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LC-MS/MS assay and microsomal half-life of pemigatinib
A two-minute LC-MS/MS method quantifies pemigatinib in human liver microsomes and finds a 27.29 min half-life and moderate CLint.
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What in vitro half-life was measured for pemigatinib?
27.29 min in HLM.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
What intrinsic clearance was calculated?
25.4 μL min−1 mg−1, a moderate hepatic clearance.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
What mean extraction recovery is reported?
101.7 ± 4.48%, better than 89.3–92.2% in a prior method.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
Which MRM transitions quantify PMB?
488 → 401 and 488 → 186.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
What are the chromatographic conditions?
30% ACN / 70% 0.1% formic acid, 0.3 mL min−1, 2 min run.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
Which QC concentrations were used?
5, 15, 150, and 400 ng mL−1 (LLQC to HQC).
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
How is PMB extracted from HLM?
Acetonitrile protein precipitation, centrifuge, 0.22 μm filter.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
Why was 0.1% formic acid chosen over ammonium formate?
pH 3.2 avoided peak tailing and long run times seen at pH 4.0–4.5.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
What metabolic-stability conclusion do the authors draw?
Moderate hepatic clearance, so they predict acceptable bioavailability without ultra-rapid liver loss.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
Which column class actually retained PMB?
ZORBAX Eclipse plus-C18; HILIC did not retain PMB or FLV.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified
What injection volume was used?
5 μL.
Source: A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes · DOI · quote verified