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Therapeutic activity of 7-[(2-trimethylsilyl)ethyl)]-20 (S)-camptothecin against central nervous system tumor-derived xenografts in athymic mice.

Publication ,  Journal Article
Keir, ST; Hausheer, F; Lawless, AA; Bigner, DD; Friedman, HS
Published in: Cancer Chemother Pharmacol
July 2001

PURPOSE: Camptothecins have emerged as an important new class of antitumor drugs. Camptothecin derivatives such as CPT-11 and topotecan are commercially available and approved for the treatment of colorectal (CPT-11) and ovarian and small-cell lung cancer (topotecan). This study was designed to test the efficacy of karenitecin, a novel highly lipophilic camptothecin derivative, against a panel of human tumor xenografts derived from adult and pediatric central nervous system malignancies growing in athymic nude mice. METHODS: Xenografts evaluated were derived from childhood high-grade gliomas (D-212 MG, D-456 MG), adult high-grade gliomas (D-54 MG, D-245 MG), medulloblastomas (D-341 MED, D-487 MED), and ependymomas (D-528 EP, D-612 EP), as well as sublines with demonstrated resistance to procarbazine (D-245 MG (PR)) and busulfan (D-456 (BR)). In replicate experiments, karenitecin was given at 1.0 mg/kg per dose via intraperitoneal injection for a period of 10 consecutive days, which is the dosage lethal to 10% of treated animals. RESULTS: Karenitecin produced statistically significant (P < or = 0.001) growth delays in all subcutaneous xenografts tested, including the sublines resistant to procarbazine and busulfan. Growth delays ranged from 12.1 days in D-456 MG (BR) to 90+ days in D-212 MG and D-341 MED. Karenitecin also produced statistically significant (P < or = 0.001) increases in survival of animals bearing D-341 MED intracranial xenografts (69% increase) and those bearing D-456 MG xenografts (62% increase). CONCLUSION: These preclinical studies confirm that karenitecin is active against human central nervous system xenografts and should undergo clinical evaluation in patients with malignant central nervous system tumors.

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Published In

Cancer Chemother Pharmacol

DOI

ISSN

0344-5704

Publication Date

July 2001

Volume

48

Issue

1

Start / End Page

83 / 87

Location

Germany

Related Subject Headings

  • Transplantation, Heterologous
  • Oncology & Carcinogenesis
  • Neoplasm Transplantation
  • Mice, Nude
  • Mice, Inbred BALB C
  • Mice
  • Male
  • Irinotecan
  • Humans
  • Female
 

Citation

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Keir, S. T., Hausheer, F., Lawless, A. A., Bigner, D. D., & Friedman, H. S. (2001). Therapeutic activity of 7-[(2-trimethylsilyl)ethyl)]-20 (S)-camptothecin against central nervous system tumor-derived xenografts in athymic mice. Cancer Chemother Pharmacol, 48(1), 83–87. https://doi.org/10.1007/s002800000274
Keir, S. T., F. Hausheer, A. A. Lawless, D. D. Bigner, and H. S. Friedman. “Therapeutic activity of 7-[(2-trimethylsilyl)ethyl)]-20 (S)-camptothecin against central nervous system tumor-derived xenografts in athymic mice.Cancer Chemother Pharmacol 48, no. 1 (July 2001): 83–87. https://doi.org/10.1007/s002800000274.
Keir ST, Hausheer F, Lawless AA, Bigner DD, Friedman HS. Therapeutic activity of 7-[(2-trimethylsilyl)ethyl)]-20 (S)-camptothecin against central nervous system tumor-derived xenografts in athymic mice. Cancer Chemother Pharmacol. 2001 Jul;48(1):83–7.
Keir, S. T., et al. “Therapeutic activity of 7-[(2-trimethylsilyl)ethyl)]-20 (S)-camptothecin against central nervous system tumor-derived xenografts in athymic mice.Cancer Chemother Pharmacol, vol. 48, no. 1, July 2001, pp. 83–87. Pubmed, doi:10.1007/s002800000274.
Keir ST, Hausheer F, Lawless AA, Bigner DD, Friedman HS. Therapeutic activity of 7-[(2-trimethylsilyl)ethyl)]-20 (S)-camptothecin against central nervous system tumor-derived xenografts in athymic mice. Cancer Chemother Pharmacol. 2001 Jul;48(1):83–87.
Journal cover image

Published In

Cancer Chemother Pharmacol

DOI

ISSN

0344-5704

Publication Date

July 2001

Volume

48

Issue

1

Start / End Page

83 / 87

Location

Germany

Related Subject Headings

  • Transplantation, Heterologous
  • Oncology & Carcinogenesis
  • Neoplasm Transplantation
  • Mice, Nude
  • Mice, Inbred BALB C
  • Mice
  • Male
  • Irinotecan
  • Humans
  • Female