PRECLINICAL STUDY OF INDOLOCARBAZOLES N-GLYCOSIDES DERIVATIVE LCS-1208 ANTITUMOR ACTIVITY. REPORT I

M. P. Kiseleva; Киселева Марина Петровна; Z. S. Shprakh; Шпрах З. С.; L. M. Borisova; Борисова Л. М.; I. Yu. Kubasova; Кубасова И. Ю.; A. V. Lantsova; Ланцова А. В.; E. V. Sanarova; Санарова Е. В.; N. A. Oborotova; Оборотова Н. А.; Z. S. Smirnova; Смирнова З. С.; A. Yu. Baryshnikov; Барышников А. Ю.

doi:10.17650/1726-9784-2015-14-2-71-77

PRECLINICAL STUDY OF INDOLOCARBAZOLES N-GLYCOSIDES DERIVATIVE LCS-1208 ANTITUMOR ACTIVITY. REPORT I

Authors: Kiseleva M.P.¹, Shprakh Z.S.¹, Borisova L.M.¹, Kubasova I.Y.¹, Lantsova A.V.¹, Sanarova E.V.¹, Oborotova N.A.¹, Smirnova Z.S.¹, Baryshnikov A.Y.¹
Affiliations:
1. ФГБНУ «Российский онкологический научный центр имени Н.Н. Блохина»
Issue: Vol 14, No 2 (2015)
Pages: 71-77
Section: ORIGINAL REPORTS
Published: 30.06.2015
URL: https://bioterapevt.abvpress.ru/jour/article/view/21
DOI: https://doi.org/10.17650/1726-9784-2015-14-2-71-77
ID: 21

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Abstract

This article presents the results of preclinical study of antitumor activity of indolo[2,3-a]carbazoles N-glycosides derivative (LCS-1208) in pharmaceutical dosage form for intravenous administration - lyophilisate for injection. LCS-1208 high antitumor efficiency has been shown by different regimens of administration on tumors of diverse histogenesis: LCS-1208 exhibited increase of life span (ILS) 76% on lympoblastosis P-388 and ILS 76 % and 33 % recovery of Fisher lympadenosis L5178Y by 25 mg/kg daily intravenous administration during 5 days. Whereas LCS-1208 demonstrated high antitumor efficiency on solid tumors by 150 mg/kg single intravenous dosing: on LLC - tumor growth inhibition (TGI) 95% - 81% during 9 days and on RShM-5 (TGI 74% - 56% during 9 days). LCS-1208 appeared statistically significant TGI 51 % and 47 % on 3rd and 7th days after 150 mg/kg single intravenous dosing on established tumor. Comparative study of LCS-1208 substance and dosage form by intraperitoneal injection has shown that decrease of therapeutic dose to 110 mg/kg, which doesn’t induce death of animals, resulted only in dosage form antitumor effect (TGI 74-75 % during 8 days after the end of treatment).

Keywords

производное индолокарбазола, ЛХС-1208, перевиваемые опухоли, противоопухолевая активность, indolocarbazole derivative, LCS-1208, transplantable tumors, antitumor activity

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PRECLINICAL STUDY OF INDOLOCARBAZOLES N-GLYCOSIDES DERIVATIVE LCS-1208 ANTITUMOR ACTIVITY. REPORT I

Full Text

Abstract

Keywords

About the authors

References

Supplementary files