Tandamine was developed as a selective serotonin reuptake inhibitor for the treatment of depression. Tandamine participated in clinical trials in hospitalized depressed patients, where it showed that the well-tolerated drug could be of some benefit for retarded depressions. In addition, was found in human volunteers, that tandamine possessed significant anticholinergic activity, to reduce appetite and to produce sedation. However, this drug has never been marketed.

Tandamine was developed as a selective serotonin reuptake inhibitor for the treatment of depression. Tandamine participated in clinical trials in hospitalized depressed patients, where it showed that the well-tolerated drug could be of some benefit for retarded depressions. In addition, was found in human volunteers, that tandamine possessed significant anticholinergic activity, to reduce appetite and to produce sedation. However, this drug has never been marketed.

R-etodolac (SDX-101) is the non-cyclooxygenase 2-inhibiting R-enantiomer of the non-steroid anti-inflammatory drug etodolac (1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid). The absolute configuration of the enantiomer is R-(-)-etodolac. R-etodolac specifically bound retinoid X receptor (RXRalpha), inhibited RXRalpha transcriptional activity, and induced its degradation by a ubiquitin and proteasome-dependent pathway. In addition R-etodolac can disrupt the beta-catenin signaling pathway. R-etodolac exerts antineoplastic properties. R-etodolac was in phase 2 studies for the treatment of hematologic malignancies however development was discontinued.

PF-04217903 is a triazolopyrazine inhibitor of c-MET that displays anticancer chemotherapeutic and anti-metastatic activities. PF-04217903 inhibits cell proliferation, invasion, and migration as well as tumor growth in various cancer models. In animal models of pancreatic neuroendocrine tumors, this compound prevents lymph node metastasis. PF-04217903 had been in phase I clinical trials by Pfizer for the treatment of solid tumors. In 2011, the company discontinued the development of the compound.

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.

Miransertib (ARQ 092) is a selective, pan-AKT (protein kinase B) inhibitor that potently inhibits AKT1, 2 and 3 isoforms. Miransertib binds inactive AKT, preventing membrane localization and subsequent AKT activation, and binds active AKT, resulting in direct inhibition. Miransertib participates in Phase 1/2 of clinical trials to treat patients at least 2 years of age with PIK3CA-related Overgrowth Spectrum (PROS) and Proteus syndrome (PS). In addition, the drug is involved in the phase I trial in patients with lymphoma, endometrial cancer, and AKT1 E17K mutations. Recently was shown that miransertib could be an excellent lead compound for the development of new oral drug therapy for visceral and cutaneous leishmaniasis.

Lixazinone selectively inhibits the high-affinity form of cyclic AMP phosphodiesterase (type IV) isolated from human platelets with only weak effects on both the nonspecific and cyclic GMP-sensitive phosphodiesterases. The inhibitor reduces both maximum velocity and substrate affinity of the type IV enzyme. Lixazinone exhibits marked selectively for the platelet high-affinity enzyme. It also has significant inhibitory effects on cardiac membrane-bound phosphodiesterase. Lixazinone may be useful as an agent to increase cardiac output in the treatment of congestive heart failure. It is a potent PDE3 inhibitor. Lixazinone suppresses folic acid-induced proliferation of rat tubular epithelial cells in vivo.

AZD-3514 is a down-regulator of androgen receptors. The drug was synthesized by AstraZeneca for the treatment of castrate-resistant prostate cancer and even reached phase I, however, its development was terminated.

Clobenzepam (tarpane) is a drug exhibiting antihistaminic properties.

Trospectomycin is an aminocyclitol antibiotic similar in structure to spectinomycin. The drug was originally developed by Pharmacia & Upjohn. It is a 6'-propyl analogue of spectinomycin, and lacks the aminosugars in glycosidic linkage which are thought to be responsible for the ototoxicity and nephrotoxicity associated with the aminoglycosides. The mechanism of action of trospectomycin is similar to that of its parent compound, spectinomycin: it binds to the bacterial 30S ribosome and inhibits protein synthesis. The transport mechanism for its delivery to its target site does not appear to be oxygen dependent, and this explains the in-vitro activity of trospectomycin against anaerobic organisms. Trospectomycin has activity against a broad spectrum of pathogenic organisms including Streptococcus, Haemophilus, Gardnerella, Neisseria, Peptococcus, Peptostreptococcus, Bacteroides, Mobiluncus, Chlamydia, Mycoplasma and Ureaplasma spp. Results of in-vivo testing suggest potential utility in a variety of clinical conditions including non-gonococcal urethritis, chlamydial cervicitis, gonorrhoea, pelvic inflammatory disease, pneumonia, anaerobic infections and meningitis. Trospectomycin progressed to late stage clinical trials for treatment of pelvic inflammatory disease (chlamydia) before being abandoned for commercial reasons as the third generation cephalosporins and second generation macrolides in development and use were judged superior at the time.