Neuropathic Pain

neuropathic painNeuropathic pain is a debilitating nervous system disorder which affects 5% of the general population and 25% of diabetics worldwide.  This disorder results from nerve damage caused by various ailments such as:  diabetes, cancer, stroke, vitamin deficiency, physical injury, and multiple sclerosis.  Unlike acute pain which protects the body from further injury, neuropathic pain has no physiological benefits, and it seriously impairs quality of life.

It has become a global medical problem because a large percentage of the general population is aging.  Furthermore, the ongoing obesity epidemic has led to an alarming increase in Type II diabetes among the general population.  Due to these dire circumstances, the current market for neuropathic pain treatment is estimated at $2.4 billion and is expected to grow to $7.5 billion by 2020 in 7 major markets:  US, UK, Japan, France, Germany, Italy, & Spain.

Neuropathic pain is still difficult to treat because the available medications are neither specific nor effective, and they often have undesirable side effects.  In fact, some medications prescribed for neuropathic pain are used to treat other central nervous system disorders.  These drugs include gabapentin (epilepsy), duloxetine (anxiety), and carbamazepine (depression).  Even chemotherapeutic drugs such as taxol and cis-platin can cause neuropathic pain.  Morphine is also prescribed because it is a potent analgesic, but there is a serious risk of abuse and tolerance among patients.  Yet, morphine and gabapentin remain the drugs of choice to treat chronic neuropathic pain.

Recent studies have revealed two new potential targets for treating chronic neuropathic pain – sigma-1 receptors (s1R) and serotonin 5-HT7 receptors.  It has been shown that pain is significantly reduced by either blocking the s1R receptors found in the pain-producing pathway or by activating 5-HT7 receptors found in the pain-reducing pathway.

DAYA has discovered a new, highly potent, and orally active small molecule (DDD-028) which binds to both s1R and 5-HT7.  In animal model studies, a 1 mg/kg orally administered dose of DDD-028 significantly reduced neuropathic pain within 30 minutes.  It was also found to be 10 times more potent than morphine and 180 times more potent than gabapentin.  The results from the study suggest that DDD-028 may be working simultaneously at both these receptors to produce the desired analgesic effect.

DDD-028 is now ready to be put through a full preclinical evaluation for IND submission, and DAYA is seeking suitable commercial partners to introduce this promising medication into the market.