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.
Source
A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes
Study at a glance
- Design
- Other — Validated C18 MRM LC-MS/MS of pemigatinib in human liver microsomes with well-stirred clearance model
- N
- Bioanalytical method validation and in-vitro HLM kinetics — no subject N
- Population
- Human liver microsome incubations of pemigatinib
- Outcome
- Quantification performance and in-vitro t½ / CLint of pemigatinib
Structured fields used in claim comparison tables when every cited study has a complete layer.
What they did
Authors developed a C18 MRM method (pemigatinib 488→401/186, flavopiridol IS), validated QCs at 5–400 ng mL−1 after ACN precipitation from HLM, and used an in vitro t1/2 well-stirred model for clearance.
What they found
Mean recovery is 101.7 ± 4.48%. In vitro t1/2 is 27.29 min and CLint is 25.4 μL min−1 mg−1, implying moderate hepatic extraction rather than ultra-rapid clearance.
The limits
What it doesn't show
No patient pharmacokinetic curves; HLM t1/2 is an in vitro predictor, and the authors note in vivo TDM still needs future work.
Key terms
- Pemigatinib (PMB)
- FGFR1–3 inhibitor; analyte quantified here.
- MRM
- Multiple reaction monitoring of precursor→product ion pairs on a triple quadrupole.
- Intrinsic clearance (CLint)
- Microsomal consumption rate used to predict hepatic extraction.
- In vitro t1/2
- Half-life of parent drug in an HLM incubation.
- HLM
- Human liver microsomes containing CYPs for metabolic stability tests.
Flashcards
Research intelligence for this paper
See its role on concept claims, tensions it is part of, placement history, and related discoveries.
Quiz yourself
PMB in vitro t1/2 in HLM is:
Common questions
How fast is the LC run?
2 min; PMB elutes at 1.2 min.
What t1/2 and CLint were found?
27.29 min and 25.4 μL min−1 mg−1.
Internal standard?
Flavopiridol (FLV).
Extraction?
Acetonitrile protein precipitation from HLM.
More on Mass spectrometry