5 ms·

Voltage-Gated Sodium Channels: Therapeutic Targets for Pain (2009) [pdf]

12 points by snake117 11y ago

refurb 11y ago
I work for a company that has a Nav1.7 candidate in the pipeline. It would be great if it was successful, but there have been many failures so far. The challenge really is that opioids work really well. The addiction potential is unfortunate, but they are very effective against pain (I acknowledge not all pain).
- jhartmann 11y ago
  I'm curious, what is the name of the potential compound? I have to take opioids for chronic pain due to Ankylosing Spondylitis and would love to stay informed on potential alternatives.
  - refurb 11y ago
    The molecule I'm thinking of has no name at this point, it's that early on. There are a number of companies working on the Nav1.7, and you can find them via google search. I think the earliest launch is close to 2020. The anti-NGF are another pain MOA that seems promising. Pfizer is moving into phase 3 in the near-term.
- noir_lord 11y ago
  I currently take Gabapentin for Neuropathic pain and numbness and it's had a remarkable effect on my quality of life. It's awesome to see research on the mechanism's behind that type of drug.
  - refurb 11y ago
    In fact, gabapentin was one of the exceptions I was thinking of. Opioids don't work well for neuropathic pain, but gabapentin was a huge leap forward. To give you a sense as to how difficult drug discovery is, just look at the discovery of gabapentin. GABA is a inhibitor neurotransmitter. The idea behind gabapentin was to create a molecule that looks just like GABA, but can't be broken down by GABAase. The logical result is more GABA would be floating around, inhibiting the transmission of painful nerve signals. The funny part is, the major effect of gabapentin isn't even through the GABA neurotransmitter. It actually binds to the alpha-2-delta subunit of calcium channels and prevents the release of excitatory neurotransmitters. The discover of gabapentin was completely serendipitous!
    - noir_lord 11y ago
      I'm incredibly glad it was discovered anyway, I have syringomyelia (cyst in spinal cord that pushes on nerves), the consistent pain and numbness was pretty bad and going onto Gabepentin wasn't easy but once I got used to it the improvement was remarkable. I went from a daily pain score of around 4-5 to 2, simply incredible, hands down one of the most effective medications I've ever taken. Also I should note that I had essentially none of the side effects the internet will have you fear, if anything the marked reduction in pain was way more beneficial than I expected, mentally I feel closer to 100% than I have in a long time. I'm also glad that Pregablin exists as my doctor mentioned that it's possible to cycle between one and the other if one begins to lose efficacy though at present I'm not screwing with what works well.

12 points by snake117 11y ago

I work for a company that has a Nav1.7 candidate in the pipeline. It would be great if it was successful, but there have been many failures so far. The challenge really is that opioids work really well. The addiction potential is unfortunate, but they are very effective against pain (I acknowledge not all pain).

jhartmann 11y ago
I'm curious, what is the name of the potential compound? I have to take opioids for chronic pain due to Ankylosing Spondylitis and would love to stay informed on potential alternatives.
- refurb 11y ago
  The molecule I'm thinking of has no name at this point, it's that early on. There are a number of companies working on the Nav1.7, and you can find them via google search. I think the earliest launch is close to 2020. The anti-NGF are another pain MOA that seems promising. Pfizer is moving into phase 3 in the near-term.
noir_lord 11y ago
I currently take Gabapentin for Neuropathic pain and numbness and it's had a remarkable effect on my quality of life. It's awesome to see research on the mechanism's behind that type of drug.
- refurb 11y ago
  In fact, gabapentin was one of the exceptions I was thinking of. Opioids don't work well for neuropathic pain, but gabapentin was a huge leap forward. To give you a sense as to how difficult drug discovery is, just look at the discovery of gabapentin. GABA is a inhibitor neurotransmitter. The idea behind gabapentin was to create a molecule that looks just like GABA, but can't be broken down by GABAase. The logical result is more GABA would be floating around, inhibiting the transmission of painful nerve signals. The funny part is, the major effect of gabapentin isn't even through the GABA neurotransmitter. It actually binds to the alpha-2-delta subunit of calcium channels and prevents the release of excitatory neurotransmitters. The discover of gabapentin was completely serendipitous!
  - noir_lord 11y ago
    I'm incredibly glad it was discovered anyway, I have syringomyelia (cyst in spinal cord that pushes on nerves), the consistent pain and numbness was pretty bad and going onto Gabepentin wasn't easy but once I got used to it the improvement was remarkable. I went from a daily pain score of around 4-5 to 2, simply incredible, hands down one of the most effective medications I've ever taken. Also I should note that I had essentially none of the side effects the internet will have you fear, if anything the marked reduction in pain was way more beneficial than I expected, mentally I feel closer to 100% than I have in a long time. I'm also glad that Pregablin exists as my doctor mentioned that it's possible to cycle between one and the other if one begins to lose efficacy though at present I'm not screwing with what works well.