EC-18 (now known as mosedipimod), a synthetic copy of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) that was developed by Enzychem Lifescience for oral administration for the treatment of immune and inflammatory related diseases, including psoriasis, rheumatoid arthritis, asthma, atopic dermatitis, and sepsis. The US Food and Drug Administration (FDA) has granted Orphan Drug Designation to EC-18 for the treatment of Acute Radiation Syndrome (ARS) and for the for the neutropenia treatment. Besides, the EC-18 is participating in phase II clinical trials to investigate the efficacy and safety of the agent for chemoradiation-induced oral mucositis and chemotherapy-induced neutropenia. This drug has a multimodal mechanism of action. It stimulates calcium influx into T lymphocytes and increases the production of various cytokines. In addition, EC-18 enhances the cytolytic activity of natural killer (NK) cells and suppresses the expression of the transmembrane protein tumor cell toll-like receptor 4 (TLR-4) on cancer cells, thus suppresses tumor cell proliferation.

ZK 200775, also known as fanapanel, an antagonist at the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor, possesses neuroprotective efficacy in patients with acute ischemic stroke. However, the phase II of clinical trials had revealed, that this compound had led to the neuronal dysfunction and the glial cell toxicity had occurred. In addition, was shown, that the antagonization of AMPA receptors by ZK200775 lead to alterations of color and dark vision, visual acuity, cone electroretinogram (ERG) modalities and the pattern-reversal visual evoked potentials and to a lesser extent on the scotopic ERG. At the same time, ZK 200775 did not alter eye morphology, the functioning of the extraocular muscles, binocular vision, visual fields or the pupil.

Bromebric Acid (Cytembena) is a derivative of bromoacrylic acid with cytostatic and antineoplastic activity. Chemical structure of Bromebric Acid is not related to any previous antineoplastic agent. In animal tumor screens, Jelinek and Semonsky noted antineoplastic activity of Cytembena against sarcoma 180, atlenocarcinoina of the lactic gland in mice, Ehrlich’s ascitic carcinoma, Yoshida’s ascitic sarcoma, and Zojdeln’s heap

Dexindoprofen is a non-steroidal drug that has analgesic and anti-inflammatory properties. Dexindoprofen is the dextrorotatory stereo-isomer of indoprofen, to which it has a similar adverse effect pattern. Gastrointestinal and nervous system effects and skin reactions are the most frequent. Following reports of severe gastrointestinal bleeding and carcinogenicity in animals indoprofen was withdrawn from the market worldwide.

Enrasentan is an orally active mixed endothelin A/B receptor antagonist with a 100-fold greater affinity for the endothelin A receptor. In an animal model of hypertension and cardiac hypertrophy the drug has reduced blood pressure, prevented cardiac hypertrophy and preserved myocardial function. In rats with hyperinsulinemia and hypertension enrasentan normalized blood pressure and prevented cardiac and renal damage. In rats with stroke the drug reduced the ischemic area in the brain. Enrasentan had been in phase II clinical trial for the treatment of heart failure but the results suggested that enrasentan does not appear to have favorable effects on ventricular remodeling.

Etersalate is a derivative of aspirin exerting antiplatelet, analgesic, anti-inflammatory and antipyretic properties. Etersalate has potential to prevent oligomerization of amyloid beta (Aβ) peptides.

Cefcanel is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcanel is active against the species E. coli, K. aerogenes and Proteus mirabilis; H. influenzae and M. catarrhalis has reasonable susceptibility. Cefcanel inhibits 90% of S. aureus strains at 2 µg/ml, irrespective of the presence of a β-lactamase. Cefcanel binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Livoletide (AZP-531) is an analog of unacylated ghrelin, a naturally occurring hormone that is thought to counteract the effects of acylated ghrelin. The drug was designed to improve glycaemic control and reduce weight. Livoletide participated in pivotal phase 2b/3 clinical study for the treatment of Prader-Willi syndrome. In addition, the drug was studied in patients with type 2 diabetes mellitus (T2D). Its pharmacokinetic profile, suitable for once daily dosing, and metabolic effects support further clinical development for T2D.

Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure (in Phase 2 of development). Omecamtiv mecarbil is an inotropic agent that prolongs systolic ejection time and increases ejection fraction through myosin ATPase activation.