Drug intelligence / Profile preview

carboxyamidotriazole orotate

Development stage
Phase 1
Lead developer
Tactical Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Carboxyamidotriazole orotate is the orally bioavailable orotate salt form of carboxyamidotriazole (CAI), a small molecule inhibitor of non-voltage-operated calcium channels. By blocking both calcium influx into cells and release from intracellular stores, it disrupts calcium channel-mediated signal transduction. This leads to inhibition of PI3 kinase activity and vascular endothelial growth factor (VEGF) signaling pathways, resulting in antiangiogenic and antiproliferative effects. Carboxyamidotriazole orotate has demonstrated promising efficacy in brain cancers such as glioblastoma and anaplastic gliomas, especially when combined with temozolomide. It shows good brain penetration and can be safely combined with standard chemoradiation regimens[1][2][5][6][8].

Other names
carboxyamidotriazole orotate1,2,3-carboxyamido-triazole orotateCAI orotate
02

Targets

CRAC (Calcium release-activated calcium channel (CRAC channel))

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