In vitro degradation of l-phenylalanine mustard (l-PAM)

Thomas L. Evans, Sai Y. Chang, David S Alberts, I. Glenn Sipes, Klaus Brendel

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Abstract

l-Phenylalanine mustard (l-PAM), a bis-choroethylamine, is an important drug in the treatment of multiple myeloma and ovarian cancer. It undergoes rapid hydrolysis in vitro and in vivo, forming the mono-and dihydroxy degradation products. l-PAM's first-order disappearance rate in a phosphate-buffered solution did not differ statistically according to the presence or absence of activated rat liver microsomal enzymes. Furthermore, l-PAM's disappearance rate in a rat whole liver perfusion system was not greater than its hydrolysis rate in water. In vitro plasma recovery studies showed that up to 85% of the <sup>14</sup>C l-PAM drug equivalents could be recovered as the parent compound and the mono-and dihydroxy degradation products. Thus, l-PAM in in vitro degradation was similar qualitatively and quatitatively to its reported in vivo degradation in animals and man. It is concluded that l-PAM does not undergo important, active in vivo metabolism.

Original languageEnglish (US)
Pages (from-to)175-178
Number of pages4
JournalCancer Chemotherapy and Pharmacology
Volume8
Issue number2
DOIs
Publication statusPublished - 1982

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ASJC Scopus subject areas

  • Cancer Research
  • Oncology
  • Pharmacology

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