Edatrexate (10-ethyl-10-deazaaminopterin or 10-EDAM) is an analog of methotrexate with improved pre-clinical antitumor activity, more selective cellular uptake, and with the more extensive formation of intracellular polyglutamate metabolites. This drug is a new dihydrofolate reductase inhibitor, which was studied in phase II clinical trial for the patients with different cancers. The studies were discontinued, for example, in advanced renal cell carcinoma edatrexate in the investigated dose and schedule had minimal activity and was toxic. In case of non-small-cell lung cancer, the dosing schedule of edatrexate did not appear to be improved compared to other chemotherapeutic regimens. In addition, edatrexate was involved in the experiment for the treatemnt of rheumatoid arthritis, but this study was also discontinued.

Idoxifene (also known as CB 7432), a novel selective estrogen receptor modulator, is originally discovered at the CRC Centre for Cancer Therapeutics, Institute. This drug participated in clinical trials phase II in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. In addition, in phase III in postmenopausal women after one year of idoxifene treatment. However, both studies were discontinued because of insufficient effectiveness.

Saracatinib (AZD0530) is an oral, dual inhibitor of c-Src/Abl kinases initially developed by AstraZeneca for the treatment of cancer. The drug was tested for many neoplasms and reached phase III for ovarian cancer (in combination with paclitaxel), however without demonstrating any significant effect. Sarcatinib is also tested in patients with Alzheimer's Disease (Phase II). Its effect on Alzheimer's Disease patients is explained by inhibition of another kinase, Fyn, which is highly expressed in brain.

An orally bioavailable imidazopyridazine and inhibitor of Janus kinase 2 mutant V617F (JAK2V617F), with potential antineoplastic activity. Upon oral administration, gandotinib selectively and competitively inhibits the activation of JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and the induction of apoptosis in JAK2V617F-expressing tumor cells. Gandotinib is in phase II clinical trials by Lilly for the treatment of myeloproliferative disorders.

Sebriplatin (also known as NK-121 or CI-973) is a platinum analog with antitumor activity. Sebriplatin participated in phase II clinical trials for the treatment of patients with metastatic breast cancer. However, the further development of this drug was discontinued.

Elisidepsin (Irvalec®, PM02734) is a depsipeptide produced by chemical synthesis and chosen for development as an antineoplastic agent based on its in vitro activity against human solid tumor cell lines, in vivo activity in hollow fibers and xenografted human tumors, as well as its acceptable preclinical toxicology profile. Elisidepsin causes a typical necrotic cell death and induces profound alterations in tumor cell morphology. Elisidepsin inserts into the plasma membrane causing rapid loss of integrity and necrotic cell death in tumor cells. PharmaMar was developing elisidepsin for the treatment of cancer. However, development of the compound has been suspended.

Semaxanib is a potent and selective vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 inhibitor that also inhibits other tyrosine kinases KIT, MET, FLT3, and RET. Semaxanib inhibited cell migration of human vascular endothelial cells expressing both Flt-1 and KDR in response to VEGF and also inhibited the cell migration in response to placenta growth factor (PIGF), a specific ligand for Flt-1. Chemotaxis of monocytes expressing only Flt-1 was also inhibited by SU5416 in a dose-dependent manner. Semaxanib targets the VEGF pathway, and both in vivo and in vitro studies have demonstrated antiangiogenic potential. On February 2002, Pharmacia, the then-parent of Sugen, prematurely ended Phase III clinical trials of Semaxinib in the treatment of advanced colorectal cancer due to discouraging results.

Galamustine (C6-galactose mustard or C6-GLM ) is a compound that has demonstrated anti-cancer activity. Its effect on cell growth and cell cycle kinetics was studied in leukemia. Because less bone marrow toxicity was reported for this compound compared to nitrogen mustard, the development of galamustine for clinical trials in humans was considered.