Cabergoline (brand names Dostinex® and Cabaser®), an ergot-derivative, is a potent dopamine receptor agonist on D2-Receptors. It also acts on dopamine-receptors in lactophilic hypothalamus cells and causes thereby a suppression of the prolactin-production in pituitary gland.

Pharmacokinetics

Following an oral single dose the drug is resorbed within 0.5 to 4 hours from the GI-Tract with considerable interindividual differences. Meals do not alter the absorption characteristic. Human bioavailibility was not determined, because the drug is intended for oral use only. In mice and rats the absolute bioavailability was 30 and 63%, respectively. Cabergoline is rapidly and to a great extend metabolized in the liver and excreted in bile and far less in urine. All metabolites are less active than the parental drug or inactive. The human elimination halflife is estimated to be 63 to 68 hours in patients with M. Parkinson and 79 to 115 hours in patients with pituitary tumors.

Carcinogenity

In rodents a dose dependent increase in malignant tumors has been found. They are thought to be species-specific. No clinical data exists on carcinogenity in humans.

Uses

Monotherapy of Morbus Parkinson in the early phase.
Combination therapy of Morbus Parkinson in the progressive phase together with levodopa and a decarboxylase-inhibitor like carbidopa.
Adjunctive therapy of prolactin-producing tumors of the pituitary gland (microprolactinomes).
In some countries also : ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, und galactorrhea).

Off-Label/Recreational Uses

It has at times been used as an adjunct to SSRI antidepressants as there is some evidence that it counteracts certain side effects of those drugs such as reduced libido and anorgasmia. It also has been suggested online that it has a possible recreational use in reducing or eliminating the male refractory period.

Contraindications and Precautions

Hypersensitivity to ergot-derivatives
Pediatric Patients (no clinical experience)
Severely impaired liver function or cholestasis
Comedication with drugs metabolized mainly by CYP P450 such as erythromycin and ketoconazole, because increased plasma levels of cabergoline may result.
Cautions : severe cardiovascular disease, Raynaud's Syndrome, gastroduodenal ulcers, active gastrointestinal bleeding, hypotension.

Pregnancy and Lactation

Pregnancy : Approximately 100 female patients became pregnant under therapy with cabergoline for hyperprolactinemic conditions. The incidence of spontanous aborts and congenital abnormalities was comparable to nontreated patients. Nonetheless womem, wishing to become pregnant, should wait a safety period of 4 weeks after discontinuation of cabergoline. Patients becoming pregant under therapy should terminate cabergoline immediately, if possible.
Lactation : In rats cabergoline was found in the maternal milk. Since it is not known, if this effect is also seen in humans, lactating women should not be treated.

Read more at Wikipedia.org

• [List your site here Free!]

Paladin Reports 2005 Second Quarter Results-Paladin Increases 2005 Revenue Guidance
From Business Wire, 7/28/05

MONTREAL -- Paladin Labs Inc. (TSX:PLB), a leading Canadian specialty pharmaceutical company, today reported its financial results for the three and six-month periods ended June 30, 2005.The Company also announced increased revenue guidance for fiscal 2005 as a result of stronger then expected sales with key promoted brands.

"Paladin achieved record-breaking prescription volumes in the quarter on all four of our key promoted brands, including Dostinex(R), Estring(R), Oxytrol(R) and Plan B(R).This strong performance in our business coupled with our strategic direction to internally develop new, late-stage innovative products is positioning Paladin for accelerated growth in the future.I look forward to providing an update to you as Paladin continues its search for innovative, promotion-sensitive brands to bring to Canada," said Jonathan Ross Goodman, President & CEO of Paladin Labs.

Financial Results

Revenue for the second quarter ended June 30, 2005 increased 23% to $7.9 million, compared to $6.4 million in the second quarter of 2004.Revenue for the six months ended June 30, 2005 increased 20% to $14.4 million, compared to $12.0 million in the first six months of 2004.Revenue from the Company's key promoted brands including, Dostinex(R), Estring(R), Oxytrol(R) and Plan B(R) increased by 50% in the first six months of 2005 compared to the same period a year ago and 60% in the second quarter of 2005 compared to the second quarter last year.

Paladin's earnings before interest, taxes, depreciation, and amortization (EBITDA(i)) remained healthy at $2.0 million for both the second quarter of 2005 and the second quarter of 2004.For the first half of 2005, Paladin's EBITDA increased 18% to $3.9 million, compared to EBITDA of $3.3 million in the first six months of 2004.

Net income for the second quarter was $585,000 or $0.04 per fully diluted share, compared to net income of $681,000 or $0.05 per fully diluted share in the second quarter a year ago.Net income remained steady at $0.07 per fully diluted share for both the six months ended June 30, 2005 and June 30, 2004.

Gross profit, as a percentage of revenues, for the second quarter and six months ended June 30, 2005 totalled 73% and 74% respectively, compared to 74% and 75% for both the second quarter and six months ended June 30, 2004, respectively.

Selling and marketing expense for the second quarter of 2005 increased to $3.1 million from $1.8 million in the second quarter of 2004.Selling and marketing expense for the first six months of 2005 increased to $5.2 million from $3.2 million in the first six months of 2004.This increase was primarily attributable to increased promotion activities associated with the launch of Oxytrol(R) and the re-launch of Plan B(R) as a non-prescription product.

At June 30, 2005, Paladin's cash, cash equivalents and investments in marketable securities totalled $44.0 million.From this strong cash position, Paladin continues to pursue product acquisition opportunities.

Product Developments

Paladin announced that Plan B(R), a safe and effective "morning-after pill," is now available at Canadian pharmacies without a prescription.The decision by Health Canada is supported by 70 percent of Canadians and every leading medical organization in the country.Plan B(R) is 95 percent effective in preventing unintended pregnancy if taken within 24 hours of unprotected sex."There has been a tremendous response in sales to our strong media plan of Plan B(R) since Health Canada's decision.Sales have increased 37% in the second quarter of 2005 compared to the first quarter of 2005 and 60% compared to the second quarter of 2004," said Mark Beaudet, Vice-President of Marketing and Sales of Paladin Labs.

The Company signed an exclusive Canadian marketing and supply agreement for Trelstar(R) with Watson Pharmaceuticals, Inc. Trelstar(R) is an injectable, luteinizing hormone-releasing hormone (LHRH) agonist indicated for the palliative treatment of advanced prostate cancer and for the treatment of endometriosis and is approved for sale in Canada.Paladin expects to launch Trelstar(R) in the first quarter of 2006.According to IMS Canada, the Canadian market for LHRH agonists for prostate cancer and endometriosis was over $125 million in 2004.Trelstar(R) compliments our established urology franchise with Oxytrol(R) and Vantas(TM) (Histrelin Hydrogel Implant), a unique, once-yearly LHRH agonist implant for the treatment of prostate cancer.

Paladin received a Notice of Non Compliance on June 16, 2005 by the Therapeutic Products Directorate (TPD) of Health Canada that it's New Drug Submission (NDS) for Vantas(TM) (Histrelin Hydrogel Implant) would not be approved at this time.The Company will submit a response to Health Canada's issues by September 15, 2005 and expects to obtain regulatory approval for Vantas(TM) during the first half of 2006.

Subsequent to the second quarter, the Company entered into a Canadian marketing and supply agreement with Verus Pharmaceuticals, Inc., to market Twinject(TM) (epinephrine).Twinject(TM) is a novel epinephrine auto-injector indicated for the emergency treatment of severe allergic reactions (anaphylaxis).Twinject(TM) comes in two dosages for self-administration - a 0.3 mg used for adults and a 0.15 mg used for children.According to IMS Canada, the anaphylaxis market was $25 million in 2004 and grew at a compounded annual growth rate of 22% since 2001.

Corporate Developments

Paladin announced that it has received regulatory approval from the Toronto Stock Exchange to carry out a normal course issuer bid effective February 22, 2005.Paladin has been authorized to purchase up to 630,000 of its common shares, or approximately 10% of its public float of 6,300,990 common shares, in the twelve-month period following the bid's effective date.To date, Paladin has purchased 107,500 shares for a total amount of $482,000.

2005 Revenue Guidance

Paladin is revising upwards its previously announced revenue guidance for fiscal 2005 from $25 million to $26 million generated in revenues to $29 million to $30 million generated in revenues, due to better than expected performance of its key promoted products.This forecast excludes the impact of acquisitions and/or new product launches that may be made by the Company between now and the end of 2005.

(i) EBITDA does not have any standardized meaning prescribed by generally accepted accounting principles (GAAP) and therefore may not be comparable to similar measures presented by other public issuers. EBITDA performance and guidance is presented herein because Paladin management believes that, in addition to net income, EBITDA is a useful supplemental measure of the Company's performance.

Conference Call Notice

Paladin will host a conference call to discuss its second quarter results on Thursday, July 28, 2005, at 10:00 a.m. EST.The dial-in number for the conference call is 1-888-509-0081 or 416-695-5275. The call will be audio-cast live and archived for 90 days at www.paladinlabs.com.

About Paladin Labs

Paladin Labs Inc., headquartered in Montreal, Canada, is a specialty pharmaceutical company focused on acquiring or in-licensing innovative pharmaceutical products for the Canadian market.With this strategy, a focused national sales team and proven marketing expertise, Paladin has evolved into one of Canada's leading specialty pharmaceutical companies.Paladin's shares trade on the Toronto Stock Exchange under the symbol PLB.For more information about Paladin, please visit the Company's web site at www.paladinlabs.com.

This news release may contain forward-looking statements or predictions.These statements represent our judgement as of this date and are subject to risks and uncertainties that could cause actual results or events to differ materially from those expressed in such forward-looking statements.Potential risks and uncertainties include, without limitation, those associated with product development, clinical trials, future revenues and profitability, and obtaining marketing approval and other factors.For additional information on risks and uncertainties related to the forward-looking statements, investors should consult the Company's ongoing quarterly filings, annual reports and Annual Information Form and other filings found on SEDAR at www.sedar.com.

PALADIN LABS INC. (TSX:PLB)

Return to Dostinex

Home

Contact

Resources

Exchange Links

ebay