aTRPV1: Lead candidate in pain

The pain receptor, transient receptor potential vanilloid 1 (TRPV1), is an ion channel that has a central role in peripheral nociception and neurogenic inflammation. As the next generation of pain therapy, TRPV1 antagonists is one of the most currently investigated in the field. Pre-clinical studies with TRPV1 antagonists have shown promising analgesic effect in several pain models but due to temperature-related side effects many development programs have been discontinued. Oblique Therapeutics has developed antagonistic stimuli-selective antibodies against TRPV1 in order to maximize pain relief and circumvent side effects

aTRPA1: A promising pain target

The transient receptor ankryrin 1, TRPA1, is related to TRPV1 as it also belongs to the family of TRP ion channels. TRPA1 is involved in pain sensation, itch, inflammation and respiratory diseases. It is suggested to be involved in cold hypersensitivity and is activated by temperature, mustard oil, cinnamon and wasabi. Oblique Therapeutics is developing antagonistic antibodies towards this promising pain target.

About treatment of severe pain

Defined as an unpleasant sensory associated with the injury of tissue, the concept of pain is a broad and multifaceted spectrum of chronic and acute conditions. While instances of minor pain are successfully managed with nonsteroidal anti-inflammatory drugs, such as Ibuprofen, severe challenges arise in the treatment of neuropathic pain (damages to the peripheral and the central nervous system) and nociceptive pain (acute pain stemming from harmful stimuli). It is estimated that more than 50 million individuals in Europe are afflicted with neuropathic pain, and, of these, 35 million suffers from severe pain.1,2 The conditions have proven difficult to treat and useful agents such as opioids have arisen as an epidemic in itself due to its addictive nature.

The market potential of replacing opioid treatments

In the U.S., the economic burden of prescription opioid misuse has been estimated to more than 78 billion USD a year by the U.S. Center for Disease Control and Prevention (CDC).3 Analysts estimate that the opioid market for the treatment of acute and chronic pain totaled to over 13.4 billion USD during 2015 in the US alone. The cost is expected to grow despite many national efforts to limit and prevent the epidemic. The market for prescription pain market is consequently expected to increase to more than 34 billion USD by year 2020. With regulatory agencies and nations eager to curb the abuse of opioids, there is a significant interest in new novel solutions for the management of severe pain.

1. Torrance N, Smith BH, Bennett MI, Lee AJ (April 2006). ”The epidemiology of chronic pain of predominantly neuropathic origin. Results from a general population survey”. J Pain. 7 (4): 281–9. 2. Bouhassira D, Lantéri-Minet M, Attal N, Laurent B, Touboul C (June 2008). ”Prevalence of chronic pain with neuropathic characteristics in the general population”. Pain. 136 (3): 380–7. 3. Florence CS, Zhou C, Luo F, Xu L. The Economic Burden of Prescription Opioid Overdose, Abuse, and Dependence in the United States, 2013. Med Care. 2016;54(10):901-906. 4. U.S. Markets for Pharmacologic and Device-Based Approaches to Pain Management, April 2016