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Quantitative analysis of the novel depsipeptide anticancer drug Kahalalide F in human plasma by high‐performance liquid chromatography under basic conditions coupled to electrospray ionization tandem mass spectrometry by E. Stokvis; H. Rosing; L. López‐Lázaro; I. Rodriguez; J. M. Jimeno; J. G. Supko; J. H. M. Schellens; J. H. Beijnen is a Chemistry article available to read on EtoBox.
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## Abstract Kahalalide F (KF) is a novel cyclic depsipeptide anticancer drug, which has shown anticancer activity both __in vitro__ and __in vivo__ especially against human prostate cancer cell lines. To characterize the pharmacokinetics of KF during a phase I clinical trial in patients with androgen refractory prostate cancer, a method was developed and validated for the quantitative analysis of KF in human plasma using high‐performance liquid chromatography (HPLC) coupled to positive electrospray ionization tandem mass spectrometry (ESI‐MS/MS). Microbore reversed‐phase liquid chromatography (LC) performed with mobile phases containing trifluoroacetic acid, an additive commonly used for separating peptides, resulted in substantial suppression of the signal for KF on ESI‐MS/MS. An alternative approach employing a basic mobile phase provided an excellent response for KF when detected in the positive ion mode. Plasma samples were prepared for LC MS/MS by solid‐phase extraction on C~18~ cartridges. The LC separation was performed on a Zorbax Extend C~18~ column (150 × 2.1 mm i.d., particle size 5 μm) with acetonitrile –10 mM aqueous ammonia (85 : 15, v/v) as the mobile phase, at a flo
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- Author
- E. Stokvis; H. Rosing; L. López‐Lázaro; I. Rodriguez; J. M. Jimeno; J. G. Supko; J. H. M. Schellens; J. H. Beijnen
- Publisher
- John Wiley and Sons; Wiley (John Wiley & Sons); Wiley-Blackwell; Wiley-Liss Inc; John Wiley & Sons Inc.; Wiley; Heyden And Son (ISSN 1076-5174)
- Published
- 2002
- Language
- EN
- Field
- Chemistry (Physical Sciences)