Influence of the synthetic microtubule inhibitor erbulozole (P.I.N.N.) (R 55 104), a new tubulozole congener, and gamma irradiation on murine tumors in vivo.

Abstract

Erbulozole (P.I.N.N.) (R 55 104) is a more water soluble congener of the synthetic microtubule inhibitor tubulozole (R 46 846) exhibiting a reversible antimicrotubular activity in vitro at a dose (1.56 x 10(-8) M) which is at least 10-fold lower. The compound also has an antiinvasive potential and shows antitumoral effects both in vitro and in vivo when administered appropriately. Eighty mg/kg R 55 104, given orally 6 h before or 3 h after radiotherapy, displays a prominent interactive effect with 10 Gy gamma irradiation in subcutaneous murine tumors which is similar to 160 mg/kg tubulozole administered 6 h before 10 Gy. The enhancing effect is also observed in a clinically relevant radiation dose fractionation schedule whereby eight fractions of 2 Gy each were pretreated 2 h before with 40 mg/kg R 55 104. Further study of this radiochemotherapeutic combination may lead to new clinical applications.

• Authors: W Distelmans, R Van Ginckel, W Vanherck, R Willebrords, M De Brabander, L Wouters, J Heeres
• Journal: European journal of cancer & clinical oncology (Eur J Cancer Clin Oncol) Vol. 25 Issue 10 Pg. 1499-504 (Oct 1989) ISSN: 0277-5379 [Print] England
• PMID: 2591442 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Dioxolanes
• Dioxoles
• tubulazole
• erbulozole

Topics

• Animals
• Antineoplastic Agents (therapeutic use)
• Combined Modality Therapy
• Dioxolanes (administration & dosage, therapeutic use)
• Dioxoles (therapeutic use)
• Drug Evaluation, Preclinical
• Fibrosarcoma (drug therapy, radiotherapy, therapy)
• Male
• Mice
• Microtubules (drug effects)
• Neoplasm Transplantation
• Time Factors