Mechanism of Action: Selective Inhibitor of Extracellular Signal-Related Protein Kinases 1 and 2 (ERK 1/2)
Indication: Advanced or Refractory Solid Tumors
How this therapy can help
The extracellular signal-related kinases 1 and 2 (ERK 1/2) are part of a key signalling pathway (the RAS-RAF-MEK-ERK pathway) activated in many tumor types including melanoma, lung, pancreatic and colorectal cancers. While inhibitors of RAF and MEK have been successfully developed and are now commercially available, to date no inhibitor of ERK is available commercially. Given the importance of this pathway in oncogenic signalling, ASTX029 has the potential, both as a single agent, and in combination with other therapies, to result in enhanced anti-tumor activity in a broad range of tumor types.
ASTX029 is currently being evaluated in a Phase 1/2 study in patients with advanced or refractory solid tumors to determine safety, pharmacokinetics and preliminary activity.
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