November 19, 2012 7:47 pm

The quest for opioids less vulnerable to abuse

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Drugs tweaked to foil those seeking highs

Drug companies may be finding it difficult to develop effective new classes of painkiller – but they are investing heavily in minor modifications to existing blockbuster medicines derived from synthetic opioids.

Since the start of the modern pharmaceutical industry in the late 19th century, developers have been reformulating versions of opium to make them less vulnerable to abuse. They were led by Germany’s Bayer, which originally marketed heroin as a less addictive alternative to morphine.

In the mid-1990s, US-based Purdue Pharma launched OxyContin, an orally administered form of morphine developed in response to a request from a London hospice. The product generated sales of up to $3bn a year, creating a fortune for owner-turned-philanthropist Mortimer Sackler.

Peter Williamson, an analyst with market research agency Visiongain, estimates that the global market for narcotic pain relief drugs led by OxyContin is nearly $7bn and will rise to $10bn in the coming decade.

The level of abuse and misuse is worrying policy makers. Michael Jackson, the pop star, was just one of many high-profile users to become addicted to a product taken by millions. Of equal concern – especially in the US, which accounts for 70 per cent of sales – is abuse by, for example, teenage children of parents for whom the drug is prescribed.

Purdue has since launched a series of tweaked versions, designed both to extend OxyContin’s dominance of the market and to respond to ever tougher regulatory requirements designed to prevent misuse and tightly control production. That includes an extended-release version, a patch to deliver the drug through the skin and another variant placed under the tongue.

Purdue and its rivals have also produced related treatments to manage the corollary of opioid dependency, such as Reckitt Benckiser’s Suboxone and Orexo’s Zubsolv. BioDelivery Sciences International is preparing a formulation attached to the cheek and designed to avoid the bitter taste of the drug.

But the risk of abuse continues, with those seeking a “high” finding ingenious ways to grind, crush, dissolve or burn the product.

“There is a huge issue of teenage abuse,” says Robert Radie, chief executive of Egalet. The Danish group has taken a different approach. It is using machines bought from toymaker Lego to coat the drug with a thin layer of digestible plastic. In tests, this destroys the blades of a coffee grinder, preventing the product being broken up in a way that can be abused.

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