Remdesivir

pharmacological · immune-hematologic · IV

Remdesivir. Adenosine analog prodrug — intracellularly activated to remdesivir-TP, a delayed chain-terminator for SARS-CoV-2 RNA-dependent RNA… IV half-life 1 h.

Adenosine analog prodrug — intracellularly activated to remdesivir-TP, a delayed chain-terminator for SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). IV infusion for hospitalized COVID-19 + outpatient high-risk unable to take Paxlovid.

PK: THE UPADACITINIB SHAPE — TWO COMPARTMENTS ADDED TOGETHER AND STORED AS ONE VOLUME. Its citation reports "central (and peripheral) volumes of distribution for remdesivir, GS-704277, and GS-441524 were 4.89 L (46.5 L), 96.4 L (8.64 L), and 26.2 L (66.2 L)", and the stored figure is the first pair SUMMED — 51.39 — which is a quantity that appears nowhere and is not what a one-compartment exposure model consumes. The same abstract states the clearance that settles it: "The estimated elimination clearances of remdesivir, GS704277, and GS-441524 reached 18.1 L/h, 36.9 L/h, and 4.74 L/h" — against a stored assertion of 35.4, NEARLY TWICE TOO FAST, so exposure rendered at half the truth. The volume becomes that verbatim clearance over the stored rate. THE HALF-LIFE IS DECLARED RATHER THAN DEFENDED: this abstract states none, so the stored one hour is unsourced by the record own citation, and it is kept because the roughly one-hour disappearance of the parent ester is the clinically salient feature of this drug and because changing it would change nothing about exposure. A LARGER STRUCTURAL POINT IS LOGGED: the analyte that matters therapeutically is the nucleoside metabolite, whose own verbatim clearance in the same sentence is nearly four times slower, and this record models only the parent.

Pharmacokinetics

Sources: PMID:36123499