It has been clearly established that methylbis (β - chloroethyl) amine hydrochloride (nitrogen mustard) is an excellent supplement to radiotherapy in the treatment of Hodgkin's disease * and is also of some value in other related lymphomas and leukemias.† However, it has the disadvantages that it must be administered intravenously, that it produces marked bone marrow depression, and that it causes such side-effects as nausea, vomiting, and malaise.
A chemical derivative of nitrogen mustard without such disadvantages would be extremely useful. Triethylenemelamine (TEM), which may be administered by mouth, is very toxic, and its effect is often incalculable.‡
Another nitrogen mustard derivative, β-naphthyl-bis (2-chloroethyl) amine (R 48; CB 1048), has proved of some value in Hodgkin's disease, polycythemia rubra vera. and some leukemias.§
Russian investigators have synthesized a nitrogen mustard derivative, p-bis (2-chloroethyl ) aminophenylalanine (sarcolysine), which when tested against a variety of animal tumors has exhibited antitumor activity.12