Simulation of metabolism-based herb-drug interaction: towards safe and efficacious use of NIPRD-AM1

Abstract

Objective: To evaluate the effect of NIPRD-AM1 on CYP3A4 in order to generate clinically significant data for its safe and efficacious use. <br/>Materials and Methods: NIPRD-AM1 is a phytomedicine developed from aqueous root extracts of <em>Nauclea latifolia</em> Smith (Rubiaceae) for the treatment of uncomplicated malaria. The effect of NIPRD-AM1 on CYP3A4 was measured with and without the addition of NIPRD-AM1, by testing different concentrations of the product at 37 °C in reactive mixtures with ketoconazole (2.5 µM) as the positive control. <br/>Results: Results showed a very low IC₅₀ value of 0.01 mg/ml similar to that of ketoconazole (0.016 mg/ml). <br/>Conclusion: Metabolic processes of NIPRD-AM1 are likely to inhibit CYP3A4, with potential implication on drugs that are CYP3A4 substrates. This is a promising approach for guidance towards the safe and efficacious use of NIPRD-AM1.