ERK1 Inhibitors Market: Competitive Landscape, Pipeline, and Market Analysis 2023

Extracellular signal-related kinase 1 (ERK1), also known as mitogen-activated protein kinase 3 (MAPK3), is an enzyme that acts in a signaling cascade regulating various cellular processes such as proliferation, differentiation, and cell cycle progression in response to a variety of extracellular signals. ERK1 signaling is often dysregulated in cancer due to activated mutations in receptor tyrosine kinase (RTK), RAS, or BRAF, resulting in constitutive pathway activation. ERK1 inhibitors downregulate ERK activity in both tumor cells and normal cells by either inhibiting ERK catalytic activity or preventing the activation of phosphorylation of ERK. ERK1 inhibitors are currently in clinical developmental phases for various disease conditions such as gastrointestinal cancer, non-Hodgkin’s lymphoma, solid tumors, uveal melanoma, acute myeloid leukemia, glioma, pancreatic cancer, and others. BioMed Valley Discoveries, Eli Lilly & Company, Asana BioSciences, Novartis, Merck (MSD), Otsuka Pharmaceutical, and BMS are some of the major players in the Extracellular signal-related kinase 1 (ERK1) inhibitors market.

Key Developments:

In Sep 2020, the US FDA granted the investigational new drug application for BioMed Valley Discoveries, Ulixertinib (BVD-523), an ERK1 inhibitor.

Drugs under the Pipeline for ERK1 Inhibitors:

• Ulixertinib (BVD-523)
• Temuterkib (LY3214996)
• ASN007
• Rineterkib (LTT462)
• MK-8353
• ASTX029
• CC-90003
• HH2710
• JSI-1187
• KO-947
• Tizaterkib (ATG-017)

Clinical Activity and Developments of ERK1 Inhibitors:

Currently, there are 11 drug products in the ERK1 inhibitors, and all of them are in various clinical development phases.

• In Jun 2023, Asana BioSciences released updated pharmacokinetics, safety and efficacy data from the phase-Ib/II HERKULES-3 trial in pancreatic cancer for ERAS 007, an ERK1 inhibitor.
• In Jan 2023, Astex Pharmaceuticals presented the efficacy data from a phase I/II trial in solid tumor for ASTX 029, an ERK1 inhibitor.