Batabulin or T138067 (2-fluoro-1-methoxy-4-pentafluorophenylsulfonamidobenzene) covalently and selectively modifies the beta1, beta2, and beta4 isotypes of beta-tubulin at a conserved cysteine residue, thereby disrupting microtubule polymerization. Cells exposed to batabulin become altered in shape, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy. Batabulin is equally efficacious in inhibiting the growth of sensitive and multidrug-resistant human tumor xenografts in athymic nude mice. Batabulin has been in clinical trials for the treatment of cancers (breast cancer, colorectal cancer, glioma, hepatocellular carcinoma, non-small cell lung cancer). It does not have clinical activity in the treatment of colorectal cancer and glioma. Batabulin development was discontinued.

Nocodazole is an anti-mitotic drug that has long been used as an experimental tool in cell biology. Nocodazole is known to bind with high affinity to tubulin and to inhibit microtubule assembly. The tubulin molecule is a α/β heterodimer; both α and β exist as various isotypes whose distribution and drug-binding properties are significantly different. Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII. In addition, nocodazole was investigated as an anticancer drug on xenografts model and it was revealed, that nocodazole possessed a high-affinity for the cancer-related kinases ABL, c-KIT, BRAF, and MEK, and inhibited Abl, Abl(E255K) and Abl(T315I).

Diminazene is an aromatic diamidine derived from Surfen C. Diminazene is used as aceturate salt. Diminazene is highly active against both Trypanosoma and Babesia spp. It is also of value in the treatment of theileriosis due to Theileria annulata. Diminazene has become the most commonly used therapeutic agent for trypanosomiasis in animals. It is said to be effective in canine, ovine and bovine babesiosis and, unlike some drugs, is less susceptible to relapse. It may also possess antibacterial properties. Diminazene binds to trypanosomal kDNA. This binding does not occur by intercalation but via specific interaction with sites rich in adenine-thymine (A-T) base pairs. Diminazene specifically inhibits mitochondrial type II topoisomerase in viable trypanosomes. Thus, inhibition of DNA replication may also occur via this interaction. Diminazene is extensively distributed in the body of treated animals. Residues of the compound may persist for several weeks, principally in the liver and kidneys, and also, to a lesser extent, in the gastrointestinal tract, lungs, muscle, brain and fat.

Sumanirole is a novel dopamine agonist with high affinity and efficacy at D2 dopamine receptors and has a substantial degree of selectivity for the D2 receptor over other dopamine receptor subtypes. It had been in clinical trials for the treatment of Parkinson’s disease and restless leg syndrome but these studies were terminated for the efficacy reason.

DAPTA (D-ala-peptide T-amide) is a synthetic peptide that prevents HIV entry by blocking binding of HIV gp120 protein with CCR5 receptor. In a small clinical study of internasal formulation of DAPTA in long-term infected HIV patients, administration of DAPTA led to decrease in the amount of virus isolated from white blood cells, an increase in gamma-interferon secreting T-cells in the absense of drug-related toxicity. In another clinical study DAPTA in combination with antiretroviral therapy reduced the peripheral (plasma and serum) viral load, but did not reduce the CSF viral load.

The carotenoids lutein (L), zeaxanthin (Z), and meso-zeaxanthin (MZ) accumulate in the central retina, where they are collectively known as macular pigment (MP). Each of these three compounds exhibit a regional dominance, with MZ, Z, and L being the dominant carotenoids at the epicenter, mid-periphery, and periphery of the macula, respectively. Meso-zeaxanthin is formed directly in the retina from lutein. MZ has potent anti-inflammatory effect, which can be due to its down-regulated expression of various inflammatory mediator genes. Meso-zeaxanthin was also found to scavenge superoxide radicals, hydroxyl radicals. MZ is a part of formulation for MacuShield, which is now the UK’s most recommended eye supplement. Also exists experiments supporting that LMZ3 (meso-zeaxanthin, lutein, zeaxanthin) supplements may stabilize vision and improve the cavitation’s in patients with macular telangiectasia type 2.

18F-THK-5351 is a novel radiotracer that demonstrates high binding selectivity and affinity for tau pathology and exhibits better pharmacokinetics in the living brain than previous THK tau probes. FluoroTau is in phase II clinical trials as a positron emission tomography (PET) imaging agent for the diagnosis and monitoring of the progression of Alzheimer's disease(AD) in South Korea. This compound was originally discovered by Tohoku University, and now is being developed by GE Healthcare, Samung Medical Centre and Asan Medical Center.

THK-5351 is a novel tau-binding quinoline derivative used as precursors of 18F-labeled radiotracer THK-5351 F-18.