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Distribution and Excretion of Radiolabeled Temoporfin in a Murine Tumor Model
Author(s) -
Whelpton Robin,
MichaelTitus Adina T.,
Jamdar Ravi P.,
Abdillahi Kaltun,
Grahn Michael F.
Publication year - 1996
Publication title -
photochemistry and photobiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.818
H-Index - 131
eISSN - 1751-1097
pISSN - 0031-8655
DOI - 10.1111/j.1751-1097.1996.tb09646.x
Subject(s) - excretion , urine , chemistry , biodistribution , feces , chlorin , distribution (mathematics) , medicine , pharmacokinetics , endocrinology , photodynamic therapy , biology , biochemistry , in vitro , microbiology and biotechnology , mathematics , organic chemistry , mathematical analysis
The biodistribution and excretion of temoporfin (tetra[ m ‐hydroxyphenyl]chlorin, m ‐THPC), a recently developed photosensitizer, was investigated in BALB/c mice. [ 14 C]temoporfin was administered intravenously (0.73 μmol/kg) to tumor‐free mice or to mice implanted with the Colo 26 colorectal carcinoma. Blood, tissue and fecal samples were collected for 35 days and 10 days postdose from tumor‐free mice and tumor‐bearing mice, respectively. Blood concentrations fell rapidly such that at later time points they were indistinguishable from background counts. Tumor concentrations rose to a peak of 0.34 μg temoporfin equivalents/mL at 2 days and then declined in parallel (log plot) with the blood concentrations. Tumor : tissue ratios at 2 days for skin, adipose tissue and skeletal muscle underlying the tumor were 1.5, 2.3 and 3.8, respectively. By 4 days the corresponding values were 1.6, 3.4 and 4.0. Nearly 40% of the administered radioactivity was excreted in the feces in the first 24 h and more than 80% had been excreted by 20 days. Less than 0.2 % of the dose was recovered from the urine. An elimination half‐life of 10–12 days was calculated from the excretion data.