Blockbusters Coming Off Patent in 2012

This page describes just a few of the drugs facing patent expiration in 2012. For an explanation of the contents of this catalog, finding other years or products, copyright information, and more, go to the Catalog Index.

Avandia (rosiglitazone maleate)

Avandia is GSK's thiazolidinedione antidiabetic agent indicated for improved glycemic control in adults with type 2 diabetes. Glaxo harbored hopes for rosiglitazone maleate as an Alzheimer's therapy, but clinical trials have not supported this conclusion. Off-label, it has been used for polycystic ovary syndrome, psoriasis, and thyroid cancer. Recently, it is best known for the black box warning added to the product labeling, warning prescribers of increased congestive heart failure and myocardial ischemia found in a meta-analysis of 42 clinical studies – a risk lawsuits claim GSK knew of but did not address.

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Diovan (valsartan)

A top-selling angiotensin blocking agent, Diovan is estimated to bring Novartis over $3 billion each year. Even though in 2004 Novartis received a Warning Letter alleging the company had promoted off-label use, literature reports of off-label prescribing abound: diabetes, migraines, as a beta-amyloid blocker in Alzehiemer's patients, protecting kidneys from diabetes damage, and many others. Generally considered to have a fairly mild adverse event profile, a search of clinical trials underway shows ongoing and completed trials for the use of valsartan in combination with other, already approved, drugs; two of these combinations are on the market. A clinical trial for children from 6 months – 5 years is still enrolling, raising the question of whether additional pediatric market exclusivity is under consideration.

Lexapro (escitalopram oxalate)

Forest Lab's biggest product, Lexapro, currently accounts for approximately 59% of company sales – leaving a huge opportunity for generic firms and a problem for Forest when the patent expires in early 2012. The revenue from the anti-depressant’s product has already seen a decrease as similar products from other companies have come off patent and patients have switched to a cheaper alternative – so the company is actively looking to license other drugs. In the interim, a little cushion may be provided by a recent price increase.

Singulair (montelukast sodium)

With $4.3 billion in 2008 sales of its top medication, Singulair, it's no wonder there has been generic interest in attacking Merck's patent, scheduled to expire in August 2012. In August, 2009, Teva Pharmaceutical Industries was turned down in its court argument that the patent was invalid; on January 7, 2010 Teva withdrew its appeals court challenge. The patent covers montelukast, the main ingredient in Singulair. The drug was approved in 1998 by FDA as an effective leukotriene-blocker, which helps asthmatics block compounds that cause muscle contractions and secretions in the lungs.

Viagra (sildenafil citrate)

The little blue pill that brought us the phrase “Erectile Dysfunction” loses patent protection in March 2012. Pfizer has enjoyed the period since the original FDA approval in 1998 and has raised the price of Viagra between 5% and 11% each year; it is now $14 per pill at wholesale. There have been no serious patent challenges in the U.S., but generic houses may be considering it – with one month’s sales worth $158 million, being able to enter the market even a few months early could be worthwhile, though Pfizer would undoubtedly aggressively defend its patent term. Clinical trials underway show Pfizer investigating additional indications and dosage forms for sildenafil citrate.

Geodon (ziprasidone HCl)

In 2001, Geodon was FDA-approved to treat patients ages 18-65 diagnosed with schizophrenia or acute manic or mixed episodes associated with bipolar disorder. An enthusiastic marketing campaign brought 2008 sales near the $1 billion mark. However, according to a whistleblower suit unsealed in September 2009, Pfizer illegally promoted the sale and use of their ziprasidone for a variety of off-label conditions, including depression, bipolar maintenance, mood disorder, anxiety, aggression, dementia, attention deficit hyperactivity disorder, obsessive compulsive disorder, autism, posttraumatic stress disorder, and for pediatric, adolescent and geriatric patients.

Detrol (tolterodine)

Pfizer's product Detrol, the world's most-prescribed product for overactive bladder, contributes about $1 billion annually to company sales. It has been a target for patent challenges; Teva Pharmaceuticals USA Inc. is appealing its February 17, 2010 loss to Pfizer Inc. in a patent infringement suit over Detrol, taking issue with a federal judge's ruling that Teva failed to show Pfizer's patent for the bladder control drug was invalid and not enforceable.

Evista (raloxifene HCl)

Lilly's Evista is a selective estrogen receptor modulator or SERM (classified by FDA as an estrogen agonist/antagonist), and was originally approved for the prevention and treatment of osteoporosis in postmenopausal women. It has since been approved to reduce the risk of invasive breast cancer in two populations: postmenopausal women with osteoporosis and postmenopausal women at high risk for invasive breast cancer. With the extensive market for these conditions, it is unsurprising that Lilly has faced patent challenges from several organizations, including Teva, Ariad Pharmaceuticals, Barr, Harvard and MIT.

Lovenox (enoxaparin sodium)

Sanofi-Aventis' exnosaparin sodium patent is scheduled to expire in 2012, but generic firms Novartis, Teva, and Watson are all looking to launch their own versions of the anti-clotting medication soon. Why? In January 2010, Sanofi claimed Lovenox is a complex biological drug, and is confident that the usual generic substitution rules will not apply – that each version will have to be evaluated on its own merits. FDA is examining the issues inherent in biogenerics, but lots of sticking points remain.

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Zometa (zoledronic acid)

Zometa, a biphosphonate, is used in treating cancer patients with bone metastases and used together with other drugs to treat multiple myeloma and to prevent bone fractures and reduce bone pain. Off-label, it has been cited for use in Paget’s disease, prevention of postmenopausal osteoporosis and prevention of breast cancer. Novartis has successfully defended zoledronic acid against patent challenges, but in February of 2010 Amgen revealed data that their product Prolia is superior in preventing bone metastases. The Prolia patent does not expire until 2013, and its longer remaining patent term and good efficacy data indicate Zometa is probably past patent challenge danger.


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