METHYLENETETRAHYDROFOLIC ACID, L-(+), an endogenous biomodulator that was developed under the brand name modufolin or arfolitixorin by the Isofol Medical. Arfolitixorin is developed to increase the efficacy of standard of care chemotherapy for advanced colorectal cancer. This drug is currently being studied in a global phase 3 clinical trial. Besides, the drug successfully completed phase II as rescue therapy for osteosarcoma. 21 May 2019 Isofol Medical has received clinical patent protection for the arfolitixorinin USA. It relates to a method of increasing blood concentration of deoxyuridine, a blood biomarker for inhibition of tumor growth in human cancer treatment.

SAMARIUM SM-153 is a β- and γ-emitter with a physical half-life around 46.8 hours. Sm-153 treatment is recommended for patients with multiple bone metastases with the osteoblastic component, regardless of the primary tumor’s location. This compound was used in prostate cancer. It was shown that the small influence of Sm-153 on hematological parameters in patients treated with Sm-153, because of the high affinity of Sm-153 to osteoblastic metastases, and of the effect of low concentration of radionuclide in healthy bone tissue.

Reparixin is a CXC chemokine receptor type 1 (CXCR1) and type 2 (CXCR2) inhibitor. This compound has potential antineoplastic activity. It can be administered orally, binds to CXCR1 (overexpressed on cancer stem cells) and prevents its activation by its ligand interleukin 8. This might result in the death of cancer cells and inhibition of cell progression and metastasis. Reparixin also inhibits CXCR2 activation, possibly reducing both neutrophil recruitment and vascular permeability during inflammation or injury. A phase II clinical trial evaluating the effects of orally administered reparixin on cancer stem cells in the primary tumor and the tumoral microenvironment in an early breast cancer population was terminated. Reparixin has also been suggested as a novel potential therapeutic strategy for aggressive forms of thyroid cancer, based on results of a xenotransplantation study in mice.

Litoxetine is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and mixed serotonin agonist-antagonist, which makes it particularly appropriate for treating continence dysfunctions. Litoxetine at concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxations in the rat isolated oesophageal muscularis mucosae, which reduced carbachol tone up to 37%. Higher litoxetine concentrations (3 microM-300 microM) were associated with marked relaxation up to the abolition of carbachol tone. The antimuscarinic activity of litoxetine, previously demonstrated in the isolated guinea-pig intestine, played a role in the rat isolated oesophageal muscularis mucosae at concentrations greater than 1 microM. The 5-HT-releasing action of litoxetine could account for the potentation by litoxetine of 5-HT-induced relaxation in tissues from untreated rats, which was reversed by pCPA treatment. Litoxetine is in phase II clinical trial for the treatment of urinary incontinence.