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 are currently one of the most investigated candidates in the field. Pre-clinical studies with TRPV1 antagonists have shown promising analgesic effects 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 ankyrin 1, TRPA1, is related to TRPV1 as it also belongs to the family of TRP ion channels. TRPA1 is involved in pain sensation, itchiness, 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 toward this promising pain target.

About treatment of severe pain

Defined as an unpleasant sensation associated with the injury of tissue, the concept of pain covers 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 (damage to the peripheral and the central nervous system) and nociceptive pain (acute pain stemming from harmful stimuli).

It is estimated that over 50 million individuals in Europe are afflicted with neuropathic pain, and of these, 35 million suffer from severe pain1,2. The conditions have proven difficult to treat and while opioids are useful agents, an opioid addiction epidemic has arisen as a result.

The market potential of replacing opioid treatments

In the US, the economic burden of prescription opioid misuse has been estimated at more than USD 78 billion annually by the US Centers for Disease Control and Prevention (CDC)3. Analysts estimate that the opioid market for the treatment of acute and chronic pain totaled over USD 13.4 billion in 2015 in the US alone. The cost is expected to rise despite national efforts to limit and prevent the epidemic.

The prescription pain treatment market is consequently expected to increase to more than USD 34 billion by 2020. With regulatory agencies and nations eager to curb opioid abuse, there is a significant interest in new solutions for managing 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