Levormeloxifene (INN) is an experimental selective estrogen receptor modulator (SERM) that was being developed as an alternative to estrogen replacement therapy for the treatment and prevention of postmenopausal bone loss. Levormeloxifene is the levorotatory enantiomer of non-hormonal, non-steroidal oral contraceptive -- ormeloxifene (trade names Novex-DS, Centron, and Sevista). The development of Levormeloxifene was stopped because of a high incidence of gynecologic adverse events during clinical trials.

Belotecan is a semisynthetic analogue of camptothecin containing a 2-(N-isopropylamino) ethyl group linkage at position C-7 of the camptothecin ring. It stabilizes the complex formed between topoisomerase I and DNA, thereby preventing the religation of DNA breaks. This leads to an inhibition of DNA replication and triggers apoptotic cell death. Belotecan was approved in Korea under the name Camtobell for the treatment of patients with ovarian and small cell lung cancers.

Dimebon (latrepirdine) is an orally available, small molecule, gamma carboline derivative that was developed and used in Russia as an over-the-counter oral antihistamine for allergy treatment since 1980s. In 1990s it was shown that Dimebon has promising potential in treating neurodegenerative diseases. In 2003, Medivation Inc acquired the rights to Dimebon. Medivation went public in December 2004, with Dimebon as the only drug in its pipeline. The product was being developed by Medivation and Pfizer as a treatment for early-stage Alzheimer's disease and Huntington's disease. However, development was discontinued by Medivation and Pfizer in early 2012. Dimebon inhibits alpha-Adrenergic receptors (alpha1A, alpha1B, alpha1D, and alpha2A), Histamine H1 and H2 receptors and Serotonin 5-HT2c, 5-HT5A, 5-HT6 receptors with high affinity. Dimebon may act by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition.

Remoxipride is a substituted benzamide. It is a weak, but relatively selective, central dopamine D2-receptor antagonist and appears to have preferential affinity for extrastriatal dopamine D2-receptors. It also has marked affinity for central sigma receptors. It was introduced by Astra (Roxiam) at the end of the eighties and was prescribed as an atypical antipsychotic. Remoxipride was withdrawn from the market worldwide by Astra because of several cases of aplastic anaemia associated with the drug.

Dodeclonium bromide, an antiseptic, is an active ingredient of multi-ingredient cream, Phlebocreme. This cream is used for symptomatic treatment of painful and pruritic manifestations, particularly in the anal hemorrhoidal crisis.

Exatecan (DX-8951f), a new hexacyclic camptothecin analogue, is a second-generation topoisomerase inhibitor that prevents rapidly dividing cells from replicating by interrupting DNA transcription, ultimately leading to cell death. Preclinical studies showed exatecan to have broad-spectrum antitumor efficacy. Exatecan is in phase III clinical trials for the treatment of pancreas cancer. However, there is no recent report of this research. The compound was co-developed by Daiichi Pharmaceutical (now Daiichi Sankyo) and Yakult Honsha.

Fencamfamin is a camphane derivative, although lacking typical sympathomimetic properties. It is structurally related to the phenylethylamines. It is a central nervous stimulant with pharmacological properties similar to amphetamine. Fencamfamin developed primarily as appetite suppressant or pscyhostimulant, not to increase awareness. Fencamfamin reduces REM sleep and prevents fatigue in subjects deprived of sleep. Fencamfamin raises a mood.

Avorelin is a superagonist of natural luteinizing-hormone-releasing-hormone. Avorelin has been formulated in high molecular weight polylactic glycolic acid to afford protracted and continuous release of the peptide from subcutaneous implants. Avorelin has been in phase II clinical trials by Mediolanum for the treatment of prostate cancer, breast cancer and endometriosis. However, this research has been discontinued. Adverse events mainly related to androgen suppression (hot flushes, decreased libido and impotence) or the nature of the disease (skeletal pain).

Xemilofiban [SC 54684, SC 54684A (HCl), xemlofiban], an orally active antiplatelet agent, is a glycoprotein IIb/IIIa receptor antagonist. This drug was in a phase III clinical trial in the US and Europe for the treatment of thrombosis in patients with unstable angina pectoris and acute myocardial infarction undergoing angioplasty. Because of insufficient evidence of efficacy and concerns about safety over this long of a period of treatment, these trials didn’t get the market approval. In Japan, Sankyo discontinued the development of xemilofiban for thrombosis at phase II following Searle's decision to drop the project.

Cyclobarbital (5-cyclohexenyl-5-ethyl-barbituric acid) is a short-acting barbiturate exerting sedative-hypnotic properties. Cyclobarbital is metabolized to inactive ketocyclobarbital. The convention on psychotropic substances, which was signed in Vienna in 1971, today regulates cyclobarbital as a schedule III barbiturate. Cyclobarbital is used in combination with diazepam tranquilizer (Reladorm).