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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.

Clinical status

ASTX029 has completed a Phase 1/2 study in patients with advanced or refractory solid tumors to determine safety, pharmacokinetics and preliminary activity.

ASTX029 was discovered by Astex Pharmaceuticals, and is licensed to Mosaic Therapeutics for further research, development and commercialisation using its proprietary platform.

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