TAT-59 (Miproxifene Phosphate) is a triphenylethylene analog of tamoxifen. TAT-59 is the phosphate ester prodrug of the practically insoluble parent drug DP-TAT-59. It is an antiestrogen developed in Japan for breast cancer. It is a potent antitumor agent for hormone-dependent tumors. Most of TAT-59 metabolites possessed remarkable binding affinity toward estrogenic receptors as well as fairly good antiuterotrophic activity.

Cytarabine ocfosfate (commercial name: Starasid) is a prodrug having stearyl group attached to phosphoric acid at 5' position of arabinose moiety of cytosine arabinoside (Ara-C). This drug is given orally. The mode of action is in the inhibition of DNA synthesis after conversion to Ara-CTP as in Ara-C. The drug is metabolized in the liver, producing the intermediate metabolite, C-C3PCA which is converted to Ara-C gradually. This property results in the maintenance of relatively long time the blood Ara-C levels. This was proved to be active clinically against acute leukemia and MDS.

Fluoroethylcholine ion F-18 is ethylcholine labeled with fluorine F 18, a positron-emitting isotope. Fluorine F18 fluoroethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, yielding a phosphoryl derivative, and finally is integrated into cellular phospholipids, probably primarily into a phosphatidyl derivative; concentration of this agent in tumor cells as various fluorine F 18 fluoroethylcholine derivatives enables tumor imaging using positron emission tomography (PET). Choline kinase, the enzyme responsible for the phosphorylation of choline, is frequently up-regulated in human tumor cell lines. F18-fluoroethylcholine is used for imaging of prostate cancer and brain tumors, mainly in Europe and Japan.

Pimasertib) (N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]isonicotinamide hydrochloride; AS703026), a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2. It binds to MEK1/2 in an allosteric site that is distinct from, yet in close proximity to, the ATP binding site. Binding to this allosteric site prevents the activation of MEK1/2. Pimasertib continues to be investigated in patients with NRAS mutant malignant melanoma in a Phase II trial. This drug was discontinued in a combination with SAR245409 for Phase II study in low-grade serous ovarian cancer. This decision was based on the results of a futility analysis, conducted by the IDMC, which indicated that the trial was no longer expected to achieve its objective of showing a meaningful difference between the efficacies of the combination compared with pimasertib alone. The further development of pimasertib in pancreatic cancer was also discontinued, as a Phase II study in this indication did not reach its primary endpoint of prolongation of progression-free survival

Myristamidopropyl dimethylamine [MAPD] is an amidoamine compound that shows activity against Acanthamoeba as well as a variety of other causal agents of microbial keratitis. MAPD, present in Opti-Free Express Multi-Purpose Disinfecting solution for contact lenses, has been shown to exhibit anti-acanthamoeba activity. Challenge test assays were used to study the efficacy of 50 mg/L MAPD against Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, Fusarium solani and Acanthamoeba polyphaga. MAPD gave a 3.7 log kill of P. aeruginosa after 60 min, 5.4 log for S. aureus by 45 min and 5 log for C. albicans and F. solani within 15 min. A. polyphaga cysts were reduced by 4 log within 120 min. MAPD also possesses excellent antifungal and antibacterial activity. MAPD may represent a broad-spectrum therapeutic antimicrobial for keratitis and surgical prophylaxis and deserves further evaluation in these roles. Myristamidopropyl dimethylamine uses and applications also include: surfactant; emulsifier for cosmetics and toiletries; conditioner; viscous builder; softener for textile finishes.

Ligustrazine (tetramethylpyrazine) is a bioactive ingredient extracted from the widely-used Chinese herb, Chuanxiong. It inhibits of platelet aggregation, enhances of vessel dilation, increases cerebral blood flow and possesses neuroprotective properties. The injection solution of ligustrazine has been used especially in China to treat ischemic stroke, coronary heart disease, diabetic nephropathy, and knee osteoarthritis. Ligustrazine was also evaluated in clinical as a remedy for pressure sores, as a salvage agent for patients with non-Hodgkin's lymphoma, as a treatment for bronchial asthma and vertebrobasilar insufficiency.

Rilmenidine (brand names Albarel, Hyperium, Iterium and Tenaxum) is an imidazoline derivative used for the treatment of hypertension. Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Rilmenidine shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists. Rilmenidine is as effective in monotherapy as all other first line classes of drugs, including diuretics, beta-blockers, angiotensin converting enzyme (ACE) inhibitors, and calcium antagonists. It is well tolerated and can be taken in combination for greater efficacy. Sedation and dry mouth are not prominent side effects and withdrawal hypertension is not seen when treatment is stopped abruptly. In addition to a reduction in blood pressure, Rilmenidine has been shown to improve glucose tolerance, lipid risk factors, and insulin sensitivity.

Antihistamine agent

Meldonium (3-(2,2,2-trimethylhydrazinium)propionate; MET-88; quaterine, trade-named as Mildronate) is an antiischemic drug developed at the Latvian Institute of Organic Synthesis. It is a clinically used in the treatment of heart failure, myocardial infarction, arrhythmia, atherosclerosis, and diabetes. Mechanism of action is based on the regulation of energy metabolism pathways through l-carnitine lowering effect. L-Carnitine biosynthesis enzyme γ-butyrobetaine hydroxylase and carnitine/organic cation transporter type 2 (OCTN2) are the main known drug targets of meldonium, and through inhibition of these activities, meldonium induces adaptive changes in the cellular energy homeostasis. Since L-carnitine is involved in the metabolism of fatty acids, the decline in its levels stimulates glucose metabolism and decreases concentrations of l-carnitine related metabolites, such as long-chain acylcarnitines and trimethylamine-N-oxide. Meldonium is used in neurological clinics for the treatment of brain circulation disorders. It appears to improve patients' mood; they become more active, their motor dysfunction decreases, and asthenia, dizziness, and nausea become less pronounced. CNS effects of Meldonium could be mediated by stimulation of the nitric oxide production in the vascular endothelium by modification of the gamma-butyrobetaine and its esters pools. It is hypothesized that mildronate may increase the formation of the gamma-butyrobetaine esters. Meldonium was on the World Anti-Doping Agency’s (WADA) list of drugs being monitored until September 2015, when it was added to the list of banned substances, effective January 1, 2016.

Dimemorfan is a nonnarcotic antitussive drug. The antitussive action of dimemorfan appears to be directly on the cough center in the medulla.