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. 2025 Apr 23;68(9):9037–9056. doi: 10.1021/acs.jmedchem.5c00007

Table 1. Summary of Representative PDCs in Clinical Trials.

drug (manufacturer) target indication peptide linker payload phase ClinicalTrials recruitment status
AEZS-108 (AEterna Zentaris) LHRH-R endometrial cancer [d-Lys6] LHRH amide doxorubicin phase III NCT01767155 completed
EP-100 (Esperance Pharmaceuticals Inc.) LHRH-R ovarian cancer LHRH amide lytic peptide phase II NCT01485848 completed
ANG1005 (Angiochem, Inc.) LRP1 breast cancer with brain metastases, leptomeningeal Angiopep-2 succinic acid ester paclitaxel phase III NCT03613181 active, not recruiting
NGR-hTNF (AGC Biologics SpA) CD13 neovasculature malignant pleural mesothelioma CNGRC amide hTNF phase III NCT01098266 completed
G-202 (GenSpera, Inc.) PSMA Solid tumors, HCC DγEγEγEE amide Thapsigargin phase II NCT01777594 completed
            
BT8009 (BicycleTx Limited) Nectin-4 advanced solid tumor bicyclic peptide Val-Cit MMAE phase I/II NCT04561362 recruiting
    urothelial Cancer       phase II/III NCT06225596 recruiting
            
PEN-221 (Tarveda Therapeutics) SSTR2 advanced neuroendocrine and small cell lung cancer octreotide disulfide DM1 phase I/II NCT02936323 completed
CBX-12 (Cybrexa Therapeutics) low pH and TOP1 platinum resistant or refractory ovarian cancer pHLIP disulfide Exatecan phase II NCT06315491 recruiting
BMTP-11 (M.D. Anderson Cancer Center) IL-11Rα osteosarcoma and prostate cancer with bone metastasis CGRRAGGSC amide peptidomimetic D(KLAKLAK)2 phase I NCT00872157 completed
TH1902 (Theratechnologies) SORT1 advanced solid tumor TH19P01 succinic acid ester docetaxel phase I NCT04706962 recruiting
BPP-PTX ACE TNBC EWPRPQIPP succinic acid paclitaxel preclinical preclinical preclinical
KCC-TGX HER2 prostate cancer KCCYSL self-cycling TGX-D1 preclinical preclinical preclinical
SAP-CPT integrin αVβ3 breast and bladder cancer RGD self-assembly camptothecin preclinical preclinical preclinical