Timcodar (also known as VX-853) is a benzenepropanamide derivative patented by Vertex Pharmaceuticals Incorporated as an efflux pump inhibitor for the treatment of multi-drug resistant bacterial infection. Timcodar potentiates the activity of ethidium bromide (EtBr), a model efflux substrate, against three clinically significant gram-positive pathogens: Staphylococcus aureus, Enterococcus faecalis, and Streptococcus pneumoniae. Timcodar weakly inhibits M. tuberculosis growth in broth culture but shows a 10-fold increase in the growth inhibition of M. Tuberculosis cultured in host macrophage cells and demonstrated synergy with rifampin, moxifloxacin, and bedaquiline. In a mouse model of tuberculosis lung infection, timcodar reduces the likelihood of a relapse infection and potentiates the efficacies of rifampin and isoniazid. Timcodar in combination with Doxorubicin was studied in phase 1/2 clinical trials in patients with solid tumors, but no results have been published.

Palinavir (formerly BILA2011BS) is a potent inhibitor of the human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) proteases and was studied for the treatment of HIV infections. However, information about the current development of this drug is not available.

Barucainide, an IB anti-arrhythmic agent, was evaluated in patients with coronary artery disease. Its antiarrhythmic effect was studied in patients with markedly depressed left-ventricular function. Barucainide was in phase II clinical trials to treat the patients with arrhythmias but the development of the drug was discontinued.

Lificiguat (YC-1) [3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole], a chemically synthetic benzylindazole compound, is a direct soluble guanylate cyclase activator. It possessed antiplatelet activity. YC-1 inhibits Hypoxia-inducible factor-1 (HIF-1). YC-1 demonstrated antineoplastic potential both in vitro and in vivo in animal models.

PAI-749 is a small molecule inhibitor of PAI-1 with proven antithrombotic efficacy in several preclinical models. PAI-1 inactivation by PAI-749 using purified components can result from a dual mechanism of action. First, PAI-749 binds directly to PAI-1, blocks PAI-1 from accessing the active site of tPA, and abrogates formation of the SDS-stable tPA/PAI-1 complex. Second, binding of PAI-749 to PAI-1 renders PAI-1 vulnerable to plasmin-mediated proteolytic degradation. Despite its efficacy in a purified human system and in preclinical models of thrombosis, the ex vivo clinical study suggests that PAI-749 does not affect thrombus formation or fibrinolysis in a range of established human plasma and whole blood-based systems.

LAROTAXEL is a taxoid with potential antineoplastic activity. It prevents microtubule depolymerization, thereby inhibiting cell proliferation. It displays a broad spectrum of antitumor activity in vitro and in vivo, including activity against P-glycoprotein expressing tumors. LAROTAXEL was in phase III clinical trials for the treatment of breast cancer, pancreatic cancer, and bladder cancer. However, its development was discontinued.

Implitapide is a microsomal triglyceride transfer protein (MTP) inhibitor with antihyperlipidemic activity. Microsomal triglyceride transfer protein (MTP) is essential for the synthesis of both chylomicron in the intestine and very low-density lipoprotein in the liver. In an animal model, inhibition of MTP by implitapide reduced both total cholesterol and triglyceride levels and suppressed progression of atherosclerotic lesions in apolipoprotein E knockout mice fed a Western-type diet.

LEMINOPRAZOLE is an inhibitor of the gastric mucosal proton pump. Its development for the treatment of peptic ulcer was discontinued.

Amelubant, its metabolite BIIL 260 (formed by removal of the ethoxycarbonyl protecting group), and its major metabolite BIIL 315 (formed by removal of the protecting group and glucuronidation) had potent in vitro and in vivo Leukotriene B4 receptor antagonistic properties. Amelubant has been in phase II clinical trials by Boehringer Ingelheim for the treatment of cystic fibrosis, chronic obstructive pulmonay disease, bronchial asthma and rheumatoid arthritis. However, this research has been discontinued. In 2002, orphan drug designation was received in E.U. for the treatment of cystic fibrosis. Serious adverse events of Amelubant were characterized by increased presentation of respiratory signs and/or symptoms associated with pulmonary exacerbation and resulted in admission to a hospital and/or administration of IV antibiotics.

Broxaldine, also known as brobenzoxaldine, is a dibromo derivative of quinaldine. It was used in combination with other halogenated hydroxyquinoline compound broxyquinoline (INTESTOPAN) for the treatment of intestinal amoebiasis and childhood diarrhea. In a specific ratio of 5/1, they were shown to act synergistically against several pathogens.