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arverapamil
- Development stage
- Discontinued
- Lead developer
- Aravis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Arverapamil (brand name Rezular, development code AGI-003) is a small molecule investigational drug that is the purified R-enantiomer of the calcium channel blocker verapamil. Developed by AGI Therapeutics, it was designed to treat diarrhea-predominant irritable bowel syndrome (IBS-D) through a "triple-action" mechanism involving L-type calcium channel blockade, 5-HT2b receptor antagonism, and melatonin MT1 receptor binding. By using the R-isomer, the developer aimed to retain gastrointestinal efficacy while avoiding the potent cardiovascular effects associated with the S-isomer found in racemic verapamil. The drug reached Phase III clinical trials in the ARDIS program but was discontinued in 2009 after failing to meet its primary efficacy endpoints.
- Brand names
- Rezular
- Other names
- arverapamildexverapamil(R)-verapamilR-verapamil
02
Targets
ABCB1 (P-glycoprotein)5-HT2 (5-HT2 receptor family)LTCC (Voltage-gated calcium channel (L-type))
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