Bicycle Therapeutics builds bicyclic peptides — short peptide sequences cyclized through a chemical scaffold to combine antibody-like specificity with small-molecule pharmacokinetics. The platform has produced multiple oncology candidates against targets that traditional ADCs struggle with.
Lead programs covered on this site: BT5528 / nuzefatide pevedotin (EphA2-targeting bicycle drug conjugate) in solid tumors — 40% confirmed ORR in EphA2+ urothelial patients on the nivolumab combination at AACR 2026; BT8009 / zelenectide pevedotin (Nectin-4) in urothelial cancer; and the EphA2 gallium-68 PET imaging program. In April 2026 Bicycle dosed the first patient in a Phase 2 nuzefatide pevedotin trial in recurrent pancreatic cancer, extending the program into a difficult tumor type where companion EphA2 imaging at AACR reinforced target validation. The Duravelo-2 dose-selection readout is set for ASCO 2026 (Rapid Oral Abstract Session, June 1).
Stories here cover trial readouts, AACR and ASCO data, and partnership announcements. See #bicyclic-peptide for the chemistry class, #nuzefatide-pevedotin for the lead program, and #peptide-drug-conjugate for adjacent platforms.
A Chemical & Engineering News feature published in June 2026, drawing on data from the CAS Content Collection, documented the cyclic-peptide patenting surge over 2020 to April 2026. Chinese universities are the top filers globally on cyclic peptides. Outside China, US universities lead. Among corporates, Bicycle Therapeutics and Bristol Myers Squibb were called out for sustained patent activity covering cancer, infectious, inflammatory, and autoimmune disease indications. The article frames cyclic peptides as bridging the small-molecule and biologic divide: enhanced conformational rigidity, elimination of unstable terminal residues, and improved metabolic stability are the structural advantages that allow some cyclic peptides to be dosed orally. Merck's enlicitide decanoate (MK-0616, oral PCSK9 macrocyclic peptide for hyperlipidemia) was cited as the proof point for oral-pill cyclic-peptide drug development; an enlicitide NDA submission was underway as of mid-2026. The broader market backdrop: macrocyclic and stapled peptides are projected to grow from $1.22 billion in 2024 to $4.76 billion by 2030 at a 21.44% CAGR, driven mostly by oncology pipelines and the macrocyclic deal flow that includes the Unnatural Products-Novartis $1.7-1.8B cardiovascular pact (February 2026), Biogen-Dayra $50M+ immunology pact (November 2025), and the Parabilis Helicon platform (Regeneron $2.3B collaboration, June 10 $670M record IPO).
In the June 1 rapid oral session (Abstract 4516, Yohann Loriot), the dose-optimization stage of the randomized Phase 2 Duravelo-2 trial showed the optimal dose of the bicyclic peptide-drug conjugate zelenectide pevedotin (BT8009) plus pembrolizumab produced response rates comparable to published standard-of-care data in previously untreated locally advanced or metastatic urothelial carcinoma, with roughly four-fold lower skin reactions and about half the peripheral neuropathy. The separate Duravelo-1 Phase 1 trial showed median progression-free survival comparable to standard of care in cisplatin-ineligible patients.
ASCO's Sunday education and poster sessions in Chicago set up the meeting's densest peptide-oncology day on Monday, June 1, when Bicycle Therapeutics presents Duravelo-2 (zelenectide pevedotin in first-line urothelial cancer, Abstract 4516), Mayo Clinic presents the TPIV200 folate-receptor-alpha vaccine in triple-negative breast cancer (Abstract 536), and Telix presents ProstACT Global PSMA radioligand data. Corbus CRB-701 and BioVaxys MVP-S round out the targeted-conjugate and vaccine slate.
ASCO 2026 Day 2 in Chicago continued the meeting's peptide-and-targeted-conjugate oncology programming. Saturday May 30 brought the Immutep eftilagimod alfa survival pooled analysis and the ImPact Biotech padeliporfin VTP pancreatic data, alongside the Bicycle Therapeutics zelenectide pevedotin dose-optimization poster (Abstract 4567, May 31) approaching. The meeting's heaviest peptide-mechanism day is Monday June 1: Bicycle Duravelo-2 zelenectide pevedotin + pembrolizumab oral presentation in 1L urothelial (Abstract 4516, 8:30 AM CT); Mayo Clinic TPIV200 folate-receptor peptide vaccine in triple-negative breast cancer (Abstract 536, 1:30 PM CT); Telix ProstACT PSMA radioligand Phase 3 Part 1; Sapience lucicebtide GBM poster. The Corbus CRB-701 Nectin-4 ADC data (42.9% OPSCC / 34.4% cervical) landed Friday May 29. The targeted-conjugate categories — Nectin-4, PSMA, B7-H3, FAP, SSTR2 — remain the densest peptide-adjacent oncology competition, with the bulk of definitive readouts concentrated in the meeting's back half through June 2.
The ASCO 2026 Annual Meeting opens tomorrow Friday May 29 at McCormick Place Chicago, running through June 2. The peptide-and-targeted-conjugate oncology slate that landed in the May 21 abstract release and the May 26 embargoed press briefing: Bicycle Therapeutics Duravelo-2 Phase 2 (zelenectide pevedotin 65% ORR / 58% BICR-confirmed in 1L urothelial, oral June 1 8:30 AM); Avacta AVA6000 FAP-Dox Phase 1a/1b in salivary gland (90% disease control); BriaCell Bria-IMT 16.6-month median OS in metastatic breast cancer; Sapience lucicebtide 28.4-month projected median PFS in glioblastoma; Corbus CRB-701 Nectin-4 ADC in HNSCC and cervical (oral May 29); Crinetics CRN09682 SSTR2 non-peptide drug conjugate BRAVESST2; Aktis AKY-2519 B7-H3 miniprotein radioconjugate; Mayo Clinic TPIV200 folate-receptor peptide vaccine in TNBC; plus the GLP-1 cancer slate (Abstract 3143, Roswell Park breast cancer). ASCO 2026 follows immediately after EASL 2026 closes May 30 — the back-to-back meeting structure makes the May 27-June 2 window the highest-density peptide-data week of 2026.
ASCO 2026 in Chicago opens Friday May 29 with the peptide-oncology calendar now fully fixed. Thursday May 29 4:57 PM CDT: Corbus CRB-701 Nectin-4 ADC oral session in cervical cancer. Friday May 30 4:30 PM CDT: Corbus CRB-701 HNSCC poster. Saturday May 30: BriaCell Bria-IMT three posters in metastatic breast cancer. Sunday May 31: Bicycle Therapeutics zelenectide pevedotin Phase 1 Duravelo-1 monotherapy update poster; Avacta AVA6000 FAP-Dox Phase 1a/1b in salivary gland cancers poster session. Monday June 1 8:30-8:36 AM CT: Bicycle Therapeutics Duravelo-2 oral abstract (Abstract 4516). Monday June 1: Sapience Therapeutics lucicebtide poster session for newly-diagnosed GBM. The peptide-oncology cohort is the largest single-meeting concentration of peptide-mechanism oncology data in recent ASCO history.
Bicycle Therapeutics' formal post-ASCO 2026 press release Friday morning specified the headline Phase 2 numbers from yesterday's abstract release. In the Duravelo-2 combination cohort, the optimal zelenectide dose plus pembrolizumab 200 mg every three weeks produced 65% ORR (17/26 evaluable patients) regardless of confirmation, with 58% BICR-confirmed ORR (15/26) at the 27-week cutoff in previously untreated locally advanced or metastatic urothelial cancer. An additional confirmed BICR response observed after the cutoff would bring the rate to 62%. The trial tested two dose schedules: 5 mg/m² weekly and 6 mg/m² two-weeks-on-one-week-off; the optimal dose moves forward in the Phase 3 expansion. Treatment retention was high and dose-limiting adverse events limited. The 65% Phase 2 ORR matches the 65% Phase 1 Duravelo-1 ORR (13/20) — pharmacology consistency across two different patient populations, an unusual durability signal for a peptide-drug conjugate.
ASCO 2026 abstract text released at 5 PM ET Thursday, ahead of the May 29-June 2 Chicago meeting. The peptide-oncology data landed simultaneously across the previously-announced slate. Bicycle Therapeutics released Duravelo-2 Phase 2/3 interim data on zelenectide pevedotin (BT8009) plus pembrolizumab in 1L locally advanced/metastatic urothelial cancer. Avacta released AVA6000 Phase 1b data in salivary gland cancers. BriaCell released final Phase 2 Bria-IMT survival data plus biomarker analyses from the ongoing Phase 3. BioVaxys's MVP-S PESCO Phase 1B/2 ovarian cancer abstract landed. Crinetics CRN09682 SSTR2 NDC BRAVESST2 abstract emerged. Pfizer released 40+ company-sponsored, investigator-sponsored, and collaborative oncology abstracts including three late-breaking sessions. The peptide-oncology cohort is the largest single ASCO presence in recent meeting history.
Bicycle Therapeutics released Duravelo-2 Phase 2/3 interim analysis data at ASCO 2026 — zelenectide pevedotin (BT8009, a Nectin-4-targeting bicyclic peptide-MMAE conjugate) plus pembrolizumab in previously untreated locally advanced or metastatic urothelial cancer. The full data presentation is scheduled for Monday June 1, 8:30-8:36 AM CT in the GU Cancers oral session (Abstract 4516). The Duravelo-1 monotherapy comparator anchor — 65% ORR (13/20) in cisplatin-ineligible 1L mUC at 5 mg/m² + pembrolizumab combination, with median DOR 11.1 months in the monotherapy expansion — sets the bar for what the Duravelo-2 combination interim must clear. Bicycle's five-abstract ASCO package includes the oral Duravelo-2 piece plus four posters covering Duravelo-1 monotherapy update, BT5528 EphA2 monotherapy and combination cohorts, and BT8009 second-line urothelial data.
ASCO 2026 abstracts will release on asco.org/abstracts beginning 5:00 PM ET on Wednesday May 21, ahead of the May 29-June 2 Chicago meeting. The peptide-oncology slate is substantial: Pfizer announced 40+ company-sponsored, investigator-sponsored, and collaborative oncology abstracts including three late-breaking sessions; Bicycle Therapeutics has an oral and four poster presentations on zelenectide pevedotin (BT8009, nectin-4 PDC) with Duravelo-2 interim data; Avacta has Phase Ia/Ib data on AVA6000 (FAP-Dox PDC) in salivary gland cancers; BioVaxys's MVP-S survivin peptide vaccine PESCO trial data; BriaCell's six Bria-IMT/Bria-OTS+ presentations on metastatic breast cancer; and Replimune's RP1 + nivolumab 3-year melanoma OS data. Crinetics CRN09682 SSTR2 NDC BRAVESST2 update expected.
Bicycle Therapeutics confirmed the Duravelo-2 oral abstract presentation slot at the ASCO 2026 Annual Meeting on Monday, June 1, 8:30–8:36 a.m. CT. The abstract reports interim analysis results from Duravelo-2, a Phase 2/3 trial of zelenectide pevedotin (BT8009) plus pembrolizumab as first-line treatment for previously untreated locally advanced or metastatic urothelial carcinoma. Zelenectide pevedotin is Bicycle's Nectin-4-targeting bicyclic peptide-drug conjugate, a separate program from the EphA2-targeting nuzefatide pevedotin (BT5528) covered earlier on this site. The Q1 2026 print (April 30) reaffirmed $559.5M cash and runway to 2030 supporting the Phase 3 expansion of the platform.
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.
On the final day of AACR 2026, the German Cancer Consortium presented first-in-human imaging data for EphA2 BIA — a gallium-68-labeled bicyclic peptide targeting EphA2 — in pancreatic ductal adenocarcinoma patients. Seven patients underwent PET/CT imaging up to three hours post-injection, with rapid tumor uptake and primarily renal excretion in six of seven. The tracer successfully detected liver, bone, lymph node, and peritoneal metastases in 15 of 18 patients imaged to date, validating bicyclic peptides as a radioconjugate imaging modality.
Bicycle Therapeutics presented first clinical experiences of a phage-display-derived EphA2-specific bicyclic peptide PET imaging agent in the Diagnostic Biomarkers 2 session at AACR. The imaging agent complements Bicycle's EphA2-targeted therapeutic pipeline (including nuzefatide pevedotin) and could enable patient selection for EphA2-targeted bicyclic peptide drug conjugates across multiple tumor types.
A new market landscape report published April 21 projects the global peptide drug conjugate market will exceed $1.5 billion by 2031, with >14% CAGR and coverage of more than 50 peptide conjugates currently in clinical development. Commercial PDC benchmarks include Novartis's Lutathera and Pluvicto and Bicycle Therapeutics' nuzefatide pevedotin, with earlier-stage pipelines from Zymeworks, Bicycle, PeptiDream, and others.
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.