Mipasetamab

Mipasetamab is an IgG1κ antibody targeting to AXL, a tyrosine kinase receptor and an TAM Receptor. Mipasetamab involves in synthesis of ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC). ADCT-601 has anti-tumor activity.

ADCT-601 (0.02-9.29 nM; 5 d) shows cytotoxicity on AXL-positive SN12C cells but ont AXL-negative Karpas-299 cells[1].ADCT-601 (0.83 nM; 2-36 h) increases the level of DNA interstrand cross-links time-dependently in SN12C cells[1].

ADCT-601 (3 mg/kg, 6 mg/kg; i.v.; single dose) is safety and tolerability in non-tumor-bearing male Sprague-Dawley rats[1].ADCT-601 (1 mg/kg; i.v.; once daily for 60 days) shows potent and sustained antitumor activity for mouse in both MDA-MB-231 TNBC xenograft model and SN12C renal cancer xenograft model[1].ADCT-601 (0.075, 0.15, or 0.3 mg/kg; i.v.; once daily for 45 days) also dose-dependently in a pancreatic cancer PDX model (PAXF1657) with heterogeneous AXL expression[1].

References:
[1]. Zammarchi F, et al. Preclinical Development of ADCT-601, a Novel Pyrrolobenzodiazepine Dimer-based Antibody-drug Conjugate Targeting AXL-expressing Cancers. Mol Cancer Ther. 2022 Apr 1;21(4):582-593.