Name: NEDMDG 2026 Winter Meeting
Start: 2026-12-02T14:51:00.0000000
End: 2026-12-02T14:51:00.0000000
Location: Takeda Pharmaceuticals, 35 Landsdowne Street, Cambridge, MA, USA

NEDMDG 2026 Winter Meeting

Wednesday, Dec 2nd at 5:30 – 8:30 pm EDT

Takeda, 35 Landsdowne St., Cambridge MA, 02139

Dr. Siennah Greenfield, Ph.D., Takeda

"A Novel In Vitro Permeability and Efflux Classification System for PROTACs"

Sponsored by:

Abstract:
PROTACs have emerged as a promising modality, but their physicochemical properties present substantial ADME challenges, particularly for oral absorption. To address this, Takeda colleagues used data from clinically advanced PROTACs to develop a novel classification system based on optimized MDCKI-MDR1 and Caco-2 permeability and efflux assays. Receiver operating characteristic analysis identified data-driven thresholds for permeability and efflux, enabling compounds to be grouped according to their likelihood of achieving mouse FaFg >20%. Both individual assay parameters and combined scores showed reasonable discriminative performance. This approach could help prioritize oral PROTAC candidates earlier, streamline in vitro workflows, and reduce the quantity of in vivo PK studies.

Takeda Pharmaceuticals, 35 Landsdowne Street, Cambridge, MA, USA Get Directions
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