Gancotamab

Gancotamab (MM-302) is a HER2-targeted antibody-liposomal Doxorubicin conjugate with antitumor activity. Gancotamab encapsulates Doxorubicin to facilitate its delivery to HER2-overexpressing tumor cells[1].

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

HER2

Gancotamab (MM-302; 0.5 μM; 72 hours) increases cell death in BT474-M3 and NCI-N87 cells[1]. Gancotamab (MM-302; 1 μM; 2-24 h) activates the p-p53 level and has no effect on p-Akt signal in BT474-M3 and NCI-N87 cells[1]. Gancotamab (MM-302) is a HER2-targeted liposome encapsulating approximately 20,000 molecules of Doxorubicin in its core and 45 single-chain anti-HER2 antibodies (scFv) conjugated to its surface[1]. Cell Viability Assay[1] Cell Line: BT474-M3 and NCI-N87 cells Concentration: 0.5 μM Incubation Time: 72 hours Result: Significantly reduced in vitro viability. Western Blot Analysis[1] Cell Line: BT474-M3 and NCI-N87 cells Concentration: 1 μM Incubation Time: 2 h, 8 h, and 24 h Result: Increased the p-p53 level and had no effect on p-Akt signal.

Gancotamab (MM-302; 3 mg/kg; i.v.; every 7 days; for 3 doses) shows tumor growth inhibition and increases the expression of the DNA damage marker p-p53[1]. Animal Model: Seven-week-old female NCR/nu mice injected with NCI-N87 cells[1] Dosage: 3 mg/kg Administration: i.v.; every 7 days; for 3 doses Result: Showed significantly antitumor activity.

[1]. Christopher W Espelin, et al. Dual HER2 Targeting with Trastuzumab and Liposomal-Encapsulated Doxorubicin (MM-302) Demonstrates Synergistic Antitumor Activity in Breast and Gastric Cancer. Cancer Res. 2016 Mar 15;76(6):1517-27.