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Peptide-drug & small-molecule-drug conjugates

Like an ADC but with a small targeting peptide instead of an antibody, so it penetrates tumours faster and is cheaper to make.

Melflufen (Pepaxto, withdrawn in US), lutetium radioligands (technically peptide-radionuclide conjugates), and clinical-stage PDCs (BT8009 zelenectide pevedotin, Nectin-4 Bicycle toxin conjugate; CBX-12 exatecan-SMDC). Bicycle's zelenectide pevedotin is in phase 2/3 in urothelial cancer.

Schematic · not to scale
Bicyclic peptide binder · Payload

How it works

Short peptide or bicyclic peptide binds the target; short half-life reduces systemic exposure.

Strengths
  • Rapid penetration, renal clearance
  • Cheaper synthesis
Limitations
  • Short half-life limits tumour exposure
  • Renal toxicity

Products

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Latest papers

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Literature trend37 papers in the last 12 months+6% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

Query for this technology: (TITLE:"peptide-drug conjugate" OR ABSTRACT:"peptide-drug conjugate" OR TITLE:"peptide drug conjugate" OR ABSTRACT:"peptide drug conjugate" OR TITLE:"bicycle toxin conjugate" OR ABSTRACT:"bicycle toxin conjugate"). Results are unfiltered search hits about Peptide-drug & small-molecule-drug conjugates, not a curated reading list.

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