Biodistribution of [¹²⁵I]Aimpila (20 mg/kg) in the tumor and normal tissues, including the mammary gland tissue, after single oral dose was studied in BALB/c nude mice with T47D/ReCAF⁺⁺⁺ human breast tumor sensitive to this drug and in closely related BALB/c nude⁺mice without tumors. The maximum concentration of [¹²⁵I]Aimpila was in fact the same in the tumor and in the mammary gland, while the time course of its accumulation/elimination differed. The time of the maximum accumulation of the drug in the tumor was shorter and its persistence longer than in normal tissue. After 24 h, label concentration in the tumor was 4.5 times higher (p=0.002). Differences in the time course of label accumulation in the tumor were detected. The maximum ratio of tumor/blood concentrations of the preparation was recorded in 1 h after administration. [¹²⁵I]Aimpila and [¹²⁵I]alpha-fetoprotein accumulated in the tumor in comparable concentrations and were eliminated simultaneously at the same rate. The results of comparative analysis of accumulation of the labeled compounds in Aimpila-sensitive T47D/RECAF⁺⁺⁺ tumor from 0.5 to 9.0 h after drug administration could be interpreted as a result of possible receptor-mediated binding of the complex with the tumor at the expense of the alpha-fetoprotein transporting part. Differences in the parameters of [¹²⁵I]Aimpila biodistribution in the tumor and normal mammary tissue indirectly attested to selective antiproliferative activity of the complex.

01 Oct 2017·Tumor Biology

Binding characterization of the targeting drug AIMPILA to AFP receptors in human tumor xenografts

Article

Author: Tcherkassova, Janneta ; Borisova, Julia ; Smirnova, Galina ; Moro, Ricardo ; Treshalina, Helen ; Tsurkan, Sergei

The main objective of this study was the characterization of preclinical tumor models based on their expression of alpha-fetoprotein receptor (RECAF) for targeting cancer cells with a new non-covalent complex (AIMPILA) containing alpha-fetoprotein as the carrier and Atractyloside as an apoptosis-inducing agent. For that purpose, we measured the amount of RECAF in the homogenates of the grafted tumors T47D and SW620 and in HepG2 cell extracts. We also determined the alpha-fetoprotein binding specificity of the targeting drug AIMPILA using a solid-phase chemiluminescent assay with AIMPILA-Acrdidinium. We found that RECAF is practically absent from healthy mice tissues (100 Units/mg) where in malignant cells, the amount of alpha-fetoprotein receptors follows this order: T47D (9152 Units/mg) > HepG2 (4865 Units/mg) > SW620 (2839 Units/mg). This agrees with our findings regarding AIMPILA-induced tumor growth inhibition (T47D (T/C = 22%) > HepG2 (T/C = 51%) > SW620 (T/C = 70%), where T/C is the ratio of tumor volume in treated vs control animals). Our results demonstrate that the therapeutic response to the targeting drug AIMPILA strongly depends on the RECAF expression by human tumors and confirms the choice of the tumor models used for an AIMPILA preclinical study.

100 Deals associated with Glycoside apoptosis inducer/alpha-fetoprotein complex(Constab Pharmaceutical)

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Indication	Highest Phase	Country/Location	Organization	Date
Colorectal Cancer	Phase 1	-	Constab Pharmaceutical Inc.	-
Colorectal Cancer	Phase 1	Canada	-	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2007	Not Applicable	Metastatic Colorectal Carcinoma	12	Aimpila	jlwdxjjthq(uabcixrnaf) = a third developed nausea and vomiting leading to interruption of treatment, the only recorded significant adverse event vrvjdttidb (qvmjdwoqws )	-	20 Jun 2007

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Glycoside apoptosis inducer/alpha-fetoprotein complex(Constab Pharmaceutical)

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