Aptamer Drug Conjugates: A Novel Targeted Delivery Platform for Oncology



Targeted therapy modality in which aptamers replace mAbs in drug conjugates

Have target specificity and affinity on par with mAbs

Can be selected for inhibitory, stimulatory, or no biological activity

Support receptor-mediated internalization

Different aptamers may be joined to form bi-specific therapeutic agents

ApDC payload can be tailored to suit therapeutic strategy:

Chemotherapeutic toxin
RNAi, ASO, miRNA, etc.

ApDCs offer significant CMC advantages over ADC

CMC Advantages of ApDC vs. ADC

Immuno-stimulatory oliogonucleotides (e.g., CpG sequences) can be directly synthesized as chimeric extension of targeting aptamer sequence


Streamlined manufacturing/analytical chemistry approach


Lower COGS


Shortened CMC development lead times

Chemotherapeutic toxin payload conjugation chemistry is simplified


Site-specific conjugation using NHS-, thiol or Click chemistry


Constant 1:1 stoichiometry of targeting and payload moieties


On equimolar basis, more payload for ApDC than ADC

MW of aptamer is between 10,000 to 15,000


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