Central nervous system (CNS) penetration of homoharringtonine (HHT) |
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Authors: | Niramol Savaraj Lynn G. Feun Katherine Lu Maam Leavens Richard Moser William S. Fields Ti Li Loo |
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Affiliation: | (1) Division of Medicine and Division of Surgery, The University of Texas System Cancer Center, M.D. Anderson Hospital and Tumor Institute, 77030 Houston, Texas, USA;(2) Dept. of Medical Oncology University of Miami, Papanicolaou Comprehensive Cancer Center, 1475 N.W. 12th Avenue, 33036 Miami, Florida, USA |
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Abstract: | Generally tritiated homoharringtonine ([3H]HHT, 150 Ci, 430 g) was administered intravenously to seven patients at varying times before surgical resection of malignant brain tumor. Plasma, urine, cerebrospinal fluid (CSF), and tumor specimens were obtained during surgery, and the concentrations of HHT, its major metabolite, and [3H]HHT equivalent were determined chromatographically and radiochemically. For [3H]HHT equivalent, the concentration in tumor ranged from 0.6 to 4.3 ng/g and the ratio of tumor to plasma concentration from 0.5 to 1.8. In one patient who had CSF available for drug determination, the CSF to plasma ratio of total [3H]HHT was 0.3 at 45 minutes after drug administration and less than 0.2 ng/ml was unchanged HHT. For unchanged HHT, drug concentration in tumor ranged from undetectable (4 patients) to 1.8 ng/g. A major metabolite of HHT was detectable in the tumor specimens of all the patients. These results indicate that homoharringtonine can penetrate into brain tumors; in 3 patients with brain tumors, the ratios of HHT concentration in the tumor to that in the concurrent plasma were greater than one.address for offprints |
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Keywords: | central nervous system homoharringtonine penetration |
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