Surprisingly, clinical trials of drug therapies aimed at targeting CCR2 receptors have failed. The only drugs targeting chemokine receptors that have been liscensed are those resulting in CCR5 inhibition for HIV/AIDS treatment and CXCR4 blockade for autologous transplantation in non-Hodgkin’s lymphoma1. This may be due to:
1) A lack of potency by targeting a single chemokine receptor
2) Activity of the rodent receptor not correlating with the amount in humans
3) Selectivity of the antagonist – targeting of other chemokine receptors unintentionally. This leads to questions of safety2.
Here is a summary table of potential CCR2 antagonists that have been largely characterised in rodents, with some going as far as being studied in phase II trials. Some I have mentioned in previous posts but hopefully you will find it useful for them to be collaborated in a single place.
As you can see, there is a vast amount of research going on out there. However, the failure of most of these agents on entering the clinical trial phase in humans, leads to the questioning of how useful CCR2 blockade actually is. For this reason, I will have a brief look at the alternatives out there and perhaps some solutions so that CCR2 can be transferred into clinical use.
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