Baloxavir Marboxil
Baloxavir Marboxil. Influenza cap-dependent endonuclease (PA subunit) inhibitor — blocks viral mRNA synthesis. Single-dose oral therapy… Oral half-life 3.3 d.
Influenza cap-dependent endonuclease (PA subunit) inhibitor — blocks viral mRNA synthesis. Single-dose oral therapy advantage over oseltamivir (5-day course). Reduced influenza A activity in some 2021 strains via PA I38T resistance mutation.
PK: THE MASS DESCRIBED A SPECIES NEVER PRESENT IN PLASMA — the fourth instance of this shape after fenofibrate, misoprostol and eslicarbazepine. The stored 571.55 is baloxavir MARBOXIL, the prodrug; the circulating and measured species is baloxavir acid at 483.5, and the record own source says so — "PK parameters of BALOXAVIR ACID were estimated by noncompartmental analysis". An 18.2% error, carried by a record whose name field compounds the conflation. That citation also states none of the four stored values, and measured against its own verbatim numbers — "Mean maximum concentration (Cmax) was 107.6 and 206.9 ng/ml, and mean ... AUC0-inf was 6955 and 9643 ng.h/ml in the 40 and 80 mg cohorts" — the record was 2.7x low on exposure and 5.2x low on peak. F 0.96 is class 6 and its likely donor is the label PRODRUG CONVERSION sentence, an "almost completely converted" efficiency read as an oral bioavailability; no absolute bioavailability has ever been determined and every published volume is explicitly apparent. The label volume and clearance are internally coherent and are adopted together. A RESIDUE REMAINS AND IS DISCLOSED: no one-compartment fit of this drug exists in the literature at all — every published model is two or three compartments WITH AN ABSORPTION LAG this solver has no term for. ANALYTE: the stored mass was BALOXAVIR MARBOXIL, the prodrug, while its own citation measured the acid — "PK parameters of baloxavir acid were estimated by noncompartmental analysis". 18.2% high for a species never present in plasma.
Pharmacokinetics
- Oral — t½ 3.3 d · F 100% · ka 1.249 h⁻¹ · Vd 1180 L
Sources: PMID:35176206