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. 2020 Apr 21;64(5):e00027-20.
doi: 10.1128/AAC.00027-20. Print 2020 Apr 21.

Accumulation of Major Linezolid Metabolites in Patients with Renal Impairment

Ernane Souza  1 , Ryan L Crass  1 , Jeremy Felton  2 , Kengo Hanaya  3 , Manjunath P Pai  4
Affiliations

Accumulation of Major Linezolid Metabolites in Patients with Renal Impairment

Ernane Souza et al. Antimicrob Agents Chemother. .

Abstract

In patients with renal impairment (n = 22 of 39), the median serum concentrations of linezolid, PNU-142300, and PNU-142586 were 1.6-, 3.3-, 2.8-fold higher, respectively, than in patients without renal impairment. Metabolite concentrations in paired samples were poorly correlated with linezolid concentrations (r2 = 0.26 for PNU-142300 and 0.06 for PNU-142586). Linezolid and its metabolites share potential toxicophores that deserve characterization to mitigate higher myelosuppression risk in patients with renal impairment.

Keywords: dialysis; myelosuppression; oxazolidinones; pharmacodynamics; toxicology.

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Figures

FIG 1
FIG 1
Comparison between parent linezolid (LZD) and metabolite concentrations. (A) Metabolite-to-parent concentration ratios stratified by renal impairment. (B) Linear regression between LZD and metabolite concentrations. Linear correlation between the concentrations of LZD and PNU-142300 was 0.98 + 0.44 × LZD (r2 = 0.26). Linear correlation between the concentrations of LZD and PNU-142586 was 9.74 + 0.57 × LZD (r2 = 0.06).
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