Methylsamidorphan (previously known as ALKS 37), an opioid receptor antagonist that was developed to treat opioid-induced bowel dysfunction. This drug participated in phase II clinical trial to evaluate the safety, tolerability, and efficacy when administered daily for 4 weeks to adults with Opioid-induced Constipation. However, the product profile did not satisfy the pre-specified criteria for advancing into phase III clinical trials. Based on this evaluation, was made the decision of discontinuation of the further methylsamidorphan study.

Thiorphan is the first potent synthetic inhibitor of enkephalinase. Thiorphan displays antinociceptive activity after systemic administration. Thiorphan also inhibits to a lesser extent the widely distributed angiotensin-converting enzyme, a carboxydipeptidase implicated in blood pressure regulation. Thiorphan failed to potentiate allergen-induced airway responses in asthma. Thiorphan significantly reduced the castor oil-induced diarrhea in rats when administered intravenously but not when administered intracerebroventricularly. Racecadotril, via its active metabolite thiorphan, was consistently effective in animal models and patients with various forms of acute diarrhea by inhibiting pathologic (but not basal) secretion from the gut without changing gastro-intestinal transit time or motility.

Ravidasvir (RDV, ASC16) is a second‐generation, pan‐genotypic non‐structural (NS) 5A inhibitor, which inhibits viral replication and assembly. Ravidasvir exhibits high antiviral potency with EC50 0.04–1.14 nM for HCV GT1–GT6. The pharmacokinetics results indicated that steady status achieved quickly after the first dose. Metabolism studies utilizing human clinical samples showed that Ravidasvir was very stable, with only modest (~2%) metabolite formation. Biliary excretion of Ravidasvir appears to be the primary route of elimination of the absorbed dose, while renal excretion of the intact drug appears to be negligible. In clinical trans twelve-week Ravidasvir and ritonavir-boosted Danoprevir in combination with ribavirinfor 12 weeks achieve the sustained virologic response rate of 100% in treatment-naïve non-cirrhotic Asian patients with HCV GT1 infection. Ravidasvir for treatment‐naïve, non‐cirrhotic HCV GT1 patients was safe and well tolerated. There was no death, treatment‐related serious adverse events, and discontinued cases due to adverse events.

Tetroquinone (Tetrahydroxy-1,4-benzoquinone, tetrahydroxy-p-benzoquinone, tetrahydroxybenzoquinone) is cyclohexadiene derivative with four hydroxyl groups and two ketone groups in opposite (para) positions, with potent prooxidant activity. The exposure of exponentially growing cultures to Tetroquinone, in the presence of Ca2+, caused a dose-dependent inhibition of cell growth and DNA synthesis. The chemical reactivity of Tetroquinone is strongly similar to those of physiological polyphenols, such as catechols and catecholamines. Despite their physiological and pharmacological roles, these compounds may, in addition, present toxicological properties due to their ability to autoxidize generating ROS and quinones Similar to catechols, the OH-substituents confer to Tetroquinone the ability to autoxidize readily in neutral aqueous solutions generating intermediate superoxide anion radicals, semiquinone radicals, and the corresponding quinone. The compound can be synthesized from glyoxal or from myo-inositol (phytic acid), a natural compound widely present in plants.

LCQ908 (Pradigastat) is a diacylglycerol acyltransferase-1 (DGAT-1) inhibitor. DGAT-1 is one of the two DGAT enzymes that catalyse the formation of triglycerides from diacylglycerol and acyl- coenzyme A. DGAT-1 catalyses the final committed step in processing dietary fatty acids into triglycerides carried on chylomicrons for transport around the body. Pradigastat may decrease the level of triglycerides in the blood and is intended for the first line treatment of FCS. It is administered orally at 10-40mg daily in addition to a low fat diet. Pradigastat is also in phase II clinical trials for type 2 diabetes and severe hypertriglyceridaemia (familial hyperchylomicronaemia phenotypes I and V). Pradigastat is a designated orphan drug in the EU. In a phase III clinical trial.

Telapristone is an orally available 21-substituted-19-nor-progestin and selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Its acetate form, the telapristone Acetate is a clinically used and a studied drug.

Bentiamine (also known as dibenzoyl thiamine), a derivative of thiamine, is rapidly absorbed and converted to thiamine. Experiments on rodent have shown that this compound had low toxicity and absence of carcinogenicity.

2,4,5-Trichlorophenol is a grey flake or needle-shaped solid. It is used as an intermediate in the manufacture of the herbicide 2,4,5-Trichlorophenoxyacetic Acid (2,4,5-T) and as a fungicide and bactericide. 2,4,5-trichlorophenol (triclofenol piperazine, Ranestol) is an antifungal agent, which was also used against light hookworm infections. Thirty persons who were positive for hookworm eggs in their stools were treated with 50 mg/kg of triclofenol piperazine dissolved in 5 per cent polyethylene glycol Ranestol® in soft gelatin capsules. Nineteen of these showed 77 to 100 % reduction in egg count average when compared with the pre-treatment counts. Side reactions were limited to mild and transient nausea in 23, vomiting in 7, transient abdominal cramps and headache in 2 each. 2,4,5-trichlorophenol complexed with dicyclohexylamine was used for treatment of experimental mycosis. From the mycological and clinical evaluation the conclusion can be drawn that the effect of phenol in lipophilic ointment is comparable to that of clotrimazole.

Fiboflapon sodium (GSK2190915) is a high affinity 5-lipoxygenase-activating protein inhibitor being developed for the treatment of asthma. The compound was originally developed by Amira Pharmaceuticals. Fiboflapon sodium (GSK2190915) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. GSK2190915 also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model. Oral administration of Fiboflapon sodium (GSK2190915) (1 mg/kg) resulted in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM. When rat lungs were challenged in vivo with calcium-ionophore, Fiboflapon sodium inhibited LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively. Fiboflapon sodium is in Phase-II for Asthma (Adjunctive treatment) in Poland, Ukraine, Bulgaria, USA, United Kingdom and Canada (PO).