GLyCanCure - a first in class new drug for treatment of advanced forms of cancer

Globally nearly 20 million new cancer cases and almost 10 million cancer deaths occurred in 2020. Beside the tremendous burden on patients and families, there is a significant impact on the global economy with annual costs of cancer of nearly 2 trillion USD. The GlyCanCure project primary objective was to achieve an advanced cancer drug candidate to be used for treating Triple negative breast cancer (TNBC). Initially the most important research activities were focused on thorough research around optimization of stability and solubility of existing compounds. Further optimization has been conducted through own research and with CROs to modify compound by systematic chemical modifications and pharmacological evaluation. All novel derivative compounds have been tested in enzyme- and cell assays and animal models. In the cell assays and animal models bioavailability and efficacy in targeting cancer growth and development have been assesed. Conclusion from the development and teste reveal that the Arctic Pharma medical candidate cannot be optimized to meet medicinal/clinical requirements for treating TNBC as monotherapy.

Effects of the medical compound developed and tested by Arctic Pharma in GlyCanCure did not meet the requirements to be used a mono-therapy for treating Triple negative breast cancer (TNBC). The Arctic Pharma compound has been thoroughly characterized to target LDH with high precision through development of metabolic inhibitors and PROTAC. This knowledge also revealed that inhibiting LDH alone is not sufficient to target TNBC. Our work has provided us with in depth knowledge on the compound AP7404, how and where it works. This knowledge will be used in our future strategy to develop combinatoric cancer therapies using AP7404 together with other metabolic drugs and/or immune therapy.

The primary objective is to achieve an advanced cancer drug candidate degrading lactate dehydrogenase A (LDHA) which is an enzyme in humans encoded by the LDHA gene. We shall be ready for starting full GMP/GLP regulatory documentation. Triple negative breast cancer (TNBC) will be chosen as the first indication. The risk for termination in later development phase should be reduced to a minimum based on performed studies in this drug discovery phase. The major research activities in the project are design and synthesis of LDHA-degrader molecules, obtain a better understanding of structure-activity relationship, chemical and pharmaceutical studies, and biological studies of new compounds, including testing on enzymes, cells and in animal models. Globally an estimated 19.3 million new cancer cases and 10 million cancer deaths occurred in 2020. Beside the tremendous burden on patients and families, there is a significant impact on the global economy with annual costs of cancer of nearly 2 trillion USD. We have shown that GLyCanCure targets the LDHA enzyme in nano-molar concentrations and inhibits TNB tumour growth in mice in micro-molar concentrations. GLyCanCure represents a first in class drug and will be used alone or in combination with other established cancer treatments such as immunotherapy for the treatment of advanced forms of cancers. The drug can be brought to market in one of two business models; raising the necessary equity funds to bring the drug to market, or engage in a strategic partnership with a major or medium size pharmaceutical company. The latter option could include full out-licensing of the asset. Arctic Pharma see GLyCanCure a very promising first in class drug which will targeting a board set of glycolytic cancers with a very high potential for value creation.