Project in brief

Opioid overdose is a life-threatening condition, characterized by loss of consciousness and respiratory depression. Based on the proprietary drug delivery platform AmorphOX, Orexo has developed a high-dose naloxone rescue medication, OX124, designed to reverse opioid overdoses, including those from highly potent synthetic opioids, such as fentanyl and fentanyl analogues.

Formulations of OX124 have shown more rapid absorption and substantially higher plasma concentrations of naloxone compared to the current market leader. These properties can be critical in avoiding brain damages and saving lives as well as preventing re-intoxification during the revival process. In addition, the AmorphOX technology, which is the backbone in OX124, contributes to improved stability of the active substance and reduces its sensitivity related to temperature changes.

OX124 is protected by patents until 2039.

Project in brief

The widespread use of synthetic opioids, also increases the need for effective and long-lasting rescue medications for use in rural areas where it takes long time for patients to reach emergency care units. With OX125, the aim is to develop an overdose rescue medication for situations where the treatment effect needs to be long-lasting while also being powerful and fast-acting. Nalmefene has a half-life of eight to eleven hours in the body versus one to two hours for naloxone.

OX125, also based on the proprietary drug delivery platform AmorphOX, has shown positive results from a human pharmacokinetic study. The study was a cross-over, comparative bioavailability study in healthy volunteers to assess nalmefene absorption from three development formulations of OX125, compared to a nalmefene intramuscular injection. Data demonstrated extensive and rapid absorption across all three OX125 formulations as well as good tolerability.

Project in brief

The aim with OX640 is to develop a powder-based nasal epinephrine product for the emergency treatment of allergic reactions. Epinephrine is commonly used for the ­emergency treatment of allergic reactions, including anaphylaxis. Epinephrine is a very unstable active ingredient sensitive to chemical degradation, which is the reason why today’s commercial epinephrine products have limited shelf-life with restrictive handling and storage.

OX640 is based on AmorphOX and its powder-based technology provides excellent chemical and physical ­stability. In addition to providing allergic patients with a more convenient, needle-free alternative to auto-injectors currently on the market, an epinephrine product that provides greater flexibility in relation to how it can be handled and stored should provide significant benefits to patients and healthcare systems worldwide.

OX640 is protected by granted patents both on the US and European markets. Furthermore, multiple patent applications have been filed protecting OX640 on a global basis until 2044.

Project in brief

OX-MPI (GS-248) is a drug candidate in clinical development. OX-MPI inhibits the proinflammatory enzyme mPGES-1, which via its product, prostaglandin E2, plays a key role in the chronic inflammatory disease endometriosis. This disease affects approximately 10 percent of women of reproductive age. Main symptoms of endometriosis are severe pain and reduced fertility, and there is a high need for nonhormonal treatment options.

Orexo’s partner Gesynta Pharma owns all rights to the drug candidate.