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

  • J Enzyme Inhib Med Chem. 2021 Dec;36(1):1056-1060. doi: 10.1080/14756366.2021.1927007.
Claudiu T Supuran  1 ,  Alessio Nocentini  1 ,  Elena Yakubova  2 ,  Nikolay Savchuk  2  3 ,  Stanislav Kalinin  4 ,  Mikhail Krasavin  4
Affiliations
  • 1. Neurofarba Department, Section of Pharmaceutical Sciences, University of Florence, Florence, Italy.
  • 2. Viriom Inc, San Diego, CA, USA.
  • 3. ChemDiv Inc, San Diego, CA, USA.
  • 4. Institute of Chemistry, St. Petersburg State University, St. Petersburg, Russia.
PMID: 34000969 DOI: 10.1080/14756366.2021.1927007
Abstract

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) hCA 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.

Keywords
N-acyl sulphonamide prodrug; Non-nucleoside reverse transcriptase inhibitor; elsulfavirine; human carbonic anhydrase; isoform selectivity; neuropathic pain.
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