Blood samples for PK determination of plasma concentrations of RO6870868 and its metabolites (including RO6871765 and RO6872373) as applicable, were collected at predose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36, and 48 h postdose. Urine samples were collected for measurement of concentrations of the drug (RO6870868) and its metabolites (RO6871765 and RO6872373) in pooled urine samples at 0–4, 4–8, 8–12, 12–24, 24–36, and 36–48 h postdose. Plasma and urine concentrations were measured by a specific and validated liquid chromatography–mass spectrometry method. Details are provided in Supplementary Section S3.

Blood samples were collected to evaluate the changes of PD markers as well as transcriptional changes of TLR7/IFN‐response genes at predose and 3, 6, 12, 18, 24, 36, and 48 h postdose in all subjects. IL‐6, TNF‐α, IL12‐p40, IL‐10, and IP‐10 levels were determined using Luminex X‐MAP; IFN‐α, using Simoa; neopterin by ELISA; ISG15, OAS1, MX1, and TLR7 mRNAs via TaqMan, as previously described. 37

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