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Resiniferatoxin is a molecule classified as an ultra-potent TRPV1 agonist (transient receptor potential cation channel subfamily V member 1). It is unlike anything currently available to manage hard-to-control chronic inflammatory pain.
In pilot studies, RTX administered as a one-time spinal injection demonstrated clinical effectiveness in relief of canine bone cancer pain. (Bone cancer pain is believed to be one of the most excruciating and difficult to control types of pain a patient can endure.)
Source: Brown et al, Anesthesiology 2005; 103:1052-9
Although the potential benefits and early results are very encouraging, we want to highlight that treating animals through spinal injections is a delicate procedure that requires a day of hospitalization and is to be performed by qualified specialists (veterinary surgeons, neurologist or anesthesiologist).
It is also important to note that systemic adverse events can be expected at therapeutic and higher doses. Initial studies showed that patients could show accelerated heart rate and increased blood pressure spikes during the administration, and some rare occurrences suggest that partial paralysis and difficulty rising at the higher doses might also occur.
The safety profile of the drug is being carefully studied to determine the best therapeutic protocol to maximize benefits and minimize risks to the patients.
The potential for such an approach is so exciting that resiniferatoxin is also being developed for human cancer pain applications by Scintilla Pharmaceuticals.
How does it work precisely?
Chronic persistent inflammatory pain is primarily transmitted through activation of afferent C- fiber pathways (and some A delta fibers), whereas the sense of touch and acute pain signals are transmitted through different subsets of nerves. Therefore, the C-fibers are a prime target for research into chronic pain control.
Medical professionals typically treat chronic pain with NSAIDs to reduce pain and inflammation locally or with opioids to modify the brain’s perception of pain levels centrally. Despite the drugs’ effects, key receptors continue to signal tissue damage. Over time, the central nervous system tends to exacerbate pain signals (called sensitization to pain). This physiological mechanism loop explains why most pain medications lose effectiveness over time and require dose adjustments or a change in therapy (class of drugs used).
RTX is a purified, active, non-opioid compound that is naturally selective and strongly binds to calcium channel gates found on C-fibers (and some A delta nerve fibers). With their calcium channel gates blocked open, substantial amounts of calcium ions enter the cell body, naturally triggering cellular programmed death (apoptosis).
Control
In green afferent nerves (transmitting pain signals) unaffected by a control solution.
RTX Dosing
Treated with resiniferatoxin, the dorsal horn of the spinal cord shows no immune-fluorescence to substance P staining (indicating that the afferent nerves have been ablated)
RTX permanently interrupts chronic excessive pain signal transmission without affecting other key signals responsible for pressure sensitivity, motor coordination, or acute pain signals that rely on distinct types of nerve wires. Interrupting the pain signal loop helps break the neurogenic inflammation cycle, which in turn helps maintain normalized pain levels.
When injected into the spinal space (epidural) the effect is permanent with just one injection. RTX is so selective, and potent, that the mechanism could be likened to “chemical surgery.”
Click the links to access recently published materials related to RTX
Understanding Resiniferatoxin potential for pain control
Resiniferatoxin potential benefits against inflammatory disease processes
Set to deliver break-through technologies for companion animal healthcare
Our most exciting pain management solution, currently in development
