Novel GPCR agonists
G protein-coupled receptors (GPCRs) are all activated by agonists, represent an important class of drug targets, and approximately 34% of all Food and Drug Administration (FDA) approved drugs target 108 members of this family. It is estimated that GPCRs are targets for about 50% of drugs currently on the market, mainly due to their involvement in signaling pathways related to many diseases i.e. mental, metabolic including endocrinological disorders, immunological including viral infections, cardiovascular, inflammatory, senses disorders, and cancer. We are developing entirely novel orally bioavailable small molecule GPCR agonists targeting diseases such as schizophrenia and epilepsy that can be synthesized by efficient synthesis routes and are protected by composition-of-matter patent applications.
Peptide-drug-conjugates for cancer treatment
Antibody-drug conjugates (ADC) provide an established therapeutic strategy to combat cancer in a targeted way and has lead to several products on the market such as for example ado-trastuzumab emtansine. A recent development is to use targeting peptides (PDC) instead of antibodies – providing higher selectivity, a straightforward, less expensive synthesis, more tunable pharmaco-kinetic properties of the drug product.
MolGenie has acquired a PDC drug discovery platform from OntoChem GmbH aiming to prevent metastasis in high risk breast cancer but also orphan diseases like Ewing Sarcoma.
MolGenie’s first PDC targets NPY1R over-expressing cancers, a modality that has been shown to correlate with a high rate of metastasis. The molecule has shown efficient activity in patient derived xenoplant animal models of breast cancer and sarcoma and are now prepared for further development in formal preclinical GLP studies.
Other diseases that could be treated with MolGenie’s PDC platform using different targeting peptides are melanoma, pancreatic or prostate cancer.
Cystein proteases inhibitors to fight viral infections
Cystein proteases are enzymes that play a significant role in the development of several diseases. Thus, the SARS-CoV2 virus needs the cysteine protease Mpro to cleave its translated protein product into functional units that are essential for viral replication and progression of the disease. Orally bioavailable Mpro inhibitors are the target of a current joint project with Anixa Inc. Our patented small molecule inhibitors have shown high activity in in vitro enzyme and cell based infection assays and are prepared for further development. This project is a collaboration with Anixa Biosciences Inc, San Jose, USA.