Drug intelligence / Profile preview

DHA-SBT-1214

Development stage
Preclinical
Lead developer
Recurv Pharma
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

DHA-SBT-1214 is a novel, second-generation **taxoid prodrug** formed by conjugating **docosahexaenoic acid** (DHA), an omega-3 fatty acid, to the potent taxane SB-T-1214. This conjugate is designed as an **anticancer agent** to improve delivery and efficacy against solid tumors, particularly those displaying multidrug resistance (MDR) and cancer stem cell (CSC)-mediated resistance. The prodrug exploits tumor-selective delivery via nanoemulsion formulations (NE-DHA-SBT-1214) that enhance uptake into tumors through the enhanced permeability and retention (EPR) effect. Upon cellular uptake, DHA-SBT-1214 releases the cytotoxic taxoid, which targets tubulin, thereby inhibiting cell division. Preclinical studies demonstrate pronounced antitumor activity, particularly in colorectal, pancreatic, prostate, breast, and non-small cell lung cancers (including MDR variants), and potent synergy when combined with immune checkpoint inhibitors such as anti–PD-L1 antibodies[1][2][3][4][5].

Other names
NE-DHA-SBT-1214NE-DHA-SBT1214NE-DHA-SBT 1214
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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