Inspra: profile and news






Cost Cuts Fuel Pfizer  Jan 19, 2006
The company pointed to the successful launches of seven new medicines over the past two years -- Inspra, Caduet, Olmetec, Macugen, Revatio, Zmax, and Lyrica ... - TheStreet.com

Pfizer Fourth-Quarter and Full-Year 2005 Financial Results Reflect ...  Jan 19, 2006
The combined sales of these products (Inspra, Caduet, Olmetec, Macugen, Revatio, Zmax, and Lyrica) generated $284 million in fourth-quarter 2005 revenue and ... - PR Newswire (press release),

Heart drug to be added to PBS  Dec 6, 2005
From February 1, Inspra - used to treat thousands of Australians with heart disease - would be added to the Pharmaceutical Benefits Scheme (PBS), Health ... - The Age,

Australia puts Pfizer heart drug on benefit scheme  Dec 6, 2005
..."From 1 February 2006, Inspra will be ... Abbott said the listing of Inspra would cost the PBS about A$27 million ($20 million) between 2005/06 and 2009/10. ... - Reuters

Advances in the treatment of heart failure  Nov 8, 2005
Eplerenone (Inspra), first approved by the FDA in 2002 for high blood pressure, is an alternative that seems to cause fewer side effects. ... - ITP.net,

MP govt eyes greater foreign investment  Sep 26, 2005
GEI Hammon, Sonic Biochem, Hotline, Haylid Chemicals, JP Cement and CII-Bhopal chapter chairman, Vipin Mullick (Inspra) - who all would join the CM in Chicago. - Business Standard,

e-Governance kiosks in shambles  Sep 15, 2005
Inspra Solutions, in collaboration with the United Technologies Limited (UTL), took up the project at a cost of Rs.1 crore to provide 61 services of 11 ... - digital opportunity channel,

Heart failure drug advised for PBS  Aug 30, 2005
At the most recent Pharmaceutical Benefits Advisory Committee meeting, the committee recommended eplerenone (Inspra) be listed as an authority-required benefit ... - AustralianDoctor.com (subscription),

Eplerenone shows benefit for patients with damaged hearts  Jul 26, 2005
...attack, one in three deaths among patients with signs of heart failure may be preventable by early treatment with a drug called eplerenone (Inspra, Pfizer Ltd ... - News-Medical.net

Maker of Heart Drug Intended for Blacks Bases Price on Patients' ...  Jul 7, 2005
BiDil would cost only about $3 a day, based on the costs of heart-failure treatments currently on the market: Coreg by Glaxo Smith Kline and Inspra by Pfizer. ... - New York Times <**results**>

PRICES FOR BLACK HEART DRUG HIGHER THAN NORMAL: Amount is nearly ...  11 Jul 2005
BiDil would cost only about $3 a day, based on the costs of heart-failure treatments currently on the market: Coreg by Glaxo Smith Kline and Inspra by Pfizer. ... - Eurweb.com

GSW Worldwide's New York Office Announces New Hires  Jul 1, 2005
Prior to GSW Worldwide, Jay served as group copy supervisor at Euro RSCG Life LM&P, where he worked on accounts including Inspra, Oporia and Berlex Female ... - PharmaLive.com (press release),

Finalists Announced For the Fourth Annual Pharmaceutical ...  May 11, 2005
AND DEVELOPMENT CATEGORY Outstanding Small Molecule Drug Product Award Amgen: Sensipar Genentech Inc.: Tarceva Pfizer, Inc.: Inspra Outstanding Biologic Drug ... - PR Newswire

How Hated Is Pfizer?  Mar 2, 2005
Case in point are Pfizer's recent releases, Inspra and Caduet, which have generated at this point substantially less revenue than anticipated. ... - Motley Fool

Research and Markets: ARBs Continue To Be The Only Class of ...  Feb 15, 2005
Pfizer's growth will be adversely affected by the continuing disappointing performance of recent launches Inspra and Caduet as well as the expiry of patents ... - Business Wire (press release),


Other information


Indication
For improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.

Pharmacology
Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors.

Mechanism Of Action
Eplerenone binds to the mineralocorticoid receptor and thereby blocks the binding of aldosterone (component of the renin-angiotensin-aldosterone-system, or RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms.

Drug Category
Antihypertensive Agents; ATC:C03DA04

Brand Names/Synonyms
Cgp 30083; Eplerenone; Eplerenone [Usan]; Epoxymexrenone; INSPRA; Inspra; SC-66110

Dosage Forms
TABLET (film-coated - 25, 50 mg)

Absorption
The absolute bioavailability of eplerenone is unknown.

Interactions
-->Interactions for Eplerenone:

Inhibitors of CYP3A4-Eplerenone metabolism is predominantly mediated via CYP3A4. A pharmacokinetic study evaluating the administration of a single dose of INSPRA 100 mg with ketoconazole 200 mg BID, a potent inhibitor of the CYP3A4 pathway, showed a 1.7-fold increase in Cmax of eplerenone and a 5.4-fold increase in AUC of eplerenone. INSPRA should not be used with drugs described as strong inhibitors of CYP3A4 in their labeling.

Administration of eplerenone with other CYP3A4 inhibitors (e.g., erythromycin 500 mg BID, verapamil 240 mg QD, saquinavir 1200 mg TID, fluconazole 200 mg QD) resulted in increases in Cmax of eplerenone ranging from 1.4- to 1.6- fold and AUC from 2.0- to 2.9- fold.

ACE Inhibitors and Angiotensin II Receptor Antagonists (Congestive Heart Failure Post-Myocardial Infarction)- In EPHESUS, 3020 (91%) patients receiving INSPRA 25 to 50 mg also received ACE inhibitors or angiotensin II receptor antagonists (ACEI/ARB). Rates of patients with maximum potassium levels >5.5 mEq/L were similar regardless of the use of ACEI/ARB.

ACE Inhibitors and Angiotensin II Receptor Antagonists (Hypertension)- In clinical studies of patients with hypertension, the addition of INSPRA 50 to 100 mg to ACE inhibitors and angiotensin II receptor antagonists increased mean serum potassium slightly (about 0.09-0.13 mEq/L). In a study in diabetics with microalbuminuria INSPRA 200 mg combined with the ACE inhibitor enalapril 10 mg increased the frequency of hyperkalemia (serum potassium >5.5 mEq/L) from 17% on enalapril alone to 38%.

Lithium-A drug interaction study of eplerenone with lithium has not been conducted. Lithium toxicity has been reported in patients receiving lithium concomitantly with diuretics and ACE inhibitors. Serum lithium levels should be monitored frequently if INSPRA is administered concomitantly with lithium.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)-A drug interaction study of eplerenone with an NSAID has not been conducted. The administration of other potassium-sparing antihypertensives with NSAIDs has been shown to reduce the antihypertensive effect in some patients and result in severe hyperkalemia in patients with impaired renal function. Therefore, when INSPRA and NSAIDs are used concomitantly, patients should be observed to determine whether the desired effect on blood pressure is obtained.



Chemical IUPAC Name
Not Available

Chemical Formula
C24H30O6

Half Life
4-6 hours

Drug Type
Approved Drug

# Accession No
APRD00707

CAS Registry Number
107724-20-9

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