Peptide-drug conjugates (PDCs) are the peptide analog of antibody-drug conjugates — a tumor-targeting peptide linked to a cytotoxic payload. The platform sits at the intersection of medicinal chemistry, peptide stability work, and ADC-style delivery.
Lead programs covered on this site: Bicycle Therapeutics' bicyclic peptide-toxin conjugates (BT5528 against EphA2, BT8009 against Nectin-4), Avacta's pre|CISION platform (AVA6103 with exatecan), Lirum's LX-101 against IGF-1R for Ewing sarcoma, and the broader academic peptide-payload work covered at AACR and ASCO. Several have followed ADC-style linker chemistry while keeping the peptide targeting moiety.
Stories here cover trial readouts, partnership deals, and the chemistry papers behind the platform. See #peptide-drug-conjugates for the alternate tag and #bicycle-therapeutics for the leading company.
Avacta Therapeutics presented April 21 data at AACR 2026 showing its FAP-enabled peptide-drug conjugate AVA6103, which delivers exatecan via the pre|CISION® platform, achieved a Tumor Selectivity Index three times higher than marketed ADC Enhertu in preclinical models, with tumor Cmax more than one log higher. AVA6103 entered the Phase 1 FOCUS-01 trial (NCT07454642) in March 2026 with initial clinical readout expected later this year.
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.