Ciprokinen is a renin inhibitor discovered by Roche. Ciprokinen inhibited human renin in a buffer and human plasma with an IC50 of 0.07 and 0.65 nmol/L, respectively. In animal models, acute and chronic administration of ciprokinen lead to a reduction in arterial blood pressure. Development of ciprokinen was discontinued at a preclinical stage.

Lerisetron is a 5-hydroxytryptamine3 receptor antagonist. It was under development by FAES Farma for the potential treatment of emesis resulting from chemotherapy. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. Lerisetron had been in phase III clinical trials for the treatment of emesis. However, this study was discontinued.

The organophosphate compound Naftalofos is an anthelmintic drug. In Australia it is approved for veterinary use. Naftalofos has been used for many years to control nematodes of livestock. Naftalofos boluses are used against nematodes of cattle. Naphthalophos (36.6 to 51.2 mg/kg) was also 93% efficient against the multiple resistant strains of Trichostrongylus colubriformis in sheep. Naphthalophos showed efficacy against Haemonchus contortus (> 99 %),Trichostrongylus axei (99.3 %), Teladorsagia circumcincta (97.8 %), Trichostrongylus colubriformis (99.2 %), Cooperia punctata/curticei/pectinata (90.4 %), Nematodirus spathiger (89.2 %) and Oesophagostomum venulosum/columbianum (93.7 %). Naphthalophos represents an effective therapeutic alternative for incorporation into worm control programmes.

Idoxifene (also known as CB 7432), a novel selective estrogen receptor modulator, is originally discovered at the CRC Centre for Cancer Therapeutics, Institute. This drug participated in clinical trials phase II in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. In addition, in phase III in postmenopausal women after one year of idoxifene treatment. However, both studies were discontinued because of insufficient effectiveness.

Pomisartan, also known as BIBR-363, is an angiotensin type 1 receptor antagonist. It was investigated for the treatment of Congestive heart failure and hypertension. However, no development reports available at this moment.

Nicainoprol, also known as RU-42924, is calcium channel antagonist and a putative class I antiarrhythmic agent. Nicainoprol was shown to be useful in the prevention and treatment of arrhythmias associated with acute myocardial infarction. Nicainoprol had been in phase II clinical trials for the treatment of arrhythmia. However, this research has been discontinued.

Rodocaine (R 22.700) is a biochemical that was found to be an effective anesthetic in ophthalmology. This compound is suitable for topical use but can be injected as well. A pharmaceutically acceptable, acid-addition salt of rodocaine can be prepared by reaction of the rodocaine free base with the desired acid. Rodocaine has furthermore been mentioned as a potential anesthetic agent in antimicrobial compositions.

Synthélabo developed a saripidem (also known as SL 850274) as a potential anxiolytic agent that modulates the benzodiazepine-binding site on GABAA receptor via primary binding with ω1 subtype. Saripidem was studied in phase II clinical trials for the treatment of patients with anxiety disorders. However, information about the further development of the drug is not available.

Saracatinib (AZD0530) is an oral, dual inhibitor of c-Src/Abl kinases initially developed by AstraZeneca for the treatment of cancer. The drug was tested for many neoplasms and reached phase III for ovarian cancer (in combination with paclitaxel), however without demonstrating any significant effect. Sarcatinib is also tested in patients with Alzheimer's Disease (Phase II). Its effect on Alzheimer's Disease patients is explained by inhibition of another kinase, Fyn, which is highly expressed in brain.

Rifalazil (also known as KRM-1648) is a derivative of the antibiotic rifamycin. This orally administered ansamycin is under evaluation for treatment of various bacterial infections. Rifalazil kills bacterial cells by blocking off the β-subunit in RNA polymerase. This drug was originally developed as a therapeutic agent to replace rifampin in the treatment of tuberculosis. It also showed potential to treat indications caused by chlamydia trachomatis and chlamydia pneumoniae. Furthermore, it has been suggested as a potential drug in the treatment of gastric ulcer disease (which is caused by Helicobacter pylori) and antibiotic-associated colitis. Phase II studies evaluated the efficacy and safety of this drug in patients with chlamydia trachomatis and chlamydia seropositive patients. A phase 3 study was initiated including chlamydia seropositive patients. However, the development of rifalazil was terminated in 2013 due to severe side effects.