Erbulozole (P.I.N.N.) (R 55 104) encapsulated into cyclodextrins: has it a combined antitumoral and radioprotective potential?

The clinically applicable formulation of the microtubule inhibitor erbulozole (R 55 104), dissolved into an aqueous hydroxypropyl-beta-cyclodextrin solution (designated as R 55 104-CYCLO), exerts a similar effect on growth delay of subcutaneous MO4 fibrosarcomas in mice, with or without 10 Gy gamma-irradiation given locally to the tumors 2 h later, compared to R 55 104 in water. The drug concentration can be reduced from 80 mg/kg to 5 mg/kg without affecting the activity of this particular drug-radiation combination. Furthermore, 80 mg/kg R 55 104-CYCLO show a radioprotective effect when given 2 h before total body irradiation of non-tumor bearing mice. A radiation dose of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 Gy respectively was given resulting in a LD50(30) of 5.97 Gy for the irradiated mice and 7.65 Gy for the drug-radiation treated animals (Dose Effect Factor = 0.78). Therapeutic implications of both observations are discussed.
AuthorsW Distelmans, R Van Ginckel, W Vanherck, R Willebrords, L Wouters, M De Brabander, J Mesens
JournalAnticancer research (Anticancer Res) 1991 Jan-Feb Vol. 11 Issue 1 Pg. 253-6 ISSN: 0250-7005 [Print] GREECE
PMID2018359 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Capsules
  • Dioxolanes
  • Radiation-Protective Agents
  • erbulozole
  • Animals
  • Antineoplastic Agents (therapeutic use)
  • Capsules
  • Cell Division (drug effects)
  • Dioxolanes (therapeutic use)
  • Fibrosarcoma (drug therapy, pathology, radiotherapy)
  • Gamma Rays
  • Mice
  • Mice, Inbred Strains
  • Radiation-Protective Agents (therapeutic use)
  • Sarcoma, Experimental (drug therapy, pathology, radiotherapy)

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