Nuzefatide pevedotin is the INN for BT5528, Bicycle Therapeutics' EphA2-targeting bicyclic peptide-drug conjugate. The molecule pairs a bicyclic peptide that homes to EphA2-overexpressing tumor cells with a cytotoxic MMAE payload, combining antibody-like specificity with small-molecule pharmacokinetics.
The AACR 2026 update reported a 40% confirmed ORR in EphA2+ urothelial cancer patients on nuzefatide 6.5 mg/m² plus nivolumab — rising to 100% confirmed ORR in MMAE-naïve patients (n=14). Bicycle has identified 8 mg/m² Q2W as the preferred monotherapy dose. The Phase 2 PDAC trial dosed its first patient in April 2026, extending the program into pancreatic cancer where companion EphA2 PET imaging at AACR 2026 reinforced target validation. ASCO 2026 will deliver Duravelo-2 dose-selection data on June 1.
Stories here cover trial readouts, AACR and ASCO presentations, and the broader Bicycle pipeline. See #bt5528, #bicycle-therapeutics, #epha2, and #peptide-drug-conjugate.
Bicycle Therapeutics reported Q1 2026 financial results April 30 — net loss of $60.8M ($0.87 per share) on R&D of approximately $44M, with $559.5M in cash and equivalents at March 31 supporting a cash runway into 2030. The pipeline update reaffirmed that nuzefatide pevedotin (BT5528) Duravelo-2 dose-selection data in EphA2-positive solid tumors will be presented at the ASCO 2026 Rapid Oral Abstract Session on June 1, the Phase 2 nuzefatide pevedotin trial in recurrent pancreatic cancer enrolled its first patient in April, and the EphA2 gallium-68 PET imaging program continues to accumulate first-in-human data. Bicycle remains the leading bicyclic-peptide-platform pure-play in oncology.
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's EphA2-targeting bicyclic peptide-drug conjugate nuzefatide pevedotin (BT8009) at 6.5 mg/m² Q2W plus nivolumab achieved 40% confirmed ORR (4/10) in metastatic urothelial patients who had progressed on checkpoint inhibitors, and 100% (3/3) in MMAE-naive EphA2+ patients. No Grade ≥3 treatment-related adverse events of clinical interest. Presented at AACR 2026 on April 20.