Piroxantrone is one of a series of compounds commonly known as anthrapyrazoles developed in an effort to combine the broad antitumor activity of the anthracyclines with decreased myocardial toxicity. The mechanism of action of piroxantrone and other anthrapyrazoles is incompletely understood but likely involves DNA binding with induction of DNA strand breaks, DNA-protein cross-linking, and inhibition of DNA, RNA, and protein synthesis. Collectively, these findings suggested an interaction with topoisomerase II. Piroxantrone demonstrated antitumor activity in a wide spectrum of experimental systems against breast carcinoma, colon carcinoma, sarcoma, melanoma and leukemia. Piroxantrone is inactive in patients with persistent, progressive, or recurrent ovarian cancer who recently had received a platinum-based regimen. Piroxantrone has detectable but minimal activity against disseminated malignant melanoma. A phase II clinical trial of the piroxantrone administration for the treatment of advanced metastatic or recurrent endometrial cancer was prematurely terminated due to lack of patient accrual.

Pinoxepin belongs to the dibenzoxepine series of drugs which are characterized by a 6-7-6 tricyclic nuclear structure. Clinical studies indicated that pinoxepin was a potent antipsychotic-sedative equally effective to chlorpromazine and thioridazine. Pinoxepin in studies with chronic schizophrenic patients displayed useful effects on behavior without unduly prominent side effects. In doses above 300 mg seizures are reported and more frequent changes in liver-function tests were noted than with standard drug, but below 300 mg pinoxepin was found to have side effects similar to chlorpromazine and marked sedative effects.

Prifuroline is a benzofuran derivative patented by French pharmaceutical company Laboratoires Jacques Logeais S. A. As an antiarrhythmic agent. After intravenous administration to pentobarbital-anesthetized dogs, Prifuroline produced a significant dose-related decrease in heart rate and in sinus node recovery time. Prifuroline dose-dependently antagonizes the arrhythmogenic action of aconitine in rats when administered either intravenously or intraduodenally. Prifuroline also diminishes ventricular susceptibility to electrical stimulation in open-chest rats; its effect is comparable to that of disopyramide and amiodarone at the same dose levels. Prifuroline was also able to restore sinus rhythm in guinea-pigs after intracardiac conduction blockade with acetylcholine, although being devoid of anticholinergic activity.

Propinetidine is a piperidinol derivative patented by Farbenfabriken Bayer Akt.-Ges. as antitussive agent.

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.

Hydroxytetracaine (also known as oxyamethocaine or hydroxamethocaine) was used as a local anesthetic. Information about the current use of this drug is not available.

Gacyclidine (GK11) is a derivative of phencyclidine with neuroprotective properties. Tritiated gacyclidine and its enantiomers bind to NMDA receptors with binding parameters similar to those of other non‐competitive NMDA receptor antagonists. Beneficial effects of gacyclidine include reduction of lesion size and improvement of functional parameters after injury. In traumatic brain injury models, gacyclidine also improves behavioral parameters and neuronal survival. In an animal model of Amyotrophic lateral sclerosis (ALS), functional alteration of locomotor activity was evident and improved the survival of mice, suggesting that chronic administration of gacyclidine beginning at early symptomatic stage may be beneficial for patients with ALS. Gacyclidine has also been associated with altered mental status and end organ damage in patients.

Ditiocarb, the sodium salt of diethyldithiocarbamate, is a drug with strong antioxidant capacity and chelating activities. It improves the depressed immune responses of newborn and aged mice and mice that are treated with chemotherapy or irradiation. Ditiocarb prevents cisplatin nephrotoxicity in animals without reducing the drug's antitumor activity. Ditiocarb has therapeutic activity in the LP-BM5 murine retrovirus-induced immunodeficiency disease. In that AIDS model, it reduces lymphadenopathy and hypergammaglobulinemia, restores immunocompetence, and prolongs survival. Ditiocarb was safe and reduced the incidence of opportunistic infections in patients with symptomatic HIV infection but ditiocarb had no positive effect on HIV patients. The administration of ditiocarb did not induce any major adverse clinical or biological reactions. Sixty-four patients with nonmetastatic high-risk breast cancer were randomized in a double-blind trial of adjuvant immunotherapy with sodium ditiocarb (DDC) versus placebo. At 6 years, overall survival was 81% in DDC group versus 55%.

Dimecolonium is the N-cholinolytic drug. It is the ganglion-blocking agent. The functional activity in some ganglioid neurones increases after administration of various doses of dimecolin during the blockade and after its termination.

GALARUBICIN (DA-125) is an anthracycline derivative with anticancer activity, containing fluorine. The mechanism of action of this drug lies in inhibition of nucleic acid synthesis through intercalation with DNA. Because the structure and DNA-intercalating properties of DA-125 are similar to adriamycin, the cytotoxic effects of the two anthracyclines probably have similar biochemical mechanisms. Preclinical studies suggest that it may have greater activity and less cardiac toxicity than adriamycin. In a rodent study, administration of D-125 in higher dose levels (25 to 50 mg/kg) has been shown to result in testicular damage.