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Ertapenem is a carbapenem marketed by Merck as Invanz®. It is structurally very similar to meropenem in that it possess a 1-β-methyl group. more...

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Ertapenem is designed to be effective against Gram negative bacteria. It is not active against MRSA, ampicillin-resistant enterococci, Pseudomonas aeruginosa or Acinetobacter species. Ertapenem also has clinically useful active against anaerobic bactera.

Ertapenem is marketed by Merck as first line treatment for community acquired infections. It should not be used as empirical treatment for hospital-acquired infections because of its lack of activity against Pseudomonas aeruginosa. In practice, it is reserved primarily for use against ESBL-producing and high level AmpC-producing Gram negative bacteria.


Ertapenem is dosed as 1g given by intravenous injection over 30 minutes, or 1g diluted with 3.2ml of 1% lignocaine given intramuscularly. There is no oral preparation of ertapenem available. Ertapenem cannot be mixed with glucose.

The marketing slogan for ertapenem is "The Power of One", because the dose is one gram, once a day.


Unlike imipenem and meropenem, ertapenem is highly protein blound, which explains its long half life (4 hours).

Renal and hepatic dosing

Ertapenem is excreted primarily (80%) by the kidneys. Metabolism by the liver is not clinically important and does not affect dosing.

Patients on haemodialysis should be given ertapenem at least 6 hours before dialysis. If it is given less than six hours before dialysis, then the patient should be given an additional dose of 150mg IV after dialysis. Ideally, patients on haemodialysis should be given ertapenem immediately following dialysis.

Adverse effects

There are few adverse effects of ertapenem. The only absolute contra-indication is a previous anaphylactic reaction to ertapenem or other β-lactam antibiotic. There are no studies done in pregnant women, so the manufacturers cannot comment on its safety in pregnancy. There are no studies in children, and therefore there is no license for use in children aged under 18 years of age.

Use of all antibiotics is associated with increased rates of resistance (although carbapenem resistance is currently rare). There is particular worry that although ertapenem has no clinically useful activity against Pseudomonas aeruginosa, widespread use of ertapenem could still lead to increased carbapenem resistance in Pseudomonas (Livermore 2005).

Like all antibiotics, C. difficile colitis has been associated with its use.


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Merck's Strong Performance in 2000 Driven by Five Key Medicines, Chairman Ray Gilmartin Tells Stockholders
From Business Wire, 4/24/01

Business Editors/Medical Writers


Company's Pharmaceutical Sales Revenue Grew

Fastest in the Industry in 2000

"By any measure, it was a year of outstanding performance," said Merck Chairman, President and CEO Raymond V. Gilmartin at today's annual meeting of stockholders. "Our key growth drivers now account for more than 60 percent of Merck's pharmaceutical sales and demonstrate our ability to effectively communicate the benefits of our excellent research discoveries in a highly competitive marketplace. When combined, sales of our key growth drivers increased by more than 40 percent in 2000."

At the meeting, Mr. Gilmartin presented an overview of Merck's results in 2000, which included solid growth in sales, income and earnings, as well as continued advances and expansion in research and production. He expressed confidence in Merck's ability to achieve its growth objectives based on the excellence of Merck's internal scientific organization and the strength of its external partnerships. "In the last six years, we have introduced 16 new medicines, we have several research programs in late-stage development and more new medicines moving through our pipeline than ever before in our history," Mr. Gilmartin said.

Merck's overall global business success translated into positive results in 2000. Last year, earnings per share increased 18 percent over 1999 to $2.90 per share. Sales rose by 23 percent to $40 billion. Net income was up 16 percent to $6.8 billion.

And the company's financial success continues. As Merck reported April 20, first quarter sales for 2001 were $11.3 billion, up 28 percent over first quarter 2000. Net income increased 11 percent to nearly $1.7 billion. And earnings per share were up 13 percent, to $0.71.

At the annual meeting, Mr. Gilmartin reiterated that Merck remains comfortable with full-year 2001 First Call range of earnings per share analyst estimates of $3.15 to $3.25.

Five Key Medicines Account for More Than 60 Percent of Pharmaceutical Sales

Merck's five key growth drivers were major contributors to the 2000 results. VIOXX, a once-a-day medicine, is the only COX-2 selective agent indicated in the United States for both osteoarthritis and acute pain. VIOXX has become the world's fastest-growing branded prescription arthritis medicine, and it is already Merck's second largest-selling medicine. VIOXX achieved $2.2 billion in sales for 2000. During the quarter, Merck submitted regulatory filings for VIOXX for the treatment of adult rheumatoid arthritis.

ZOCOR, Merck's cholesterol-modifying medicine, grew 17 percent and achieved sales of nearly $5.3 billion in 2000, despite strong competition. Physicians continue to prescribe ZOCOR in large part because of the medicine's demonstrated ability to act favorably on all three key lipid parameters - LDL (bad cholesterol), HDL (good cholesterol) and triglycerides - in patients with elevated LDL.

COZAAR and HYZAAR grew 24 percent in 2000 and maintained strong leadership in a class of highly effective and well-tolerated high blood pressure medicines called angiotensin II antagonists. Sales for the two products were $1.7 billion in 2000. Despite an intensely competitive market, physicians continue to show confidence in these products, prescribing them for more than 10 million patients worldwide.

FOSAMAX, the leading product worldwide for the treatment and prevention of postmenopausal osteoporosis, continues to outperform the competition because it is the only osteoporosis medicine indicated and consistently proven to reduce the incidence of osteoporotic fractures of the hip as well as the spine. FOSAMAX grew 22 percent and achieved sales totaling nearly $1.3 billion in 2000.

Merck's recent introduction of FOSAMAX Once Weekly, the first and only oral once-weekly treatment for osteoporosis, continues to bolster the competitive position of FOSAMAX. In the United States, FOSAMAX Once Weekly has become the No. 1 new prescription medicine for osteoporosis. Regulatory approvals for FOSAMAX Once Weekly continue in all parts of the world. So far, the medicine has received regulatory approval in more than 35 countries and has been launched in 20 countries. In addition, earlier this month, 15 European Union countries received medical approval of FOSAMAX Once Weekly. In January, the FDA granted approval for FOSAMAX Once Weekly to be considered by physicians as an alternative to once-daily treatment for increasing bone mass in men with osteoporosis.

SINGULAIR, Merck's once-a-day leukotriene-antagonist, is the world's fastest-growing asthma medicine. SINGULAIR grew 72 percent and achieved sales totaling $860 million in 2000. After only three years on the market, SINGULAIR has become the No. 1 asthma controller in terms of total prescription sales on a weekly basis in the United States. SINGULAIR is the first asthma controller therapy in more than 15 years to be approved for children as young as 2. Other benefits include that it is a once-a-day tablet rather than an inhaled medication and that it is not a steroid.

In January, the FDA approved CANCIDAS as the first in a new class of antifungal medications introduced in more than a decade. Merck launched this new medicine in February. CANCIDAS will be used to treat certain life-threatening fungal infections that are becoming more prevalent as the number of people with compromised immune systems is increasing. The new medicine is indicated for the treatment of invasive aspergillosis in patients who do not respond to or cannot tolerate other antifungal therapies, such as amphotericin B, lipid formulations of amphotericin B and/or itraconazole. CANCIDAS has not been studied as an initial therapy for invasive aspergillosis. Merck is studying CANCIDAS as a potential treatment for the fungal infection Candida.

Merck-Medco Drives Innovation Through Web Technology

Merck-Medco continued its strong contribution to Merck's revenue growth in 2000. For the year, the volume of prescriptions handled increased 22 percent to 452 million and drug spend increased 32 percent to more than $20 billion. By far the world's largest pharmacy, now processes more than 120,000 prescriptions per week and is growing 30 percent per quarter.

Merck-Medco grew significantly in 2000 with the incorporation of 10 million new members under the UnitedHealthcare contract, and through the acquisition of ProVantage Health Services, with 5 million new members.

A View From Merck Research Laboratories

Edward M. Scolnick, M.D., executive vice president, Science and Technology, and president, Merck Research Laboratories (MRL), and Peter Kim, Ph.D., executive vice president, MRL, reviewed Merck's internal scientific work and research pipeline, highlighting key investigational products in development. Key research initiatives were:

Proof of principle has been confirmed in the company's substance P antagonist program for depression, and Dr. Scolnick announced that plans are under way for expanded clinical studies in 2001.

Last year, Merck invested $2.3 billion in research and development. This year, the company expects to spend $2.8 billion. In addition, the company has extensive research collaborations with universities, institutes and companies throughout the world.

Commitment to Global Health

According to Mr. Gilmartin, "Our mission as a company to improve global health cannot be fully accomplished unless we have done all we can to make sure that people around the world who need our medicines can get our medicines."

To demonstrate Merck's commitment to access in the United States, he outlined Merck's support of legislation to add prescription drug coverage to Medicare and the launch of two important programs through Merck-Medco to address the rising costs of prescription drugs. The first, YOURx PLAN, provides access to affordable prescription drugs for Americans who lack adequate insurance and helps them better manage their health and medical costs. The other program is a unique national generic drug education and sampling campaign known as Generics First, where Merck-Medco pharmacists call on physicians to provide information about the appropriate use of generics and materials to order generic samples.

As an example of Merck's commitment to access outside the United States, Mr. Gilmartin highlighted the Company's recent announcement to sell its two HIV/AIDS medicines - CRIXIVAN and STOCRIN - at no profit to developing countries.

Mr. Gilmartin pointed out that in addition to these humanitarian efforts, Merck will "continue to do what we do best: to search for and develop breakthrough medicines and vaccines. Our ultimate contribution in the global fight against HIV/AIDS would be a safe and effective vaccine."

Merck & Co., Inc. is a leading, research-driven pharmaceutical products and services company. Merck discovers, develops, manufactures and markets a broad range of innovative products to improve human and animal health, directly and through its joint ventures. Merck-Medco manages pharmacy benefits for employees, insurers and other plan sponsors, encouraging the appropriate use of medicines and providing disease management programs. Through these complementary capabilities, Merck works to improve the quality of life and contain overall health care costs.

This press release contains "forward-looking statements" as that term is defined in the Private Securities Litigation Reform Act of 1995. No forward-looking statement can be guaranteed, and actual results may differ materially from those projected. We undertake no obligation to publicly update any forward-looking statement, whether as a result of new information, future events, or otherwise. Forward-looking statements in this document should be evaluated together with the many uncertainties that affect our businesses, particularly those mentioned in the cautionary statements in Item 1 of our Form 10-K for the year ended Dec. 31, 2000, and in our periodic reports on Form 10-Q and Form 8-K (if any) which we incorporate by reference.

COPYRIGHT 2001 Business Wire
COPYRIGHT 2001 Gale Group

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