Developping the therapeutic potential of CB1-SSi, the first biased allosteric inhibitors
Signaling Specific inhibitors of the CB1 receptor (CB1-SSi) are a proprietary new pharmacological class never tested in humans before.
They are probably the most potent and safest pharmacological inhibitors currently in development.
CB1-SSi open a new frontier in pharmacology.
Molecular Target
The CB1 receptor is the molecular target of CB1-SSi
The CB1 is one of the main neurotransmitter receptors of the brain involved in a large range of diseases.
The stimulation of the CB1 receptor by the endocannabinoid system plays a major role in cognition, motivation and mood.
Over-activation of the CB1 receptor by THC, the active ingredient of cannabis, leads to its intoxicating effects.
Mechanism of Action
CB1-SSi have a unique mechanism of action
CB1-SSi are new molecular entities (NME) that mimic a natural defense mechanism of the brain (Science, 2014).
CB1-SSi, unlike available antagonists, do not block all the cellular activities of a receptor but exercise a biased allosteric inhibition.
CB1-SSi selectively correct the hyperactivated cellular activity of certain pathological states.
CB1-SSi do not modify normal physiology and behaviors and consequently have no identifiable behavioral side effects.
Aelis Farma’s Target Diseases
Cannabis-Related Disorders (AEF0117)
Aelis Farma is developing AEF0117, the first CB1-SSi to fight Cannabis-related disorders, an emerging unsatisfied medical need.
Cannabis can induce three major disorders:
1.
Severe addiction
There are more than 120 million cannabis users worldwide, 10% of which will become severely addicted. 4.5 million cannabis addicts are present in the US alone.
2.
Acute psychosis
Cannabis is the major single cause of acute psychosis, whose prevalence is increasing with the legalization of recreational cannabis and the availability of products with high THC content.
3.
Acute toxicity
Cannabis causes 500 000 Emergency Room entries per year in the US alone with a high prevalence in states in which recreational cannabis has been legalized. Panic attacks and hyperemesis syndrome are among the most reported causes of ER entries due to cannabis.
Cognitive Deficits (AEF0217)
Aelis Farma is developing AEF0217 to treat cognitive deficits, a major unsatisfied medical need of modern society.
The CB1 receptor is involved in several cognitive deficits:
1.
Developmental: Down syndrome and Fragile X syndrome
There are more than 1 million children with Down syndrome in the US and EU alone.
2.
Aging-related: Subjective Memory Impairments (SMI) and Alzheimer's
11% of individuals 65 years and older are affected by SMI.
24 million individuals worldwide have Alzheimer's disease.