Amino thiol compounds and compositions for use in conjunction with cancer therapy

Patent Number: 7,314,959

One of the important areas of drug development is protecting stem cells and healthy tissue from the damaging effects of cytotoxic chemotherapy and radiation therapy. In fact, a "stem cell therapy" that has become a multi-billion dollar product is the use of G-CSF to stimulate hematopoietic recovery after cancer therapy or bone marrow transplantation. In fact, numerous patents have been filed for all sorts of ways of stimulating hematopoiesis or protecting the bone marrow compartment using agents such as Oxypurine nucleosides, mutants of interleukin-3, stromal stem cells, and Cofilin a protein which binds actin and is believed to be involved in disassembly of actin filaments is a protein which binds actin and is believed to be involved in disassembly of actin filaments.

In the current patent the inventors cover the composition of matter for a series of polyamine and amino thiol compounds that have protective activity on hair loss, dermatitis, mucositis or gastrointestinal distress caused by chemotherapy or radiotherapy. One of the proposed mechanisms of actions of these compounds is protection of epidermal and follicular matrix stem cells.

Polyamines are interesting since they have been associated with tumor suppression of immunity (Kano Y et al. Increased blood spermine levels decrease the cytotoxic activity of lymphokine-activated killer cells: a novel mechanism of cancer evasion. Cancer Immunol Immunother. 2007 Jun;56(6):771-81), so perhaps the analogues generated in this patent are not immune suppressive. Another interesting fact about some polyamines is that they can directly bind DNA since the amine group is positively charged and the DNA backbone is negative. Since polyamines can alter the B-DNA structure (which is sensitive to free radicals), the treatment with polyamines may temporarily protect from radiation. However it is interesting to ponder whether this would have any epigenetic effects as well.

View this patent on the USPTO website.