Derenofyllin (SLV320) is a selective adenosine A1 receptor antagonist, which is under investigation for the treatment of heart failure with renal dysfunction. Adverse events considered related to SLV320 were dizziness, nausea, transient hypertension and transient hypotension.

ISOMAZOLE is a cardiovascular agent with both inotropic and vasodilator activities. It acts primarily as a phosphodiesterase inhibitor.

Ombrabulin is an experimental drug candidate discovered by Ajinomoto and further developed by Sanofi-Aventis for cancer treatment. Ombrabulin is a synthetic water-soluble analog of combretastatin A4, derived from the South African willow bush (Combretum caffrum), with potential vascular-disrupting and antineoplastic activities. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrate, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis. Ombrabulin has been used in trials studying the treatment of Sarcoma, Neoplasms, Solid Tumor, Neoplasms, Malignant, and Advanced Solid Tumors, among others. In January 2013, Sanofi said it discontinued development of Ombrabulin after disappointing results from phase III clinical trials.

Solpecainol [EGIS 2936, EGYT 2936] is a sodium channel antagonist with antianginal and class I antiarrhythmic effects. It was in phase II clinical trials with Egis Pharmaceuticals for the treatment of angina pectoris and arrhythmias, but this development was discontinued.

Talarozole (formerly R115866) is a new highly potent and selective azole derivative, which inhibits cytochrome-P450-dependent all-trans-retinoic acid catabolism by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase. It is in clinical development for the treatment of psoriasis and acne. However, no local pharmacokinetic data on the diffusion behaviour of talarozole in the skin itself are available. As topical application might be an interesting alternative to oral therapy because of the reduced systemic side effects. The distribution of talarozole within the skin was investigated: 80% was located in the epidermis, while the remaining 20% was found in the dermis. The epidermal concentration of talarozole achieved after a single topical application was sufficiently high to enable the potential induction of local retinoid-like effects.

Napitane [A 75200, ABT 200] is a norepinephrine uptake inhibitor and α2 adrenoceptor antagonist. It was undergoing clinical trials with Abbott in the USA as a treatment for depression. However it was discontinued later. Napitane is a potent alpha 2-adrenoceptor antagonist (Ki = 1.2 nM) with modest norepinephrine uptake-blocking activity (IC50 = 841 nM).

Orvepitant is a novel generation brain penetrant, selective and potent, small molecule NK-1 receptor antagonist. Orvepitant’s (GW823296) mode of action and developability characteristics made it a suitable development candidate for the treatment of common anxiety disorders, posttraumatic stress disorder and major depressive disorder. It’s in phase II clinical trials as an effective inhibitor of itch-associated response.

NMS-P937 is a selective PLK1 inhibitor. It was developed by Nerviano Medical Sciences and tested in phase I clinical trials.

Henagliflozin (also known as SHR3824) was developed by Jiangsu HengRui Medicine as a sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. This drug successfully passed phase I clinical trials, however, information about further development is not available.

Masilukast (ZD 3523) is an antagonist of leukotriene D4 (LTD4). It opposes LTD4-induced bronchoconstriction. It was being developed for the treatment of asthma.