The invention relates to novel RNA nucleic acids (aptamers) capable of inhibiting DNA methyltransferase 1 (DNMT1), enzyme involved in DNA methylation, strictly linked to tumorogenesis. The invention therefore claims the use of such aptamers for treatment of neoplastic diseases.
Patent status
SUBMITTED
Priority Number
102019000019822PCT
Priority Date
28/10/2019
License
INTERNATIONAL
Market
The global cancer therapeutics market size was valued at $98 billion in 2018 and is estimated to reach at $180 billion by 2026, registering a CAGR of 7.7%.
The global epigenetics drugs and diagnostic technologies market size was valued at $5.24 billion in 2017.
DNA methylation dominated the epigenetics market: Global Market estimated to Reach $8.88 Billion by 2030 with a GAGR of 13%
Drivers:
Global Increase in Cancer Prevalence
Increasing Government Funding for Healthcare. Major players: DNA methylation market is mainly dominated by several diagnostic majors, such as Exact Sciences Corporation, Illumina, Inc., QIAGEN N.V., and Thermo Fisher Scientific Inc., which offer a wide variety of diagnostics and research-based products for the detection of DNA methylation.
The Drugs market is consolidated with few players such as Celgene Corporation, Otsuka America, Inc. patent owners), Merck & Co., Inc., Novartis AG.
Target Audience:
Research institutes
Physicians and surgeons
Hospital
Problem
Lack of smart and safe therapeutic strategies for cancer treatment. DNA methylation is an epigenetic modification regulating gene expression.
Numerous studies have established a link between aberrant DNA methylation and cancer. In this view, the targeting of DNA methylation by specific and effective inhibitors could lead to the development of clinically relevant strategies for cancer therapy.
Current Technology Limitations
So far, there are only two FDA approved compounds to inhibit DNMTs and reduce global DNA methylation: 5-Azacytidine and 5-Aza 2’ deoxy-cytidine (decitabine). However, they are limited by the low selectivity and high instability and toxicity.
Killer Application
Possible development of nanostructures containing anti DNMT1 aptamers and other aptameric molecules able to recognize neoplastic cells and allow the release of inhibitors to tumor cells.
Our Technology and solutions
The invention protect RNA aptamers inhibiting DNMT1 that is the main mediator of DNA methylation and is involved in cancer development. The invention thus claims the use of new aptamers in cancer therapy.
Advantages
The developed molecules can overcome the toxicity of in-use demethylating protocols and provide high stability, selectivity and safety. High affinity and specificity
(No recognition of other DNMTs or unrelated RNA binding proteins)
No binding to human serum albumin
High stability (over 48h in 85% human serum) and safety
Low batch variability
Simple production, easy modification and cost effectiveness
No toxicity and immunogenicity, suitable for repeated doses
Roadmap
We are planning a start-up that will develop the nanostructure system.
The technology development plan includes:
1. The pre-clinical analysis aimed at setting the optimization of the nanoparticle system and their administration and evaluating Pharmacodynamic and Pharmacokinetic.
2. The subsequent clinical development for the evaluation of safety, dosage, efficacy and comparison with standard treatments.
TRL
The team
