Rylomine™ (intranasal morphine)

Morphine, the analgesic standard to which all other opioids are usually compared, is a potent agonist at the mu-opioid receptor. When morphine binds to this receptor, it inhibits the transmission of pain signals from nerve endings to the central nervous system. For millennia, morphine has been among the most important naturally-occurring therapeutic compounds. Morphine is a strong analgesic used for the relief of moderate-to-severe acute and chronic pain, pre-operative sedation, and as a supplement to anesthesia.

Conventional oral formulations of morphine do not provide rapid relief of pain in many patients. Aside from its slow and variable onset of action, oral morphine demonstrates considerable patient-to-patient variability in absorption. Clinicians often rely on injectable types of morphine preparations to assure rapid and effective pain relief. Injection of morphine often requires professional assistance or hospitalization. Therefore, alternative formulations of morphine that are easy to administer by a patient or caregiver, and deliver rapid onset of action with clinically meaningful blood levels of active drug offers significant medical benefit.

Javelin believes that Rylomine™ (intranasal morphine) represents such an alternative formulation that combines patient convenience, ease of use, and cost-effectiveness with the rapid onset of pain relief and the well-accepted potency of injectable delivery routes. Rylomine™ is in development in the U.S. and Europe for the treatment of acute pain in medically supervised settings. Previous single- and multiple-dose Phase I clinical studies of Rylomine™ have demonstrated similar pharmacokinetics to intravenous morphine. Rylomine™ is rapidly absorbed producing blood levels of morphine typically associated with analgesic effectiveness. These data were presented at the 10th World Congress on Pain, San Diego.

In December 2002, IDDS completed a large randomized, placebo- and comparator-controlled, double-blind, phase II trial which evaluated the safety and effectiveness of Rylomine™ in 225 patients suffering from moderate-to-severe post-operative pain. Rylomine™ provided statistically superior total pain relief as compared to placebo (p <0.05) with appreciable pain relief occurring five to ten minutes following nasal administration. Rylomine™ delivered statistically similar onset of action and total pain relief compared to intravenous morphine infused over 10 minutes. Rylomine™ also demonstrated a lower side effect profile and faster onset of action than oral morphine.

In September 2004, the European Agency for the Evaluation of Medicinal Products (“EMEA”) appointed France as the rapporteur country and Germany as the co-rapporteur country. In October 2004 a successful pre-MAA submission meeting was held between the representatives of the EMEA and Javelin. In recognition that Rylomine™ represents a significant innovation and a potential benefit to the European Community, Part B status was granted by the EMEA making the product eligible for review through the Centralized Procedure. In January 2005, Javelin initiated a randomized double-blind, placebo- and comparator-controlled trial comparing the safety and analgesic efficacy of Rylomine™ to intravenous morphine.

Product candidate		Indication			Development stage
Rylomine™		U.S.	Acute moderate-to-severe pain		Phase III
(intranasal morphine 75 mg/mL)		Europe	Acute moderate-to-severe pain, breakthrough pain		Phase II

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