Benzylpenilloic acid is a metabolite of benzylpenicillin. It is produced by hydrolysis of when beta-lactam ring of benzylpenicillin. Along with some other metabolites of penicillin, benzylpenilloic acid is responsible for the allergic reaction to beta-lactam antibiotic. It is a component of a minor determinant mixture (MDM) reagent which is used to evaluate sensitivity to penicillin in the clinic.

THYMIDINE 5'-MONOPHOSPHATE (or thymidine monophosphate, or TMP), a substrate of thymidylate kinase, transforms into the thymidine diphosphate that is essential in both the de novo and salvage pathways of DNA synthesis of the thymidine triphosphate. In mammalian cells, thymidine deprivation induces chromosome aberrations such as chromatid breaks, chromatid interchanges, and chromosome fragmentation.

Deoxycitidine 5'-monophosphate (dCMP) is a deoxynucleotide. It is one of the four monomers that make up DNA. In a DNA double helix, dCMP pairs with deoxyguanosine monophosphate.

Plevitrexed is an orally bioavailable, small molecule, non-polyglutamatable, antifolate quinazoline derivative thymidine synthetase inhibitor with potential antineoplastic activity. This compound belongs to the class of organic compounds known as hippuric acids, which consist of a benzoyl group linked to the N-terminal of a glycine. Plevitrexed is transported into the cell via the physiological reduced folate carrier (RFC) system. Intracellularly, this agent selectively binds to the folate binding site of thymidylate synthase and inhibits thymidine synthesis, which may result in DNA synthesis inhibition and apoptosis. Plevitrexed has been investigated for use/treatment in pancreatic cancer, solid tumors, gastric cancer, lung cancer, and colorectal cancer.

Ribavirin elaidate (CP-4033; TRX-201), a Lipid Vector Technology derivative of ribavirin. It inhibits elongation factor F4E (elF4E), which stimulates cell growth. Translational Therapeutics Inc. received orphan drug status from the U.S. Food and Drug Administration (FDA) in 2011 for ribavirin elaidate in the treatment of aggressive follicular, medullary and anaplastic thyroid carcinoma.

Florilglutamic acid enters cells through a transport system known as xC- (cystine/glutamate antiporter) which is more abundant in cancer tissue. Florilglutamic acid (18F) is a radioactive compound for use with an imaging method known as positron emission tomography (PET). When injected into the patient, florilglutamic acid (18F) is more effectively taken up by the cancer cells in the liver from where it is expected to emit radiation that can be detected in a PET scan, thereby allowing the cancer to be diagnosed. Orphan designation (EU/3/16/1632) was granted by the European Commission to Piramal Imaging GmbH, Germany, for florilglutamic acid (18F) for the diagnosis of hepatocellular carcinoma.

Bromopyruvate is an halogenated analogue of pyruvic acid known as an alkylating agent reacting with thiol groups of many proteins. Bromopyruvate exerts anticancer action. It is based on the impairment of energy metabolism of tumor cells by inhibiting enzymes in the glycolysis pathway (hexokinase II, glyceraldehyde 3-phosphate dehydrogenase, phosphoglycerate kinase) and the oxidative phosphorylation (succinate dehydrogenase). Bromopyruvate induces endoplasmic reticulum stress, inhibits global protein synthesis further contributing to cancer cell death. Treatment with bromopyruvate has been administered in several cancer type models both in vitro and in vivo, either alone or in combination with other anticancer therapeutic approaches. These studies clearly demonstrate bromopyruvate broad action against multiple cancer types. This compound has also antifungal and antiparasitic activity.

3,3',5,5'-Tetraiodothyroacetic acid (Tetrac) is a deaminated analog of L-thyroxine (T4) that blocks the proangiogenesis actions of T4 and 3, 5, 3’-triiodo-L-thyronine as well as other growth factors at the cell surface receptor for thyroid hormone on integrin αvβ3. 3,3',5,5'-Tetraiodothyroacetic acid blocks the transcriptional activities directed by L-thyroxine (T4) and 3,5,3’-triiodo-L-thyronine (T3) at αvβ3, but, independently of T4 and T3, 3,3',5,5'-Tetraiodothyroacetic acid modulates transcription of cancer cell genes that are important to cell survival pathways, control of the cell cycle, angiogenesis (VEGFA, FGF), apoptosis, cell export of chemotherapeutic agents, and repair of double-strand DNA breaks. 3,3',5,5'-Tetraiodothyroacetic acid was found to perturb the angiogenesis process stimulated by VEGF (Vascular Endothelial Growth Factor) or FGF (Fibroblast Growth Factor) without influencing the preexisting blood vessels.