Fluoroacetic acid F-18 (18F-Fluoroacetate,18F-FAC) is an analog of acetate with a longer radioactive half-life (18F=110 min). Fluoroacetic acid F-18 was under investigation as a PET imaging agent. 18F-FAC was considered a promising alternative to 11C-ACE for positron tomographic imaging of prostate cancer, and possibly of other neoplasms with relatively low glucose use.

The labeled 4-IODOPHENYLALANINE I-131 is used for proteomics research. It’s also can be used for the chemoselective modification of proteins.

Diazepinomicin is a structurally novel farnesylated dibenzodiazepinone discovered through DECIPHER technology, Thallion's proprietary drug discovery platform. A small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. Diazepinomicin binds to and inhibits Ras kinase, thereby preventing the phosphorylation and activation of proteins downstream of the Ras signal transduction pathway, including serine/threonine kinase RAF (BRAF) and extracellular signal-regulated kinases 1 and 2 (ERK1 and ERK-2). This agent also selectively binds to the peripheral benzodiazepine receptor (PBR), a receptor highly expressed in certain tumor cell types, inducing cell cycle arrest and apoptosis in PBR-expressing cells. The compound was shown to have a broad cytotoxic activity in the low micromolar range, when tested in the NCI 60 cell line panel. Diazepinomicin can cross the blood-brain barrier. Diazepinomicin is in phase II clinical trials for the treatment of Telomeric 22q13 Monosomy Syndrome and phase I for the treatment of Fragile X syndrome.

2,2-DIMETHYLBUTYRIC ACID (HQK-1001) is an orally administered SCFAD (Short Chain Fatty Acid Derivative), which has shown an excellent safety profile and biologic effects on fetal hemoglobin induction and red blood cell production in the laboratory, relevant animal models, and in clinical trials carried out in healthy human subjects as well as patients with sickle cell disease and beta thalassemia. The compound has received Orphan Drug Designation in the United States and Europe for both sickle cell disease and beta thalassemia. HemaQuest Pharmaceuticals was developing HQK-1001 for the oral treatment of sickle cell anaemia and beta thalassaemia. HQK-1001 has been evaluated in phase II trials for beta thalassaemia and sickle cell anaemia.

Apitolisib, a dual inhibitor of mTOR and phosphatidylinositol 3-kinase (PI3K), was being developed by Roche and Genentech as an orally administered therapy of cancer. Apitolisib is a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase (PI3K) and mTOR kinase (TORC1/2) with excellent pharmacokinetic and pharmaceutical properties. Apitolisib displayed excellent potency against class I PI3K isoforms (IC50 PI3K-α, β, δ and γ = 4.8, 27, 6.7 and 14 nM) and mTOR kinase (IC50 = 17 nM) and selectivity against a large panel of other kinases. Apitolisib is in phase II trials by Genentech for the treatment of breast cancer, prostate cancer, endometrium cancer, kidney cancer. However, no recent development has been reported. It is also in phase I trials by Genentech for the treatment of non-Hodgkin's lymphoma.

FERMAGATE is a phosphate binder with phosphate plasma levels lowering activity. It is in Phase 3 development in the US and in Europe for the treatment of hyperphosphatemia in dialysis patients. It is made up of magnesium and ferric iron atoms held in an insoluble, rigid, crystalline-layered structure, with carbonate groups lying between the layers. Upon oral administration, the carbonate ions in FERMAGATE are exchanged for free phosphate ions released from food in the gastrointestinal tract; thereby, strongly binding phosphate. This inhibits phosphate uptake and preventing hyperphosphatemia.