PRC050

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PRC050
PRC050 is an arylalkanolamine NSDRI (c.f. SNDRI) currently under development by the Mayo Clinic.[1]

Since this drug contains 2 chiral carbons, clearly there is 4 possible isomers: (SS), (RR), (RS), and (SR);

often referred to as a diastereomeric pair of enantiomers.

PRC050 is racemic PRC200-SS.

Most of the activity resides in the (SS) enantiomer (hence a high eudysmic ratio).

For this reason it would be ideal to crystallize out the (SS) enantiomer only.

However in "real life" situations it is not always cost effective to do this, or is not worth the effort.

This is particularly true if the unrequired isomer is simply an inactive "dummy" and does not add to the overall toxicity of the compound.

^That is not always the case though.

However, methylphenidate is a specimen example of where the unwanted isomer is usually not separated so that profits can be maximized.

This helps buy time. It speeds up process development meaning the product can get put onto the market quicker.

The whole time that the racemic product is being sold money can be funneled back into process development of a single enantiomer.

As the patent for the racemic drug is about to expire, a new application is filed for a single enantiomer of the same drug.

Sales reps draw up a dozen reasons why having only a single enantiomer is in some way "superior" to the racemic version.

References

  1. ↑ Y. Liang, E. Richelson. Triple Reuptake Inhibitors: Next-Generation Antidepressants. Primary Psychiatry. 2008;15(4):50-56.


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