Ibrotamide (also known as 2-Bromo-2-ethylisovaleramide) was developed as a hypnotic and sedative agent. Information about the current use of this drug is not available.

AMOXECAINE is an local anaesthetic.

Alemcinal (ABT-229), a 12-deoxymotilide, is a potent motilin agonist stereoselectively designed by Abbott researchers as an orally active gastroprokinetic agent. ABT-229 is selective agonist of the motilin receptor. ABT-229 is a synthetic derivative of erythromycin with no antibiotic activity, it has been shown to bind to motilin receptors and stimulate contractile activity of the antrum and small intestine. However, the development of Alemcinal was discontinued.

Beperidium (also known as SX-810 ) is a competitive antagonist against acetylcholine. Experiments on animal have shown that this compound exhibited spasmolytic and antiulcerative activities without exerting systemic antimuscarinic side effects.

Navuridine (AzddU) is a nucleoside analogue which demonstrated significant anti-HIV activity and low toxicity in preclinical studies. The drug was originally developed by University of Georgia. Navuridine is a dideoxyuridine inhibitor of HIV reverse transcriptase that is related to zidovudine. Navuridine exhibits a relatively short half-life and incomplete oral bioavailability and has not been developed into a clinical drug.

Cromakalim is an ATP-sensitive potassium (KATP) channel opener, which was studied for the treatment of gastric ulcer, hypertension and preventing a cardiomyopathy. But the development of this drug was discontinued due to heart lesions found in monkey chronic toxicity studies.

Indole-3-carbinol (I3C), a common phytochemical in cruciferous vegetables, and its condensation product, 3,3'-diindolylmethane (DIM) exert several biological activities on cellular and molecular levels, which contribute to their well-recognized chemoprevention potential. ndole-3-carbinol is used for prevention of breast cancer, colon cancer, and other types of cancer. The National Institutes of Health (NIH) has reviewed indole-3-carbinol as a possible cancer preventive agent and is now sponsoring clinical research for breast cancer prevention. Indole-3-carbinol is also used for fibromyalgia, tumors inside the voice box (laryngeal papillomatosis) caused by a virus, tumors inside the respiratory tract (respiratory papillomatosis) caused by a virus, abnormal cell growth in the cervix (cervical dysplasia), and systemic lupus erythematosus (SLE). Indole-3-carbinol scavenges free radicals and induces various hepatic cytochrome P450 monooxygenases. Specifically, this agent induces the hepatic monooxygenase cytochrome P4501A1 (CYP1A1), resulting in increased 2-hydroxylation of estrogens and increased production of the chemoprotective estrogen 2-hydroxyestrone. Accumulating evidence indicates that the antitumor activity of indole-3- carbinol is attributable to its ability to interfere with multiple oncogenic signaling pathways governing cell cycle progression, survival, invasion, and other aggressive phenotypes of cancer cells. Reported signaling targets of indole-3- carbinol in various cancer cell lines include EGFR/Src, Akt/NF-B, stress responses, elastase, and Rho kinase. Moreover, indole-3-carbinol functions as a negative regulator of estrogen action in hormonesensitive cancer cells through the inhibition of estrogen receptor (ER)-alpha signaling and/or induction of cytochrome P-450-mediated estrogen metabolism, suggesting its clinical use in hormone-sensitive cancers.

Aderbasib, also known as INCB007839, is an orally bioavailable low nanomolar hydroxamate-based inhibitor of the ADAM (A Disintegrin And Metalloprotease) family of multifunctional membrane-bound proteins with potential antineoplastic activity. Aderbasib represses the metalloproteinase "sheddase" activities of ADAM10 and ADAM17, which may result in the inhibition of tumor cell proliferation. In preclinical studies, Aderbasib with lapatinib prevented the growth of HER-2/neu–positive BT474-SC1 human breast cancer xenografts in vivo. Aderbasib was being developed by Incyte as a potential adjunctive treatment for metastatic breast cancer. Aderbasib in combination with trastuzumab increased the response rate in HER2 positive metastatic breast cancer patients with advanced disease, relative to historical controls (50% versus 15–35%). INC7839 also improved progression-free survival in a subset of the patients expressing the p95 fragment of HER2. Aderbasib development was halted in 2011 after positive findings from Phase II trials were contradicted by further research. Aderbasib is currently being tested in combination with rituximab for diffuse large B cell non-Hodgkin lymphoma.