Sabarubicin (previously known as MEN-10755), a disaccharide analog of doxorubicin that was developed by Menarini Pharmaceuticals for the treatment of solid tumors, including small cell lung cancer and prostate cancer. Sabarubicin exhibits a superior antitumor efficacy, presumably related to the activation of p53-independent apoptosis. The drug participated in phase II clinical trials to study its effectiveness in treating patients who have progressive prostate cancer that has not responded to hormone therapy and in chemotherapy-naive patients with extensive stage small cell lung cancer. On 21 December 2004, the European Commission granted the orphan designation to Menarini for sabarubicin for the treatment of small cell lung cancer.

Adoprazine (SVL-313) is a full 5-HT1A receptor agonist and full D2/3 receptor antagonist possessing characteristics of an atypical antipsychotic, representing a potential novel treatment for schizophrenia and bipolar disorder. This drug together with some others, e.g. Mazapertine succinate, PF-217830 was discontinued from clinical trials due to either non-optimal pharmacokinetic properties or insufficient therapeutical efficacy.

Benzethidine an opioid analgesic that was forbidden for use.

Lidorestat is a highly potent and selective aldose reductase inhibitor with good oral bioavailability that is reported to improve nerve conduction and reduce cataract formation. Lidorestat reduced mortality rates in hAR transgenic mice. Mice receiving lidorestat had similar survival rates as nonhAR-expressing diabetic mice. Lidorestat treatment did not affect plasma lipids, glucose, or weights of diabetic mice. Drugs such as lidorestat will improve human health by reducing the production of toxic products of the polyol pathway. Lidorestat was developed for the treatment of diabetic complications, including neuropathy, retinopathy, cataracts, nephropathy.

Boehringer Ingelheim is developing BI-671800, an orally administered treatment for seasonal allergic rhinitis and asthma. BI-671800 is an antagonist of the PGD2 receptor, CRTH2. PGD2 stimulates bronchoconstriction and allergic airway inflammation in animal models. Inhibition of CRTH2 may reduce airway inflammatory cells, IL -4, -5, -13 production, serum IgE and airway hyper reactivity. Treatment with BI-671800 in poorly controlled asthmatic patients receiving FP was associated with a significant improvement in FEV1. BI-671800 was well tolerated at a total daily dose of 800 mg for 6 weeks.

Homocysteine, an amino acid synthesized intracellularly by removal of the N-methyl group from the essential amino acid methionine. High plasma level of homocysteine is called hyperhomocysteinemia is a clinical biomarker for increased risk of cardiovascular disease, thromboembolic diseases, and myocardial infarction. It was shown, that hyperhomocysteinemia could be an independent risk factor for dementia and Alzheimer's disease. The falling of homocysteine concentrations in response to increasing B-group-vitamin status, have the hope that mental decline, or Alzheimer's disease, could be prevented by dietary modification or food fortification. Besides, homocysteine can behave as an anti-oxidant agent by increasing the antioxidant capacity of the tumor and endothelial cells.

Cromitrile is an antiallergic developed by Miles Laboratories Inc. The compound was also shown to possess bronchodilator and anti-inflammatory activity.

Cyclazocine is a mixed opioid agonist/antagonist, an agonist of kappa opioid receptor, and a partial agonist of mu opioid receptor. The drug has analgesic activity and dose 0.25-0.5 mg/70 kg is equivalent to 10 mg/75 kg of morphine. Cyclazocine is a long-acting mu-opioid antagonist in human and was studied for the treatment of addiction to opioids and cocaine. Induction of the drug leads to dysphoria, hallucination, irritability, and sleeplessness.

Moxadolen is tricyclo-[5.2.1.0.2.6endo]decenone derivative. Moxadolen pharmacokinetics were investigated after oral application in male Wistar rats. The compound is extensively absorbed and mainly renally eliminated. Within 60 h, 63% of the activity is recovered in urine and feces. After 12 h 27% of the activity is eliminated (application in polyethylene glycol). The highest total concentration of the activity in the plasma is found after 2 h, the highest of the unchanged drug is found after 1 h. The half-life is 2.9 h.