(+)-Fadrozole (FAD-286) is an aldosterone synthase inhibitor. The drug was tested in vivo in preclinical models of hypertension, heart failure and was shown to reduce retinal neovascularization in rats with oxygen-induced retinopathy.

Dexamisole is the dextro-isomer of tetramisole, a broad spectrum anthelmintic. Dexamisole significantly improves mood and psychotonicity. In adrenergically innervated blood vessels dexamisole inhibits neuronal uptake of norepinephrine more than levamisole. Dexamisole antagonized the reserpine-induced hypothermia but was ineffective in the apomorphine-induced hypothermia in mice. It reduced ptosis produced by reserpine in mice but this effect was very weak. The effect of dexamisole on the amphetamine-induced hyperactivity depended upon the animal species. Dexamisole reduced the duration of immobility in the despair test in rats. It did not modify the 5-HTP-induced head twitch reaction in mice but produced stimulation of the hind limb flexor reflex in spinal rats. The latter effect was blocked by phenoxybenzamine but not by cyproheptadine and metergoline. Dexamisole also exerted a sedative and hypothermic effect. The above findings indicate that the pharmacological profile of dexamisole resembles in some respects that of tricyclic antidepressants; they also point out that this drug has a central noradrenergic activity.

Enpiroline (WR 180,409) is an antimalarial compound. It demonstrates activity against Plasmodium falciparum both in vitro and in non-immune infected subjects. Additionally, it exerts antischistosomal activity.

Foretinib is an orally available multikinase inhibitor that targets c-MET and VEGFR2 with high affinity, which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib is an experimental drug candidate for the treatment of cancer. It was in Phase II trials for the treatment breast cancer, non-small cell lung cancer, gastric cancer, head and neck cancer and papillary renal-cell carcinoma. The most frequent adverse events of any grade associated with foretinib were fatigue, hypertension, gastrointestinal toxicities, and nonfatal pulmonary emboli.

Dipraglurant (ADX48621) is a novel, potent mGluR5 negative allosteric modulator that reduced the severity of drug-induced dyskinesia in Parkinson's disease. Dipraglurant pharmacokinetic variables were similar to those of levodopa, suggesting that both drugs can be co-administered simultaneously in further studies. Dipraglurant might be useful in torsion dystonia treatment also. Detected adverse events are: sweating, dyskinesia, nausea, dizziness, and anxiety. One serious adverse event described as possible syncope.

Mannose 6-phosphate (M6P) has type-I integral membrane receptors. M6P-receptors bind and transport M6P-enzymes to lysosomes, but it can also modulate the activity of a variety of extracellular M6P-glycoproteins (i.e., latent TGFbeta precursor, urokinase-type plasminogen activator receptor, Granzyme B, growth factors, Herpes virus). M6P has been demonstrated to reduce active TGF-β1 expression on cultured tendon fibroblasts and improved range of movement in a rabbit flexor tendon injury model. Studies of M6P in relation to skin scarring demonstrate improvement in scar cosmesis and accelerated return of normal dermal architecture. Juvidex, a formulation of M6P, inhibits the activation of TGF-beta1 and TGF-beta2, which are present at high levels in adult wounds that scar. On the other hands, M6P in a 600 mM hypertonic solution (Adaprev) potentially acts via a physical, non-chemical, hyperosmotic effect.

TrioxBio's API, S-ethylisothiouronium diethylphosphate, MTR-104 (MTR- 105), is a nitric oxide synthase (NOS) inhibitor which blocks the production of nitric oxide, preventing the dilation of blood vessels and the other detrimental effects caused by excessive NOS activity. MTR-105, a fast-acting synthetic NOS inhibitor with rapid onset of action when administered parenterally, has been effective in alleviating hypotension experimentally and in several observational studies while reducing NO production. MTR-105 is registered and approved for clinical use in the Republic of Moldova where data have been collected from 434 patients exposed to the drug in pre- and postapproval clinical investigations.