Background: The representative cardiovascular herbs, i.e. Panax, Ligusticum, Carthamus, and Pueraria
plants, are traditionally and globally used in the prevention and treatment of various cardiovascular diseases. Modern
phytochemical studies have found many medicinal compounds from these plants, and their unique pharmacological
activities are being revealed. However, there are few reviews that systematically summarize the current trends of
Drug Metabolism/Pharmacokinetic (DMPK) investigations of cardiovascular herbs.
Methods: Here, the latest understanding, as well as the knowledge gaps of the DMPK issues in drug development
and clinical usage of cardiovascular herbal compounds, was highlighted.
Results: The complicated herb-herb interactions of cardiovascular Traditional Chinese Medicine (TCM) herb
pair/formula significantly impact the PK/pharmacodynamic performance of compounds thereof, which may inspire
researchers to develop a novel herbal formula for the optimized outcome of different cardiovascular diseases. While
the Absorption, Distribution, Metabolism, Excretion and Toxicity (ADME/T) of some compounds has been deciphered,
DMPK studies should be extended to more cardiovascular compounds of different medicinal parts, species (including
animals), and formulations, and could be streamlined by versatile omics platforms and computational analyses.
Conclusion: In the context of systems pharmacology, the DMPK knowledge base is expected to translate bench
findings to clinical applications, as well as foster cardiovascular drug discovery and development.