Evobrutinib is a highly selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK). It potently inhibits BCR- and Fc receptor-mediated signaling and, thus, subsequent activation and function of B cells and innate immune cells such as monocytes and basophils. Evobrutinib demonstrated effectivity in autoimmune disease preclinical models. Evobrutinib is being developed by Merck Serono for the treatment of various autoimmune disorders.

Emricasan (IDN- 6556 or PF-03491390) (3-[2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid) is a pan-caspase inhibitor. Testing in vitro enzyme assays demonstrated that emricasan efficiently inhibits all human caspases at low nanomolar concentrations. Preclinically, emricasan was effective in inhibiting apoptosis of sinusoidal endothelial cells. Emricasan has marked efficacy in models of liver disease after oral administration and thus, is an excellent candidate for the treatment of liver diseases characterized by excessive apoptosis. This drug is a first-in-class anti-apoptotic caspase inhibitor with demonstrated preliminary efficacy in liver-impaired patients in humans.

Setileuton [MK-0633] is a selective inhibitor of the 5-lipoxygenase enzyme, which was under investigation for the treatment of asthma and atherosclerosis. Setileuton has been in phase II clinical trials by Merck Sharp & Dohme for the treatment of asthma, chronic obstructive pulmonary disease (COPD) and atherosclerosis. However, this research has been discontinued.

Netobimin is a carbamate compound which is used as an anthelmintic drug in veterinarymedicine. Netobimin-containing products are available as liquid suspensions which are intendedfor oral administration. Products are available for sheep and cattle. An oral dose of 7.5 mg/kg bw is recommended for the treatment of gastrointestinal infestations of roundworms and tapeworms;and 20 mg/kg bw is recommended for type II ostertagiasis and adult flukes. In order to be pharmacologically active, netobimin needs to be converted to the broad spectrumanthelmintic drug albendazole, by the splitting off of a side-chain and the formation of abenzimidazole group. This occurs naturally in the ruminant gut.

Sufosfamide is an oxazaphosphorine derivative patented by Asta-Werke A.-G as immunosuppressives agent. Sufosfamide is a mixed-function oxazaphosphorine differing from ifosfamide in that the extracyclic 2-chloroethyl function has been replaced by a mesyl-oxyethyl group. It is characterized by an extraordinary intensifi¬cation of the immunosuppressive component of action compared to the carcinotoxic component. Sufosfamide activates of a specific immune tolerance in models of humoral end cell-bound antibodies.

Adibendan [BM 14478] is a phosphodiesterase inhibitor that increases the calcium sensitivity of the myocardium. Adibendan selectively inhibited phosphodiesterase III (PDE III) activity concentration-dependently (IC50 = 2.0 umol/l). The IC50 values for the inhibition of PDE I or II were more than 60-fold higher. Adibendan has both vasodilator and positive inotropic properties. Adibendan was investigated as the potential treatment of heart failure and ischaemic heart disorders. However, research has been discontinued at phase II of development.

Examorelin (Hexarelin) is a hexapeptide (His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2) that stimulates the release of growth hormone lease through binding to the growth hormone secretagogue receptor (GHSR). Hexarelin might have direct cardiovascular actions beyond growth hormone release and neuroendocrine effects. Europeptides and Mediolanum Farmaceutici were developing examorelin for the treatment of somatotropin deficiency.

Zimidoben was developed as an antiinfective drug. Information about the current use of this compound is not available.

Temarotene (also known as Ro 15-0778), the arotinoid with immunosuppressive and immunostimulatory activities. Temarotene was also studied as a chemopreventive agent. Information about the current development of this compound is not available.