Saturday, November 1, 2014

ALKS-5461: A Novel Antidepressant

Opiates have long been known to alleviate anxiety and depression with one small caveat:  the risk of life-ruining addiction.  One theory of depression is that it's caused by a dysfunctional endorphin system.  Now that theory is being put to good use.  Enter ALKS-5461, the latest antidepressant in the pipeline.  ALKS-5461 contains buprenorphine--a component of the addiction drug Suboxone--and samidorphan, an opioid blocker.

Buprenorphine stimulates the mu opioid receptor--you know, the one that produces insane euphoria and drug-seeking behavior--while blocking the kappa receptor.  Drugs that agonize the kappa opioid receptor like salvia are known to trigger dysphoria and feelings of intense fear, so it makes sense that blocking this nasty receptor would alleviate those feelings for some people.  Meanwhile, samidorphan blocks buprenorphine's effect on the mu receptor, thus removing its addictive potential.

The drug was so effective in clinical trials that it was granted fast-track designation by the FDA.  Despite its potential, ALKS-5461 is not a cure and could carry side effects of its own.  It is intended as a second-line (or third-line) treatment for patients whose depression is not helped by mainstream medications.  And if you're looking for a cheap high, look elsewhere.  This is not a "fun" drug by a long shot.  However, those of us with treatment-resistant depression should rejoice at the possibility of a new treatment option on the horizon.

ALKS-5461 is expected to hit the market in 2016.         


  1. Hi, stumbled upon this site while searching up for information on ALKS-5461. Doesn't seem like there's much being written about it but I was just curious on your thoughts about the kappa-opioid receptor theory. Do you think ALKS-5461 is promising enough or do you feel like it's gonna be another one of those drugs that these big pharma companies are just saying to build up hype but not really do anything?

    As someone who's suffering from depression, this is one of the drug I have a good interest in. Wondering if you had any more information on it.

  2. I recently read that Alkermes stock was down-graded from hold to sell (March 2015). I thought this rather suspect in light of the new miracle antidepressant they have in the pipeline.

  3. Stop & Prevent Opiate Withdrawal

  4. I agree that opiate is helpful in alleviating anxiety and depression but in my case I had got addiction for this drug which made my life even hard so I had to join the suboxone treatment virginia beach center where I got proper treatment.