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.

Pexiganan is a 22-amino-acid synthetic cationic peptide. It is an analog of magainin 2, which is a host defense peptide isolated from frog skin. The drug is thought to act by disturbing the permeability of the cell membrane or cell wall. Pexiganan exhibited in vitro broad-spectrum antibacterial activity when it was tested against 3,109 clinical isolates of gram-positive and gram-negative, anaerobic and aerobic bacteria. It is currently in phase 3 clinical trials as a topical antimicrobial agent for the treatment of mild infections associated with diabetic foot ulcers. In vitro data for pexiganan acetate suggest that the drug does have hemolytic activity at concentrations relevant for antibacterial activity. In association with tigecycline, pexiganan administration could overcome antibiotic resistance and increase the effectiveness of treatment against P. aeruginosa sepsis.

Roxifiban (also known as DMP754), a potent antiplatelet agent in inhibiting platelet aggregation, and has a high specificity and affinity for human platelet glycoprotein IIb/IIIa complex (GPIIb/IIIa) receptors. Roxifiban participated in clinical trials phase III for the treatment of peripheral arterial disorders. This drug was also well tolerated in patients with chronic stable angina pectoris and was studied in the treatment of heparin-induced thrombocytopenia, and thrombosis. However, the development of this drug appears to have been discontinued.

Lutrelin is an agonist of gonadotropin-releasing hormone receptor exerting antineoplastic properties.

Colterol is a beta-2 adrenoreceptor agonist. Bitolterol, a diester prodrug of colterol, was marketed by Elan Pharmaceuticals for the treatment of reversible bronchospasm associated with asthma or chronic obstructive pulmonary diseases.

Quindecamine (also known as UCL-1407) is quinaldine derivative with antibiotic and fungicidal activity. Treatment of rats and mice with Quindecamine (250 mg/kg/ day) each day for 4 weeks followed by 500 mg/kg/day for 2 more weeks reduced spontaneous motility and body weight but produced no pathological abnormalities of the various organs studied. In vitro, the drug showed very good activity against Staphylococcus aureus, Streptococcus hemolyticus, Candida albicans, Trichophyton mentagrophytes, and T. vaginalis. The drug had very good activity in 180 human subjects with various bacterial and mycotic diseases of the skin and mucosa when applied as a 1% salve.

Delmitide is the decapeptide with antiinflammatory activity. It is the first low molecular weight compound inhibiting TNF production at a translational level. Also, delmitide inhibits production of IFN-gamma, IL-12 and IL-2. It targets TRAF6/IRAK4/MyD88 complex and inhibits phosphorylation of SAPKs (p38 and JNK). Delmitide inhibits AP1 and NFkB activation. Delmitide was developed for the potential treatment of Crohn's disease and ulcerative colitis; phase II trials for both these indications commenced in October 2001. Phase I trial in chemotherapy-induced diarrhea and the gastrointestinal complications of HIV were also initiated. However, no recent development has been reported.

Prazarelix is gonadorelin (GnRH) antagonist. It is primarily used in assisted reproduction to control ovulation. The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Ularitide is a recombinant form of urodilatin, a natriuretic peptide synthesized in the distal tubular cells of the kidney. It regulates renal sodium and water excretion through binding to natriuretic peptide type A receptors, increasing intracellular cyclic guanosine monophosphate (cGMP) levels. While these effects, as well as others such as vasodilation, are also exhibited by other natriuretic peptides, urodilatin has a terminal extension that brings resistance to biological inactivation by neutral endopeptidase, whose activity is increased in decompensated heart failure. Animal studies have demonstrated enhanced diuresis and natriuresis and reduced PCWP (pulmonary capillary wedge pressure) and systemic vascular resistance relative to atrial natriuretic peptide (ANP [99-126], the active circulating isoform). When injected into the blood, ularitide appears to cause diuresis (urine output) and natriuresis (sodium excretion), as well as vasodilation. Ularitide is currently in Phase 3 development as a potential treatment for patients with acute decompensated heart failure (ADHF).