Ilomastat (also known as galardin or GM 6001) is a broad-spectrum matrix metalloproteinase inhibitor. It is a member of the hydroxamic acid class of reversible metallopeptidase inhibitors. The hydroxamic acid binds the catalytic zinc(2+) ion in a bidentate manner, blocking substrate access to the active site and rendering the metal incapable of peptide hydrolysis. Preclinical studies have shown that ilomastat can inhibit conjunctival scarring after glaucoma filtration surgery in rabbits, in lens capsules following simulated cataract surgery, and in models of vitreoretinal contraction.

GENISTEIN is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA topoisomerases, type II) activity and is used as an antineoplastic and antitumor agent. Experimentally, it has been shown to induce G2 phase arrest in human and murine cell lines. Additionally, genistein has antihelmintic activity. It has been determined to be the active ingredient in Felmingia vestita, which is a plant traditionally used against worms. It has also been demonstrated to be effective against intestinal parasites such as the common liver fluke, pork trematode and poultry cestode. Further, genistein is a phytoestrogen which has selective estrogen receptor modulator properties. It has been investigated in clinical trials as an alternative to classical hormone therapy to help prevent cardiovascular disease in postmenopausal women. Genistein can be found in food sources such as tofu, fava beans, soybeans, kudzu, and lupin. It is also present in certain cell cultures and medicinal plants.

Atrimustine [bestrabucil, busramustine, KM 2210, kregan], a conjugate of estradiol and chlorambucil, is a DNA antagonist that was developed by Kureha Corporation (Japan). Atrimustine is an antineoplastic drug that was used for the treatment of breast cancer, non-Hodgkin's lymphoma, as well as Graft-versus-host disease. Side effects of atrimustine in clinical trials included vaginal bleeding and gynecomastia. Atrimustine reached preregistration in Japan for the treatment of cancer, however, its development has been discontinued.

Batimastat is a powerful broad spectrum hydroxamate-type matrix metalloproteinases inhibitor(MMPI), with potent anticancer activity. Batimastat inhibits the growth and spread of lung tumors, breast cancer regrowth, and human colon tumor growth and spread in mouse models. Batimastat reduces MMP-mediated vascular dysfunction and vessel wall damage and enhances the sealing ability and bond strength of dental adhesives. Batimastat was the first MMPIs evaluated in cancer patients and to be used in a clinical trial. Batimastat was administered by the intraperitoneal and intra-pleural route in clinical trials. The Phase I and II clinical trials of Batimastat, when administered intraperitoneally, did not show a good response. Due to its poor water solubility, it is not well accepted for cancer treatment.

Zeniplatin is a third-generation organoplatinum compound used in cancer treatment. It is a more water-soluble organoplatinum than cisplatin. On the phase I clinical trial the most prominent non-hematological side-effect of zeniplatin was nausea and vomiting. Other non-hematological side-effects were mild or absent. Zeniplatin did not induce significant neurological or auditory toxicity. Phase II study of zeniplatin on patients with advanced ovarian cancer revealed that zeniplatin may be active in relapsing, platinum-pretreated patients, and has no direct effects on renal function as measured by isotope clearance. Despite these findings, occasional nephrotoxicity may occur in patients with compromised kidney function, even with prophylactic hydration, and thus limit the application of this new analogue. Zeniplatin has a pharmacokinetic profile similar to that of carboplatin. Zeniplatin demonstrated only modest activity in melanoma with significant gastrointestinal and hematologic toxicity.

Acefluranol is a nonsteroidal antiestrogen of the stilbestrol group that was never marketed.

Carmofur, also known as 5-fluoro-N-hexyl-2,4-dioxo-pyrimidine-1-carboxamide and as 1-hexylcarbamoyl-5-fluorouracil, is a pyrimidine analogue which acts as an antineoplastic agent through inhibition of thymidylate synthase. It has been used in the treatment of breast and colorectal cancer. Carmofur is approved in Japan for the treatment of cancer.

Vinflunine (Javlor) is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine, at the lowest effective concentrations, interacts with the Vinca alkaloid binding site on tubulin, suppresses microtubule dynamics (switching at microtubule ends between phases of slow growth and rapid shortening) and microtubule treadmilling (growth at the plus end and shortening at the minus end of the microtubule), causes cell cycle arrest which appears on fluorescence-activated cell sorting analysis as a G2 + M phase arrest, and is associated with an accumulation of cells in mitosis leading to cell death via apoptosis. Vinflunine has been been approved for advanced or metastatic transitional cell carcinoma of the urothelial tract. Pierre Fabre submitted an extension to the EU authorisation to add treatment of advanced breast cancer.

Arzoxifene (LY353381) is a synthetic, nonsteroidal ligand termed selective estrogen receptor modulator. Arzoxifene has antiestrogenic effects on the breast and endometrium, but pro-estrogenic effects on bone and lipids. Arzoxifene has been studied in the treatment of various hormone-responsive neoplasms. Its development has been discontinued.

ANTHRAMYCIN, a member of the pyrolobenzodiazepine family, is an antineoplastic antibiotic derived from a thermophilic actinomycete Streptomyces refuineus var. thermotolerans (NRRL 3143). It binds covalently to DNA, thereby inhibiting replication and transcription processes.