Novel clozapine mimetics
Clozapine is used to treat severely ill patients with schizophrenia who have used other medicines that did not work well. It is also used to lower risk of suicidal behavior in patients with schizophrenia or schizoaffective disorder. Although the risk of severe neutropenia with clozapine still exists, it was recently removed by the FDA from participating in the risk evaluation and mitigation strategies (REMS) program to report results of absolute neutrophil count (ANC) blood tests before pharmacies dispense clozapine.
We have designed and are synthesizing, testing and patenting novel molecular scaffolds that are clozapine mimetics with a better safety/activity profile. This project is a collaboration with Actyon Discovery Inc, San Diego, USA and Systasy Biosciences GmbH in Munich, Germany.
Novel modafinil mimetics
Modafinil is a drug medication used primarily to treat narcolepsy, a sleep disorder characterized by excessive daytime sleepiness and sudden sleep attacks. Modafinil is also approved for stimulating wakefulness in people with sleep apnea and shift work sleep disorder.
We have designed and are synthesizing, testing and patenting novel molecular scaffolds that are Modafinil mimetics with a better safety/activity profile. This project is a continuation of our long interest in sleep disorders that lead to the discovery of the first small molecule Orexin receptor antagonists as described in WO2001068609A1.
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.