Trimeperidine (promedol) is the earliest and mostly studied opioid analgesic. Trimeperidine stimulates opioid receptors in the central nervous system. Compared with morphine, it has a weaker and shorter analgesic effect, less affects the respiratory, vomiting and vagal centers, does not cause smooth muscle spasm (except for the myometrium), and has a moderate antispasmodic and hypnotic effect. It is used to treat severe pain syndrome, acute left ventricular failure, pulmonary edema, cardiogenic shock, preparation for surgery, childbirth, high fever, post-transfusion complications, poisoning with atropine, barbiturates, barium, gasoline, boric acid, strong acids, carbon monoxide, turpentine, formalin, formalin. It has several side effects. Administration of this substance is associated with the development of life-threatening conditions accompanied by the suppression of respiration center. Analgesic trimeperidine (promedol) was included into the health care kits by various Ministries of the Russian Federation at different times.

3'-C-ethynylcytidine (Ethynylcytidine, TAS-106) is a synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule. Development of a cytosine derivative of 3'-ethynyl ribonucleoside, TAS-106, as an intravenously administered treatment for solid tumours was discontinued. A phase II trial in patients with head and neck cancer was terminated in the US.

Cefuroxime Pivoxetil is an ester prodrug of cefuroxime, a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. Cefuroxime binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

TS-410 (Amelometasone), is a topical anti-inflammatory steroid. Amelometasone lotion - external steroid preparation - is marketed in Japan.

Dimepregnen is an antiestrogen agent.

UK-432097 is a selective adenosine A2a agonist which was in development with Pfizer as an inhaled treatment for asthma and chronic obstructive pulmonary disease. UK-432097 had been in phase II clinical trials by Pfizer for the treatment of chronic obstructive pulmonary disease (COPD). However, this study was terminated prematurely due to futility based on results of interim analysis.

Imitrodast is thianaphthene derivative and thromboxane A2 inhibitor patented by Japanese pharmaceutical company Sankyo Co as antithrombotic agent.

Norgesterone (norvinodrel, vinylestrenolone) is a progestin medication which was formerly used in birth control pills for women. The compound shows no androgenic and very little estrogenic activity; its progestational effect, as well as other properties, suggests its use as claudogenic agent. Norgesterone is an agonist of the progesterone receptor. It was used in combination with ethinylestradiol in birth control pills to prevent pregnancy.

Sonedenoson (MRE0094) is a topical adenosine A2A-receptor agonist which was under clinical development for the treatment of for diabetic foot ulcer. The compound was originally developed by New York University, and licensed to Medco Research (King Pharmaceuticals). King Pharmaceuticals was acquired by Pfizer in 2010. Sonedenoson has been in phase II clinical trials for the treatment of chronic diabetic neuropathic foot ulcers. However, this research has been discontinued.