
Xanomeline, an old drug
Xanomeline is an old drug. Back in the 1990s, Novo Nordisk and Eli Lilly carried out a large number of clinical trials on it, mainly for the indication of Alzheimer's disease (AD). Regrettably, the trials were forced to terminate in 1998 owing to its notable gastrointestinal and cardiovascular side effects.
Old drugs regain brand-new vitality!
Cobenfy (Xanomeline/Trospium) emerges as a novel therapeutic agent for schizophrenia.
In the early 2000s, Danish scientists accidentally discovered that xanomeline also exerts anti-schizophrenic activity. Karuna Therapeutics acquired its global development rights and redesigned its formula and dosage regimen. The company ingeniously combined xanomeline with trospium chloride to develop the combination drug KarXT, which effectively alleviated the gastrointestinal side effects caused by xanomeline.

On September 26, 2024, the U.S. FDA officially approved Cobenfy (Xanomeline/Trospium) for oral treatment of schizophrenia in adult patients. It marks the first schizophrenia drug with an innovative mechanism of action to gain approval in 35 years. Impressively, Cobenfy generated revenue of 10 million US dollars within just two months after its launch, fully demonstrating its tremendous commercial potential.
Xanomeline
| Target: | M1 receptor × M4 receptor |
| Originator: | Eli Lilly & Co., Novo Nordisk A/S |
| Developers: | Bristol Myers Squibb Co., Karuna Therapeutics, Inc., Bristol Myers Squibb (China) Investment Co., Ltd. |
| Indications Under Development: | Agitation, Alzheimer’s Disease, Dementia-related Agitation |
| Highest R&D Phase: | Phase 3 Clinical Trial |
| First Approval Date: | Not yet approved |
| First Approved Country/Region: | Not yet approved |
Xanomeline Starting Materials and Intermediates
| Intermediates Name | CAS NO. |
| Pyridine-3-carbaldehyde | 500-22-1 |
| 3-(4-Chloro-1,2,5-thiadiazol-3-yl)pyridine | 131986-28-2 |
| 3-(4-HEXYLOXY-1,2,5-THIADIAZOL-3-YL)-1-METHYLPYRIDINIUM IODIDE | 131988-19-7 |
RELYBO is committed to providing global customers with high-purity, high-quality Xanomeline intermediates with stable supply from kilogram to ton cales, accelerating the innovation and commercialization.
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