ambamustine

Ambamustine (PTT-119) is a **bifunctional alkylating agent** and synthetic tripeptide, chemically described as p-fluoro-L-phenylalanine-m-bis-(2-chloroethyl)-amino-L-phenylalanine-methionine ethoxy hydrochloride. Its main mechanism is DNA alkylation, leading to interstrand cross-linkage and cytolytic activity against tumor cells. Ambamustine has demonstrated preclinical and clinical antitumor activity in multiple models resistant to L-phenylalanine mustard, methotrexate, and cisplatin, as well as activity against acute nonlymphoblastic leukemia and non-Hodgkin's lymphoma. It was evaluated in clinical studies for use in resistant/relapsed non-Hodgkin's lymphoma and small cell lung cancer, showing efficacy and acceptable tolerance. The drug also exhibits immunopharmacological and antiviral activity and may be used for ex vivo tumor cell elimination in bone marrow grafts. It is considered non-cross-resistant with other alkylating agents and has a low propensity to induce drug-resistant phenotypes[1][2][3][4][5][7][10].

Other names

p-F-Phe-m-bis-(2-chloroethyl)amino-L-Phe-Met ethoxy HClp-fluoro-L-Phe-m-bis-(2-chloroethyl)amino-L-Phe-Met ethoxy HCl