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total coumarin extract
- Development stage
- Preclinical
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Total coumarin extract (TCE) is a botanical extract derived from Radix Angelicae dahuricae (Baizhi), a traditional Chinese medicinal herb. It contains a variety of furanocoumarins, most notably imperatorin and isoimperatorin. TCE is primarily investigated for its synergistic effects when co-administered with other drugs, such as ligustrazine, in the treatment of migraine. Its mechanism involves the inhibition of several cytochrome P450 (CYP450) enzymes, including CYP1A2, CYP2C9, CYP2D6, and CYP3A4, which reduces the metabolism of co-administered substrates, thereby increasing their plasma concentration and prolonging their therapeutic effect. Additionally, TCE has demonstrated direct anti-migraine activity by modulating levels of calcitonin gene-related peptide (CGRP), nitric oxide (NO), and endothelin.
- Other names
- TCERadix Angelicae dahuricae total coumarin extractBaizhi coumarin extract
02
Targets
CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP1A2 (Cytochrome P450 1A2)
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