Understanding analgesic concepts does not need to be complicated. WEX Pharmaceuticals is determined to make pain management both achievable and easily understood, by providing insights into how pain operates and how certain treatments alleviate these conditions. Here, we discuss what sodium channel blockers are, how they work, and the medical conditions they help to manage.
In the world of analgesia, sodium channel blockers (SCBs) hold a unique position. In our previous article in this series, we explored prominent SCBs, their mechanisms, and how they are used in different medical contexts. In particular, we discussed their remarkable versatility – how many widely-known SCBs are used to treat more than one medical condition. For the SCB known as Tetrodotoxin (TTX), this is also the case. However, the ways in which TTX shows its medicinal versatility, and its lack of common side effects many SCBs present, that make TTX a unique step forward in the world of non-opioid analgesia.
TTX: How It Differs from Prior SCBs
While some SCBs demonstrate their versatility in treating unrelated conditions, TTX’s efficacy in clinical trials highlights its considerable potential in treating a wide variety of pain. From CINP to burn pain, TTX has shown promising medical potential in providing analgesic relief for a number of painful conditions. While this in itself is encouraging, a way in which TTX stands apart is its ability to function without the more severe side effects common to other prominent SCBs. A significant reason for this is TTX’s ability to function without crossing the blood-brain barrier.
The Blood-Brain Barrier: A Protective Shield
As we briefly discussed, the blood-brain barrier (BBB) regulates the passage of molecules between the circulatory and nervous systems. In doing so, it protects the brain from harmful substances and compositional fluctuations in the bloodstream while allowing essential nutrients to pass through. When certain SCBs penetrate this barrier, this can cause troubling side effects in the brain, such as sedation, euphoria, and respiratory depression. Due to TTX’s selective mechanism of action, it does not cross the BBB[1], meaning the brain can function relatively unimpeded as TTX performs its analgesic functions in the peripheral nervous system.
A Pathway to Safer SCBs
Its inability to cross the BBB is not the only reason why TTX has an attractive safety profile compared to other SCBs. While drugs like Lidocaine can sometimes trigger life-threatening allergic reactions, TTX’s side effects manifest themselves in comparably minor ways, with the most prominent being brief, mild-to-moderate tingling and numbness in the mouth, fingers, and toes.[2]
TTX represents a significant step forward in the advancement of sodium channel blockers. While it is still undergoing clinical trials and is not yet available for sale, TTX may prove to be a safe, reliable analgesic without many of the drawbacks traditionally associated with SCBs. As research progresses, TTX holds great promise for providing safe, effective, and targeted pain management solutions, and may one day prove to be a viable alternative not just to other SCB analgesics, but opioid pain solutions as well.
DISCLAIMER:
Halneuron ® is still being developed and tested in clinical trials and has not yet been
approved for sale by Health Canada, the United States Food & Drug Administration (US
FDA), or any equivalent medical authority. This article contains forward-looking
statements and information under applicable Canadian securities laws (collectively
“forward-looking statements”), including statements regarding the safety and
therapeutic efficacy and utility of Halneuron ® and Tetrodotoxin (TTX) as a peripheral-
acting, non-opioid analgesic. Statements in this document regarding future expectations,
beliefs, goals, plans, or prospects constitute forward-looking statements that involve
risks and uncertainties, which may cause actual results to differ materially from the
statements made. For this purpose, any statements that are contained herein that are
not statements of historical fact may be deemed to be forward-looking statements.
Without limiting the foregoing, the words “believes”, “anticipates”, “plans”, “intends”,
“will”, “should”, “expects,” “tolerates,” “projects,” “manages,” “reduces,” “shows,”
“promises,” “outperforms,” “affirms”, “acceptable”, “accepts”, “establishes”, “continued
advancement”, “in time,” “may prove to be,” and similar expressions are intended to identify forward- looking statements. You are cautioned that such statements are subject to a multitude of risks and uncertainties that could cause actual results, future circumstances, or events to
differ materially from those projected in the forward-looking statements. These risks
include, but are not limited to: those associated with the success of research and
development programs, the Company’s ability to raise additional funding and the
potential dilutive effects thereof, the regulatory approval process, competition, securing
and maintaining corporate alliances, market acceptance of the Company’s products, the
availability of government and insurance reimbursements for the Company’s products,
the strength of intellectual property, reliance on subcontractors and key personnel and
other risks detailed from time-to-time in the Company’s public disclosure documents and
other filings with the U.S. Securities and Exchange Commission and Canadian securities
regulatory authorities. Forward-looking statements are developed based on assumptions
about such risks, uncertainties and other factors, including, but not limited to: obtaining
positive results of clinical trials, obtaining regulatory approvals, TTX is a more potent
analgesic than standard analgesics, safety of product, effectiveness of drug, general
business and economic conditions, the Company’s ability to successfully develop and
commercialize new products, the assumption that the Company’s current good
relationships with third parties will be maintained, the availability of financing on
reasonable terms, the Company’s ability to attract and retain skilled staff, market
competition, the products and technology offered by the Company’s competitors, and the
Company’s ability to protect patents and proprietary rights. Forward-looking statements
are made as of the date hereof, and the Company disclaims any intention and has no
obligation or responsibility, except as required by law, to update or revise any forward-
looking statements, whether as a result of new information, future events, or otherwise.
[1] Melnikova, D. I., Khotimchenko, Y. S., & Magarlamov, T. Yu. (2018). Addressing the issue of tetrodotoxin targeting. Marine Drugs, 16(10), 352. https://doi.org/10.3390/md16100352
[2] Goldlust, Samuel A., et al. “Tetrodotoxin for Chemotherapy-Induced Neuropathic Pain: A Randomized, Double-Blind, Placebo-Controlled, Parallel-Dose Finding Trial.” Toxins, vol. 13, no. 4, 2021, p. 235, https://doi.org/10.3390/toxins13040235.
