Intranasal NSAID a first for pain relief

Little-known US pharmaceutical company Roxro Pharma announced its intranasal analgesic formulation of ketorolac, ROX-888, had proved in Phase III studies that it rapidly and effectively eased pain on the same par as an intramuscular injection.

The intranasal drug delivery market continues to grow, and the current scene reflects a move to developing products for different diseases via this method.

What was confined to allergies, asthma and pulmonary diseases, intranasal drug delivery is now moving into areas of sexual dysfunction, vaccines and pain management because of convenience and the rapid therapeutic response.

The intranasal formulation of ketorolac, which is currently undisclosed, is a first for the industry because other NSAIDs, unlike ketorolac, can not exist in a soluble form because of their chemical properties.

That coupled with the intranasal route for drug delivery, gives ROX-888 a lot of weight for being approved in the market.

Currently, ketorolac, which works by inhibiting an inflammatory response to relieve pain, is administered as an intramuscular injection or intravenously for the short-term treatment of moderately sever pain.

There is also an oral form, but it is not viewed as being particularly effective.

Ketorolac has been around since the early 1990s and is a potent analgesic.

Roxro Pharma chief executive Dr Roberto Rosenkranz said the beauty of ROX-888 was that its intranasal delivery removed the hindrance of having the drug delivered in a hospital setting.

With an intranasal system, the patients could take the drug home, administer it themselves and receive the same level of pain relief as if they had had an intramuscular injection, Rosenkranz said, when contacted by US-PharmaTechnologist.com.

"It really is a significant improvement and a significant product because it gives flexibility to the physician."

Beside this advantage, the product was also easy to administer, quickly absorbed into the bloodstream with a quick therapeutic response, caused no sedation or side effects of pain-relieving opiates, such as morphine, and was not addictive, reducing the possibility for drug abuse, he said.

Los Angeles Huntington Memorial Hospital director of clinical research Dr Neil Singla said in a statement : "ROX-888 is an important breakthrough in treating pain."

"It is rapidly absorbed into the bloodstream, and relieves pain as fast as an intramuscular injection.

There is a need for new analgesics like ROX-888 that do not have the troublesome side effects and abuse risks associated with narcotic pain relievers.

With the continued increase in out-patient surgeries, there is a growing need for alternatives to injections and intravenous administration of pain killers."

The Phase III study on the intranasal formulation showed patients required 22 per cent less morphine in the first 24 hours following surgery compared to patient who access to morphine alone.

Roxro Pharma intends to file a new drug application (NDA) in the first half of 2008.

The intranasal route is becoming an increasingly popular choice for pain relief.

Just this week, Javelin Pharmaceuticals announced Phase II results for an intranasal morphine and Nasalfent (fentanyl) for severe cancer pain is in Phase III trials.

Already on the market is Stadol (butorphanol tartrate) analgesic nasal spray and Migranal (dihydroergotamine mesylate) nasal spray for migraines.

Market reports suggest the reformulation of injectable and oral drugs will drive the intranasal pain relief market forward.

The current pain relief market is a more than $25bn industry.