AlzeCure Pharma is developing a novel clinical drug candidate for peripheral neuropathic pain, which is based on the seminal discoveries of TRPV1 by Professor Julius, and for which he is awarded the Nobel Prize in Medicine 2021.
David Julius has together with Ardem Patapoutian recently been awarded the 2021 Nobel Prize in Physiology or Medicine. Prof. Julius’s work has focused on how we can sense heat, cold, and chemical irritants, leading to new insights about the fundamental nature of pain and new targets for pain therapy. His fundamental research led to the identification and cloning of the specific protein responsible for the sensation of burning pain, TRPV1, in 1997.
TRPV1 are specialized cation channels, primarily expressed in sensory neurons. TRPV1 are activated by e.g. heat, acidic pH and capsaicin in “hot” peppers, and play a crucial role in heat sensation and nociception. They are sensitized from noxious stimuli, leading to inflammatory conditions and pain. In chronic pain states, TRPV1 are up-regulated on neurons, have reduced stimulation thresholds, and cause an increased perception of pain. Interestingly, it is also upregulated in the skin of individuals with certain types of neuropathic pain.
ACD440 – a TRPV1 antagonist
A potent topical compound acting by inhibiting the TRPV1 channel would be a novel non-opioid mechanism to obtain an analgesic effect without the associated side-effects observed with the existing therapies, describes AlzeCure.
ACD440 is a TRPV1 antagonist that is in the clinical development by AlzeCure Pharma, and the company’s aim is to develop a new topical, local treatment for neuropathic pain. The drug candidate, an important strategic in-licensing arrangement carried out in January 2020, and has its origins in Big Pharma. The compound is being developed for local use, thereby keeping the systemic exposure very low, while the concentration of the compound locally can be kept high for maximum analgesic effect, states AlzeCure.
In December 2020, AlzeCure initiated a phase Ib clinical trial for ACD440 according to plan to assess both tolerability and early signals of efficacy. The positive study results were communicated during April 2021. AlzeCure is currently preparing for a phase II study with the drug candidate. The compound is currently being developed as a gel for topical use, but AlzeCure is also evaluating other formulations such as spray or patch to further broaden the area of indication.
Photo of Martin Jönsson, CEO, AlzeCure Pharma