Drug intelligence / Profile preview

benzarubicin

Development stage
Preclinical
Lead developer
Paradox Pharmaceuticals
Modality
Small Molecules
Administration
Parenteral, Intravenous, Intramuscular, Intra-arterial, Subcutaneous, Intraperitoneal, Topical, Inhalation, Rectal
01

Overview

Benzarubicin (AD 198) is a small molecule anthracycline derivative being developed by Paradox Pharmaceuticals as a veterinary antitumor agent. Unlike conventional anthracyclines that primarily target DNA topoisomerase II, benzarubicin possesses a dual mechanism of action. It targets the cytoplasm of cancer cells, binding to the C1b regulatory domain of protein kinase C (PKC) family members, as well as other C1b-containing proteins like RasGRP and β2-chimaerin. Specifically, it activates the PKC-delta isoform to trigger rapid apoptosis through a mitochondrial pathway. It is currently in development for the treatment of osteosarcoma and lymphoma in canine and feline patients, particularly those where standard anthracycline therapy has failed to achieve durable remission.

Other names
N-benzyladriamycin-14-valerateN-benzyladriamycin14-valerateN-benzyladriamycin 14-valerate
02

Targets

CHN2 (Chimerin 2)PRKCD (Protein kinase C delta)TOP2A (DNA topoisomerase II)RASGRP1 (RAS guanyl-releasing protein 1)

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