TWEAKR-KSPi-ADC

TWEAKR-KSPi-ADC is a preclinical antibody-drug conjugate (ADC) developed by Bayer AG, targeting the TWEAK receptor (TWEAKR), also known as fibroblast growth factor-inducible 14 (Fn14). The ADC utilizes a novel pyrrole-based kinesin spindle protein inhibitor (KSPi) as its cytotoxic payload. KSP (also known as Eg5 or KIF11) is a motor protein essential for bipolar spindle formation during mitosis; its inhibition leads to cell cycle arrest in the M-phase and subsequent apoptosis. By targeting TWEAKR, which is frequently overexpressed in various solid tumors, the ADC aims to deliver the KSPi payload selectively to malignant cells, potentially overcoming the systemic toxicity issues associated with small-molecule KSP inhibitors. Preclinical data presented at AACR 2017 demonstrated significant anti-tumor efficacy and complete regressions in xenograft models of non-small cell lung cancer (NSCLC), urothelial cell carcinoma (UCC), and renal cell carcinoma (RCC).

Other names

Fn14-KSPi-ADCFn-14-KSPi-ADCFn 14-KSPi-ADCTWEAKR-KSP inhibitor ADC