Abstract
Cancer is one of the leading causes of death worldwide. In cancer therapy, anti-cancer drugs are the current treatment-of-choice for patients with metastatic cancers, but these drugs present a major drawback: they destroy healthy cells along with cancerous cells. Unfortunately, the drug discovery process for de novo drugs is costly and time-consuming. To address this global problem, our research team has established the concept of "Chemotherapy with a molecular rational basis", which focuses on the identification of molecular targets in tumor cells, whose activation or inhibition induces apoptosis or sensitizes the tumor cells to apoptosis. Here we review the experimental and clinical evidence of pentoxifylline (PTX) in the setting of chemotherapy with a molecular rational basis. A search of the literature was conducted for articles published during the period from 2 January 2003 to 21 October 2024. Articles published in English or Spanish were included. The keywords "Pentoxifylline" OR "BL 191" OR "trental" AND "cancer" were used for in vitro, in vivo, and clinical studies. PTX is an approved, accessible, and relatively safe drug. Furthermore there is a large body of experimental and clinical evidence of the beneficial effects of PTX in cancer therapy, either alone or in combination with antitumor drugs, sometimes even more effective than traditional chemotherapy regimens. However, it is necessary to carry out larger clinical trials in cancer patients to identify the benefits, adverse effects and even pharmacological interactions of PTX with current chemotherapy regimens and thus achieve a new drug repositioning that benefits our patients.