Daledalin is a norepinephrine reuptake inhibitor, developed in the 1970s by Pfizer. In animal models, daledalin potentiates the action of catecholamines, reverses the hypothermia induced by noradrenaline or noradnamine injected into the cerebral ventricles of mice. Daledalin potentiates amphetamine-induced excitation in rats and antagonizes reserpine-hypothermia in mice, tetrabenazine-sedation in rats and reserpine- and tetrabenazine-induced ptosis in mice. It inhibits noradrenaline and 5-hydroxytryptamine uptake by rat brain slices in vitro. In a clinical trial on patients with a depressive illness, no difference in efficacy between daledalin and amitriptyline was found.

Diflumidone is a non-steroidal antiinflammatory drug. It inhibits the biosynthesis of prostaglandin by bovine seminal vesicle microsomes and arachidonic acid-induced aggregation of human platelets in a concentration-dependent manner. Diflumidone is a competitive inhibitor of prostaglandin synthetase. Diflumidone also inhibits equally the formation of PGE2 and PGF2a, which suggests blockade of endoperoxide formation. The relative topical efficacy of indomethacin and diflumidone for the suppression of ultraviolet-light-induced erythema has been compared in a randomized, double-blind, placebo-controlled study in man. At 24 h after application, the indomethacin-treated sites had significantly less erythema than did the diflumidone-treated sites.

Dazopride is an antagonist of the 5-HT3 receptor and agonist of the 5-HT4 receptor, structurally related to metoclopramide. Dazopride was developed by A. H. Robins Company as an antiemetic and gastroprokinetic drug. Dazoptide demonstrated an antiemetic effect in the clinic after i.v. infusion to patients, receiving anticancer therapy.

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.

Barucainide, an IB anti-arrhythmic agent, was evaluated in patients with coronary artery disease. Its antiarrhythmic effect was studied in patients with markedly depressed left-ventricular function. Barucainide was in phase II clinical trials to treat the patients with arrhythmias but the development of the drug was discontinued.

Milipertine was studied in patients with severe schizophrenia. Information about the current use of the drug is not available.

GSK-2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK-2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. On April 1 2016 GlaxoSmithKine completes a phase-I/II trial for Solid tumours (Late-stage disease) in USA, United Kingdom and South Korea (NCT01458067).

Nafoxidine is a nonsteroidal antiestrogen available as an investigational agent from the Investigational Drug Branch of the National Cancer Institute. It has been used effectively in the treatment of breast cancer patients. Nafoxidine competes with endogenous estrogen for binding to specific estrogen receptors. This agent also inhibits angiogenesis in some tissues by blocking the effects of fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF); paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces oxidative stress, protein kinase C and calcium signaling.

Metethoheptazine (WY-535) is an analgesic agent.