amorphOX™ - a novel and inventive drug delivery platform with significant potential

Orexo has successfully developed a drug delivery platform, amorphOX™, a novel and inventive powder-based technology, that is very rapidly dissolving, stable and works with different APIs, dosage forms and administration routes. This makes it a versatile platform with significant potential.

Amorphous solids are non-crystalline solids, possessing no long-range order. This gives them unique and highly sought-after properties, such as very rapid dissolution in water. Therefore, they enable formulation of drugs in a manner that allows for a faster onset and a higher bioavailability.

Historically however, amorphous drug compositions have been found to be both chemically and physically unstable and therefore to degrade during storage. This problem has now been solved by Orexo with the development of a drug delivery platform, amorphOX™, a powder-based technology that is both chemically and physically stable when stored in even elevated temperatures, while still being rapidly dissolving.

A versatile drug delivery platform

The powder-based technology is made up of particles which are built using a unique combination of a drug, carrier materials and, optionally, other excipients such as a permeability enhancer. The particles are presented as an amorphous composite of the various ingredients providing for excellent chemical and physical stability. The surface structure can be tuned for optimal process ability, and the size of the particle can be tailored to suite different administration routes.

Orexo is in the process of developing an aspect of the amorphOX™ platform to formulate and administer naloxone (OX124) and nalmefene (OX125) to reverse opioid overdoses. The number of deaths from opioid overdoses have grown in recent years, particularly in the US, creating a need for new and improved rescue medications, particularly for overdoses caused by synthetic opioids such as fentanyl.

Validated in humans

Both OX124 and OX125 are administered nasally and have shown very promising results in human clinical trials. Besides being well tolerated, the amorphOX™ platform provided for higher exposure, faster onset and lower variability in comparison to market leading products. OX124, which successfully completed pivotal trial in November 2021, has shown near instant dissolution in minimal amount of liquid as well as remarkable chemical and physical stability, even under accelerated conditions.

These properties make it ideal for a nasally administered emergency medication to reverse opioid overdoses. First, it needs to be storable so that it works when it is needed. Second, it needs to be easy to administer and have a very rapid onset as an overdose from an opioid progresses rapidly.

Wide applicability

The amorphOX™ platform has also showed good results in accelerated stability studies when used with numerous other APIs with very different chemical structures. The technology also suits very well with various dosage forms and administration routes and the properties of the powder can be tailored to meet specific needs such as particle size, dissolution, and mucosal retention. This makes it a versatile technology with broad applicability that can be used in the development of pharmaceuticals within multiple therapeutic areas.