Orexin-1 antagonists for the treatment of addiction

The treatment of addiction represents a substantial area of unmet medical need, forecast to be worth an estimated $13 billion per annum by 2018. C4X Discovery's lead programme, targeting Orexin-1, could represent a major new method of treating addiction.


Oral Orexin-1 Antagonist

The Orexin-1 receptor is considered to be central to the brain’s ‘craving’ and ‘reward’ pathways with pre-clinical efficacy observed in multiple addiction models. However, to date no drug candidate that targets Orexin-1 has progressed into clinical development, in large part due to the difficulty in identifying candidates that are specific only to Orexin-1. Orexin-2 has high structural similarity to Orexin-1, but has a very different biological function. Orexin-2 is targeted in the treatment of insomnia, and it has historically proved highly challenging to develop drug candidates which will target Orexin-1 selectively without targeting Orexin-2.
C4XD’s primary indication for its oral Orexin-1 antagonists is for the treatment of nicotine addiction as an aid to smoking cessation. The current market-leading product in this indication is Chantix (varenicline) which is effective on quit rates but has minimal prevention of relapse and also has a black box warning on label.

Oral Orexin-1 antagonists aim to deliver superior clinical benefit to Chantix with a much improved safety profile. Other treatment markets for Orexin-1 antagonists include alcohol addiction, panic, cocaine and opiate addictions.