"Dream, Dream, Dream! Conduct these dreams into thoughts, and then transform them into action."
- Dr. A. P. J. Abdul Kalam
24 Nov 2023
A recent scan of 27 million compounds has led to the discovery of a new molecule that surpasses existing pain medications, offering hope for more effective pain relief. The bi-institutional team behind the breakthrough identified compounds that outperformed popular pain medications, gabapentin and pregabalin, which are prescribed to millions of Americans.
Calcium channels, known for their role in pain signaling, were the focus of the research. The newly identified molecule was found to bind to an inner region of a calcium channel, indirectly regulating it and demonstrating superior performance to gabapentin, but without the harmful side effects associated with existing medications. This promising candidate has the potential to revolutionize pain management.
The research team, led by Rajesh Khanna, director of the NYU Pain Research Center, discovered a peptide derived from a protein called CRMP2 that could uncouple CRMP2 from the calcium channel. By blocking CRMP2 from binding to the channel, the new compound reduced calcium influx and neurotransmitter release, leading to a decrease in pain.
To create a viable drug based on the peptide, the researchers honed in on two specific amino acids responsible for inhibiting calcium influx and mitigating pain. Through a computer simulation and experimental testing, they identified a small molecule called CBD3063 as the most promising candidate for pain treatment.
Further studies using animal models of different types of chronic pain demonstrated CBD3063's efficacy in alleviating pain, comparable to gabapentin but without the side effects. The research team now aims to advance CBD3063-derived drugs to clinical trials, offering a safer and more effective alternative for chronic pain management.
This groundbreaking discovery marks a significant step forward in the pursuit of improved pain relief options for millions of individuals suffering from chronic pain.