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Last Updated: 04/06/22

Information below provided by the Pharmaceutical Company.

Elzovantinib (TPX-0022)

Agent Description

Elzovantinib (TPX-0022) is an orally bioavailable multi-targeted kinase inhibitor with a novel macrocyclic structure that inhibits the MET, CSF1R (colony stimulating factor 1 receptor) and SRC kinases. Elzovantinib is being evaluated in the ongoing SHIELD-1 clinical trial in patients with MET-driven advanced solid tumors.

Mechanism of Action

Tyrosine Kinase Inhibitor of METR, SRC and CSF1R.


Small (low molecular weight), macrocyclic tyrosine kinase inhibitor

Molecular Targets



Elzovantinib Development Designations

  • Fast Track designation by the FDA in patients with MET amplified advanced or metastatic gastric cancer or GEJ adenocarcinoma after prior chemotherapy
  • Elzovantinib was also granted Orphan Drug designation in 2021 for the treatment of gastric cancer, including gastroesophageal junction adenocarcinoma.

Studies of Interest

Non-small Cell Lung Cancer: Combination studies with Checkpoint Inhibitors, EGFR inhibitors, KRAS Inhibitors

Gastric Cancer: Combination studies with Checkpoint inhibitors, MAbs (HER-2 inhibitor), and Sequencing studies post FGFR failure

Colorectal Carcinoma: Single-agent studies, Combinations studies with EGFR inhibitors, KRAS Inhibitors

Hepatocellular Carcinoma: Combination studies with Chemotherapy, Checkpoint Inhibitors

Pancreatic Carcinoma: Single-agent studies, Combination studies with Checkpoint inhibitors, Chemotherapy

Cholangiocarcinoma: Combination studies with Chemotherapy, Checkpoint inhibitors

Information collaborator would like included in investigator proposals