Taltobulin, also known as HTI-286 and SPA-110, is a fully synthetic analog of the natural tripeptide hemiasterlin, inhibits tubulin polymerization and circumvents transport-based resistance to taxanes. Taltobulin was a potent inhibitor of proliferation (mean IC50 = 4 nm in 18 human tumor cell lines) and had substantially less interaction with multidrug resistance protein (P-glycoprotein) than currently used antimicrotubule agents, including paclitaxel, docetaxel, vinorelbine, or vinblastine. Taltobulin showed strong antitumor activity both in androgen-dependent and androgen- independent tumors and may be a promising agent in second- line treatment strategies for patients suffering from docetaxel- refractory prostate cancer.

Oxodipine is a dihydropyridine calcium channel blocker that has been developed by IQB as an antihypertensive agent. Experiments on dogs have shown that oxodipine exerted a relatively specific action on blood vessels without significant intrinsic negative chronotropic properties. in addition, in Europe, the drug was involved in phase III clinical trials in and in phase II for the treatment of Hypertension. Besides, oxodipine was studied for the treatment of ischaemic heart disorders. However, these studied were discontinued.

Ancriviroc (SCH 351125) is a small-molecule antagonist of the human immunodeficiency virus type 1(HIV-1) coreceptor CCR5. It has in vitro activity against R5 viruses with 50% inhibitory concentrations ranging from 1.0 to 30.9 nM. Ancriviroc is an orally bioavailable small molecule inhibitor of HIV-1 entry via CCR5 coreceptor interaction. Ancriviroc has potent activity against RANTES binding (K(i) = 2 nM), possesses subnanomolar activity in blocking viral entry and has excellent antiviral potency versus a panel of primary HIV-1 viral isolates. Ancriviroc had been in phase I clinical trials by Schering-Plough (subsidiary of Merck Sharp & Dohme) for the treatment of HIV infection. However, this research has been discontinued.

BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. Hsp90 is overexpressed in many types of cancer and acts to stabilize malignancy producing oncoproteins. Therefore, inhibition of Hsp90 with BIIB021 leads to the degradation of oncoproteins that drive malignancy.

S-(+)-niguldipine is a more active enantiomer and is a selective antagonist for the and α1A-adrenoceptor. In addition, it can be used for discriminating of alpha 1A- from alpha 1B-adrenoceptors. There were made attempts to investigate the antidepressant action of S-(+)-niguldipine on rats, but that studies were unsuccessful.

IZONSTERIDE, a benzoquinolinone, is a selective inhibitor of the 5-alpha reductase, with antagonistic effect on both the type I (liver, skin, hair follicles) and type II (prostate) isoforms of the enzyme. It is a competitive inhibitor of type I 5-alpha reductase and a non-competitive inhibitor of type II 5-alpha reductase. It was under development for the treatment of prostatic cancer.

Azamethiphos, an organothiophosphate insecticide, initially was used in 1991 for the treatment against sea lice. However, because of reduced sensitivity in 1999, the use of this compound was terminated. Azamethiphos was re-introduced in 2008; it’s the main component of Salmosan, a pesticide presently used for treatment against sea lice. Salmosan is applied as a bath treatment and then released into the surrounding seawater

Rebimastat (BMS-275291) is a broad-spectrum matrix metalloproteinase (MMP) inhibitor free from toxicity-related inhibition of sheddases (cleaving membrane proteins at the cell surface). This MMP2 and MMP9 inhibitor may stop the growth of cancers by stopping blood flow to the tumor (stopping them from dividing). It might also block the enzymes necessary for growth of the tumor cell. Multiple phase II trials and a phase III clinical trial have been completed, testing the efficacy and safety of the compound in prostate cancer, HIV-related Kaposi’s Sarcoma, non-small cell lung cancer (phase II and III) and breast cancer.

Litracen revealed very potent thymoleptic properties with a weak sedative action. Melitracen is gradually metabolized to litracen, and after repeated doses of melitracen, the organs will, for the most part, contain the metabolite. Litracen was developed as an antidepressant agent.

Licofelone (ML 3000) is a pyrrolizine derivative originally discovered by Merckle GmbH and developed by EuroAllaince with a unique pharmacological profile, which comprises optimal gastrointestinal tolerability and high analgesic and anti-inflammatory activity. These effects are due to balanced and selective inhibition of both cyclo-oxygenase and 5-lipoxygenase. Inhibition of 5-lipoxygenase may reduce the gastrointestinal toxicity associated with other non steroidal anti-inflammatory drugs, which only inhibit cyclooxygenase. Licofelone also has antipyretic and antiaggregatory properties. Clinical and preclinical trials were also undertaken for osteoarthritis, rheumatoid arthritis, asthma, pain and inflammation. However, development for these indications appear to have been discontinued.