Doxylamine is an antihistamine commonly used as a sleep aid. This drug is also used to relieve symptoms of hay fever (allergic rhinitis), hives (rash or itching), and other allergic reactions. Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power far superior to virtually every other antihistamine on the market, with the exception of diphenhydramine (Benadryl). It is also the most powerful over-the-counter sedative available in the United States, and more sedating than many prescription hypnotics. In a study, it was found to be superior to even the barbiturate, phenobarbital for use as a sedative. Doxylamine is also a potent anticholinergic. Like other antihistamines, doxylamine acts by competitively inhibiting histamine at H1 receptors. It also has substantial sedative and anticholinergic effects. Used alone as a short-term sleep aid, in combination with other drugs as a night-time cold and allergy relief drug. Also used in combination with Vitamin B6 (pyridoxine) to prevent morning sickness in pregnant women.

Carsatrin (also known as RWJ 24517) is purinylpiperazine derivative patented by Ortho Pharmaceutical Corp. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+,K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin

Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.

Tazadolene was developed as a novel non-opioid analgesic with antidepressant properties. Experiments on rodents have revealed that unique analgesia properties of tazadolene was due to the ability of this compound to activate both serotonergic and alpha 2 adrenergic antinociceptive systems. Information about the current use of this drug is not available.

LAVOLTIDINE, also known as loxtidine, is a highly potent and selective histamine H2-receptor antagonist. It is a member of triazoles. It produces gastric carcinoid tumors in rodents that is why its clinical development was discontinued.

Mazapertine (RWJ-37796) is an arylpiperazine antipsychotic with high affinity to dopamine D2 and D3, serotonin 5-HT1A and alpha 1A-adrenergic receptors. It was being studied in the treatment of schizophrenia.

Vatalanib a potent oral tyrosine kinase inhibitor with a selective range of molecular targets, has been extensively investigated and has shown promising results in patients with solid tumors in early trials. Vatalanib selectively inhibits the tyrosine kinase domains of vascular endothelial growth factor (VEGF) receptor tyrosine kinases (important enzymes in the formation of new blood vessels that contribute to tumor growth and metastasis), platelet-derived growth factor (PDGF) receptor, and c-KIT. The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.

Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.