Defosfamide (Mitarson) was developed as antineoplastic agent. Mitarson and radioactive gold were used in some patients with poor results. The most serious complication resulting from therapy was hemorrhagic cystitis.

Acodazole is a synthetic imidazoquinoline with antimicrobial and antineoplastic activity. Acodazole intercalates into DNA, resulting in disruption of DNA replication. Use of this agent has been associated with significant cardiotoxicity, especially prolonged cardiac output interval (Q-Ti) on electrocardiogram and polymorphic ventricular tachycardia ("torsades des pointes").

Etoglucid is a cytotoxic drug used as neoplastic agent for the treatment of malignant tumors. Etoglucid was synthesized by reacting a diol with two equivalents of an alkyl chloride. This alkylating agent is commonly used in Europe but is not available in the United States. It is readily diffusible into the cerebral fluid into cerebrospinal fluid but has a metabolic half-life of only 10 to 15 min. It has been shown in animal experiments to be rapidly destroyed in the liver and thus possibly less damaging to the bone-marrow. Only the polymorphonuclear leucocytes being greatly reduced. The blood returned to normal in two to three weeks, and no other important toxic changes were observed.

Fadrozole (CGS 16949A) is a tetrahydroimidazole-pyridine derivative is a non-steroidal inhibitor of aromatase. In the third phase of clinical trials it was shown, that this drug has good therapeutic effect as a second-line treatment in postmenopausal women with metastatic breast cancer.

Efaproxiral is a synthetic, small molecule, radiation-sensitising agent being developed by Allos Therapeutics primarily for the treatment of cancer. It works by binding and allosterically stabilising deoxyhaemoglobin in hypoxic regions of tumour tissue. This increases oxygen uptake of the tumour tissue and restores its sensitivity to radiation therapy, making therapy potentially more successful. But no benefit was seen for efaproxiral in phase III clinical trials. The only serious adverse effect detected was hypoxaemia. Efaproxiral is explicitly excluded from the 2012 World Anti-Doping Agency list of Prohibited Substances and is explicitly included in the Prohibited Methods section M1 as a forbidden procedure to alter the oxygen-haemoglobin dissociation curve in order to allosterically modify haemoglobin.

Zorubicin is a benzoylhydrazone derivative of the anthracycline antineoplastic antibiotic daunorubicin, but it introduces lower cardiomyopathy and bone marrow toxicity. Zorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair as well as RNA and protein synthesis. The cytotoxic effect results from intercalation between DNA pairs. To minimize toxicity, individualized dose regimens are given preferentially over prolonged periods of time by carefully inspecting i.v. administration to prevent extravasation.

Cyclofenil is a anti-estrogen drug developed for the treatment of female infertility and for induction of ovulation. Cyclofenil exerts its action by binding to estrogen receptor beta and demonstrates agonism or antagonism depending on tissues type. The drug was withdrawn from the market due to high risk of hepatotoxicity.

Lasofoxifene is an active component of Fablyn. Fablyn is used for the treatment of osteoporosis in postmenopausal women. Lasofoxifene is a nonsteroidal selective estrogen receptor modulator. Lasofoxifene has no effect on CYP2E1- or CYP2D6-mediated drug metabolism and should not affect drugs metabolized by other cytochrome P450 isoenzymes. Common adverse reactions considered to be related to Fablyn therapy were muscle spasms, hot flush and vaginal discharge. Lasofoxifene approved in the EU in 2009 is now withdrawn from use in the European Union.

Elliptinium is an antineoplastic agent, which was used in the treatment of metastatic breast cancer in France under the name Celiptium. The drug is known to intercalate into DNA and inhibit topoisomerase II. Several studies have demonstrated that this molecule can be oxidized, yielding a reactive electrophilic form, which is able to bind covalently to a nucleophilic biological molecule.