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 First Quarter Financial Results
From Business Wire, 5/5/05

MONTREAL -- Paladin Labs Inc. (TSX:PLB), a leading Canadian specialty pharmaceutical company, today reported its 2005 first quarter financial results.

"We remain focused on pursuing additional acquisition opportunities to bring innovative, promotion-sensitive brands to the Canadian market, while continuing to grow sales of our existing products.I am pleased to report that our business is healthy and we continue on track with our strategic direction of focusing on internally developing new, late-stage innovative products.This plan will position Paladin to accelerate the organization for long term growth," said Jonathan Ross Goodman, President & CEO of Paladin.

Financial Results

Revenue for the three-month period ended March 31, 2005 increased 16% to $6.5 million compared to $5.6 million in the first quarter of 2004.Revenue growth resulted primarily from a 37% increase in sales of the Company's key promoted brands, including Dostinex(R), Estring(R), Oxytrol(R) and Plan B(R), compared to the same period a year ago.

Paladin's 2005 first quarter earnings before interest, taxes, depreciation, and amortization (EBITDAv) increased 44% to $1.88 million compared to EBITDAv of $1.31 million in the first quarter of 2004.

Net income for the quarter was $499,000 or $0.03 per fully diluted share compared to net income of $344,000 or $0.02 per fully diluted share in the first quarter a year ago.

Selling and marketing expense for the first quarter of 2005 increased 48% to $2.1 million from $1.4 million in the first quarter of 2004.This increase was primarily attributable to increased sales and marketing spending associated with the launch of Oxytrol(R) and the re-launch of Plan B(R) as a non-prescription product.

Research and development expense for the first quarter of 2005 decreased to $331,000 from $1.2 million in the first quarter a year ago.Paladin's Scientific Affairs team is focusing on investigating product opportunities for internal development.

Amortization expense for the first quarter of 2005 increased to $1.1 million from $791,000 in the first quarter of 2004.This increase in amortization expense is a result of the Company's decision to reduce the estimated useful life of the carrying value of the intellectual property associated with products that face a heightened risk of generic competition.

At March 31, 2005 Paladin's cash, cash equivalents and investments in marketable securities totalled $43.6 million.From this strong cash position, Paladin continues to pursue product acquisition and development opportunities.

Product Developments

During the first quarter, The Conseil du medicament of Quebec, which provides drug insurance coverage for an estimated 3.2 million residents of Quebec, gave its approval to list Oxytrol(R) (oxybutynin transdermal system).Oxytrol(R), a unique patch medication, is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.According to the Canadian Continence Foundation, approximately 1.5 million Canadians suffer from overactive bladder and according to IMS Canada, the total Canadian market for overactive bladder in 2004 was $50 million.

Subsequent to the first quarter, 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.

Subsequent to the first quarter, Paladin 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 fourth quarter of 2005.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 implant for the treatment of prostate cancer.

Subsequent to the first quarter, Tapazole(R), a leading anti-thyroid drug which Paladin acquired from Eli Lilly and Company in 2000 was genericized.Paladin has increased sales of Tapazole(R) 130% since its acquisition in 2000 from $780,000 to $1.8 million in 2004 according to IMS Canada.Tapazole(R) remains a successful acquisition for Paladin, having generated net operating cash flows of $2.9 million to date.

Corporate Developments

Dr. Patrice Larose was appointed to Paladin's management team as Vice-President, Regulatory Affairs, Drug Safety and Medical Services. Before joining Paladin, Dr. Larose was Vice-President, Regulatory Affairs, Drug Safety and Medical Services at Schering Canada Inc. Dr. Larose obtained a Ph.D. in Pharmaceutical Sciences from the University of Montreal in 1987 and is a licensed pharmacist.

During the quarter, 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 not purchased shares.

2005 Financial Outlook and Strategic Update

Paladin reiterates its previously announced financial outlook for fiscal 2005, as it expects to generate $25 million to $26 million in revenue.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.

During the quarter, the Company held its first investor conference to discuss the Company's year-end financial results, strategic direction and 2005 revenue guidance.Paladin announced its plan to increase internal development of innovative new drugs.

Conference Call Notice

Paladin will host a conference call to discuss its first quarter results on Thursday, May 5, 2005, at 10:00 a.m. EST.The dial-in number for the conference call is 1-888-789-0150 or 416-695-6120. The call will be audio-cast live and archived for 90 days at www.paladinlabs.com.

(1) 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 is presented herein because Paladin management believes that, in addition to net income, EBITDA is a useful supplemental measure of the Company's financial performance.

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 Website 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