Neostigmine is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. By inhibiting acetylcholinesterase, more acetylcholine is available in the synapse, therefore, more of it can bind to the fewer receptors present in myasthenia gravis and can better trigger muscular contraction. Neostigmine is used for the symptomatic treatment of myasthenia gravis by improving muscle tone.

E-7090 is a novel selective inhibitor of fibroblast growth factor receptors, that displays potent anti-tumor activity. It is a promising candidate as a therapeutic agent for the treatment of tumors harboring FGFR genetic abnormalities. E-7090 is an orally available and selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses E-7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E-7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. E-7090 showed selective antiproliferative activity against cancer cell lines harboring FGFR genetic abnormalities and decreased tumor size in a mouse xenograft model using cell lines with dysregulated FGFR. Furthermore, E-7090 administration significantly prolonged the survival of mice with metastasized tumors in the lung. It is being investigated in a Phase I clinical trial for treatment of patients with solid tumors.

Talmapimod is a p38 MAPK kinase inhibitor that inhibits p38 alpha with IC50 value of 9 nM which is 10-times lower then IC50 for p38 beta. Talmapimod was under clinical development for the treatment of Myelodysplastic Syndromes, Multiple Myeloma and Rheumatoid Arthritis (phase II), however, it seems to be discontinued as no longer presents in Janssen's pipeline.

Prinoxodan (also known as RGW2938) is a benzodiazinone derivative patented by Rorer International (Overseas), Inc as inotropic agents, useful in treating congestive heart failure. Prinoxodan administered intravenously (i.v.) to anesthetized dogs increased contractile force while decreasing arterial pressure and total peripheral resistance (TPR) in a dose-related manner. A single oral dose of Prinoxodan administered to conscious chronically instrumented dogs produced a marked and sustained increase in contractility 15-240 min after treatment.

METHYLPARABEN SUBEROHYDROXAMIC ACID PHENYL ESTER (more known as Remetinostat), a histone deacetylase (HDAC) inhibitor, was developed for the treatment of cutaneous T cell lymphoma (CTCL). This drug is participating in phase II clinical trial to evaluate the efficacy, safety, and tolerability to skin lesions in patients with early-stage cutaneous T-cell lymphoma. In May 2019 was announced the positive results from phase II trial of remetinostat in basal cell carcinoma (BCC) patients. Initial results suggest that remetinostat gel offers a potentially effective and well-tolerated, non-surgical intervention for the treatment of localized BCCs. The unique design of remetinostat enables topical application, making it active only in the skin. As soon as it reaches the blood stream, it is degraded, avoiding the side effects associated with other HDAC inhibitors. Besides, remetinostat was studied as the treatment of plaque psoriasis; however, this study was discontinued.

Nebicapone (BIA 3-202) is a reversible, and tight-binding peripheral inhibitor of the enzyme catechol-O-methyltransferase (COMT) being developed for use as an adjunct to levodopa/dopa decarboxylase inhibitor in the treatment of PD. Nebicapone dose dependently and significantly decreased COMT activity. Nebicapone also increased systemic exposure to levodopa and improved motor response. The tight-binding nature of the inhibition produced by BIA 3-202 was evaluated by performing an Ackermann-Potter plot. The true K(i) for BIA 3-202, derived from the nonlinear regression analysis, was 0.19+/-0.02 nM. In substrate competition studies, an increase in the concentration of adrenaline resulted in a linear increase in IC(50) values for BIA 3-202.

Esuprone (LU 43839) is a monoamine oxidase type A inhibitor. Esuprone proved to be an effective anticonvulsant in the kindling model. Esuprone was undergoing phase II clinical trials with Knoll (BASF Pharma) in Germany as an antidepressant.

Telatinib (Bay-579352) developed by Bayer is an orally available and highly potent inhibitor of tyrosine kinases VEGFR2,VEGFR3, PDGFR and c-Kit. Telatinib is a potent inhibitor of angiogenesis. Telatinib caused a significant decrease in endothelium-dependent and endothelium-independent vasodilation. Telatinib demonstrates anti-tumor activity in various cancer models. Telatinib is ready for phase III clinical trials for the treatment of gastric cancer. In 2010, it has been granted orphan drug status by the FDA. Most frequent adverse events were pain, nausea, voice changes and fatigue.

Balamapimod, also known as MKI 833, a mitogen-activated protein kinase (Ras/Raf/MEK) inhibitor with potential anti-tumor activity. This compound can be used for the treatment of diseases that are results of deregulation of Ras/Raf/MEK kinases.