SGX523 is a selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase. SGX523 was able to inhibit HGF-induced cell migration and cell scatter. SGX523 inhibition of MET in vivo was associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma and lung and gastric cancers. The clinical development of SGX523, however, was discontinued at Phase I due to renal toxicity manifested by an early rise of serum blood urea nitrogen and creatinine.

MK-6186 is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) which displays subnanomolar potency against wild-type (WT) HIV virus and the two most prevalent NNRTI-resistant RT mutants (K103N and Y181C) in biochemical assays. In addition, it showed excellent antiviral potency against K103N and Y181C mutant viruses. In 2010 MK-6186 was studied in phase I clinical trials but no further development reports were published.

Fevipiprant is a selective reversible antagonist of the prostaglandin D2 receptor (also known as CRTH2). It is currently in development for the treatment of allergic diseases.

MK-8033 is a dual c-Met/Ron inhibitor, which is under investigation by Merck for the treatment of cancer.

Relamorelin (also known as BIM28131 or RM-131) is a synthetic, selective, prokinetic ghrelin analog that was developed for treatment of gastrointestinal motility disorders (such as chronic constipation and diabetic gastroparesis). Relamorelin was shown to relief symptoms such as nausea, fullness, bloating and abdominal pain. It is safe and well-tolerated in healthy individuals, and has no neurological or cardiovascular adverse effects, making this a promising drug with an advantage over other available therapies. A phase III clinical trial comparing the efficacy of relamorelin with that of placebo in participants with diabetic gastroparesis (DG) was still ongoing in 2019.

FLORTAUCIPIR is a gamma-carboline derivative. Its 18F radiolabelled form is a highly selective positron emission tomography (PET) tracer targeting paired helical filament (PHF)-tau in the brain. This tracer is studying for clinical assessment in patients with various tauopathies, including Alzheimer's disease.

The sesquiterpene lactone thapsigargin is found in the plant Thapsia garganica L., and is one of the major constituents of the roots and fruits of this Mediterranean species. In 1978, the first pharmacological effects of thapsigargin were established and the full structure was elucidated in 1985. Thapsigargin is a potent inhibitor of Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) and is widely used to study Ca2+-signaling. Thapsigargin is a non-cell-type specific toxin with documented ability to kill a broad spectrum of cancer cell lines as well as normal endothelial cells, fibroblasts and osteoblasts. It induces a rapid and pronounced increase in the concentration of cytosolic calcium, due to blockade of the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA) pump to which it binds with high affinity. The increase in cytosolic calcium leads to induction of apoptosis and ensuing cell death. A prodrug, G-202 (mipsagargin) has been designed to target the blood vessels of cancer cells; the death of these blood vessels then leads to tumor necrosis. G-202 consists of a cytotoxic analog of thapsigargin coupled to a masking peptide which inhibits its biologic activity until proteolytic cleavage at the tumor site. The first clinical trials of this drug were initiated in 2008 for the treatment Advanced Solid Tumors.

The receptor tyrosine kinase c-Met is an attractive target for therapeutic blockade in cancer. MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met, was synthesized by Merck and was investigated in phase I of clinical trial for the potential treatment of patients with advanced solid tumors.

VLX600 - is a lipophilic cation-based triazinoindolyl-hydrazone compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. VLX600 is designed to increase the efficacy of radiotherapy and to kill cancer cells that survive traditional chemotherapy. VLX 600 is a small molecule that inhibits deubiquitinating enzymes USP14 (a ubiquitin thiolesterase) and UCHL5 (a carboxypeptidase). Upon infusion, in normal cells and proliferating tumor cells where glucose is readily available, inhibition of OxPhos by VLX600 induces a hypoxia-inducible factor 1-alpha (HIF-1alpha)-dependent shift to, and an increase in glycolysis. Glycolysis alone does not produce enough energy to support the growth of tumor cells in this environment, and the induction of autophagy occurs. In the metabolically compromised tumor microenvironment, the availability of oxygen and glucose is limited due to poor vascularization and perfusion of tumor micro-areas. Tumor cells growing in this environment are thus unable to compensate for decreased mitochondrial function by increasing glycolysis. This leads to nutrient depletion, decreased energy production, induction of autophagy, tumor cell death and an inhibition of cell proliferation in quiescent tumor cells. Mitochondrial OxPhos, which is hyperactivated in cancer cells, plays a key role in the promotion of cancer cell proliferation. VLX-600 is in phase I clinical trials for the treatment of solid tumours. This compound was originally jointly discovered and developed by Vivolux and Karolinska Institute.

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.