Simotaxel (MST-997) is a semi-synthetic, orally bioavailable, third-generation taxane derivative and microtubule-stabilizing agent, with potential antineoplastic activity. Simotaxel was being developed through a collaboration between Wyeth (later Pfizer) and Taxolog as a potential treatment for cancer. Upon administration, simotaxel binds to tubulin, promotes microtubule assembly and stabilization, and prevents microtubule depolymerization. This results in G2/M arrest, apoptosis and the inhibition of cell proliferation in susceptible tumor cells. This agent is a poor substrate for P-glycoprotein-related drug resistance mechanisms; therefore, it may be useful for treating multi-drug resistant tumors. MST-997 is more potent than paclitaxel and docetaxel and overcomes paclitaxel and docetaxel resistance in certain tumor cell types. Simotaxel is under investigation in clinical trial NCT00088647 (study evaluating MST-997 in advanced malignant solid tumors).

Phenampromide is an opioid analgesic, which is considered to be structurally similar to isomethadone. Phenampromide belongs to the ampromide family of drugs, which also include propiram and diampromide. According to the literature, (R)-phenampromide has greater analgesic potency than its (S)-enantiomer. Synthetic narcotic analgesic phenampromide is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.

Flavodic acid is a synthetic hydrosoluble derivative of natural flavonoids. It has been shown to reduce capiliary fragility and permeability. Sodium flavodate was marketed by the Italian pharmaceutical company Farmaceutici under tradename Pericel.

Etisulergine (CQ 32-084) is an ergoline derivative. Etisulergine stimulates both dopamine D1- and D2-receptors, antagonizes alpha-adrenergic and serotonin 5-HT2 receptors. Etisulergine demonstrated antiparkinsonian activity in patients.

Leucocianidol is a vasoprotector. It increases the resistance of vessels and decreases their permeability. Leucocianidol increases the tonicity of the veins. Leucocianidol is used in the management of capillary fragility, hemorrhoids, venolymphatic insufficiency. In combination with lidocaine and hydrocortisone, it is used in the symptomatic treatment of hemorrhoidal crisis. Leucocianidol inhibits 12-lipoxygenase.

Betaprodine is an opioid analgesic under international control according to the UN Single Convention 1961. It has been used in obstetrics, as pre-operative medication, for minor surgical procedures.

Homocysteine, an amino acid synthesized intracellularly by removal of the N-methyl group from the essential amino acid methionine. High plasma level of homocysteine is called hyperhomocysteinemia is a clinical biomarker for increased risk of cardiovascular disease, thromboembolic diseases, and myocardial infarction. It was shown, that hyperhomocysteinemia could be an independent risk factor for dementia and Alzheimer's disease. The falling of homocysteine concentrations in response to increasing B-group-vitamin status, have the hope that mental decline, or Alzheimer's disease, could be prevented by dietary modification or food fortification. Besides, homocysteine can behave as an anti-oxidant agent by increasing the antioxidant capacity of the tumor and endothelial cells.

Norleucine (L-norleucine) is a 2-aminohexanoic acid is an alpha-amino acid that is caproic acid substituted by an amino group at position 2. It derives from a hexanoic acid. It is used experimentally to study protein structure and function. Norleucine appears to inhibit bacterial growth due to incorporation into proteins in place of methionine, as the analogue inhibits methionine incorporation but does not significantly reduce its synthesis. L-norleucine had antiviral activity in thermophile. In vitro and in vivo assays revealed that L-norleucine significantly suppressed metastasis of gastric and breast cancer cells. L-norleucine interacted with hnRNPA2/B1 protein to inhibit the expressions of Twist1 and Snail, two inhibitors of E-cadherin, and promote the E-cadherin expression, leading to the inhibition of tumor metastasis.