Pharmaceutical compositions comprising of arsenous acid, its sodium salt and its derivatives intended for the treatment or urogenital cancer and its metastasis

Abstract

The present application relates to pharmaceutical compositions and methods for treatment of urogenital diseases and bone metastasis in a human, which pharmaceutical composition contains an effective amount of arsenous acid alkaline or earth alkaline metal salt and/or a pharmaceutically acceptable adjuvant. According to the present invention, the alkaline arsenous acid metal salt is sodium meta-arsenita (AsO₂Na) or potassium meta-arsenite (AsO₂K). The effective amount of arsenous acid alkaline or earth alkaline metal salt is 0.0001-1500 mg/kg, preferably 1-1000 mg/kg, more preferably 1-150 mg/kg, and most preferably 50-100 mg/kg of body weight/day. The administration form of the pharmaceutical compositions of the invention is preferably oral, such as a tablet, capsule, powder and/or solution with a pharmaceutically acceptable carrier, diluent or excipient.

Description

1. INTRODUCTION[0001]Cancer is a significant health problem in the world. Although advances have been made in cancer detection and treatment, no vaccine or other universally successful preventive or therapeutic method is currently available. Management of the disease currently relies on a combination of early diagnosis and aggressive treatment, which may include one or more of a variety of therapies such as surgery, radiotherapy, chemotherapy and hormone therapy. While such therapies provide benefit to many patients, a high mortality continues to be observed for many cancers. The development of improved anti-tumour agents would facilitate cancer prevention and treatment.[0002]Unfortunately, cancer is the leading cause of death, second only to heart disease, of both men and women. In the fight against cancer, numerous techniques have been developed and are the subject of current research directed to understanding the nature and cause of the disease and to providing methods for the co...

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Benefits of technology

[0051]The Inventor has explored the potency of three arsenic compounds of different valence and methylation in panels of human tumour cell lines in vitro, arsenous acid sodium salt (As3+), dimethylarsinic acid (As5+) and arsenic acid (As5+). Surprisingly arsenous acid sodium salt was the most potent and showed anti-tumour activity in a human tumour model in vivo, reason to develop arsenous acid sodium salt further as a novel arsenic compound. Arsenous acid sodium salt surprisingly was more potent in vitro and showed differential activity in leukaemia, melanoma and mammary cancer lines than As2O3. Arsenous acid sodium salt is surprisingly capable of shortening telomeres of human cancer cells, inducing cellular senescence and chromosomal abnormalities, but does not directly inhibit the telomerase activity. The effects indicate that arsenous acid sodium salt is a telomere inhibitor. Arsenous acid sodium-salt was rapidly absorbed after both i.v. and p.o. administration and remained in the plasma for prolonged periods. Surprisingly the bioavailability of oral arsenous acid sodium salt was ...

Problems solved by technology

Intravenous (iv) administration is a major source of discomfort and stress for cancer patients and approximately 90% of patients asked, express a preference for oral versus iv chemotherapy, predominantly because of the convenience of administration outside a clinical setting or current concerns about previous problems with intravenous access.

Chemotherapy has not yet been shown to be helpful in treating cancer of th...

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