1Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development, PMB 21, Abuja, Nigeria
2Department of Medicinal Chemistry and Quality Control, National Institute for Pharmaceutical Research and Development, PMB 21, Abuja, Nigeria
3African Institute of Biomedical Science and Technology (AiBST), Cnr Chinhoyi Str./Jason Moyo Ave. No. 9 at LAPF Centre, Harare, Zimbabwe
4Director General/Chief Executive Officer, National Institute for Pharmaceutical Research and Development, PMB 21, Abuja, Nigeria
Objective: To evaluate the effect of NIPRD-AM1 on CYP3A4 in order to generate clinically significant data for its safe and efficacious use. Materials and Methods: NIPRD-AM1 is a phytomedicine developed from aqueous root extracts of Nauclea latifolia 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. Results: Results showed a very low IC50 value of 0.01 mg/ml similar to that of ketoconazole (0.016 mg/ml). 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.
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