Malignant, long-lasting pain is an imminent component in advanced cancer. Such pain is still not successfully managed since oftentimes it shows a complex nociceptive-neuropathic mechanism. Morphine is still a major drug of choice in terminal cancer treatment. However, there is much doubt around the use of such therapy because of common undesirable side effects, which may hinder the quality of life to a great extent. Hence, the pressing need for development of novel opioid analgesics demonstrating high analgesic and antitumor potency and simultaneously lack the shortcomings typical for morphine. Particularly, novel neuropeptide analogues offer numerous opportunities for the development of new analgesics and show promise in alleviation of cancer-evoked pain. In a murine skin cancer pain model developed by an intraplantar inoculation of B16T0 melanoma cells signs of thermal hyperalgesia were attenuated by repeated daily injections of biphalin a dimeric enkephalin analog. The antinociceptive effect of biphalin was greater in the tumor bearing paw than in the contralaeral paw. Apart from showing an antinociceptive effect in the periphery, biphalin also exerted a central antinociceptive effect as measured in the tail-flick test. Thus, biphalin, may become a useful drug in cancer pain treatment because it also shows low tolerance liability and relatively high antinociceptive potency.

Financial support:  6FP STREP Normolife grant (LSHC-CT-2006-037733)

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