Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist

a technology of adenosine receptor and a drug composition, applied in the field of cancer, can solve the problems of increasing the morbidity and actual of patients with life-threatening diseases, limiting the administration of larger, potentially more effective doses of chemotherapy to patients with malignancies, and reducing the number of hospital stays. , to achieve the effect of inhibiting the proliferation and growth of tumor cells, and reducing the number of hospital stays

Inactive Publication Date: 2006-04-20
CAN-FITE BIOPHARMA LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006] In accordance with the present invention it was found that adenosine A3 receptor agonists (A3RAg) have a dual effect in that they inhibit proliferation of malignant cells on the one hand, and counter toxic side effects of chemotherapeutic drugs on the other hand. Specifically, the A3RAg compounds inhibit proliferation and growth of tumor cells, synergize with an anti-tumor cytotoxic drug in reducing the tumor load, induce proliferation and differentiation of bone marrow cells and white blood cells and counter toxic side effects of other drugs, particularly chemotherapeutic drugs. Furthermore, it was discovered in accordance with the invention that the A3RAg exerts t

Problems solved by technology

It causes more life threatening patient morbidity and actual mortality than any other chemotherapeutic side effect and may result in an increased number of hospital stay days.
In addition, drug induced myelosuppression lim

Method used

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  • Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist
  • Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist
  • Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist

Examples

Experimental program
Comparison scheme
Effect test

example 1

Effect of Adenosine and Adenosine Receptor Antagonists and Agonists on G-CSF Production and Bone Marrow Cell Proliferation

[0193] To test the assumption that adenosine exerts its biological effect through stimulation of G-CSF production, normal cells were cultured in the presence adenosine or an adenosine agonist or antagonist.

[0194] For this purpose, bone marrow cells obtained from the femur of C57BL / 6J or ICR mice were first disaggregated by passing through a 25G needle. Then, the cells (3×105cells / well, in 96 microtiter plates) were incubated with RPMI medium containing 10% fetal bovine serum (FBS) in the presence of adenosine (25 μM). Adenosine or agonists to the Al and A3 adenosine receptors—CPA (an A1RAg, 0.01 μM), CCPA (an A1RAg, 0.01 μM), or IB-MECA (an A3RAg, 0.01 μM), were added to the bone marrow cultures in the absence of adenosine; an A1 adenosine receptor antagonist, DPCPX (0.1 μM), was added to a bone marrow culture in the presence of adenosine (25 μM).

[0195] Cultur...

example 2

Modulation of Tumor Cell Growth by Adenosine and its Agonists

[0201] Nb2-11C rat lymphoma cells (1.2×104 cells / ml) were incubated for 48 hours in 96 well microtiter plates with 1 ml RPMI medium containing 5% fetal bovine serum. Either 25 μM adenosine, 0.01 μM of an adenosine receptor agonists (CPA, an A1RAg; DPMA, an A2RAg or IB-MECA, an A3RAg) or 0.1 μM of an adenosine receptor antagonists (DPCPX, an A1RAn; DMPX, an A2RAn; or MRS-1220, an A3RAn) in combination with adenosine (25 μM) was added.

[0202] Cultures containing cells suspended in RPMI medium with 5% FBS served as controls for the above detailed experiment. Extent of cell proliferation was measured by a cell count assay.

[0203] The results shown in FIGS. 5A and 5B, are comparable to the inhibition with adenosine. As can be seen, the proliferation of Nb2-11C cells was markedly inhibited following incubation with IB-MECA, an A3RAg. No growth inhibition was seen in the presence of CPA, an A1RAg, and a lower growth inhibition w...

example 3

Adenosine A3 Receptor Agonists Exert a Differential Effect on Tumor and Normal Cells

[0206] The effect of adenosine, A3RAns and A3RAgs, on the growth of tumor cells was examined, following the experimental procedure described above.

[0207] Briefly, Nb2-11C lymphoma or bone marrow cells were incubated in the presence of either adenosine, or IB-MECA. The dual effect of A3RAg is inhibiting the growth of tumor cells while stimulating the proliferation of bone marrow cells is depicted FIGS. 7A and 7B.

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Abstract

Adenosine receptor agonists, particularly an agonist which binds to the A3 adenosine receptor, are used for induction of production or secretion of G-CSF within the body, prevention or treatment of toxic side effects of a drug or prevention or treatment of leukopenia, particularly drug-induced leukopenias; and inhibition of abnormal cell growth and proliferation.

Description

FIELD OF THE INVENTION [0001] The present invention is generally in the field of cancer and concerns a cancer therapy or a therapy intended to counter the side effect of cancer treatment. BACKGROUND OF THE INVENTION [0002] Myelotoxicity is a prevailing, severe, complication of chemotherapy and is one of the factors that limit the administrable dose of the chemotherapeutic drug. It causes more life threatening patient morbidity and actual mortality than any other chemotherapeutic side effect and may result in an increased number of hospital stay days. In addition, drug induced myelosuppression limits the administration of larger, potentially more effective doses of chemotherapy to patients with malignancies. Several approaches to resolve this adverse event have included the use of lithium, prostaglandin E, interferon, lactoferrin and the growth factors granulocyte-macrophage colony-stimulating factor (GM-CSF) and granulocyte-colony stimulating factor (G-CSF). To date, use of growth f...

Claims

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Application Information

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IPC IPC(8): A61K31/7076A61K31/695A61K31/52A61K31/00A61K45/00A61K31/70A61K31/708A61K45/06A61P35/00A61P35/02A61P39/00A61P43/00
CPCA61K31/00A61K31/52A61K31/70A61K31/706A61K31/7076A61K31/708A61K45/06A61K31/505A61K2300/00A61P35/00A61P35/02A61P37/00A61P39/00A61P43/00
Inventor FISHMAN, PINA
Owner CAN-FITE BIOPHARMA LTD
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