Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1. It is primarily metabolized by CY2B6.
A standard dose of efavirenz has been associated with serious adverse reactions in poor metabolizers (PMs) of CYP2B6, necessitating a reduction in dose. In industrialized countries, clinicians typically genotype patients in order to identify PMs and make the appropriate dose reduction. However, genotyping is not feasible in developing countries. How can we ensure safe dosing for these patients in the absence of this information?
Certara’s Dr. Manoranjenni Chetty explained how she helped develop a PBPK model that was able to predict drug exposure in virtual patients of varying genotypes based solely on input data from a single plasma concentration.
