Cannabinoid CB1 Receptor Blockade Indications

The endocannabinoid system (ECS): the body’s regulatory dashboard

Through CB1 receptors, located in the central nervous system and selectively on various peripheral tissues, the ECS regulates important bodily functions including:

Hunger & Satiety


Glucose Homeostasis

Emotional Welfare

Reward Processing






The ECS is a vast network of lipid based signaling molecules, cellular-level receptors and regulatory proteins that control many of our most critical bodily functions. Signaling through these receptors control physiological homeostasis. The CB1 receptor is an integral part of this network. Compounds that modulate signaling through the CB1 receptor have the potential to treat a multitude of indications. This receptor is also turned on by THC, the principal psychoactive component of marijuana. Pathological overstimulation of the CB1 receptor can have many adverse consequences. Overactivation of the ECS has been implicated in obesity, liver disease, diabetes, and a host of other indications. These studies led to the development of compounds that can selectively block or antagonize the CB1 receptor.

First generation CB1 antagonists, while efficacious, unfortunately produced adverse effects in a sampling of patients which rendered these compounds unsuitable for chronic use. Therefore, there is an immediate need to develop refined antagonists that do not produce adverse effects in a clinical setting. Artiam’s portfolio of cutting-edge compounds do exactly that. These compounds preserve the benefits of blocking CB1 activation but do not produce adverse effects based on preclinical studies.

Non-alcoholic steatohepatitis (NASH)

Non-alcoholic steatohepatitis (NASH)

Non-alcoholic fatty liver disease (NAFLD) is an increasingly common form of chronic liver disease, NAFLD currently affects about one-quarter of the population in the US and nearly 300 million people worldwide.

Many people living with NAFLD will develop nonalcoholic steatohepatitis (NASH), an aggressive form of fatty liver disease, which is marked by liver inflammation and left untreated, NASH may progress to advanced scarring (cirrhosis) and liver failure. Liver disease is the 9th leading cause of mortality in the US.

FDA guidance highlights the urgent need for therapies for NASH. Cases in the U.S. are projected to increase 63% to nearly 27 million by 2030.  There is a critical unmet need for safe, effective treatment options.

Cannabis Use Disorder (CUD)

Cannabis use disorder (CUD) is a term used to describe addiction to marijuana and other products containing natural and synthetic cannabinoids that are psychoactive. Marijuana is gaining popularity in the United States as more states legalize recreational use of this drug and other related products.

Although it is often promoted as a “safe” drug, epidemiological studies indicate that dependent marijuana users often experience harmful short and/or long-term side effects. Roughly 13% of US adults use cannabis products and about 10% of these people become addicted. As many as 1 in 6 users attempt to quit, translating to approximately 4 million patients in the US alone.

Outside of cognitive-behavioral therapy, there is no FDA-approved pharmacotherapy for CUD, cannabis intoxication or related substance use disorders.

Cannabis Use Disorder (CUD)
Prader-Willi Syndrome (PWS)

Prader-Willi Syndrome (PWS)

Prader-Willi syndrome (PWS) is a neurodevelopmental genetic disorder, occurring in approximately one out of every 15,000 births. Affecting both males and females, PWS is the most common genetic cause of serious childhood obesity.

Likely related to a dysfunction of the hypothalamus, PWS is highlighted by dysregulation of many crucial metabolic bodily functions. Patients develop comorbid conditions that can become life threatening such as extreme obesity, cardiovascular disease, and diabetes. There are approximately 350,000-400,000 cases worldwide. There is no FDA approved therapy for this orphan indication making this an area of urgent need.