4 To 5 More Years Of Research Needed In Making Painkiller Less Attractive
To Abusers

OXYCONTIN SUBSTITUTE STALLED

In Southwest Virginia, More Than 60 People Have Died From Overdoses Of The Drug

The manufacturer of OxyContin, which has seen the painkiller's benefits
eclipsed by reports of addiction and death, said Tuesday that development
of an abuse-resistant alternative drug is taking longer than anticipated.

Purdue Pharma had hoped to submit a new opium-based painkiller for approval
to the Food and Drug Administration by the end of the year.

But those plans have now been pushed back four to five years to allow
additional research into the possibility of combining the active
painkilling ingredient oxycodone with an antagonist, or a blocker that
would make the drug less attractive to abusers.

"We are disappointed at this delay in our efforts to introduce a more
abuse-resistant medication," said Paul Goldenheim, Purdue Pharma's
executive vice president for research and development.

"Developing new medications that are safe and effective for patients in
pain, and at the same time resistant to abuse, is a very complex scientific
and technical challenge," Goldenheim said.

The Connecticut-based company has been working to develop a new painkiller
since abuse of OxyContin surfaced several years ago. In Southwest Virginia,
more than 60 people have died from overdoses of the drug's active
ingredient, and authorities attribute rising crime rates to the drug's
popularity among abusers.

Since it was approved by the FDA in 1995, OxyContin has been hailed as a
miracle drug because of a formula that gradually releases oxycodone into a
patient's bloodstream over 12 hours.

But it didn't take long for drug abusers to circumvent the time-release
mechanism by chewing the tablets or crushing them and snorting or injecting
the powder for an immediate, heroin-like high.

Purdue Pharma said last year that it was hoping to add the antagonist
naloxone to rob intravenous abusers of the drug's high. Meanwhile, the
company is also studying the introduction of a second antagonist,
naltrexone, that would also render the painkiller useless to abusers who
chew or inhale it.

The company said Tuesday that its research has found that metabolism of
naloxone was more variable than expected among legitimate patients, raising
concerns that pain relief might be compromised.

The setback with naloxone has prompted Purdue Pharma to shift its emphasis
to the naltrexone formulation, company spokesman Jim Heins said. That
formulation is seen as more promising, because its effectiveness would not
be limited to intravenous abuse.

Under the proposal, naltrexone, which has been used as a treatment for
alcoholism, would be coated with a chemical that would prevent it from
dissolving. The antagonist would pass through legitimate patients, who
would still benefit from the full dose of oxycodone over a 12-hour period.

But abusers who crush the pills would break up the coating and allow the
naltrexone to enter the bloodstream, immediately counteracting any high the
oxycodone would have produced.

The company said it will take at least five years to develop a
naltrexone-based drug, which had been viewed as more complicated than the
naloxone version.

Meanwhile, Purdue Pharma will continue to produce OxyContin, which
accounted for $1.5 billion in sales last year.