Diapamide is an effective diuretic and saluretic agent in rats, dogs, and monkeys. A pharmacologic animal study indicated that diapamide may be equal or superior to furosemide in experimentally induced congestive failure. Diapamide possessed the ability to induce water loss approximately equally from cells and extracellular fluid with or without the presence of excess water. The most frequently occurring ad- verse reaction was mild to moderate nausea, diarrhea and vomiting. In human, urine output with furosemide was significantly greater than with diapamide. Thus, diapamide would appear to serve a role between the milder thiazide diuretics and the more effective furosemide.

Damotepine is a derivative of thiepin, structurally related to doxepin. Damotepine was discovered by the Swiss pharmaceutical company Geigy A.G. and was evaluated in clinical trials for the treatment of anxiety in the early 1970s.

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.

Orotirelin (previously known as CG 3509) was investigated as a thyrotropin-releasing hormone. Experiments on rats have shown that compound could increase dopamine release from rodent brain. Information about the current study of this drug is not available.

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.

Ofornine is a vasodilator with antihypertensive activity. Experiments on rats have shown that ofornine reduced spontaneously hypertensive (SH) blood pressure through vasodilating and presynaptic adrenolytic activities, and that a dopaminergic mechanism may be involved. Information about the current use of this drug is not available.

Cericlamine (INN) is a potent and moderately selective serotonin reuptake inhibitor (SSRI) of the amphetamine family that was investigated as an antidepressant for the treatment of depression, anxiety disorders, and anorexia nervosa by Jouveinal

Cenicriviroc (also referred to as TBR-652 and TAK-652) is an orally active, potent inhibitor of ligand binding to C-C chemokine receptor type 2 (CCR2) and C-C chemokine receptor type 5 (CCR5). Cenicriviroc does not inhibit ligand binding to CCR1 (an alternative target of CCR5 ligands). The mean half-life in healthy volunteers is 35 to 40 hours, which allows daily dosing of the drug. Due to its CCR5 blocking activity, Cenicriviroc has initially been tested as a drug against CCR5-tropic HIV infection. In a double-blind placebo-controlled trial involving 54 HIV infected participants, Cenicriviroc monotherapy at different doses (25, 50, 75, 100, or 150 mg) led to a dose-dependent reduction in HIV-1 RNA levels and concomitant increases in circulating levels of the CCR2 ligand monocyte chemoattractant protein 1 (MCP-1, or CCL2), suggesting potent CCR2 and CCR5 inhibition in vivo. According to clinical trials, Cenicriviroc is a very safe drug with a wide therapeutic range and fairly low pharmacokinetic variability. In animal models of liver diseases, Cenicriviroc potently inhibits macrophage accumulation in the liver and ameliorates fibrosis. In a phase 2b clinical trial on 289 patients with NASH and fibrosis, Cenicriviroc consistently demonstrated liver fibrosis improvement after 1 year of therapy and had an excellent safety profile.

Cemadotin (LU103793) is a cytotoxic water-soluble pentapeptide analogue of dolastatin 15. The dolastatin peptides were originally isolated from the shell-less mollusc Dolabella auricularia. Cemadotin blocks cells at mitosis. It exerts its antitumor activity by suppressing spindle microtubule dynamics through a distinct molecular mechanism by binding at a novel site in tubulin. Cemadotin was in phase II clinical trials as a promising cancer chemotherapeutic agent. However, this agent appears to be inactive in the treatment of advanced non-small-cell lung cancer and other tumors and this research has been discontinued.