11C-JHU75528 (also known as 11C-OMAR) is a radiotracer with suitable imaging properties for quantification of cannabinoid receptor, CB1R in the human brain. 11C-JHU75528 is participating in an ongoing phase I clinical trial to examine whether the use of cannabis alters CB1R availability in females and if the severity of cannabis withdrawal is correlated with CB1 receptor availability.

Lisavanbulin, also known as BAL-101553, a prodrug of the molecule BAL-27862 with potential antitumor activity. BAL-27862 binds to tubulin, prevents tubulin polymerization, destabilizes microtubules, arrests tumor cell proliferation, and induces cell death in cancer cells. Lisavanbulin participated in phase II clinical trials for the treatment of advanced solid tumors. Besides, the drug participates in a 1/2a clinical study in patients with recurrent glioblastoma and in patients with platinum-resistant or refractory ovarian cancer. In this study, will be characterized the safety and tolerability and to obtain efficacy data in these selected cancer types.

Bristol-Myers Squibb developed BMS-919373, a selective IKur inhibitor for use in atrial fibrillation, acute coronary syndromes, and paroxysmal atrial fibrillation. IKur is a repolarizing K+ current encoded by the KCNA5 gene and is expressed predominantly in the atrium of human. IKur is a potential atrial-selective target for the treatment of atrial fibrillation. BMS-919373 participated in phase II clinical trials to evaluate the effect on atrial fibrillation burden in patients with paroxysmal atrial fibrillation. In addition, in phase I clinical trials for patients with acute coronary syndromes. However, further, developments have been discontinued.

KX-02 is a compound demonstrating dual inhibitory activity against Src kinase and tubulin polymerization. It readily crosses the blood-brain-barrier in mice. It is under development for the treatment of solid tumors.

HCI-2084 (wider known as TP-0903) is developing by Tolero Pharmaceuticals for the treatment of different cancers. HCI-2084 is a small molecule AXL receptor tyrosine kinase (RTK) inhibitor. AXL is involved in maintaining a mesenchymal phenotype in cancer cells that enhanced cell survival in stressed environments, and increased resistance to targeted therapies compared to epithelial cells. AXL overexpression has been observed in multiple tumor types that have acquired resistance to various agents. TP-0903 is participating in phase I/II clinical trial in patients with previously treated chronic lymphocytic leukemia (CLL). This study will investigate the safety, pharmacokinetics, pharmacodynamics, and clinical activity of TP-0903. Besides, phase I is currently being conducted in patients with advanced solid tumors in the presence of TP-0903. In addition, TP-0903 was investigated in neuroblastoma (NB) cells, where this drug makes NB cells more vulnerable to the conventional chemotherapeutics.

Russian Pharmaceutical Technologies is developing alofanib, a first in class, allosteric inhibitor of fibroblast growth factor receptor type 2 (FGFR2) for the treatment of tumours expressing FGFR2, including ovarian cancer, colorectal cancer and lung cancer. Alofanib is a potential allosteric inhibitor of FGFR2 used in oncology. Alofanib has potent effects on ovarian cancer growth in preclinical studies.The inhibitor blocks the extracellular part of the receptor and prevents its binding with the ligand. Alofanib suppressed proliferation of endothelial cells, their migration activity, and ability to form vessellike structures in vitro and significantly decreased the number of microvessels in Matrigel implant and in ovarian cancer (SKOV-3) xenograft in vivo. The results indicate that Alofanib can inhibit angiogenesis.