The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis. MK 0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. MK 0457 effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50s < 10 µM) and blocks the growth of tumors in a rodent model of cancer (80 mg/kg), inhibiting histone H3 phosphorylation and increasing apoptosis. By depleting Aurora activity, MK 0457 disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.

Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.

Elafibranor is a dual PPARα/δ agonist. Elafibranor increases plasma HDL and expression of Acox1, a PPARα target gene, and decreases plasma triglycerides and total cholesterol in the liver of ApoE2-KI wild-type mice. Elafibranor is identified as a drug candidate for the treatment of cardiometabolic diseases such as diabetes, insulin resistance, dyslipidemia, and non-alcoholic fatty liver disease (NAFLD).

Lobenzarit disodium is an immunomodulator commonly used for the treatment of arthritis.

Fenretinide is an orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types. This agent also inhibits tumor growth by modulating angiogenesis-associated growth factors and their receptors and exhibits retinoid receptor-independent apoptotic properties.

Thiamine, also called as vitamin B1, is used in combination with other B vitamins to regulate important functions of the cardiovascular system, endocrine system, and digestive system.

Zonisamide is the first agent of this chemical class to be developed as an antiepileptic drug blocks repetitive firing of voltagesensitive sodium channels and reduces voltage-sensitive T-type calcium currents.

Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist used in the treatment of Parkinson’s disease psychosis.