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

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

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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