methotrexate + phenylalanine

Methotrexate + phenylalanine (commonly described as MTX-Phe) is an experimental **prodrug** in which **methotrexate** is chemically conjugated to the amino acid **phenylalanine** through its alpha position. This conjugate is designed specifically for use in antibody-directed enzyme prodrug therapy (ADEPT) and related drug targeting strategies for cancer. MTX-Phe itself is largely inactive (non-toxic) until enzymatically cleaved, typically by carboxypeptidase A (CP-A), at the tumor site, releasing active methotrexate. This approach aims to localize toxic effects to cancer cells and spare normal tissue, increasing selectivity relative to conventional methotrexate therapy. The conjugate was shown preclinically to be an effective substrate for enzymatic activation and exhibits activity in tumor cell lines when combined with specific antibody-enzyme constructs[5][7].

Other names

methotrexate-phenylalanine