Peptide-Drug Conjugates in Oncology

How peptide-drug conjugates and peptide receptor radionuclide therapy are expanding the role of peptides in cancer treatment.

Filed under evidence research, written for researcher, clinician, investor, evidence level A.

Not medically reviewed. Last updated 2026-04-15. Nothing here is medical advice.

Peptides are increasingly used as targeting vehicles in oncology, delivering cytotoxic payloads or radioactive isotopes directly to tumor cells. This approach combines the specificity of peptide-receptor interactions with the potency of traditional cancer therapies.

Peptide Receptor Radionuclide Therapy (PRRT)

PRRT uses radiolabeled peptides that bind to receptors overexpressed on tumor cells:

Approved Therapies

• **Lutetium Lu-177 dotatate (Lutathera)**: FDA-approved for gastroenteropancreatic neuroendocrine tumors (GEP-NETs). Targets somatostatin receptors overexpressed on NET cells.
• Phase III NETTER-1 trial showed significant improvement in progression-free survival.

Mechanism

1. Radiolabeled somatostatin analog injected intravenously

2. Peptide binds to somatostatin receptors on tumor cells

3. Radioactive isotope delivers localized radiation

4. Minimizes radiation exposure to healthy tissue

Peptide-Drug Conjugates (PDCs)

PDCs are an emerging class of targeted therapies:

• Peptide targeting moiety binds a tumor-specific receptor
• Linker connects the peptide to a cytotoxic payload
• Payload is released inside the tumor cell

Advantages Over Antibody-Drug Conjugates

• Smaller size allows better tumor penetration
• Easier and cheaper to manufacture
• Potentially faster blood clearance (reduced systemic toxicity)
• Can target intracellular receptors

Pipeline Activity

Multiple PDCs are in clinical development targeting various solid tumors. The field is attracting significant investment from pharmaceutical companies and biotech startups.

This article provides oncology research education and does not constitute treatment recommendations.

More guides: All guides, Safety centre, Peptide library.