RGB-286638 is a multi-targeted protein kinase inhibitor currently in Phase 1 clinical testing. In vitro cell-free kinase assays indicated that RGB-286638 inhibits CDK1, 2, 3, 4, 5, and 9 and is less active against CDK6 and 7. The RGB-286638 compound has been shown to inhibit the processes controlling cell division in cancer cells by targeting multiple cyclin-dependent kinase proteins involved in regulating the cell cycle. RGB-286638 has also been shown to induce apoptosis (programmed cell death) and to inhibit other important protein kinases involved in the proliferation of cancer cells. RGB-286638 treatment results in tumor regression and increased survival in a number of pre-clinical models of solid and hematological tumors.

Freselestat (ONO-6818) is reversible, nonpeptide high affinity and selective human neutrophil elastase inhibitor, which was under development by Ono for the potential treatment of inflammatory conditions, such as rheumatoid arthritis, inflammatory bowel disease and chronic obstructive pulmonary disease (COPD). Freselestat mediated neutrophil elastase inhibition, leads to the reduction of interleukin 8 production and the reduction of the complement membrane attack complex formation. Freselestat competitively inhibits neutrophil elastase in humans, rats, and hamsters, but does not inhibit other proteases such as pancreatic elastase, trypsin, proteinase 3, cathepsin G, or matrix metalloproteinases. Freselestat inhibits acute lung injury induced by neutrophil elastase in rats, minimizing lung hemorrhage, the accumulation of neutrophils in the lung and suppresses leukocyte levels in an in vivo model of COPD. Freselestat was in phase I studies for COPD in Japan and the US. However, due to abnormal variations in liver function, the development of Freselestat was terminated.

Silmitasertib (CX-4945) is a potent and selective orally bioavailable small molecule inhibitor of Casein kinase II (CK2). The antiproliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. CX-4945 caused cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells. When administered orally in murine xenograft models, CX-4945 was well tolerated and demonstrated robust antitumor activity. Senhwa Biosciences is developing silmitasertib for the treatment of cholangiocarcinoma, other solid tumours, Castleman's disease (giant lymph node hyperplasia) and multiple myeloma. The compound was originally developed by Cylene Pharmaceuticals. Phase Ib/II development is underway in the US and South Korea for the treatment of cholangiocarcinoma, and development in the remaining indications is at the phase I stage. As at July 2016, no recent reports of development had been identified for phase-I development in Giant-lymph-node-hyperplasia in USA (PO, Capsule), phase-I development in Multiple-myeloma in USA (PO, Capsule), phase-I development in Solid-tumours (Late-stage disease) in USA (PO, Capsule).

Tomeglovir (BAY 38-4766) is a human cytomegalovirus (CMV) terminase complex inhibitor. Treatment with BAY 38-4766 reduced both viremia and DNAemia, as determined by a real-time PCR assay, following guinea pig cytomegalovirus (GPCMV) infection of cyclophosphamide-immunosuppressed strain 2 guinea pigs. BAY 38-4766 also reduced mortality following lethal GPCMV challenge in immunosuppressed Hartley guinea pigs. a combination of BAY 38-4766 with anti-cytomegalovirus drug ganciclovir showed antagonism. Interaction of viral DNA processing inhibitor 2-bromo-5,6-dichloro-1beta-D-ribofuranosyl benzimidazole (BDCRB) with BAY 38-4766 showed a mixed pattern of synergy and antagonism. Tomeglovir had been in phase II clinical trials by Bayer for the treatment of CMV infection. However, this development was discontinued.

Arctigenin is a plant lignan extracted from Arctium lappa that has been shown to have estrogenic properties. In ER-positive MCF-7 cells, arctigenin efficiently inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cell migration and invasion. Arctigenin confers anti-metastatic effects by inhibiting MMP-9 and uPA via the Akt, NF-κB and MAPK signaling pathways on breast cancer, regardless of ER expression. Intake of arctigenin could be an effective supplement for breast cancer patients. Arctigenin is a phenylpropanoid dibenzylbutyrolactone lignan compound possessing antitumor, anti-inflammatory, anti-influenza, antioxidant, antibacterial, and hypoglycaemic activities. Arctigenin exhibited significant antiproliferative activity against CCRF-CEM cells after 72 h treatment with IC50 values of 1.21 ± 0.15 um. It arrested CCRF-CEM cells in the S phase. It induced apoptosis in CCRF-CEM cells in a concentration- and time-dependent manner. Arctigenin is a good candidate for the development of novel agents against T-cell lymphoma. Arctigenin has been found to act as an agonist of adiponectin receptor 1 (AdipoR1). Arctigenin is an antagonist of MR and effectively decreases the Na/K-ATPase 1 gene expression, thus highlighting its potential as an anti-hypertensive drug lead compound.

Tetrasul is a largely obsolete non-systemic pesticide that was used to control mites and small insects. It has been used in clinical trials studying the treatment of erythematous (type 1) rosacea.

Ilmofosine (1-hexadecylthio; 2-methoxyethyl-racglycero-3-phosphocholine) is a synthetic 1-S-thioether alkyl lysophospholipid derivative with potential antineoplastic activity. In extensive preclinical evaluation against tumor cell lines and in the human tumor colony-forming assay, Ilmofosine was cytotoxic against both leukemias and solid tumors. Ilmofosine was effective against many tumor types, including ovary, non-small cell lung, kidney, and melanoma. Ilmofosine exhibited competitive inhibition of protein kinase C activity with respect to phosphatidyl-serine and inhibited the enzyme activated by diolein.

Mocimycin (also known as kyrromycin) was isolated from Streptomyces ramocissimus and tested in vitro against wide range of bacterias. Although having showed good results, drug did not enter clinical trials. Mocimycin acts by binding tightly and specifically to bacterial EF-Tu. Upon administration the antibiotic prevents EF-Tu-GDP from leaving the ribosome and thus inhibits bacterial protein synthesis. Nowadays, the antibiotic is mainly used to study bacterial protein synthesis at the level of elongation factor EF-Tu-GDP release.