BromopyruvicacidisahexokinaseIIinhibitorandaneffectiveantitumoragent.Thecharacteristicsof3-bromopyruvateinvitroandinvivohavebeenreportedinthescientificliteraturesincethe1940s.Becauseitisahighlyreactivealkylatingagentanditisinherentlyunstable,ithadbeendescribedasametabolicpoison.ResearchatJohnsHopkinshassuggestedthat3-bromopyruvatecouldbeusedtoselectivelykillcancercells,whileleavingnormalcellsintact.Recently,theFDAacceptedanINDapplicationfortheuseof3-bromopyruvateforaPhaseIclinicaltrialinlivercancer.(lastupdated:5/23/2016).
http://www.medkoo.com/products/6689
In1993,researchersattheJohnsHopkinsSchoolofMedicinereportedthatapyruvatetransportersystemcouldbeusedtodeliverbromopyruvateinsidetrypanosomalcellswhereitsprimarytargetisglyceraldehyde-3-phosphatedehydrogenase,whichishighlysensitivetoinhibitionbybromopyruvate.Thepyruvatetransportersystem,whichisknowntobeoverexpressedincancercells,waslateridentifiedtobeaMCTcalledMonocarboxylateTransporter1.A2002studysuggestedthatintra-arterialdeliveryofbromopyruvicaciddirectlytothesiteoftumorsinrabbitscouldrepresentastrategyforstoppingthegrowthoflivercancerwhileminimizingtoxicside-effects.Anapplicationforpatenthasbeensubmitted.
ResearchatJohnsHopkinshassuggestedthatbromopyruvatecouldbeusedtoselectivelykillcancercells,whileleavingnormalcellsintact.AJohnsHopkinspressreleasedatedOctober14,2004statedthat,"Buildingontheirearlierwork,JohnsHopkinsresearchershavediscoveredthatanapparentlynontoxiccellular"energyblocker"canerADIcatelargelivertumorsgrowninrats.InJuly2013,theFDAacceptedanINDapplicationfortheuseofbromopyruvateforaPhaseIclinicaltrialinlivercancer.
https://en.wikipedia.org/wiki/Bromopyruvic_acid
