Avitriptan (BMS-180048), a new 5-HT 1B/1D receptor agonist, has been studied in phase II clinical trials in patients with migraine headaches. Later experiments have confirmed antimigraine activity together with coronary side-effect potential that is why further studies were discontinued.

Sibrafiban (G-7453) is the orally administered, nonpeptide, double-prodrug of Ro 44-3888 which is a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban is a double prodrug that undergoes bioconversion to the inactive prodrug Ro 48-3656 and to the active IIb/IIIa antagonist, Ro 44-3888, after oral administration. Sibrafiban was undergoing clinical trials for secondary prevention of cardiac events in patients stabilised after acute coronary syndromes. Sibrafiban has been shown to have comparable efficacy to aspirin in preventing recurrent ischemic events in patients suffering from acute coronary syndromes. Sibrafiban was under development by Genentech and Hoffmann-La Roche, and in phase III trials as an antithrombotic. The development of sibrafiban was discontinued in 1999 following unfavorable Phase III efficacy data.

Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.

Biricodar (also known as VX-710) was developed by Vertex as a chemosensitizing agent designed to restore the effectiveness of chemotherapeutic agents in tumor multidrug resistance. The phase II trials had commenced for biricodar, in combination with chemotherapy, for five common cancer indications: breast, ovarian, soft-tissue sarcomas, small cell lung cancer, and prostate cancer. In spite of completed trials, development of biricodar was discontinued because of the adverse effects.

Ibutamoren (L-163,191 MK-0677) is a spiropiperidine agonist of the ghrelin receptor and a growth hormone secretagogue. Ibutamoren mimics the actions of growth hormone releasing peptide-6 to increase serum levels of serum insulin-like growth factor-I (IGF-I). Orally active Ibutamoren was being developed by Merck & Co. for a variety of indications, including fibromyalgia, muscle wasting/weakness in patients with chronic kidney disease, Alzheimer's disease and fractures.However, there has been no recent development reported or development has been discontinued for these indications.

Moxilubant is an orally active leukotriene B4 antagonist patented by Ciba-Geigy A.-G. and studied for psoriasis, rheumatoid arthritis, and chronic obstructive pulmonary disease treatment. Moxilubant inhibits LTB4 signaling with a potency of 2–4 nM. In a phase 1 study in 10 healthy volunteers, Moxilubant was administered orally once or twice daily for 7 days at doses ranging from 100 to 500 mg. At dose levels of 150 mg and above, LTB4 pathway inhibition reached at least 75%. At doses of 300 mg and above, pathway inhibition reached 100%. A Phase 2 study was conducted in 24 patients with COPD treated with 240 mg/day Moxilubant for 4 weeks. In this study, there were no changes in sputum cell counts or biomarkers or in spirometry measures, even though plasma levels of Moxilubant were sufficient to significantly reduce pathway signaling.

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.

Emedastine is an antihistaminic agent, which was approved by FDA for the treatment of allergic conjunctivitis (Emadine brand name). The drug acts selectively on H1 receptors with lower affinity to H2 and H3 subtypes. Emedastine has a relatively unfavorable CNS effect profile. A small percentage of patients reported somnolence as an adverse effect after administration.

Indinavir is an antiretroviral drug for the treatment of HIV infection. Indinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Indinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.

Iobenguane I-131 is a radioactive therapeutic agent. The drug contains radioactive isotope I-131, which decays by electron emission with a half-life of about 8 days. By the chemical structure, iobenguane is similar to the neurotransmitter norepinephrine and is subject to the same uptake and regulation pathways. After intravenous administration, iobenguane I-131 accumulates within pheochromocytoma and paraganglioma cells, and radiation from the radioactive decay causes cell death and tumor necrosis. Iobenguane I-131 was approved by the FDA for the treatment of adult and pediatric patients with iobenguane scan positive, unresectable, locally advanced or metastatic pheochromocytoma or paraganglioma who require systemic anticancer therapy. Iobenguane I-131 is investigated in clinical trials as a treatment of neuroblastoma, ganglioneuroblastoma and other tumors of neuroendocrinal origin.