [Spanish]; Mifepristone; Mifepristone [Usan:Ban:Inn]; Mifepristonum [Latin]; RU 486; RU-486; RU-486, MIFEPRISTONE

Dosage Forms
Tablet

Absorption
The absolute bioavailability of a 20 mg oral dose is 69%

Interactions
Interactions for Mifepristone:

Although specific drug or food interactions with mifepristone have not been studied, on the basis of this drugís metabolism by CYP 3A4, it is possible that ketoconazole, itraconazole, erythromycin, and grapefruit juice may inhibit its metabolism (increasing serum levels of mifepristone). Furthermore, rifampin, dexamethasone, St. Johnís Wort, and certain anticonvulsants (phenytoin, phenobarbital, carbamazepine) may induce mifepristone metabolism (lowering serum levels of mifepristone).

Based on in vitro inhibition information, coadministration of mifepristone may lead to an increase in serum levels of drugs that are CYP 3A4 substrates. Due to the slow elimination of mifepristone from the body, such interaction may be observed for a prolonged period after its administration. Therefore, caution should be exercised when mifepristone is administered with drugs that are CYP 3A4 substrates and have narrow therapeutic range, including some agents used during general anesthesia.



Chemical IUPAC Name
11-(4-dimethylaminophenyl)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one

Chemical Formula
C29H35NO2

Half Life
18 hours

Drug Type
Approved Drug

# Accession No
APRD00432

CAS Registry Number
84371-65-3

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