# Treatment for cannabis use disorder

> **NIH NIH R43** · ARTIAM BIO INC. · 2022 · $319,898

## Abstract

Abstract
Our goal is to develop an innovative pharmacotherapy for cannabis use disorder (CUD) that affects over 4 million
Americans. We propose to develop a novel second generation PARTIAL inverse agonist of the cannabinoid 1
receptor (CB1) that has a benign behavioral profile for CUD. Cannabinoids are the second most abused class of
drug in the world and there is no FDA approved medication for CUD -- making this an area of urgent need. The
psychoactive effects of cannabis and synthetic cannabinoids result from activation of central CB1 receptors.
Blocking the rewarding and craving properties of drugs of abuse is a well-validated and accepted strategy for
substance use disorders (SUD) without a strong adverse physical withdrawal component. Rimonabant is a potent
FULL inverse agonist of the CB1 receptor that was approved in Europe as an anti-obesity agent. Unfortunately,
rimonabant produced adverse dysphoric effects in ~6% of users -- effects likely due to sustained high brain
exposure and potent inverse agonism, which led to its eventual discontinuation. In human studies, rimonabant
was efficacious in treating many aspects of CUD. Artiam Bio is developing the next generation of CB1 antagonists
that are expected to have a superior adverse effect profile compared to rimonabant and previous clinical
candidates. Artiam Bio’s lead compound is an orally active, potent, and selective CB1 partial inverse agonist with
limited brain penetration. This compound is functionally as efficacious as rimonabant but produces no
dysphoria/anhedonia in rodent studies. Further development of this compound is proposed through three aims.
Through aim 1, ~500 g of the compound will be synthesized using an established chemical route leveraging upon
Artiam’s experience with a congener. Through aims 2 and 3, dose range finding toxicological studies will be
performed in two species and toxicokinetic parameters will be established. Successful completion of this phase 1
SBIR application will pave the way for GLP regulatory studies and other IND-enabling activities of Artiam’s lead
candidate for CUD.

## Key facts

- **NIH application ID:** 10546566
- **Project number:** 1R43DA057168-01
- **Recipient organization:** ARTIAM BIO INC.
- **Principal Investigator:** HERBERT H SELTZMAN
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $319,898
- **Award type:** 1
- **Project period:** 2022-08-01 → 2025-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10546566

## Citation

> US National Institutes of Health, RePORTER application 10546566, Treatment for cannabis use disorder (1R43DA057168-01). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/10546566. Licensed CC0.

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