In the HER2-positive breast tumor model, in vitro experiments revealed a higher cytotoxicity of MF-TTZ-MMAE (IC50 = 1 nM) on BT-474 cell line compared to the SOC (IC50 ≈ 100 nM). In vivo, the treatment with MF-TTZ-MMAE was well tolerated at all tested doses (1 and 5 mg/kg). At 5 mg/kg, the MF-TTZ-MMAE compound induced a full regression of tumors after second treatment.