Pipratecol is substituted thienoimidazole. It is the H+/K(+)-ATPase inhibitor. In a high concentration of 10(-4) g/ml, pipratecol increased the amplitude of isolated guinea-pig atrial contractions while decreased the rate. But, in a low concentration of 10(-8) g/ml, the drug decrease the amplitude and increased the rate slightly. The effects of adrenaline and noradrenaline were suppressed by the preceding addition of pipratecol, while that of isoproterenol was scarcely. The effect of pipratecol on atrial contractions was hardly influenced by reserpine with which the animal had been pretreated 24 hours before the sacrifice of animal. The augmentative effect of nicotine on atrial contractions was slightly suppressed by the preceding addition of pipratecol. From these results, it was assumed that pipratecol has some affinity with the adrenergic receptor of atria. As a peripheral vasodilator it has been used in conjunction with raubasine in the treatment of cerebrovascular disorders. Pipratecol was used as antiulcerative agent also.

Volixibat (SHP626; formerly LUM002) is a potent inhibitor of the apical sodium-dependent bile acid transporter (ASBT) that was developed for the treatment of nonalcoholic steatohepatitis. Volixibat participated in phase II clinical trial to investigate its safety, effectiveness in adults with nonalcoholic steatohepatitis. However, this study was discontinued, without any further explanation for the possible causes. In addition, volixibat was studied in a clinical trial in healthy adults and in patients with type 2 diabetes mellitus, where was shown that the drug was generally well tolerated.

Ethylmethylthiambutene is a potent analgesic compatible with morphine. It possesses addiction liability similar to that of morphine.

HaiHe Biopharma (Shanghai HaiHe Pharmaceutical) is developing simmitecan, an ester pro-drug of chimmitecan for the treatment of cancer. Simmitecan is in phase I development for solid tumours and colorectal cancer in China. Simmitecan (L-P) is a water-soluble ester prodrug of chimmitecan (L-2-Z) with potent anti-tumor activities in different experimental animals. Chimmitecan，a novel CPT derivative, exhibited potent antitumor activities both in vitro and in vivo by inhibiting topoisomerase I.

Acridine carboxamide (XR5000) is a tricyclic acridine-based (or carboxamide-based) drug with dual topoisomerase inhibitor and potential antineoplastic activities. Acridine carboxamide inhibits both topoisomerases I and II and intercalates into DNA, resulting in DNA damage, the disruption of DNA repair and replication, the inhibition of RNA and protein synthesis, and cell death. Acridine carboxamide has been used in trials studying the treatment of lung cancer and brain and central nervous system tumors. In clinical trials acridine carboxamide did not show efficacy when tested against various types of cancers.

Axelopran (previously known as TD-1211), a peripherally selective, multivalent µ-opioid receptor antagonist that is under development by Theravance Biopharma. This drug participated in phase II clinical trials in subjects with opioid-induced constipation. The most common adverse events were abdominal pain, nausea, and diarrhea. There were no indications of opioid withdrawal effects or reductions in opioid analgesia in patients treated with axelopran.

Primidolol (also known as UK-11,443) is an imidazolidinone derivative patented by American pharmaceutical corporation Pfizer Corp as a specific β-adrenergic blocker. In clinical trials, Primidolol shows some antihypertensive activity but the overall change in the cardiovascular parameters failed to demonstrate a significant difference compared to placebo.