Talisomycin (former trivial name: tallysomycin A), a third generation bleomycin analog that was studied as an antitumor antibiotic. The drug cleaved DNA preferentially at G-C and G-T sequences and produced specific cleavages at G-A sequences. Talisomycin participated in phase II clinical trial for the treatment of cancer; however, the further development of the drug was discontinued.

Millennium Pharmaceuticals Inc's tandutinib (MLN-518), a piperazinyl derivative of quinazoline, is an orally active inhibitor of FLT3 kinase and family members PDGFR beta and c-Kit. Tandutinib inhibited FLT3 phosphorylation, downstream signaling and malignant growth in vitro and in animal models. The drug exhibited limited activity as a single agent in phase I and II clinical trials in patients with AML and myelodysplastic syndrome, but displayed promising antileukemic activity (90% complete remissions) in a phase I/II trial in patients with newly diagnosed AML when administered in combination with cytarabine and daunorubicin. Phase II clinical trials for tandutinib in patients with Glioblastoma have being discontinued. The use of tandutinib to treat AML has been granted fast-track status by the U.S. Food and Drug Administration. Phase II trials were underway., but later withwrawn.

Bromofos is an organic thiophosphate used as pesticide and insecticide for apple-pest control. Bromophos possesses remarkable stability in alkaline media and extremely low mammalian toxicity. The oral toxicity for small rodents is 3.75 to 13.4 mg/kg. body wt. Bromofos acts as contact and stomach poison. Very good efficacy is obtained against flies and their larvae, especially against parasitic species on sheep. Bromopros in sheep dip soln. is as effective as diazinon. It is effective in stables for fly control, depending on the surface, for up to 14 weeks.

Amifloxacin [WIN 49375] is a fluoroquinolone antibacterial with a broad range of activity against aerobic Gram-negative and some aerobic Gram-positive organisms. Amifloxacin is a DNA gyrase inhibitor. The 50% inhibiory concentration for supercoiling activity of E.coli KL16 DNA gyrase of amifloxacin (MIC, 0.10 ug/ml) was 2.47 ug/ml. Amifloxacin was in trials for the treatment of gram-negative infections, septic shock and urinary tract infections. However, development of amifloxacin has been discontinued.

Halofuginone is a low molecular weight quinazolinone alkaloid, and a potent inhibitor of collagen alpha1(I) and matrix metalloproteinase 2 (MMP-2) gene expression. Halofuginone also effectively suppresses tumor progression and metastasis in mice. Halofuginone is a potent inhibitor of collagen a1(I) and matrix metalloproteinase 2 (MMP-2) gene expression. Halofuginone also suppresses extracellular matrix deposition and cell proliferation. Also was shown that halofuginone increased apoptosis in α smooth muscle actin- and prolyl 4-hydroxylase β-expressing cells in mdx diaphragm and in myofibroblasts, the major source of extracellular matrix. The profound antitumoral effect of halofuginone is attributed to its combined inhibition of tumour-stromal support, vascularization, invasiveness, and cell proliferation. HT-100 (delayed-release halofuginone), currently in clinical phase 1b/2a in five U.S. hospitals, is a small molecule drug candidate taken orally for the treatment of Duchenne muscular dystrophy (DMD) patients primarily through its ability to reduce fibrosis and inflammation and promote muscle fiber regeneration. The medicine candidate has been granted orphan drug designation in the U.S. and the EU — meaning it has been commercially undeveloped due to its limited profitability — and fast-track designation in the U.S. — an FDA process that aims to facilitate the development and patients’ reach to novel therapies for unmet medical needs.

Lexipafant is a platelet-activating factor (PAF) antagonist. It was hypothesized that the substance could beneficially affect the cognitive performance of HIV infected people. Lexipafant was as tolerable as placebo. At week 6 and week 10 after baseline evaluations, the lexipafant group showed trends toward improvement on the Rey Auditory Verbal Learning test as well as the timed gait test. A phase IIa placebo-controlled study reported that lexipafant was not effective in patients with severe ulcerative colitis receiving corticosteroids. Two lexipafant treated patient had adverse events: severe influenza-like symptoms in one and hypotension with iliac artery thrombosis in one. The clinical trials of lexipafant in the treatment of acute pancreatitis were undertaken with considerable optimism. There was a significant reduction in the incidence of organ failure and in total organ failure score at the end of medication (72 h).

Triapine (3-aminopyridine-2-carboxaldehyde thiosemcirbazone, (3-AP; NTO-1151; OCX-0191) is a novel small molecule ribonucleotide reductase inhibitor that acts on the M2 (R2) subunit. Ribonucleotide reductase is an enzyme involved in the de novo synthesis of deoxyribonucleotides, which are critical for DNA replication and DNA repair. Triapine has been used in trials phase II studying the treatment of Lung Cancer, Kidney Cancer, Prostate Cancer Pancreatic Cancer, among others. Recently was published the article describing, that the triple combination triapine-cisplatin-paclitaxel was safe and provided a rational basis for a follow-up phase II trial to evaluate the efficacy and progression-free survival in women with metastatic or recurrent uterine cervix cancer.

Phenylthilone is an anticonvulsant, hypnotic and spasmolytic agent.

Salnacedin (also known as G 201) was developed as a topical anti-inflammatory agent; Salnacedin participated in phase II clinical trials in the USA for the treatment of dermatitis, acne, and psoriasis. However, all these studies were discontinued.

Disermolide (discodermolide) is the immunosuppressant and antineoplastic agent. The marine natural product discodermolide was first isolated in 1990 from the deep-water Caribbean sponge Discodermia dissoluta. It attacks cancer cells in a similar way to the successful cancer drug Taxol that has become the best-selling anticancer drug in history. Discodermolide is a microtubule-stabilizing agent with potential for the treatment of taxol-refractory malignancies. Discodermolide is a drug that functions as an immunosuppressant and induces G2/M phase cell-cycle arrest in lymphoid and non-lymphoid cells. The cytotoxicity of discodermolide cause cell-cycle arrest by mitosis and an important alteration at the level of microtubules. Discodermolide is a potent inducer of accelerated senescence. At present, Phase I trials with discodermolide has been discontinued as a consequence of unsafe efficacy and toxicity results.