Casopitant (GW679769) is a novel substituted piperidine derivative that competitively binds with NK1 receptors. The full occupancy of the receptor by their piperidine compound inhibits its binding with tachykinin neurotransmitters, including SP. Casopitant, in a series of in vitro and in vivo experimentations, has exhibited a potent NK1 receptor antagonism. On 29 May 2008, GlaxoSmithKline announced the submission of a new drug application to the FDA for intravenous and oral formulations of casopitant mesylate. This drug was proposed for the prevention of chemotherapy-induced nausea and vomiting as an add-on therapy to the standard dual therapy of 5-HT3 receptor antagonists + dexamethasone. The submission also included a proposed indication for postoperative nausea and vomiting prevention. Rezonic™ is the proposed trade name for casopitant mesylate in the United States; Zunrisa™ is the proposed trade name for casopitant mesylate for GlaxoSmithKline’s global group of companies. In September 2009, GlaxoSmithKline decided to discontinue all regulatory filings for casopitant based on an estimate of the amount of additional safety data.

Icotinib is an orally available quinazoline-based inhibitor of epidermal growth factor receptor. It selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. The major organ of icotinib metabolism is the liver, with the primarily enzymes being CYP2C19 and CYP3A4 from the cytochrome P450 monooxygenase system. Icotinib Hydrochloride was approved for the treatment of patients with advanced stage Nonsmall cell lung cancer by the State Food and Drug Administration (SFDA) of China. The major drug related adverse reactions of the traditional cytotoxic agents include rash, diarrhea, severe bone marrow suppression, neuropathy, hair loss, and gastrointestinal reactions. Icotinib is under investigation as an active agent against other EGFR mutation-positive cancers, like lung adenocarcinoma, oesophageal cancer, nasopharyngeal cancer and others.

Fenproporex is a central and indirect-acting sympathomimetic. It was developed as an anorectic drug. Their anorectic effects are believed to be a result of adrenergic activation. Fenproporex has never been approved by the US Food and Drug Administration (FDA) for sale in the US due to lack of efficacy and safety data. There is a paucity of randomized, placebo-controlled trials on Fenproporex. These studies suggest that Fenproporex is modestly effective in promoting weight loss. Data from these studies are insufficient to determine the risk-benefit profile of Fenproporex. Abuse potential and amphetamine-like adverse effects are causes for concern. Adverse effect most frequently reported are: insomnia, anxiety, depression, irritability, dry mouth.

Hydrocotarnine is a crystalline alkaloid, obtained from opium and also formed by the reduction of cotarnine. It is a non-narcotic opium alkaloid. Hydrocotarnine is supposed to potentiate the analgesic effect of oxycodone with unknown mechanism.

α-Asarone is a phytochemical compound with neuroprotective, anti-oxidative, anticonvulsive and cognitive enhancing action, isolated from the Chinese medicinal herb Acorus tatarinowii. Numerous clinical studies in China had indicated the effectiveness of α-asarone against respiratory disorders and epilepsy. Asarone tablets have been clinically used as bronchial asthma and bronchitis prescription drug in China. Unfortunately, toxic and genotoxic studies of a-asarone have indicated that this compound may pose a risk to human health, including embryotoxicity and maternal toxicity in rats, hepatotoxicity in rat-cultivated hepatocytes, and in vivo and in vitro genotoxic damage in mammalian cells.

Glurenorm is an anti-diabetic drug in the sulfonylurea class. It is used in the treatment of diabetes mellitus type 2. It is an ATP-dependent K+ (KATP) channel blocker. This block causes a depolarization which leads to activation of voltage-dependent Ca channels and Ca2+ influx, and eventually increases insulin release. Minor skin allergies, gastric upsets and other non-specific side effects have been reported. Hypoglycaemic reactions have been reported but they are infrequent. Glurenorm effect increase butadion, chloramphenicol, tetracycline, coumarin derivatives, cyclophosphamide, sulfonamides, MAO inhibitors, thiazide diuretics, beta-blockers, salicylates, alcohol.

Enilconazole is a synthetic broad-spectrum antimycotic with a high activity against most of the common dermatophytes and various other fungi and yeasts. It is a selective inhibitor of ergosterol biosynthesis, an essential component of the cell membrane of fungi and yeasts. This results in irreversible changes which are the origin of the fungicidal effect. Enilconazole is marketed under the brand name Imaverol among others. Imaverol concentrated solution is a synthetic antimycotic with a potent antifungal action against dermatophytes such as: Trichophyton verrucosum, Trichophyton mentagrophytes, Trichophyton equinum, and Microsporum canis in horses and dogs.

Rosin is a natural product derived from pine trees and consists of a complex mixture of mutually soluble organic compounds. Rosin (colophony) is composed of approximately 70% resin acids. Rosins are produced commercially by one of the following three methods: (1) solvent extraction of aged and ground pine stumps (wood rosin), (2) extraction of crude tall oil as a byproduct of the Kraft pulping process for making paper followed by acidification and fractional distillation (tall oil rosin) and, (3) tapping the living tree to collect oleoresin followed by distillation to yield turpentine and a resinous substance (gum rosin). Because, gum, tall oil and wood rosins are obtained from pine trees, they are similar in composition. Rosin and its derivatives also exhibit wide ranging pharmaceutical applications. Rosin derivatives show excellent film forming and coating properties. They are also used for tablet film and enteric coating purpose. Rosins have also been used to formulate microcapsules and nanoparticles. Glycerol, sorbitol, and mannitol esters of rosin are used as chewing gum bases for medicinal applications. The degradation and biocompatibility of rosin and rosin-based biomaterials has been examined in vitro and in vivo. Rosin Gum is an important raw material for the manufacture of soap, paper, paint, and rubber; intermediate material for synthetic organic chemicals. Rosin in Rhodiola rosea L. preparations can effect the central nervous system by increasing the ability to concentrate, the mental and physical power; they are efficient in the asthenic states and improve general resistance of the cells and the organism against the harmful outer influence. They also prevent the heart system from stress and arrhythmias, and posses some antioxidant activity. Some data confirm that the Rhodiola rosea L. preparations stop the growth of the malignant tumors and metastases in the liver.

Dronedarone is an antiarrhythmic that is FDA approved for the treatment of atrial fibrillation in patients in sinus rhythm with a history of paroxysmal or persistent atrial fibrillation (AF). Dronedarone is multichannel blocker. Common adverse reactions include abdominal pain, diarrhea, indigestion, nausea, vomiting, asthenia and raised serum creatinine. Dronedarone has potentially important pharmacodynamics interactions: Digoxin: Consider discontinuation or halve dose of digoxin before treatment and monitor; Calcium channel blockers (CCB): Initiate CCB with low dose and increase after ECG verification of tolerability; Beta-blockers: May provoke excessive bradycardia, Initiate with low dose and increase after ECG verification of tolerability.

Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer. Azelastine is oxidatively metabolized to the principal active metabolite, desmethylazelastine, by the cytochrome P450 enzyme system. It is indicated for the relief of the symptoms of seasonal allergic rhinitis and perennial allergic rhinitis. The most common adverse reactions are: pyrexia, dysgeusia, nasal discomfort, epistaxis, headache, sneezing, fatigue, somnolence, upper respiratory infection, cough, rhinalgia, vomiting, otitis media, contact dermatitis, and oropharyngeal pain. Concurrent use of Azelastine with alcohol or other central nervous system depressants should be avoided because reductions in alertness and impairment of central nervous system performance may occur.