Painkiller aimed at promising target now studied in phase III trial

The global opioid crisis has shown the growing need for adequate analgesics that do not have the disadvantages of opioids. 'An analgesic that targets peripheral pain nerves and not the central nervous system is unlikely to be addictive. Also, the respiratory depression that we usually see with opiates is a CNS effect that will not be a problem with peripherally acting analgesics,' said Prof. Geert Jan Groeneveld, CHDR’s CMO/CSO and head of the Pain group.

In recent years, the Pain group investigated several candidate drugs targeting the conduction in pain nerves. They specifically blocked voltage-gated sodium channels which play a crucial role in nerve signal transduction. The sodium channels NaV 1.7 and NaV 1.8 occur mainly in pain nerves. Therefore, blocking these channels offers opportunities for pain relief without serious side effects. Non-selective sodium channel blockers such as lidocaine can be very effective locally, but serious side effects occur when they are administered systemically.

The Pain group investigated several compounds that specifically block sodium channel NaV 1.8. The PainCart®, the battery of pain tests that Groeneveld and his team validated for drug development, proved valuable in demonstrating the effect of these compounds in healthy volunteers. Similar compounds are currently being investigated by the Experimental Medicine group using excitability methods. Groeneveld: 'One of our clients, Vertex Pharmaceuticals, has announced that a NaV 1.8 blocker similar to the one we investigated in the early phase of drug development, has successfully progressed to phase III, where it is now being studied in patients with neuropathic pain. It is a special occasion when a first-in-class compound reaches that important milestone, and I am proud of our group for being able to contribute to that.'