Drug intelligence / Profile preview

dofequidar

Development stage
Phase 1
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Dofequidar is an orally available synthetic quinoline derivative and small molecule antineoplastic agent developed to overcome multidrug resistance (MDR) in cancer therapy. It acts primarily by inhibiting the activity of ATP-binding cassette (ABC) transporters such as P-glycoprotein (ABCB1/P-gp), multidrug resistance-associated protein 1 (ABCC1/MRP1), and breast cancer resistance protein (ABCG2/BCRP). By blocking these efflux pumps, dofequidar increases the intracellular concentration of chemotherapeutic agents in tumor cells, thereby sensitizing them to anticancer drugs and reversing drug resistance. Dofequidar has been investigated mainly for its ability to enhance the efficacy of standard chemotherapy regimens in advanced or recurrent cancers, including breast cancer[2][3][4][5][6].

Other names
dofequidar fumarate129716-58-1UNII-0BJK6B565BUNII0BJK6B565BUNII 0BJK6B565B
02

Targets

ABCC1 (MRP1)ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)

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