Spirotriazine is a dihydrotriazine derivative patented by Burroughs Wellcome & Co. (U.S.A.) Inc. as the anthelmintic agent. In preclinical models, Spirotriazine shows potent activity against intestinal parasites and negligible microbiological activity.

Galunisertib is a potent inhibitor of TGF beta type 1 receptor. The drug is under clinical development for the treatment of different cancers: pancreatic, hepatocellular, breast, rectal, prostate etc. and reached phase 2/3 in patients with myelodysplastic syndromes.

LAROMUSTINE is a sulfonylhydrazine alkylating agent. It is metabolized to yield a chloroethylating compound (VNP-4090-CE) and a carbamoylating compound (methyl isocyanate). The former is primarily responsible for the antineoplastic effect of LAROMUSTINE. It alkylates the O6 position of guanine, resulting in DNA crosslinking, strand breaks, chromosomal aberrations, and disruption of DNA synthesis. The carbamoylating species contribute to antitumor activity by inhibiting O6-alkylguanine transferase, an enzyme involved with DNA repair. It was studied in the treatment of several types of cancer, however, its development was discontinued.

Caldaret is intracardiac calcium (Ca2+) handling modulator whose cardioprotective actions are presumed to be due to inhibition of the NCX exchanger and increasing the uptake of Ca2+ via the sarcoplasmic reticulum (SR). Unfortunately, Caldaret failed to demonstrate efficacy in Phase II clinical trials as an adjunct to standard therapy with primary percutaneous coronary intervention patients diagnosed as having an acute myocardial infarction

L-778123 is a dual inhibitor of Farnesyl Protein Transferase (FPTase) and Geranylgeranyl Protein Transferase type-I (GGPTase-I), which can completely inhibit Ki-Ras prenylation. L-778123 has been used in phase I clinical trials to determine its effectiveness in treating patients with recurrent or refractory solid tumors. L-778123 was also studied in combination with paclitaxel to determine efficacy as a treatment for both recurrent or refractory solid tumors, and lymphomas.

Fostriecin, an antitumor antibiotic produced by Streptomyces pulveraceus, is a strong inhibitor of serine/threonine protein phosphatases type 2A and type 4, and inhibits the catalytic activity of partially purified Topo II (type II topoisomerase) in a non-competitive manner.

Xorphanol (also known as TR5379M) is a full κ-opioid receptor agonist and is a partial agonist at μ opioid receptor. Clinically, xorphanol was studied as an orally active analgesic that provided effective pain relief but showed low physical dependence liability. Further development of this drug was discontinued.

Cizolirtine is a potent analgesic in mice and rats, with an efficacy superior to that of aspirin and other nonsteroid anti-inflammatory drugs. Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P and calcitonin gene-related peptide release. Cizolirtine has been in clinical trials for the treatment of pain and overactive bladder. Reported adverse events are: dry mouth, dizziness, nausea, vomiting, blurred vision.

Omigapil (CGP 3466 or TCH346) is a structurally related analog of R-(-)-deprenyl that exhibits virtually no monoamine oxidase type B inhibiting activity but is neuroprotective in the picomolar concentration range. It binds to glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and at subnanomolar concentrations prevent the S-nitrosylation of GAPDH, inhibit GAPDH-Siah binding and prevent the nuclear translocation of GAPDH. Omigapil demonstrated promising potential in the treatment of Parkinson's disease and motoneuron disease in animal models, however, it did not show efficacy in clinical trials. Omigapil is in development for the treatment of congenital muscular dystrophy.