Metamelfalan is an antineoplastic agent. Metamelfalan is the meta form of the levo isomer melphalan. Metamelfalan causes crosslinking of DNA, thereby preventing DNA replication and eventually cellular proliferation.

Mitoclomine, an alkylating agent was developed to treat cancer. This drug was involved in phase I/II clinical trial to treat patients with chronic lymphocytic leukemia. Information about the further development of a drug is not available.

Bofumustine, also known as RFCNU was studied as an antitumor agent. Bofumustine participated in phase II trials in patients with digestive tract tumors. It was shown that 30% has remissions among which 13% were greater than 50%. In addition, bofumustine participated in phase II clinical trials, where it showed to be effective in 8% of digestive tumors, in 1 out of 7 pancreatic cancers and in 3 out of 10 hepatic and pulmonary metastases from an undiscovered primary adenocarcinoma. However, further information is not available.

Sarcolysin is the isomeric form of melphalan with alkylating activity. Sarcolysin is a bifunctional alkylating agent. The cytotoxicity of sarcolysin appears to be related to the extent of its interstrand cross-linking with DNA, probably by binding at the N7 position of guanine. Like other bifunctional alkylating agents, it is active against both resting and rapidly dividing tumor cells. The levo-isomer - melphalan (L-sarcolysin) is approved under the brand name ALKERAN for the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. In addition, the drug was approved under the trade name Evomela. Evomela is indicated for use as a high-dose conditioning treatment prior to hematopoietic progenitor (stem) cell transplantation in patients with multiple myeloma. In addition, for the palliative treatment of patients with multiple myeloma for whom oral therapy is not appropriate.

Ambamustine (PTT-119) is a bifunctional alkylating agent. Its antitumour effect is reported to mainly be through alkylation and interstrand cross-linkage of DNA. The drug was awaiting registration in Italy for the treatment of non-Hodgkin's lymphoma, and was also in phase-II clinical trial for small cell lung cancer, but was discontinued.

Mafosfamide is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. The effects of mafosfamide on various types of cancer cells were determined during preclinical investigations and clinical trials. Its development has been discontinued.

Spiromustine is a bifunctional nitrogen alkylating agent with antineoplastic activity and lipophilic properties. Preclinical screening has shown activity against a variety of tumors, including an intracranially implanted ependymoblastoma. Alkylating activity has been demonstrated in an intracerebral glioma in the rat. Spiromustine is a cell cycle non-specific agent. Animal pharmacology studies have shown a biphasic plasma decay curve, with hepatic metabolism and excretion, an enterohepatic circulation of metabolites, and approximately 50% renal excretion of unchanged drug. Toxicology studies in mice, rats, and dogs showed that dose-related myelosuppression and neurotoxicity predominated; other organ toxicities were mild. In Phase I clinical trials Neurotoxicity was the dose-limiting toxicity presenting as alterations in cortical integrative functions (orientation, language, coordination), leading to a decrease in the level of consciousness.

Enpromate is an antineoplastic agent.