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.

Classification

Small (low molecular weight), macrocyclic tyrosine kinase inhibitor

Molecular Targets

MET, SRC, CSF1R

Monograph

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

N/A