| Target | Program | Indication | Preclinical | IND | Phase I | Global Rights |
|---|---|---|---|---|---|---|
| CDK2 | ETX-197/BG-68501 | Oncology |  | |||
| Mutant PI3Kα | ETX-636 | Oncology |  | |||
| Pan-KRAS | ETX-929 | Oncology | | |||
| WRN | ETX-880 | Oncology | | |||
| Preclinical | IND | Phase I | Global Rights |
CDK2 - ETX-197/BG-68501 - Oncology | |||
| |||
Mutant PI3Kα - ETX-636 - Oncology | |||
| |||
Pan-KRAS - ETX-929 - Oncology | |||
| |||
WRN - ETX-880 - Oncology | |||
| |||
ETX-197: A Potential Best-In-Class Oral CDK2 Inhibitor
- Cyclin-dependent kinase 2 (CDK2) is critical to cell cycle regulation and is often hyper-activated in a variety of cancers. It is a critical component of the abnormal growth of cancer cells. While a preclinically validated oncology target, there is no CDK2-specific drug on the market.
- We believe ETX-197 has the potential for treating patients with tumors that have cyclin E amplification and patients who have acquired resistance to standard of care due to dysregulation of CDK2 activity.
ETX-636: A Differentiated Approach to Target Mutant PI3Kα
- Phosphoinositide 3-kinase alpha (PI3Kα) is one of the most frequently over-activated pathways in a variety of cancers and contributes to the metastasis of tumor cells.
- While there are two approved PI3Kα drugs, we believe ETX-636, our potent and selective molecule, can target mutant PI3Kα without impacting glucose homeostasis.
ETX-929: A potent, oral, potential best-in-class pan-KRAS inhibitor
- ETX-929 is a pan-KRAS inhibitor, which spares HRAS and NRAS, and demonstrates potent dual GTP (on) / GDP (off) – state inhibitory activity for the treatment of diverse KRAS-mutant (G12X/G13X/Q61H) and wildtype amplified tumors.
- ETX-929 has an excellent in vitro safety profile and drug-like properties, with good oral bioavailability across species, including nonhuman primates.
ETX-880: An oral, potent and selective covalent inhibitor of Werner helicase
- In vitro, ETX-880 potently suppresses viability and promotes cell death in microsatellite instability-high (MSI-H) cancer cells with no measurable impact on microsatellite-stable (MSS) cells. In vivo, ETX-880 achieves near complete and sustained target occupancy in tumors, triggers the DNA damage response, and induces significant and durable tumor regressions in MSI-H xenograft model.
- ETX-880 has an excellent in vitro safety profile and drug-like properties and is being developed for the treatment of MSI-H cancers including colorectal, gastric and endometrial cancers.
Expanded Access Policy
Expanded access, or compassionate use, is the use of an investigational medicine prior to regulatory approval and outside of a clinical trial.
At this early clinical stage of our development, we do not have sufficient evidence of clinical safety and efficacy of our investigational drugs to support an expanded access program. Therefore, Ensem Therapeutics does not currently offer expanded access to our investigational products. However, we may reevaluate the status of our Expanded Access Policy as additional clinical data become available.
For more information on accessing our investigational medicines via participation in a clinical trial, please visit the clinicaltrials.gov website.