Exaprolol is a non-selective antagonist at beta-adrenoceptors exerting antiarrhythmic and local anesthetic activity. It inhibits the inotropic and chronotropic responses. Exaprolol liberates histamine from isolated mast cells and decreases the uptake of extracellular histamine. It acts on mast cells due to the direct and indirect ion exchange mechanism resulted in disproportion between histamine and granule liberation.

Vebufloxacin (OPC-7241) is a nalidixic acid analog. It exhibited potent antibacterial activity against gram-positive and -negative bacteria, including Staphylococcus aureus and Pseudomonas aeruginosa.

Mivebresib (ABBV-075) is a small molecule Bromodomain and Extra-Terminal motif (BET) inhibitor being studied in a Phase 1 clinical trial in patients with advanced hematologic malignancies and solid tumors. Mivebresib binds to BRD4 with a Ki of 1.5 nM. Comprehensive preclinical characterization of ABBV-075 demonstrated broad activity across cell lines and tumor models, representing a variety of hematologic malignancies and solid tumor indications. In most cancer cell lines derived from solid tumors, ABBV-075 triggers prominent G1 cell-cycle arrest without extensive apoptosis. Consistent with its broad spectrum of activities in vitro, ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia.

Nocodazole is an anti-mitotic drug that has long been used as an experimental tool in cell biology. Nocodazole is known to bind with high affinity to tubulin and to inhibit microtubule assembly. The tubulin molecule is a α/β heterodimer; both α and β exist as various isotypes whose distribution and drug-binding properties are significantly different. Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII. In addition, nocodazole was investigated as an anticancer drug on xenografts model and it was revealed, that nocodazole possessed a high-affinity for the cancer-related kinases ABL, c-KIT, BRAF, and MEK, and inhibited Abl, Abl(E255K) and Abl(T315I).

Diproleandomycin is a semisynthetic antibacterial agent. This antibiotic produced by Streptomyces antibiotocus.

Atilmotin (also known as BAX-ACC-1638), a motilin receptor agonist, is short acting, with t1/2 less than 10 min. It was shown that at doses of 6, 30 or 60 mg intravenously, it affected esophageal, lower esophageal sphincter (LES), and gastric motility. LES and gastric pressures were increased, whereas there was disruption of esophageal peristalsis characterized by lower amplitude and failed contractions. The drug can have the clinical implementation for stomach motility disorders but is needed further study.

Encyprate (MO-1255) is a unique drug in being inactive as an MAO inhibitor in vitro but very active in vivo. It most probably is converted by the body to ethyl-N-benzyl-N-cyclopropylcarbamate which is an active MAOI in vitro. I was studying in the treatment of depression.

Tasuldine is as an orally active bronchosecretolytic agent that was clinically effective in human. However, information about the further development and use of this drug is not available.

Tisocalcitate is the vitamin D derivative. Tisocalcitate ointment is currently in phase 2 clinical development for mild to moderate psoriasis. Early studies have shown that, unlike other vitamin D3 analogues, tisocalcitate does not affect calcium metabolism. Tisocalcitate ointments were tolerated well and were safe to use on healthy skin. Tisocalcitate had been in phase II clinical trial for the treatment of psoriasis. However, this development was discontinued.

Pelitrexol (also known as AG2037) was developed by Pfizer as a glycinamide ribonucleotide formyltransferase inhibitor. This drug was studied in phase II clinical trials in patients with metastatic non-small cell lung cancer and in patients with metastatic colorectal cancer who failed treatment. In addition, the drug participated in a phase I clinical trial in treating patients who have advanced, metastatic, or recurrent solid tumors. Information about the further development of pelitrexol is not available.