BT5528

P1/2, N=288, Recruiting, BicycleTx Limited | Trial completion date: Dec 2024 --> Oct 2026

P1/2, N=312, Recruiting, BicycleTx Limited | N=166 --> 312 | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Dec 2022 --> Dec 2023

Here we report on EphA2 expression in well characterized and clinically annotated patient derived xenografts (PDX) of NSCLC including EGFR mutant NSCLC derived either from erlotinib or osimertinib resistant patients. BCY6033 is a potentially promising drug effective against EphA2 expressing PDX models. Future studies and clinical trials will seek to determine the efficacy of BT5528 in EphA2 expressing tumors.

In contrast, BT5528 achieves prolonged toxin delivery to tumors, following transient exposure in plasma of less than one hour. A Phase I/II study of BT5528 in patients with solid tumors is ongoing, which will investigate if this PK novel, differentiated pharmacokinetic profile, unique to Bicycle toxin conjugates, gives rise to a favorable balance of efficacy and safety.

BT5528-100 (NCT04180371) is a Ph I/II study to evaluate safety and tolerability of weekly BT5528 alone and in combination with Q4W nivolumab. Enrollment is ongoing. Research Funding: Bicycle Tx Limited