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Mutation Information

Mutation Site	G190A
Mutation Type	Amino acid level
Gene/Protein/Region Type	RT
Relevant Drug	doravirine (DOR)

Literature Information

PubMed PMID	32816220
Published Year	2020
Journal	Clinical drug investigation
Title	Clinical Pharmacokinetics of the Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor Doravirine: An Assessment of the Effect of Patient Characteristics and Drug-Drug Interactions.
Author	Khalilieh S,Yee KL,Sanchez R,Stoch SA,Wenning L,Iwamoto M
Evidence	Even at this decreased C24, doravirine plasma concentrations exceed the pharmacokinetic target of 78 nM, which is greater than 6-fold the in vitro IC50 for inhibition of wild-type virus, and exceeds IC50 values for common single resistance mutations (K103N, Y181C, G190A), and of the K103N/Y181C double mutant. Steady-state AUC was selected as the exposure measure from which to judge clinical relevance from a safety perspective, as this parameter is an integration of concentrations over the 24-h dosing interval in which individuals are exposed to doravirine at steady state.

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Description

Mutation Information Note

Gene/Protein/Region Type: Virus Gene (e.g. LMP-1) or Virus Protein (e.g. Rep 68) or Virus Region (e.g. S, X)

Literature Information Note

Evidence: sentence contains this mutation information in the citation