The three major isoflavones present in kudzu extracts, daidzin, daidzein and puerarin are responsible for the beneficial effects in reduction of alcohol consumption. It has been discovered, that daidzin was a strong, selective and reversible inhibitor of mitochondrial aldehyde dehydrogenase. Daidzin did not inhibit human class I, II, or III alcohol dehydrogenases. However further studies for daidzin’s treatment in alcohol addiction were discontinued.

Ferroheme is formed when iron is inserted into protoporphyrin IX. The active center of hemoglobin and myoglobin consists of iron Ferroheme complex bound through a single, “proximal”, axial histidine (His) to the protein It is an iron containing cofactor that is involved with a wide range of cellular functions including oxygen transport. The antimalarial activity of a number of artemisinin derivatives, both newly synthesized and currently used as drugs, against Plasmodium falciparum in culture shows a correlation with their affinity of binding with Ferroheme.

Relenopride (YKP-10811) is a serotonin 4 (5-HT4) receptor agonist that was developed for regulation of gastric motility. It improved antral contractions and accelerated gastric emptying in dogs and had no adverse effects. Phase II clinical trials have investigated the efficacy and safety of relenopride in patients with (chronic and functional) constipation and irritable bowel syndrome (IBD). Relenopride was reported to accelerate gastrointestinal motility and colonic transit and improve bowel functions in patients with functional constipation, compared with placebo.

Safotibant (previously known as LF22-0542) was developed as an antagonist at bradykinin B1 receptor for the topical treatment of diabetic macular edema. This drug participated in phase II clinical trials in Australia, in Belgium and in the Czech Republic. However, further, development was discontinued.

Pevonedistat (MLN4924), discovered by Millennium, is a small molecule inhibitor of the NEDD8-Activating Enzyme (NAE), a key component of the protein homeostasis pathway. MLN4924 is a mechanism-based inhibitor of NAE and creates a covalent NEDD8-MLN4924 adduct catalyzed by the enzyme. The NEDD8-MLN4924 adduct resembles NEDD8 adenylate, the first intermediate in the NAE reaction cycle, but cannot be further utilized in subsequent intraenzyme reactions. The stability of the NEDD8-MLN4924 adduct within the NAE active site blocks enzyme activity, thereby accounting for the potent inhibition of the NEDD8 pathway by MLN4924. This drug is in phase II clinical trial for the treatment acute myeloid leukemia, chronic myelomonocytic leukemia and myelodysplastic syndromes. In addition in phase I for treatment acute lymphoblastic leukemia. The ability of MLN4924 to cross the blood-brain barrier, its low toxicity, and clinical efficacy in other cancers suggests that this drug is an attractive treatment against glioblastomas.

Pictilisib is an oral potent inhibitor of class I PI3K with nanomolar activities against p110alpha, p110beta, p110delta, and p110gamma. The drug was developed for the treatment of solid tumors and reached phase II in patients with breast cancer and lung carcinoma, however its development was terminated.

FG 2216 is an erythropoietic small molecule prolyl hydroxylase inhibitor, originally developed by FibroGen, that is undergoing development for the treatment of anemia. PDH inhibitor FG-2216 was orally bioavailable and induced significant and reversible EPO induction in vivo. Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry. FG 2216 had been in phase II clinical trials for the treatment of anemia, however, all researchers on this drug candidate were discontinued.