Canosimibe is diphenyl azetidinone patented by German pharmaceutical company Aventis Pharma Deutschland GmbH as hypolipidemic agent. Canosimibe acts as pre-systemic inhibition of intestinal cholesterol absorption. Unfortunately, during phase II clinical trials Canosimibe failed to demonstrate efficacy in in patients with primary severe hypercholesterolemia.

Metenkephalin (Met-enkephalin) is an endogenous opioid peptide that acts as an agonist at μ-opioid receptors (μORs) and δ-opioid receptors (δORs). Met-enkephalin exhibits neuromodulatory, antinociceptive/analgesic, antidepressant, and gastrointestinal motility modulating activities. Like other endogenous opioids, met-enkephalin modulates expression of opioid receptors and plays a role in reward/reinforcement signaling. Met-enkephalin is also involved in exercise-induced reversal of neuropathic pain and in animals undergoing the forced swim test, decreases immobility time. Met-enkephalin inhibits gastrointestinal muscle contractility, inhibiting motility and gastric emptying. Additionally, analogs of this peptide display anticancer and antiepileptic/anticonvulsant activities.

Levcycloserine is a general inhibitor of pyridoxal 5'-phosphate (PLP)-dependent enzymes. It is an excellent inhibitor of threonine deaminase and serine palmitoyltransferase. Levcycloserine is a ceramide synthesis inhibitor. Levcycloserine is a selective antitumoral agent for neuroblastoma and medulloblastoma cells with the ability to reduce expression of tumour associated gangliosides. In vivo experiments suggest that levcycloserine may be effective drug for treatment of neuroblastoma and medulloblastoma. Levcycloserine interferes with the life cycle of HIV. Levcycloserine selectively down-modulated CD4 expression without affecting the expression of CD3 and CD8. Levcycloserine also inhibited T cell mitogen responses without affecting IL-2 production. Selective inhibition of CD4 by levcycloserine together with its antiviral effects may offer a novel approach for interfering with HIV cell binding and infectivity.

Devazepide (L-364718 or MK-329) is a nonpeptide antagonist for the peripheral (type-A) cholecystokinin (CCK) receptor, which has proved effective in blocking the actions of both exogenous and endogenous CCK in several species. It is an orally active antagonist of CCK-stimulated pancreaticobiliary output in man. Devazepide has been developing for the treatment of anxiety, cancer, neuropathic pain however development discontinued.

9-(N-methyl-L-isoleucine)-cyclosporin A (NIM-811, SDZ 811) is a cyclosporin A analog that is completely devoid of immunosuppressive capacity but exhibits potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity. NIM-811 interferes at two stages of the viral replication cycle: (i) translocation of the preintegration complex to the nucleus and (ii) production of infectious virus particles. NIM-811 induces a concentration-dependent reduction of HCV RNA in the replicon cells with an IC50 of 0.66 uM at 48 h. NIM-811 blocks the mitochondrial permeability transition induced by calcium and inorganic phosphate. NIM-811 blocks cell killing and prevents in situ mitochondrial inner membrane permeabilization and depolarization during tumor necrosis factor-α–induced apoptosis to cultured rat hepatocytes.Novartis discontinued development of SDZ 811 as an oral therapy for hepatitis C and HIV-1 infections.

Masilukast (ZD 3523) is an antagonist of leukotriene D4 (LTD4). It opposes LTD4-induced bronchoconstriction. It was being developed for the treatment of asthma.

Narlaprevir (formerly SCH 900518), a NS3 protease inhibitor is being developed by R-Pharm for the treatment of a chronic hepatitis C (genotype 1). Narlaprevir is a potent inhibitor of hepatitis C virus (HCV) NS3 protease with a Ki of 7 ± 1 nM and a 90% inhibitory concentration (IC90) of ∼28 ng/ml for HCV genotype 1 replicon in vitro. Narlaprevir successfully passed extensive pre-clinical and clinical trials in Schering-Plough Research Institute (USA) and in a variety of clinical centers of Europe, USA and Russia. Based on clinical findings R-Pharm obtained a registration certificate for Arlansa (Narlaprevir) ЛП-003622 dd 12.05.2016 issued by Ministry of Healthcare of the Russian Federation.

Lometrexol, formerly known as DDATHF; LY 264618; T-64 was the first glycinamide ribonucleotide formyl transferase (GARFT) inhibitor to be investigated clinically. Lometrexol had been in phase II clinical trial for the treatment non-small cell lung cancer (NSCLC). However, the studies have been discontinued by Tularik Inc, because Company had suggested, that drug would face competition from other companies in the indication

Medorubicin is an antineoplastic agent.

Glutaurine is formed from the amino group of taurine with the gamma-carboxy group of L-glutamic acid. It was originally discovered in the parathyroid. Evidence has been found suggesting that glutaurine plays a role in peripheral thyroid hormonal regulation. Glutaurine increases triiodothyronine (T3) levels, but does not alter thyroxine (T4) levels. Glutaurine was also shown to prevent electroconvulsive shock-induced amnesia by counteracting the shock effect on the memory consolidation phase. Other roles that have been suggested for glutaurine include roles as a mouse metabolite, a mammalian metabolite, a human metabolite, an anticonvulsant, an anxiolytic drug and a hormone.