Ibuterol, a prodrug that is rapidly hydrolyzed to form a drug, terbutaline. Terbutaline, a beta-2 adrenergic agent used to treat asthma.

Edotecarin (J-107088 or [6-N-(1-hydroxymethyl-2-hydroxy)ethylamino-12,13-dihydro-2,10-dihydroxy- 13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]-pyrrolo[3,4-c]-carb azo le-5,7(6H)-dione]) is a DNA topoisomerase I inhibitor. The antitumor activity of edotecarin has been tested in vitro and in vivo, and inhibition of tumor growth has been observed in breast, cervix, pharynx, lung, prostate, colon, gastric, and hepatic cancer models. Banyu Pharmaceutical Co Ltd and Pfizer Inc were developing edotecarin for the potential treatment of solid tumors. Edotecarin development has been discontinued.

Carperone is a fluorobutyrophenone compound which in animal studies has showed calming or tranquilizing effects resembling those of haloperidol, trifluperidol, and other antipsychotic drugs

Terbuficin was studied as a hypolipidemic agent. However, information about the current development and use of this drug is not available.

Prifelone (also known as R-830) is a thiophene derivative patented by American pharmaceutical company Riker Laboratories, Inc. As an antiinflammatory, analgesic, and antipyretic compound. In vitro, Prifelone acts as a nonsteroidal anti-inflammatory drug and inhibits guinea pig lung lipoxygenase and bovine seminal vesicle cyclooxygenase. In preclinical studies, Prifelone shows potent anti-inflammatory activity in carrageenan-induced edema and adjuvant arthritis of the rat and ultraviolet-induced erythema in the guinea pig

Revospirone (BAY VQ 7813) is a pyrimidinylpiperazine derivative that acts as partial agonist at 5-HT1A receptors. Head shakes were reported after administration of revospirone in pigs, and once daily administration for 3-5 days led to a reduction in this head shake response. No behavioral alterations were observed. This compound was never marketed

Ciglitazone, 5-[4-(1-methylcyclohexylmethoxy) benzyl]-thiazolidine-2,4-dione, is a hypoglycemic agent and a thiazolidenedione derivative. Ciglitazone binds to the PPAR gamma receptor and possesses agonist activity. This drug was in clinical trials in Japan for the treatment Diabetes mellitus, but that study has been discontinued. Ciglitazone was able to decrease the production of vascular endothelial growth factor (VEGF) in an in vitro human granulosa cell model. That result together with the pivotal role of VEGF in ovarian hyperstimulation syndrome suggests that ciglitazone may have a high potential as a therapeutic agent.

Methoxyphedrine (para-methoxymethcathinone, 4-methoxymethcathinone, bk-PMMA, PMMC, Methedrone, 4-MeOMC) is a phenethylamine, amphetamine, and cathinone derivative that acts as a triple reuptake/release/reversible monoamine oxidase inhibitor and used as a recreational drug. Methedrone has been found to be a potent serotonin transporter (SERT) and norepinephrine transporter (NET) inhibitor, but a weak dopamine transporter (DAT) inhibitor. Methedrone induces the transportation mediated release of NE, DA, and 5-HT from cells preloaded with monoamines making it a serotonin-norepinephrine-dopamine (SNDRA) releasing agent, also known as triple releasing agent (TRA), which is a common characteristic among drugs of abuse. The health risks associated with Methedrone are unknown but are expected to be similar to other cathinones. The deaths of two young men in southeast Sweden in 2009 were attributed to Methedrone overdose.