Drug intelligence / Profile preview

DHA-dFdC

Development stage
Preclinical
Lead developer
Dominari Holdings
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intravenous, Intraperitoneal (preclinical), Injection
01

Overview

**DHA-dFdC** (4-(N)-docosahexaenoyl 2',2'-difluorodeoxycytidine) is a small molecule drug conjugate consisting of **gemcitabine** (2',2'-difluorodeoxycytidine, dFdC) covalently linked to **docosahexaenoic acid** (DHA)[2][5][3]. This conjugation aims to improve the efficacy, selectivity, and pharmacokinetics relative to gemcitabine alone. DHA-dFdC shows markedly improved antitumor activity, especially against pancreatic cancer in preclinical models, where it achieved higher pancreatic tissue concentrations and extended animal survival compared to equivalent doses of gemcitabine or DHA alone, and showed strong activity in pancreas, leukemia, renal, and CNS cancer cell lines[2][5][1][3]. The mechanism includes inhibition of DNA synthesis (as a nucleoside analog), as well as induction of immunogenic cell death and modulation of oxidative stress responses[2][4][5]. The compound is being developed by Dominari Holdings (formerly AIkido Pharma) and originated at the University of Texas at Austin[3][1].

Other names
DHA-gemcitabineGemcitabine DHA conjugateGemcitabine docosahexaenoic acid conjugate
02

Targets

DNA

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