Abamectin B1b (Avermectin B1b) is a macrocyclic lactone containing an isopropyl reside in the 25-position broad anthelmintic activity. The oral administration of this formulation of avermectin B1 appeared to be highly efficacious against intestinal strongyles and Onchocera microfilaria. Avermectin B1b is a component of marketed and provided commercially Abamectin, which is used to control livestock parasitic nematodes. It is a broad-spectrum acaricide with additional insecticidal action on a limited number of insects. Abamectin acts on insects by increasing the membrane permeability to chloride ions, and it mainly stimulates the release of Ȗ-aminobutyric acid (GABA). The affected arthropod becomes paralysed, stops feeding, and dies after a few days. It exerts contact and stomach action, with limited plant systemic activity, but exhibits translaminar movement into treated leaves. Abamectin is also used as an anthelmintic drug in veterinary medicine.

Gevotroline (WY 47,384) is an atypical antipsychotic compound, which was developed for use in the treatment of schizophrenia. Gevotroline has some clinical efficacy, and equal affinity for D2 (dopamine) and 5-HT2 (serotonin) receptors. Gevotroline was also found to have affinity for sigma receptors, which are thought to be involved in certain neuropsychiatric disorders (because of their ability to regulate the hypothalamic-pituitary-adrenal axis), explaining the interest in this compound for therapeutic use in schizophrenia. Gevoltrine is thought to increase activity in the hypothalamic-pituitary-adrenal axis to elevate levels of corticosterone in plasma. Gevotroline is well tolerated and phase II clinical trials have been conducted, but the compound was never marketed.

Rispenzepine (DF 594) is a muscarinic receptor antagonist. Rispenzepine has high affinity for intestinal muscarinic receptors, with preferential action at M1 and M3 receptor subtypes. This drug shows potent inhibitory effects on intestinal motility. In guinea pigs, rispenzepine significantly increases acetylcholine release in the trachea. A phase II study to test efficacy in asthma patients has been discontinued.

MK-3207 represents the third CGRP receptor antagonist to display clinical efficacy in migraine trials. It is a potent CGRP receptor antagonist with IC50 and Ki of 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. MK-3207 had been in phase II clinical trials by Merck Sharp & Dohme for the treatment of migraine. But the company had discontinued the research due to asymptomatic liver test abnormalities in 2010.

Isoxepac (also known) as HP-549 is a non-steroidal anti-inflammatory drug with analgesic activity. Isoxepac was studied in the clinical trial for the treatment of postoperative pain after knee surgery for meniscectomy. It was shown, that 200 mg of isoxepac would appear to be the minimal effective dose. In case of rheumatoid arthritis, isoxepac showed significantly fewer adverse effects.

KALAFUNGIN is an antimicrobial agent obtained from the culture broth of a soil isolate of Streptomyces tanashiensis, designated Streptomyces tanashiensis strain Kala UC-5063. It has in vitro activity against a variety of pathogenic fungi, yeasts, protozoa, and bacteria.

Fluradoline (also known as HP-494), a centrally acting antinociceptive agent with antidepressant properties. Experiments on rodents have shown that fluradoline blocked the reuptake of NE, 5-HT, and DA in the brain. Besides, fluradoline was studied for the prevention of acute and chronic postsurgical pain.

Quarfloxin (also known as CX-3543) is a fluoroquinolone derivative patented by Cyclene Pharmaceuticals, Inc. as an antitumor agent. Quarfloxin selectively disrupts nucleolin/rDNA G-quadruplex complexes in the nucleolus, thereby inhibiting DNA polymerase I transcription and inducing apoptosis in cancer cells. CX-3543 was evaluated in phase II clinical studies for the treatment of low or intermediate grade neuroendocrine carcinoma, including carcinoid and islet cell cancer. In 2008, a trial for the treatment of chronic lymphocytic leukemia (CLL) was withdrawn prior to patient enrollment. In 2010, phase I clinical studies for the treatment of solid tumors and for the treatment of lymphoma were terminated upon the observation that the modified dose schedule presented no advantage over previously studies schedule solid tumors/ Cylene discontinued development of quarfloxin in 2010.

SGI-1776 is a PIM-kinase inhibitor, developed by SuperGen Inc. SGI-1176 was tested in clinical trials against relapsed/refractory leukemias, prostate cancer and Non Hodgkin's Lymphoma, but the dose limiting toxicity of cardiac QTc prolongation was identified and clinical development of SGI-1776 was terminated.

Ganstigmine is an orally active, carbamate-based acetylcholinesterase (AChE) inhibitor developed for the treatment of Alzheimer's disease. It is a newer generation AChE than BChE inhibitor, derived from genserine, and has a long duration of action in vivo. Studies have shown it significantly prevented the progressive neuronal cell death due to growth factor deprivation and decreased neurodegeneration. Ganstigmine may be a suitable candidate for the treatment of cholinergic deficit in Alzheimer's disease because it was found to significantly increase basal extracellular concentrations of acetylcholine in rat prefrontal cortex, and does not affect the concentrations of serotonin, noradrenaline and levels of dopamine and metabolites. It is safe and well tolerated at 5–10 mg doses as the study conducted in Phase I randomized, double-blind, placebo-controlled clinical trial. It was dropped from phase II trials because of its adverse effects reported in some patients.