Algeta ASA is focused on the development of novel targeted cancer therapeutics, has exercised its option to take an exclusive worldwide license to patented Lumi4 bi-functional chelator technology from California-based, Lumiphore, Inc. and has extended the collaboration to include additional chelator families. These technologies are currently being developed by Algeta to conjugate thorium-227 to tumour-targeting molecules to create Targeted Thorium Conjugates (TTCs).

Lumiphore's Lumi4 technology is based on a unique class of bi-functional chelators that forms a novel cage structure surrounding and tightly binding thorium-227, which can then be covalently attached to a range of tumour-targeting molecules, such as monoclonal antibodies, to create potential cancer therapeutics. Algeta originally signed an option/license agreement with Lumiphore around this technology in 2010 and subsequently extended it to enable further evaluation to be conducted. This stage of evaluation has now been completed successfully.

In parallel with this license agreement, Algeta has also been granted a license by Lumiphore covering a second class of bi-functional chelators that bind strongly to thorium-227, with the option of including a further selection of compounds within that license if future exploratory work confirms their promise.

Under the terms of the agreements, Algeta will pay Lumiphore the option exercise fee for the Lumi4 chelators, and a signature and option fee for the second class of chelators, plus development and sales milestones and a royalty on product sales. Further financial details have not been disclosed.

Thomas Ramdahl, Algeta's chief technology officer, said, "Algeta is assembling a broad portfolio of proprietary technologies (including bi-functional chelators, linkers and tumor-targeting molecules), intellectual property and expertise as a platform for generating Targeted Thorium Conjugates, or TTCs. The addition of the Lumiphore technologies to the portfolio through this license and further option agreements will ensure that we have access to the best bi-functional chelators for thorium-227 as we seek to create a pipeline of TTCs designed to address multiple high-value opportunities in targeted cancer therapy."

Algeta's TTC strategy is based on gaining access to carefully selected tumour-targeting molecules, via in-licensing, collaboration or via third parties, to which it links thorium-227 thereby creating potential new therapeutics. Algeta's disclosed TTC programmes include collaborations with Sanofi and Ablynx; programmes based on CD22- (haematological cancer) and HER2-targeting (breast/ovarian cancer) molecules in-licensed from Immunomedics and Affibody, respectively; and a fully owned TTC programme targeting haematological cancers. Algeta is advancing its preclinical pipeline with the aim of entering its first TTC into clinical trials in 2014.

Algeta is evaluating the potential utility of alpha-particle emitting elements in the treatment of cancer. Previous studies have indicated that such elements may have value in treating cancers by causing double-strand DNA breaks that trigger cell death, and have also shown that the effects of alpha-emission are highly localized as a result of the very short range of the alpha particle (2-10 cell diameters), potentially minimizing off-target effects. Thorium-227 is one alpha-particle emitting element (radionuclide) that has been selected by Algeta for further investigation. By linking thorium-227 to cancer-targeting molecules such as monoclonal antibodies, Algeta believes it may be possible to develop a pipeline of targeted alpha-pharmaceuticals, termed Targeted Thorium Conjugates, or TTCs. Algeta intends to evaluate TTCs in a broad range of cancer types to determine whether the TTC platform could offer advantages over naked (un-armed) antibodies or antibody-drug conjugate technologies that use cytotoxic drugs (rather than alpha-emitting elements) as payloads. Such advantages may include increased potency, a more localized tumouricidal effect and the potential to address drug resistance by virtue of the physical action of the alpha particles.

Lumiphore Inc is a biotechnology leader in the development of proprietary luminescent-metal lanthanide and bi-functional chelation technology for use in high-value imaging and therapeutic applications which are commercialized through market-specific alliances with corporate partners.