Acapatamab (AMG-160) is a Half-Life Extended (HLE) Bispecific T-cell Engager (BiTE) with domains that bind to PSMA and CD3. It exhibits Kd values of 14.8 nM for hPSMA and 22.4 nM for hCD3. This compound is utilized in cancer research.

Acapatamab (AMG-160; 0-10000 pM; 48 h) induces T cell activation characterized by increased expression of CD25, CD69, 4-1BB, and PD-1 in T cells. Additionally, Acapatamab at the same concentration and duration promotes a dose-dependent secretion of cytokines, including IL2, IL4, IL6, IL10, IFNγ, and TNFα when co-cultured with T-cells. Moreover, the compound effectively lyses prostate-specific membrane antigen (PSMA) positive prostate cancer cell lines when co-cultured with PBMCs, with an EC50 value of 6-42 pM.

Administered intravenously on days 16, 23, and 31 at dosages of 0.02, 0.2, and 2 mg/kg, Acapatamab demonstrated antitumor properties by inhibiting the growth of CA prostate cancer xenograft tumors in NOD/SCID mice, specifically the 22Rv-1 CRPC model.