Deferitazole is an iron chelator, developed by the FerroKin BioSciences (later acquired by Shire, and then by Takeda). Deferitazole is a member of the desazadesferrithiocin class of siderophore-related tridentate chelators. It binds Fe(III) with very high affinity and selectivity over Fe(II) and other biologically important metals. Deferitazole was investigated in phase 2 clinical trials in patients with iron overload due to repeated red blood cell transfusion and beta-thalassemia, however, the development of the drug was discontinued. In preclinical models, deferitazole demonstrated efficacy for the treatment and prevention of malaria.

FLOVAGATRAN is a potent, reversible, low-molecular-weight, highly selective synthetic direct thrombin inhibitor that has demonstrated promising pharmacokinetic properties and biological activity in preclinical studies. However, its development for thrombosis was discontinued in Phase II.

Monalazone is a sulfonylbenzoic acid derivative used as vaginal disinfectant or antiseptic and spermicidal contraceptive.

Nafenodone [LU 39821] is a potent and selective inhibitor of norepinephrine and serotonin uptake. Its development for the treatment of anxiety disorders, major depressive disorder and psychotic disorders has been discontinued.

Avoralstat, a small molecule inhibitor of plasma kallikrein, participated in clinical trials phase III to prevent hereditary angioedema, but these studied were discontinued due to insufficient efficacy study. Recently published article has described that avoralstat could improve the quality of life in C1‐INH‐HAE patients. Hereditary angioedema (HAE) with C1 inhibitor deficiency (C1‐INH‐HAE) is an autosomal dominant disorder characterized by recurrent episodes of swelling of the skin, pharynx, gastrointestinal tract, genitals, and is due primarily to mutations in the SERPING1 gene that results in insufficient production of the natural plasma kallikrein inhibitor, C1 inhibitor (C1‐INH).

IPROFENIN is an iminodiacetic acid derivative. Its 99mTc radiolabelled form was used in cholescintigraphy and hepatobiliary scintigraphy to diagnose problems of the liver, gallbladder and bile ducts.

Palytoxin is the most potent marine toxin known that was isolated from a zoanthid of the genus Palythoa and Cyanobacteria (Trichodesmium). Palytoxin is a potent vasoconstrictor that damages the ionic gradient of the cells, causing cell death. This toxin has a strong potential for toxicity in humans and animals that is why it causes great concern worldwide. It is crucial to remove this toxin and start an aggressive topical therapy as soon as possible.

Arno Therapeutics is developing AR-12, an orally available, targeted therapy for cancer and infectious diseases. AR-12 is a potentially first-in-class, orally available, targeted anti-cancer agent that has been shown in preclinical studies to inhibit phosphoinositide-dependent protein kinase-1, or PDK-1, a protein in the PI3K/Akt pathway that is involved in the growth and proliferation of cells, including cancer cells. Although FDA-approved drugs that target the Akt pathway have shown efficacy in treating cancer, some tumors either do not respond to these drugs or eventually become resistant to therapy. Scientists hypothesize that a combination of drugs that inhibit different targets in this pathway could provide synergistic or additive benefits to increase efficacy and potentially overcome drug resistance. For this reason, there has been particular interest within the biopharmaceutical industry in developing inhibitors of PI3K, PDK-1, and Akt. AR-12 was licensed to Arno in January 2008 by The Ohio State University Research Foundation for commercial development by Arno as a potential treatment for solid tumors and hematological malignancies. In preclinical studies, AR-12 has shown efficacy in a wide range of tumor types, including breast, lung, prostate, pancreatic, brain and hematological cancers, as both a single-agent as well as in combination with leading oncology therapeutics. Also AR-12 represents a promising class of small molecules with broad-spectrum antifungal activity. AR-12 inhibits fungal acetyl coenzyme A (acetyl-CoA) synthetase in vitro and is fungicidal at concentrations similar to those achieved in human plasma. AR-12 has a broad spectrum of activity, including activity against yeasts (e.g., Candida albicans, non-albicans Candida spp., Cryptococcus neoformans), molds (e.g., Fusarium, Mucor), and dimorphic fungi (Blastomyces, Histoplasma, and Coccidioides) with MICs of 2 to 4 ug/ml. AR-12 is also active against azole- and echinocandin-resistant Candida isolates, and subinhibitory AR-12 concentrations increase the susceptibility of fluconazole- and echinocandin-resistant Candida isolates. Also AR-12 acts as a broad-specificity anti-viral drug in vitro and in vivo. AR-12 (OSU-03012) interacts with multiple chaperone proteins of the HSP90 family and the HSP70 family resulting in a broad spectrum of chaperone inactivation. This overall loss of chaperone functionality results in cells being more readily capable of undergoing autophagic processes and in cells that have a reduced competency for virus replication.

Ponfibrate is clofibrate derivative. It is an antilipidemic agent with demonstrated hypobetalipoproteinemic effect.

Indoxole is phenylindene derivative patented by Mead Johnson & Co. as antidepressants. Indoxole have potent activity in the prevention of reserpine-induced ptosis in mice.