Chlorophyllin is a water soluble derivative of chlorophyll. It has chemopreventive properties and forms a non-covalent complex with many mutagenic/carcinogenic molecules. Chlorophyllin inhibits cancer initiation and progression by targeting multiple molecules and pathways involved in the metabolism of carcinogens, cell cycle progression, apoptosis evasion, invasion, and angiogenesis. The modulatory effects of Chlorophyllin to be mediated via abrogation of key oncogenic signal transduction pathways such as nuclear factor kappa B, Wnt/β-catenin, and phosphatidylinositol-3-kinase/Akt signaling. Chlorophyllin sodium copper salt mitigates radiation-induced hematopoietic syndrome by increasing the abundance of hematopoietic stem cells, enhancing granulopoiesis, and stimulating prosurvival pathways in bone marrow cells and lymphocytes. In addition, chlorophyllin exhibits antioxidant, antiapoptotic and immunostimulatory effects. Chlorophyllin is intended to improve the quality of life in people who have fecal incontinence due to spinal cord injury, bowel cancer, psychotic disorder, terminal illness, or other disorders. Chlorophyllin is also used by people who have had a colostomy or ileostomy

Betanin (betanidin-5-O-beta-glucoside, Beetroot Red) is a red glycosidic food dye obtained from beets. Betanin is the most common betacyanin in the plant kingdom. According to the regulation on food additives betanin is permitted quantum satis as a natural red food colorant (E162). Moreover, betanin is used as colorant in cosmetics and pharmaceuticals. Recently, potential health benefits of betalains and betalain-rich foods (e.g. red beet, Opuntia sp.) have been discussed. Betanin is a scavenger of reactive oxygen species and exhibits gene-regulatory activity partly via nuclear factor (erythroid-derived 2)-like 2-(Nrf2) dependent signaling pathways. Betanin may induce phase II enzymes and antioxidant defense mechanisms. Furthermore, betanin possibly prevents LDL oxidation and DNA damage. Potential blood pressure lowering effects of red beet seem to be mainly mediated by dietary nitrate rather than by betanin per se.

A-443654 is a potent and selective AKT inhibitor. A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition. A-443654 interferes with mitotic progression by regulating aurora a kinase expression. A-443654 inhibits all three Akt isoforms in FL5.12 cells stably transfected with constitutively active myristoylated Akt1/2/3, and showed moderate selectivity when screened against related kinases in the AGC family, such as PKA and PKC20. A-443654 has being shown to extend survival in an intracranial glioma animal model. A-443654, either alone or in combination with existing drugs, may be a useful therapy for primary and drug-resistant T-ALL.

Vipadenant (V2006) is a small molecule, adenosine A2A receptor antagonist that was being investigated in Parkinson's disease. Due to safety concerns development ceased in 2010 and the rights were regained from Biogen Idec in 2011 with no further investment made. In October 2014, RedoxTherapies licensed Vipadenant as it has the potential to disrupt an immunosuppressive mechanism of tumour protection, generating improved efficacy for immunotherapies of certain cancers when used in combination with other drugs.

Siramesine is a sigma2 opioid agonist under development by H Lundbeck as a potential treatment for anxiety. In March 1998, the compound was licensed to Forest Laboratories under a strategic alliance. In August 2000, siramesine entered phase II trials. Siramesine has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Siramesine involves lysosomal leakage and oxidative stress.

Lificiguat (YC-1) [3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole], a chemically synthetic benzylindazole compound, is a direct soluble guanylate cyclase activator. It possessed antiplatelet activity. YC-1 inhibits Hypoxia-inducible factor-1 (HIF-1). YC-1 demonstrated antineoplastic potential both in vitro and in vivo in animal models.

Brequinar is a synthetic quinolinecarboxylic acid analogue with antineoplastic properties. Brequinar inhibits the enzyme dihydroorotate dehydrogenase, thereby blocking de novo pyrimidine biosynthesis. This agent may also enhance the in vivo antitumor effect of antineoplastic agents such as 5-FU. Brequinar had been in phase II clinical trials by Bristol-Myers Squibb for the treatment of cancer and transplant rejection. However, this research has been discontinued. Brequinar had been also in preclinical studys for the treatment of cytomegalovirus infections. However, this research has been discontinued.

SITOGLUSIDE (Daucosterol) inhibits cancer cell proliferation by inducing autophagy through reactive oxygen species-dependent manner. It also perturbs cell cycle and induces apoptotic cell death in A549 cells. Daucosterol has being shown to promote the proliferation of neural stem cells. Daucosterol also protects neurons against oxygen-glucose deprivation/reperfusion-mediated injury by activating IGF1 signaling pathway. Daucosterol could be potentially developed as a medicine for ischemic stroke treatment.

Dexverapamil (R-verapamil) is an enantiomer of verapamil. R-isomer behaved as an inhibitor of multidrug-resistant protein MRP1 (involved in the cancer cell multidrug resistance phenotype). It was developed by Knoll (BASF Pharma) as a chemosensitiser and/or modulator of multidrug resistance for use in combination with cancer chemotherapy. Dexverapamil was undergoing phase II clinical studies in France, Italy, Spain, United Kingdom and the US in patients with various cancers. It was also undergoing phase I clinical trials in Japan where it was licensed to Mitsui and Mitsui Toatsu Chemicals. However, development was discontinued. Dexverapamil (R-verapamil) has been developing by AGI therapeutics for the treatment of Irritable bowel syndrome however development was discontinued.

Nocodazole is an anti-mitotic drug that has long been used as an experimental tool in cell biology. Nocodazole is known to bind with high affinity to tubulin and to inhibit microtubule assembly. The tubulin molecule is a α/β heterodimer; both α and β exist as various isotypes whose distribution and drug-binding properties are significantly different. Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII. In addition, nocodazole was investigated as an anticancer drug on xenografts model and it was revealed, that nocodazole possessed a high-affinity for the cancer-related kinases ABL, c-KIT, BRAF, and MEK, and inhibited Abl, Abl(E255K) and Abl(T315I).