Drug intelligence / Profile preview

diethylhomospermine

Development stage
Phase 1
Modality
Small Molecules
Administration
Intravenous
01

Overview

Diethylhomospermine is a synthetic polyamine analogue and small molecule with antiproliferative and potential anti-diarrheal activities. It acts by antagonizing polyamine activity via the NMDA receptor glutamine binding site, modulating inotropic stasis and reducing stool volume. Diethylhomospermine also suppresses the activity of key biosynthetic enzymes in polyamine metabolism—ornithine decarboxylase and S-adenosylmethionine decarboxylase—which are important for cell proliferation. It has been investigated primarily for AIDS-related chronic diarrhea and HIV infections but development was discontinued due to toxicity concerns at higher doses (notably neurotoxicity and hepatic damage). The drug reached up to phase II clinical trials for these indications[1][2].

Other names
N(1),N(14)-Bis(ethyl)homospermine1,14-Bis(ethylamino)-5,10-diazatetradecane
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)ODC1 (Ornithine decarboxylase)AMD1 (S-adenosylmethionine decarboxylase)

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