Vorasidenib (also known as AG 881) was developed as an isocitrate dehydrogenase (IDH) type 1 in the cytoplasm and type 2 in the mitochondria, with potential antineoplastic activity. It is known that IDH is an essential enzyme for cellular respiration in the tricarboxylic acid (TCA) cycle. Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes that catalyze the conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. Vorasidenib participated in phase I clinical trials in patients with advanced hematologic malignancies and in gliomas.

Ioversol is an organoiodine compound that used as a contrast medium. It features both a high iodine content, as well as several hydrophilic groups. It is indicated in adults for peripheral and coronary arteriography and left ventriculography, for excretory urography and computed tomography. Injections of contrast media are often associated with sensations of warmth and pain. Renal toxicity has been reported in a few patients with liver dysfunction who were given oral cholecystographic agents followed by intravascular contrast agents.

Iohexol is a nonionic, water-soluble radiographic contrast medium. Organic iodine compounds block x-rays as they pass through the body, thereby allowing body structures containing iodine to be delineated in contrast to those structures that do not contain iodine. It is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Drugs which lower seizure threshold, especially phenothiazine derivatives including those used for their antihistaminic or antinauseant properties, are not recommended for use with Iohexol. Others include monoamine oxidase (MAO) inhibitors, tricyclic antidepressants, CNS stimulants, psychoactive drugs described as analeptics, major tranquilizers, or antipsychotic drugs. The most frequently reported adverse reactions are headache, mild to moderate pain including backache, neckache and stiffness, nausea, and vomiting.

Iopamidol is a nonionic, low-osmolar iodinated contrast agent. Iopamidol is indicated for angiography, pediatric angiocardiography, selective visceral arteriography and aortography, peripheral venography, and adult and pediatric intravenous excretory urography and intravenous adult and pediatric contrast enhancement of computed tomographic. Renal toxicity has been reported in a few patients with liver dysfunction who were given oral cholecystographic agents followed by intravascular contrast agents. Intravascular injection of contrast media is frequently associated with the sensation of warmth and pain especially in peripheral arteriography and venography. In angiocardiography the adverse reactions are: hot flashes, angina pectoris, flushing, bradycardia, hypotension, hives.

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.

Temperocol is an investigative anti-cancer drug that inhibits the expression of survivin and CDK-1; discovered at Johns Hopkins University and under development by Erimos Pharmaceuticals. It has been tested in phase I/II clinical trials for Leukemia, and several forms of neoplasms including gliomas. Results of these clinical trials have shown promise, however treatment regimes produce several toxic side effects that need to be balanced against efficacy. Temperocol is a fully methylated derivative of the natural product Nordihydroguaiaretic acid.

An orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. Milciclib is currently in phase II clinical trials for thymic carcinoma, glioma and liver cancer. The most common adverse events are nausea and asthenia, vomiting, myasthenic syndrome, dehydration, hypophosphatemia, cytolytic hepatitis and plantar fasciitis.

DMH1 is a potent and selective inhibitor of BMP signaling. DMH1 is a direct inhibitor of ALK2 BMP type-I receptor ALK2 (activin receptor like kinase-2). DMH1 potently inhibits neoplastic phenotype in cancer cells.

KU-60019 is a selective ATM kinase inhibitor. ATM is an ataxia telangiectasia (A-T) mutated, which plays a critical role in cell cycle checkpoints and DNA repair. Thus, specific small molecule inhibitors targeting ATM could perhaps be developed into efficient radiosensitizers. KU-60019 was a highly effective radiosensitizer of human glioma cells. A-T fibroblasts were not radiosensitized by KU-60019 and were suggested that the ATM kinase was specifically targeted. In xenograft models was shown, that the combination of KU-60019 and radiation significantly increased survival of mice than KU-60019 alone, radiation alone, or no treatment. In addition, p53-mutant gliomas were much more sensitive to KU-60019 radiosensitization than wild-type glioma.

BAY-36-7620 is a potent and selective antagonist at mGlu1receptors and inhibits >60% of mGlu1a receptor constitutive activity (IC50 = 0.38 uM). BAY-36-7620 is thus the first described mGlu1 receptor inverse agonist. It impairs classical conditioning and associated synaptic plasticity in hippocampal neurons. BAY-36-7620 exhibits neuroprotective and anticonvulsive effects in vivo following systemic administration.