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.

Eniluracil (5-ethynyluracil, GW 776, 776C85) is a potent irreversible inhibitor of dihydropyrimidine dehydrogenase, the first enzyme in the catabolic pathway of 5-fluorouracil (5-FU), the most widely used drug in cancer chemotherapy. Eniluracil increases the oral bioavailability of 5-FU to 100%, facilitating uniform absorption and predictable toxicity. Eniluracil was being developed as a novel modulator of 5-FU for the treatment of cancer.

Phenethyl isothiocyanate (PEITC) presents in cruciferous vegetables which have been shown to decrease the risk of various types of malignancies. PEITC targets multiple proteins to suppress various cancer-promoting mechanisms such as cell proliferation, progression and metastasis. PEITC induces apoptosis in human colon cancer HT-29 cells, prostate cancer cells, and osteogenic sarcoma U-2 OS cells. Unique to prostate cancer is that PEITC downregulates the transcriptional factor Sp1, a regulator of AR expression. PEITC suppresses 4-(methylnitrosamino)-1-(3-pyridyl)-1-butoneinduced pulmonary neoplasia in A/J mouse lung, exhibits cancer chemopreventive activity in rat and reduces azoxymethane-induced colonic aberrant crypt foci formation. PEITC appears to be a promising agent for cancer therapy and is already under clinical trials for leukemia and lung cancer.

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.