Alkermes Talks ALKS 9070
Jan12

Alkermes Talks ALKS 9070

Yesterday I sat down with Alkermes CEO Richard Pops to learn about the science behind ALKS 9070, the first drug to come out of its LinkeRx drug delivery technology. ALKS9070 is a long-acting version of aripiprazole, the active ingredient in Bristol-Myers Squibb’s anti-psychotic Abilify. Alkermes already has a wealth of experience designing a long-acting antipsychotic through its work developing Risperdal Consta. But instead of using the same microsphere technology used to deliver Risperdal over time, Alkermes challenged itself to make a “virtual” microsphere, Pops says. The goal was to make a prodrug by finding a linkage site on aripiprazole that could accommodate a fatty acid tail. The drug could then be injected into the muscle, where it would stay. For chemists working on prodrugs, the approach likely sounds, well, backwards. Normally, scientists work hard to take a molecule with poor bioavailability, and design a prodrug that can be swallowed and then metabolized (often in the gut) into the active drug. In the case of ALKS 9070, Alkermes was taking a pill and turning it into a prodrug that would be injected. The good news is, the strategy means “there’s some open space from an IP point of view,” Pops says. The company has yet to unveil details of the linker chemistry behind its prodrug of aripiprazole, but so far it appears to work in animal models, where a once-monthly injection has proven feasible. The beauty of the compound, Pops adds, is that the efficacy of the anti-psychotic is already established. “We don’t have to ask if aripiprazole works,” he adds. “The first clinical trial we do is meaningful." If patients injected with ALKS 9070 show the appropriate concentrations of the prodrug and Abilify in the right places, the company should be able to move right into Phase III trials. Pops adds that the company is so committed to the approach that a backup compound is waiting in the wings. Alkermes started a Phase I trial of ALKS 9070 in November, and expected to see results from the study in the first half of this year. If commercialized, ALKS 9070 would enter an enormous market: Abilify brought in $2.6 billion in sales in 2009. And if the success of Risperdal Consta is any indication--the long-acting version represented nearly two-thirds of sales of the Risperdal franchise in 2009--the potential for market penetration is high. Stay tuned for those Phase I...

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Obesity Musings On Alkermes, J&J News
May25

Obesity Musings On Alkermes, J&J News

I am always on the lookout for news in the obesity drug area. But lately two of the molecular components of experimental obesity drugs in late-stage clinical trials-naltrexone and topiramate- are in the news for other reasons. Alkermes announced this morning that it will receive priority review from FDA for VIVITROL, an injectable extended-release formulation of naltrexone, for treating opioid-dependent patients, with a PDUFA date of October 12, 2010. The idea is that a once-monthly injection of VIVITROL would be given to lower cravings in people with a dependence on opioids such as heroin, Vicodin, or Oxycontin. VIVITROL is already approved for treating alcohol dependence. It's Alkermes's formulation that's new. Naltrexone as a chemical entity has been around for some time. DuPont originally marketed it as Trexan in 1984 but that form is now off-patent, as C&EN's Ann Thayer wrote back in 2006. I also promised that there was an obesity connection here, and indeed there is. Naltrexone is one of the two components in Orexigen's experimental obesity medication, Contrave, as I explained last year. Orexigen has developed its own proprietary sustained-release formulation of naltrexone and the experimental drug's other active ingredient-bupropion, an antidepressant and smoking-cessation aid that boosts dopamine signaling. Ortho-McNeil Pharmaceutical, a subsidiary of Johnson & Johnson, has agreed to pay $81 million (that's $6.1 million in criminal fines and $75.37 million from civil suits) for promoting its epilepsy medication Topamax for several uses not approved by FDA. This story has been in the news for nearly a month now (see Pharmalot's entry about it here) but the company pled guilty to the illegal marketing just last Friday, placing this item back at the top of my Google News list. One of the off-label indications J&J was promoting turns out to be obesity, according to the whistleblower who brought the case. Read the legal documents here [pdf format]. Thanks to Jim Edwards at BNET for posting these. Topiramate (the active ingredient in Topamax) is one of the two active ingredients in Vivus's experimental obesity drug Qnexa. But Vivus's formulation uses topiramate at a much lower dose than would be taken as a standalone...

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