| 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 | | |||
| Discovery Programs | TBD | Oncology | | |||
| Preclinical | IND | Phase I | Global Rights |
CDK2 | ETX-197/BG-68501 | Oncology | |||
| |||
Mutant PI3Kα | ETX-636 | Oncology | |||
| |||
Pan-KRAS | ETX-929 | Oncology | |||
| |||
Discovery Programs | TBD | 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 monkey.
Discovery Programs
We have a number of early-stage discovery programs at various stages of maturity launched with our Kinetic Ensemble® platform. With an initial focus on oncology, our team is looking at a variety of different exploratory and novel targets.