Key Patent Covering Click-to-Release Granted in the United States

A key patent that encompasses the therapeutic application scope of the Click-to-Release platform has been granted in the US (US 10,967,069 B2), further strengthening Tagworks’ IP portfolio.

The patent titled “BIO-ORTHOGONAL DRUG ACTIVATION”, covers the invention of the pyridazine elimination reaction that underlies the Click-to-Release approach. The patent protects a broad scope of TCO linkers and tetrazine activators and their application in selective on-target release and activation of a wide range of constructs, including small molecule prodrugs, antibody-drug conjugates, and caged proteins.

Tagworks wins 2019 World ADC Award for Best Publication

Tagworks is pleased to announce that on the 10th of October, it won the World ADC Award for Best Publication during the 10th World ADC Summit 2019 in San Diego. The World ADC Awards exist to commend excellence across nine categories within antibody-drug conjugate research and development.

Tagworks applies its Click-to-Release platform for the selective release of anticancer drugs in the tumor microenvironment. The  publication Rossin et al. Nature Comm. 2018, 9, 1,  1484, is the result of a collaboration between 5 companies (Tagworks, Avipep, SyMO-Chem, Syncom, Levena) and the Radboud University & Medical Center. It demonstrates strong therapeutic proof of concept of a first in class click-cleavable ADC, expanding the scope of ADC therapy to non-internalizing cancer receptors. Tagworks and partners are pleased that the jury recognised the impact of this novel approach.


Tagworks featured in Nature Biotechnology news

“Click chemistry targets antibody-drug conjugates for the clinic”. Nature Biotechnology news reports on the current scope and status of the use of click chemistry in vivo, including Tagworks programs, and concludes that bioorthogonal chemistry, already a workhorse of drug discovery research, is ready for the leap into human testing.

Tagworks publishes convincing results of cancer therapy in mice in Nature Communications

In mouse models of ovarian and aggressive colon cancer, Tagworks Pharmaceuticals has demonstrated the potent antitumour effect of the company’s ‘click-to-release’ bioorthogonal chemistry approach. The results are published in the journal Nature Communications

Raffaella Rossin, et al., Chemically triggered drug release from an antibody-drug conjugate leads to potent antitumour activity in mice, Nature Communications (2018), doi:10.1038/s41467-018-03880-y

Tagworks paper on triggered drug release in Bioconjugate Chemistry

In a recent publication in the scientific journal Bioconjugate Chemistry, Tagworks Pharma describes its success in using a bioorthogonal reaction for the selective cleavage of tumor-bound ADCs in mice. This represents a powerful new tool for ADC therapy as it does not rely on the currently used biological activation mechanisms, thereby potentially expanding the scope of ADC therapy to noninternalizing cancer targets.

Read the full paper – doi:10.1021/acs.bioconjchem.6b00231


Tagworks partner in €6 million EU Horizon2020 grant

A consortium of five European partners, among which Tagworks Pharmaceuticals, has secured a €6 million grant from the EU Horizon2020 program for their research action entitled In Vivo Click PET Imaging Agents: Improving clinical companion diagnostics – Click-It. Coordinator of the Click-It consortium is the University of Copenhagen and next to Tagworks, the other partners are the Technical University of Vienna, the Austrian Institute of Technology and the Johannes Gutenberg University in Mainz (Germany).

Companion diagnostics are crucial for drug development and disease management with regard to patient selection, therapy planning and monitoring. Antibodies have been proven to be optimal disease-targeting and -modulating agents. However, to date, nuclear imaging of antibodies has been limited to the use of long-lived isotopes to be compatible with their slow pharmacokinetics. Major drawbacks include high radiation doses, precluding routine and repeated companion imaging procedures.

The Click-It consortium aims to circumvent this issue by using a pretargeting approach, which centers on the administration and target binding of a tagged antibody followed by administration and binding of a small, fast-clearing, short-lived radiolabeled probe to the tag of the antibody. This results in lower absorbed radiation doses and in a boost in target-blood ratios, which in turn leads to a superior imaging contrast. PET scan snapshots at multiple time-points provide long-term imaging information by applying short-lived nuclides. So far, only the fastest click reaction, the tetrazine ligation, has demonstrated potential in clinically relevant conditions. Tagworks has shown in SPECT imaging studies that this click reaction can be applied for the imaging of non-internalizing antibodies in vivo. This project aims at expanding the scope of click-pretargeted imaging to 18F-labeled tetrazines for PET imaging and to internalizing antibodies.