Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida ® ) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms.

The non-nucleoside reverse transcriptase inhibitor VM1500A is approved for the treatment of HIV/AIDS in its N -acyl sulphonamide prodrug form elsulfavirine (Elpida ^® ). Biochemical profiling against twelve human carbonic anhydrase (CA, EC 4.2.1.1) isoforms showed that while elsulfavirine was a weak inhibitor of all isoforms, VM1500A potently and selectively inhibited human (h) h CA VII isoform, a proven target for the therapy of neuropathic pain. The latter is a common neurologic complication of HIV infection and we hypothesise that by using Elpida ^® in patients may help alleviate this debilitating symptom.