Enzastaurin

We have said before that given the much larger amount of money available to cancer and heart disease, and due to the recently recognized link with inflammation in these conditions, that central pain might well be cured as a spinoff. Here is a new drug that stops Protein Kinase C.


Any of a number of articles here at painonline describe in detail the role of Protein Kinase C in pain chemistry. Taking that as a given, it is interesting to watch the studies being performed on Enzastaurin, a potent blocker of Protein Kinase C. Enzastaurin is said to be owned by Lilly.

Interest in the drug has been almost exclusively on its ability to block angiogenesis (vessel formation), one of the avenues of cancer treatment. However, the drug is a potent blocker of Protein Kinase C (PKC). PKC is probably necessary for central pain to be expressed. This is very interesting. It shouldn’t be too hard to change whatever part of Enzastaurin is responsibie for inhibiting angiogenesis and just use the PKC block. Alternatively, we may find out HOW and WHY angiogenesis and PKC action are linked and thereby develop new PKC blockers.

Robertson et al writing in J Clin Oncol (2007) in an article entitled “Phase II Study of Enzastaurin, a Protein Kinase C Beta Inhibitor, in Patients With Relapsed or Refractory Diffuse Large B-Cell Lymphoma” we learn that Enzastaurin is relatively nontoxic, causing one case of hypomagnesemia, but magnesium can be replaced readily. If this drug is safe, and apparently it is, there is no reason not to study it in central Pain.

We hope those drug firms who visit here will consider trials of this drug for nerve injury pain in animals, and possibly humans.