New Experimental Opioid Makes Some Awfully Big Promises

Will Nektar Therapeutics' experimental non-euphoric painkiller really quell addiction?

For many, getting hooked on opioids starts innocently enough. Typically, it’s a way to find relief from chronic pain. But the feeling of euphoria – or “high” – that accompanies each dose is ultimately what keeps users coming back for more, eventually leading to abuse and addiction.

But what if those euphoric effects were taken away from the whole painkiller experience – would Americans stop abusing them or becoming addicted to opiates altogether?

Nektar Therapeutics is delving into this possibility, with its new experimental opioid designed to achieve pain relief without the euphoria – a feat reportedly achieved in a key late-stage study.

A Breakthrough or Just Another Opiate?

The drug – tentatively known as NKTR-181 – is as effective as existing long-acting opioids, according to Chief Scientific Officer Dr. Stephen Doberstein, yet has one key difference: it’s designed to reach the brain slower. This plays a big part in deterring substance abuse, says Doberstein, especially since science suggests the euphoric effect of opioids is influenced by their rate of entry into the brain.

Basically, “the faster the drug enters the brain – across the blood-brain barrier – the more dopamine is released,” Doberstein said. Which explains why drugs, such as cocaine and nicotine, are so addictive.

NKTR-181 recently underwent various testing, with successful results. In one “human abuse liability” study, Doberstein reported that subjects – those who were familiar with the “high” feeling opioids produce – found the experimental opioid was “virtually indistinguishable” from a placebo, as far as euphoric effects were concerned. In another study, the experimental opioid showed its effectiveness in achieving pain relief, when it outperformed a placebo in over 600 patients with chronic lower back pain. In all tests, NKTR-181’s effects were the same, whether it was snorted or injected.

What’s the Bottom Line?

Though NKTR-181 isn’t yet approved by the U.S. Food and Drug Administration (FDA), the company plans to discuss its next steps with the agency in the near future. They’re also looking for a partner to sell the drug, if and when it’s approved. Nektar Therapeutics hopes to secure a Schedule III classification for NKTR-181 under the Controlled Substances Act, one category lower – and safer – than most opioids, which are classified as Schedule II drugs.

Could altering the chemical makeup of opioids themselves be an effective means for tackling the opioid epidemic? We likely won’t know the answer to that question for several years, but there seems to be an equal number of skeptics and supporters. One thing’s for sure, though: We need all the help we can get to beat this deadly epidemic ravaging our country.

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