[BillJames]

Why have such prodrugs if they are not utilised for the purpose of increasing the rate of transportation across the cell membrane? Google doesn't tell me the answer, oddly enough

[macman104]

Another example is when prodrugs may not be susceptible to metabolism in the presystemic passing before entering the target cell, but maybe the drug itself is.  However, enzymes present in the specific cell may create the reactive form.  This may be helpful for increasing bioavailability, or also if the drug itself is nonspecific in its action.  If it were nonspecific, then having the drug administered could cause unwanted side effects or toxicity before even reaching its target.

[BillJames]

Awesome, that makes a lot of sense. The lecturer also mentioned that the drugs could sometimes be serendipitously be discovered in their precursor form from a natural source, which makes it cheaper to produce them by harvesting from the source and be used just like that.

Thanks!

[macman104]

Awesome, that makes a lot of sense. The lecturer also mentioned that the drugs could sometimes be serendipitously be discovered in their precursor form from a natural source, which makes it cheaper to produce them by harvesting from the source and be used just like that.

Well, that may be sometimes true, but not always, especially if the drug becomes very popular and harvesting/isolation cannot keep up.  For a perfect example, see the story behind Taxol.