Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4; along with other anthraquinones and anthracyclines, it shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding. Ametantrone is anticancer drug candidate targeting DNA. Ametantrone is a topoisomerase II inhibitor of the anthrapyrazole family. Ametantrone induces interstrand DNA cross-links in HeLa S3 cells. These cross-links were observed only in cellular system suggesting that metabolism of the drugs is a necessary step leading to DNA cross-linking. Ametantrone appeared to be very well tolerated and easy to handle. A dose-schedule of 135 mg/m2 q 2–3 weeks was recommended for phase II studies in solid tumors.

Ozarelix is a luteinizing hormone-releasing hormone (LHRH) antagonist. It is known that LHRH antagonist exerts rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones. Thus this inhibitor can be effective in a variety of hormonally dependent disease including prostate cancer, benign prostatic hyperplasia (BPH), and endometriosis. Ozarelix was developed for the treatment of all these diseases including Alzheimer's disease. However, in January 2010 Spectrum Pharmaceuticals announced that it was discontinuing development of ozarelix in BPH. Because the low-dose intermittent therapy was disappointing in the treatment of lower urinary tract symptoms in men with BPH. The development of the drug for Alzheimer's disease was also discontinued. Ozarelix completed phase II trials for the treatment of prostate cancer and is in preclinical trials for the treatment of endometriosis and ovarian cancer.

DAPTA (D-ala-peptide T-amide) is a synthetic peptide that prevents HIV entry by blocking binding of HIV gp120 protein with CCR5 receptor. In a small clinical study of internasal formulation of DAPTA in long-term infected HIV patients, administration of DAPTA led to decrease in the amount of virus isolated from white blood cells, an increase in gamma-interferon secreting T-cells in the absense of drug-related toxicity. In another clinical study DAPTA in combination with antiretroviral therapy reduced the peripheral (plasma and serum) viral load, but did not reduce the CSF viral load.

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.

Gemopatrilat is a vasopeptidase inhibitor, that was found to inhibit plasma and renal angiotensin converting enzyme (ACE), as well as renal neutral endopeptidase (NEP). Gemopatrilat is rapidly absorbed, and causes inhibition of circulating and renal ACE and renal NEP after a single oral dose for up to 48 hours in rats. Potentially, this is because the free sulfhydryl group of gemopatrilat forms reversible disulfide linkages with plasma and tissue proteins and is thus eliminated from the body at a very slow rate. Similar metabolism of the compound was found in rat, dog, and human. Gemopatrilat was evaluated for its potential in treatment of antihypertensive activity in hypertension (independent of age, renin and salt status or ethnic origin), as well as its potential as a new therapeutic modality for the treatment of congestive heart failure. The drug was never marketed. A phase II study for treatment of hypertension and heart failure has been discontinued.

Cetylamine is an aliphatic primary amine that possesses surface-active properties and widely used in water treatment. Cetylamine shows moderate anti-tuberculosis activity. Cetylamine also may be used as a source of fluoride in the prevention of dental caries.

CBP-501 is a chemically modified duodecapeptide and an analog of M-phase inducer phosphatase 3 (CDC25C) that increase cisplatin influx into tumor cells through an interaction with calmodulin enhancing cisplatin cytotoxicity, and affects cell cycle progression by abrogating DNA repair at the G2 checkpoint. CBP501 selectively inhibits the kinases MAPKAP-K2, C-TAK1, and CHK1 in vitro. Cell lines exposed to CBP501 plus bleomycin show a dose-dependent reduction of phosphorylated Ser216 on CDC25C. In addition to these effects on the G2 checkpoint, CBP501 also increases platinum concentration and DNA-platinum adduct formation in tumor cells through binding with calmodulin. In an in vitro panel testing the sensitivity of several tumor-derived cell lines to CBP501 in combination with a variety of anti-cancer agents, the combination of CBP501 with cisplatin was particularly effective against all four mesothelioma cell lines tested. Unfortunately, CBP-501 does not improve the efficacy of standard chemotherapy for malignant pleural mesothelioma.

Deterenol is a beta-adrenoceptor agonist. It is an effective nonmydriatic and nonmiotic hypotensive agent, which can be used in antiglaucoma treatment.

Phorbol 12-myristate 13-acetate (PMA) also commonly known as 12-O-Tetradecanoylphorbol-13-acetate (TPA) is a phorbol ester that is commonly used to activate phospholipid-dependent protein kinase (protein kinase C). PMA/ TPA possesses potential antineoplastic effects and was studied in phase II clinical trials together with dexamethasone in patients with relapsed or refractory acute myeloid leukemia. In addition, PMA/ TPA participated in phase I trial for treating patients with hematologic cancer or bone marrow disorder that has not responded to previous treatment. Nevertheless, both clinical trials were terminated. Besides, PMA/ TPA was studied in patients with solid tumors, which had depressed white blood cell and neutrophil counts because of prior treatment with cytotoxic cancer chemotherapeutic drugs. It was shown, that the drug increased the low white blood cell and neutrophil counts toward the normal range.