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.

PYM50018 (also known as Myogane or SARSAGENIN) has demonstrated neuroprotective effects in several preclinical models. It was observed that PYM50018 protects against neuronal damage, increases neurite outgrowth, reverses oxidative damage and reversed neuronal apoptosis. PYM50018 is in phase I clinical study for the treatment of amyotrophic lateral sclerosis (ALS).

Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR, originally being developed by Wyeth. Upon intravenous administration, gedatolisib inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. Significant antitumor efficacy and a favorable pharmacokinetic/safety profile justified clinical evaluation of Gedatolisib. Gedatolisb is in phase II clinical trials by Pfizer for the treatment of acute myeloid leukaemia. Gedatolisb is in phase I clinical trials for the treatment of solid tumours.

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.

Axomadol is a centrally active analgesic agent with opioid agonistic properties and with inhibitory effects on the reuptake of the monoamines noradrenaline and, to serotonin [5‐hydroxytrypyamine (5‐HT)]. The drug participated in phase II clinical trials in the treatment of patients with moderate to severe chronic low back pain. As a result, the axomadol didn’t meet predetermined study endpoint, and studies were discontinued.

Sprodiamide is a nonionic paramagnetic dysprosium chelate agent patented by Salutar, Inc.as diagnostic imaging contrast media. Compare with gadolinium-based agents Sprodiamide shows a stronger T2 effect and negligible T1 effect. This property makes Sprodiamide useful for blood volume imaging. In a preclinical model of reperfused ischemia of the rat intestine administration of Sprodiamide improved the contrast between the normal and ischemic intestine on T2-weighted images, and administration of both gadodiamide and Sprodiamide improved the contrast on T1- and T2-weighted images.

Binodenoson, a selective adenosine A(2A) receptor agonist, was being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging. Binodenoson for injection under the brand name CorVue was developed for use in patients with or at risk for coronary artery disease (CAD) who are unable to perform a cardiac exercise stress test. CorVue was designed to minimize side effects such as dyspnea, flushing, heart block, and chest pain. Binodenoson did not achieve FDA approval in 2009 due to concerns over equivalence of its efficacy with adenosine.