Tumour-homing aptamers for targeted delivery of chemodrugs to nasopharyngeal carcinoma
Overview
We has developed ‘Target Killer’, a novel Aptamer-Drug Conjugate (ApDC) for Nasopharyngeal Carcinoma (NPC). Using Cell-SELEX technology, we identified aptamers that specifically home to EBV-positive cancer cells. By conjugating chemotherapy directly to these tumour-homing aptamers, we enable targeted drug delivery, killing cancer cells while sparing healthy tissue.
Commercialisation opportunities
technology licensing agreement
Problem addressed
Current treatments for Nasopharyngeal Carcinoma (NPC) rely on non-targeted chemotherapy and radiotherapy, causing severe side effects like mucositis, myelosuppression, and organ toxicity. No FDA-approved targeted therapy exists for NPC. This lack of precision significantly diminishes patient quality of life and limits treatment efficacy, creating an urgent need for a therapy that spares healthy cells.
Innovation
- Tumour-Homing Aptamers: Utilising advanced Cell-SELEX, we discovered novel G-quadruplex aptamers that bind with high affinity (nanomolar range) specifically to marker proteins on EBV-positive NPC cells, ensuring precise tumour targeting.
- Chemotherapy as Payload: Rather than attaching drugs as 'cargo', we directly incorporate chemotherapeutic agents (5-FU, Gemcitabine) into the aptamer's nucleotide backbone. This creates a bifunctional molecule where the aptamer itself becomes the targeted delivery vehicle for the drug.
- G-Quadruplex Stability: Our aptamers are guanine-rich, forming stable G-quadruplex (G4) structures. This unique conformation provides high resistance to nuclease degradation in the bloodstream, ensuring the therapeutic reaches the tumour site intact and maintains its efficacy.
Key impact
- Reduced Side Effects: By delivering chemotherapy directly to tumour cells, our ApDC spares healthy tissues. In vivo studies confirmed no toxicity to major organs and no adverse effects on mouse body weight, offering patients a much safer profile than conventional chemotherapy.
- Dramatic Dose Reduction: Our targeted delivery amplifies the drug's power. In vivo models showed that our Apt-2019-5FU conjugate achieved potent tumour suppression using a dose of 5FU that was ten times lower than the standard effective dose.
Award
- Silver Medal, 49th International Exhibition of Inventions Geneva
- Gold Medal at the 5th Aisa Exhibition of Innovations and Inventions Hong Kong
Application
- Treatment of EBV-associated nasopharyngeal carcinoma, gastric cancer, Hodgkin disease, Burkitt lymphoma and diffuse large B cell lymphoma.
Patent
- Title: Aptamers specific to EBV-associated malignancies and their applications in cancer imaging and therapies
- Chinese Regular Patent Application No. 202380015639.4; filed on 23 July 2024
- US national phase Application No. 18/833,184; ; entered national phase on 25 July 2024
- European Regular Patent Application No. EP23752376.6 national phase filed on 5 Aug 2024
- Hong Kong Patent Application No.: 62025104371.2; filed on 6 March 2025 based on Chinese patent application
The Chinese University of Hong Kong (CUHK)
Founded in 1963, The Chinese University of Hong Kong (CUHK) is a forward-looking comprehensive research university with a global vision and a mission to combine tradition with modernity, and to bring together China and the West. CUHK teachers and students hail from all around the world. Four Nobel laureates are associated with the university, and it is the only tertiary institution in Hong Kong with recipients of the Nobel Prize, Turing Award, Fields Medal and Veblen Prize sitting as faculty in residence. CUHK graduates are connected worldwide through an extensive alumni network. CUHK undertakes a wide range of research programmes in many subject areas, and strives to provide scope for all academic staff to undertake consultancy and collaborative projects with industry.
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