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Transforming cancer R&D with aptamers

Cancer remains a mammoth challenge, accounting for one in every six deaths globally. But aptamers are offering new solutions from reagents to next-gen ADCs.

Cancer in aptamer group blueDespite the scale of the challenge, over the past years, we have made huge leaps in our understanding of cancer as well as in delivering better ways of fighting it. As we drive towards personalised medicines, the precision in cancer treatments, trials, and patient monitoring is improving, meaning more effective solutions without side effects.

Revolutionising cancer treatment with Optimer

Optimer binders, as as optimised aptamers, are offering innovative ways to address cancer, from identifying new cancer biomarkers to delivering better treatments. Here we take a look at how Optimer technology is changing the landscape of cancer research in ways both expected and surprising.

Precision chemotherapy with Optimer-drug conjugates

Just like antibody-drug conjugates (ADCs) that deliver highly potent cancer-killing drugs directly to the cancer cells using a targeted antibody, Optimer-drug conjugates can precisely target chemotherapy for new cancer treatments. By delivering chemotherapy drugs directly to the inside of cancerous cells, this approach to cancer treatment prevents damage to nearby healthy cells, potentially reducing treatment side effects.

Optimer drug conjugates for cancer treatment

Optimer gives precise control of drug-Optimer ratios through simple chemical modifications, allowing tuneable dosing for the best therapeutic effects. Also, the half-lives of these delivery reagents can be simply tuned to meet rapid hit-and-run strategies or give longer in vivo half-lives as needed.

Being smaller than antibodies, Optimer-drug conjugates can penetrate deeper into solid tumours than antibodies for improved delivery, inhibition and more effective treatment. Also, as Optimer are oligonucleotide-based ligands, they are less immunogenic than antibodies, allowing repeat dosing of patients.

Advanced cancer-fighting conjugates

But next-gen ADCs aren’t the only cancer-fighting conjugates that Optimer can deliver.

Conjugation of radionuclides to Optimer binders creates Optimer-radioconjugates that target the radiotherapy directly to tumour cells. Using this approach cancer cells can be destroyed in a more targeted way than traditional external beam radiation, or Optimer-radioconjugates can support cancer imaging and diagnostics.

Optimer-oligonucleotide conjugates, using RNA therapies, such as siRNA and ASOs, are creating new precision cancer treatments that can modulate the expression of genes important in tumour development or drug resistance.

Optimer antagonists: a new frontier in cancer treatment

Targeting Optimer binders to inhibit specific enzymes or prevent protein-protein interactions creates new therapeutic antagonists that can inhibit cancer cells. An aptamer-based therapy is currently in mid-stage clinical development for glioblastoma in combination with radiotherapy, and for pancreatic cancer in combination with immune checkpoint inhibitors. The opportunity to target new biomarkers with Optimer opens the door to the development of antagonists for new cancer treatment strategies.

We are working with scientists at Cancer Research UK to develop new treatments for chronic myelogenous leukaemia using antagonistic Optimers. The developed Optimer binds to a specific protein involved in cancer progression and edits the erroneous gene splicing seen in cancer cells, to return to a normal wild type and healthy mRNA.

Early functional studies show a developed antagonistic Optimer partially restores WT splicing activity with a concurrent reduction in aberrant splicing in in vitro cell models of chronic myelogenous leukaemia . 

Precision patient dosing with Optimer assays

In standard chemotherapy, most patients receive a dose based on body weight. However, this doesn’t account for variance in an individual’s metabolism and can give rise to doses that are too low and so ineffective or too high and create excessive side effects. Monitoring the amount of active drug in each patient can allow clinicians to tailor these doses for better effect. Until now, this has always been done using HPLC-MS, which is slow and expensive.

Optimer-based point-of-care assays can offer high-precision information on the amount of chemotherapy in a patient’s bloodstream for tailored dosing regimes. These tests are as accurate as the current HPLC-MS methods but with faster results, enabling real-time treatment changes.

“This represents an innovative approach in the field of drug monitoring. The use of Optimer to optimise drug dosage looks toward the horizon of personalised and tailored medicine, which is a new frontier in oncology.”
Dr Giuseppe Toffoli, Director of Experimental & Clinical Pharmacology, CRO Aviano

Advancing cancer research with Optimer assay reagents

New cancer biomarkers are continuously being identified and validated in research. A major bottleneck in translating these biomarkers from bench to bedside is the lack of specific reagents for their analysis. These biomarkers can be used in assays like IHC for biopsy analysis to guide clinical decision making, screen for cancers, predict risk, develop new therapies and monitor patient responses to cancer treatments.

The in vitro development methods of Optimer binders overcome the reliance on the immune system that antibodies have, meaning there is a wider target range for these binders to support novel targets. Additionally as each Optimer is tuned to the end assay during development with simple conjugation of the full range of fluorophores, tags and labels, Optimer reagents offer high performance and full assay compatibility, whatever your target and methods.

 

If you would like to discuss your needs to see how Optimer could help break down the scientific barriers to your research success, get in touch with the team today.

 

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