OB-001 + Enhertu

OB-001 + Enhertu is an investigational combination therapy consisting of OB-001, a novel KinetiSol amorphous solid dispersion formulation of the selective P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) efflux pump inhibitor elacridar, and Enhertu (trastuzumab deruxtecan), a HER2-directed antibody-drug conjugate (ADC). Developed by OncoBayes, OB-001 is designed to overcome ADC resistance by inhibiting efflux pumps on tumor cells that actively pump out the cytotoxic payload of Enhertu (DXd, an exatecan derivative). By blocking these efflux transporters, OB-001 increases the intracellular retention and concentration of the DXd payload within cancer cells, thereby re-sensitizing resistant tumors to Enhertu. The combination is being evaluated for the treatment of HER2-expressing solid tumors, including breast cancer, that have developed resistance to trastuzumab deruxtecan.

Other names

OB-001 + trastuzumab deruxtecanelacridar + trastuzumab deruxtecan