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Product pipeline

Breaking Grounds - A Novel Approach to Targeting Cancer

Our innovative small molecule drugs exhibit exceptional selectivity and precise targeting capabilities. Termed Anaphase-Promoting Complex/Cyclosome (APC/C) inhibitors, they hold great promise for cancer treatment. Based on compelling evidence from preclinical studies and disease models, these small molecules, designed to specifically inhibit APC/C, offer immense potential for the treatment of various cancers. The strong scientific rationale supports our commitment to advancing these novel drugs through clinical trials for the benefit of cancer patients worldwide.

How our drugs work

Therapeutic Areas

Oncology

The APC/C pathway has potential in treating cancer because it plays a critical role in regulating the cell cycle and ensuring proper chromosome segregation during cell division. Dysregulation of this pathway has been linked to the development and progression of many types of cancer.

Anti-virals

The APC/C pathway has also potential in treating viral infections because many viruses have been shown to manipulate this pathway to promote their own replication and spread within the host. By targeting the APC/C pathway, it may be possible to disrupt this process and prevent viral infection.

Neurodegeneration

The APC/C plays a role in neurogenesis and neurodegeneration, particularly in Alzheimer's disease - it is involved in the degradation of tau protein, which is a key component of neurofibrillary tangles. It is therefore a potential therapeutic target for neurodegenerative diseases.

Unlocking New Horizons in Cancer Treatment

Targeting the APC/C Pathway

The APC/C (Anaphase-Promoting Complex/Cyclosome) plays a crucial role in regulating mitotic progression and cell division, making it an attractive therapeutic target for cancer treatment. Current investigations focus on developing small molecule inhibitors that selectively suppress cancer growth and induce cell death, providing a potential therapeutic window for diverse cancer types. These novel inhibitors offer hope for more effective and personalized cancer therapies, with the aim of addressing unmet medical needs.

An exciting mechanism

Novel Therapeutic Strategy: Our drug candidates offer a groundbreaking approach in cancer therapy. Their unique mode of action presents an innovative avenue for treating cancer that may be particularly challenging with traditional approaches.

Precision Medicine: By selectively targeting specific APC/C coactivators, we can reduce off-target effects and minimizing harm to healthy cells, making it a potential game-changer in precision medicine.

Potential Prognostic Marker: The identification of APC/C dysregulation as a key factor in cancer development opens new doors for early diagnosis and personalized treatment strategies.

Triple Negative Breast Cancer (TNBC), highly aggressive cancers, pancreatic cancer, lung cancer, Squamous Cell Carcinoma of the Head and Neck (SCCHN), Colorectal Cancer (CRC) , Non-Small-Cell Lung Cancer (NSCLC), Multiple Myeloma (MM), Bladder Cancer / Urothelial Carcinoma (UC), treatments, therapeutics, drugs

Unlocking Cancer Treatment Potential

Targeting APC/C Deregulation

Dysregulation of APC/C has been linked to faulty mitotic checkpoint signaling, genome instability, and cancer. Numerous studies have identified mutations and abnormal expression levels of APC/C subunits in various cancer types, including breast, colon, lung, and more.

In particular, the co-activators of APC/C, Cdc20, and Cdh1, have emerged as key players in tumourigenesis. Overexpression of Cdc20 has been observed in cervical, lung, prostate, gastric, and other cancers, while Cdh1 is downregulated in breast, prostate, liver, and colon tumours. Dysregulation of these co-activators leads to abnormal cell proliferation, defective chromosome segregation, and genomic instability.

Our findings suggest that APC/C deregulation offers a promising target for cancer treatment. Inhibition of Cdc20 and restoration of Cdh1 activity show potential as novel therapeutic approaches. By targeting APC/C-mediated tumourigenesis, we are developing new avenues for effective cancer treatments. Together with pharma companies as partners, we can pave the way for groundbreaking collaborations that bring us closer to turning these findings into effective cancer therapies.

Novel treatments, therapies, new drugs, oncology, cancer

Our lead drug – Aptegrenix™

Broad-spectrum Efficacy: Aptegrenix™ (o-TFB-Tyr) has shown promising results in a wide range of tumour types, including lung cancer, hepatocellular carcinoma, colorectal carcinoma, soft tissue sarcoma, gastric cancer, malignant lymphoma, and head and neck cancers. It exhibits potent anti-mitotic effects, making it an attractive candidate for combating diverse cancer forms.

Targeting Multiple Coactivators: The drug's unique mechanism involves targeting two crucial APC/C coactivators - Cdc20 and Cdh1. By specifically inhibiting these coactivators, o-TFB-Tyr achieves a precise and efficient regulation of the APC/C complex, avoiding undesirable side effects common in other anti-mitotic agents.

Synergistic Effects: Combining o-TFB-Tyr with other APC/C inhibitors, such as proTAME and Apcin, has shown a synergistic inhibition of mitotic exit. This highlights the potential of perturbing protein complex function by simultaneously inhibiting multiple protein-protein interactions.