BT5528 — INN nuzefatide pevedotin — is Bicycle Therapeutics' EphA2-targeting Bicycle Drug Conjugate. The drug pairs a bicyclic peptide targeting EphA2-overexpressing tumors with a cytotoxic MMAE payload, combining antibody-like specificity with small-molecule pharmacokinetics.
At AACR 2026, Bicycle presented Phase 1/2 clinical results for BT5528 in combination with nivolumab in patients with advanced solid tumors — 40% confirmed ORR in EphA2+ urothelial patients on nuzefatide 6.5 mg/m² + nivolumab, rising to 100% confirmed ORR in MMAE-naïve EphA2+ patients (n=14). The company has identified 8 mg/m² Q2W as the preferred monotherapy dose. In April 2026 Bicycle dosed the first patient in a Phase 2 trial of BT5528 in recurrent pancreatic ductal adenocarcinoma, extending the program into a difficult tumor type where companion EphA2 PET imaging at AACR reinforced target validation. The Duravelo-2 dose-selection readout is set for ASCO 2026.
Stories here cover trial readouts, AACR and ASCO presentations, and the broader Bicycle pipeline. See #nuzefatide-pevedotin, #bicycle-therapeutics, #epha2, and #peptide-drug-conjugate.
Bicycle Therapeutics confirmed in its AACR 2026 update that the company began enrolling patients in a Phase 2 study of nuzefatide pevedotin (BT5528) in adults with recurrent pancreatic ductal adenocarcinoma in March 2026, with the first patient successfully dosed in April. The bicyclic peptide-drug conjugate targets EphA2-expressing tumor cells. Earlier Phase 1/2 data — through a February 9, 2026 cutoff — showed 40% confirmed ORR in EphA2+ urothelial cancer patients on nuzefatide 6.5 mg/m² plus nivolumab, rising to 100% confirmed ORR in MMAE-naïve EphA2+ patients (n=14). The company has identified 8 mg/m² Q2W as the preferred monotherapy dose. The PDAC trial extends Bicycle's footprint into a difficult tumor type where EphA2 imaging readouts at AACR 2026 reinforced target validation.
Bicycle Therapeutics announced April 21 its program for the 2026 ASCO Annual Meeting (May 29-June 2 in Chicago), with an oral presentation and five poster abstracts on nuzefatide pevedotin — its EphA2-targeting bicyclic peptide drug conjugate. Key data from Phase 1/2 include the recently disclosed 40% ORR in checkpoint-refractory urothelial cancer, expanded head-and-neck squamous cell carcinoma preclinical data, and the selected 8mg/m² Q2W dose for the Phase 2 recurrent pancreatic cancer trial. The program solidifies Nuzefatide's positioning as a leading bicyclic peptide drug conjugate in oncology.
Bicycle Therapeutics delivers an oral presentation (Sunday, April 19, 4:05-4:20 PT) on preclinical activity of BT5528 (nuzefatide pevedotin), its EphA2-targeting bicycle drug conjugate, in cell-line-derived xenograft models of head and neck squamous cell carcinoma. Lukas Stanczuk, Ph.D. leads the presentation under abstract 1325. The HNSCC program complements ongoing Phase 1/2 clinical work combining BT5528 with nivolumab in advanced solid tumors.
Bicycle Therapeutics will present Phase 1/2 clinical results for BT5528 (nuzefatide pevedotin), an EphA2-targeting Bicycle Drug Conjugate, in combination with nivolumab in patients with advanced solid tumors at AACR 2026. Additional preclinical posters cover BT5528 activity in head and neck squamous cell carcinoma and pancreatic ductal adenocarcinoma xenograft models, plus a novel phage-display-derived bicyclic peptide for EphA2-specific PET imaging.