Vatalanib: Effects, Uses & Risks

Vatalanib is a compound that may be used in the future to treat certain cancers. Currently, the compound is still in development and has not been approved. The potential mechanism of action of vatalanib is based on the fact that it inhibits vascular endothelial growth factor (VEGF) receptors.

What is vatalanib?

Vatalanib is a substance that may be used in the future to treat certain cancers. Vatalanib is a pharmaceutical agent that may have applications in the treatment of cancer. Vatalanib has the molecular formula C20H15ClN4; medical researchers also use the code number PTK787/ZK 222584 as its designation. Vatalanib represents a derivative of pyridine and aminophthalazine and is one of the vascular endothelial growth factor inhibitors. To date, vatalanib has not been approved as a drug because it is still in development and there are insufficient studies. Although some findings support the notion that vatalanib may be beneficial in the treatment of cancer, the data are inconsistent and further research is needed. Nevertheless, vatalanib is of increasing interest to the medical community.

Pharmacologic action

Based on current research, vatalanib appears to inhibit the vascular endothelial growth factor receptor, or VEGF-R in English. VEGF is a molecule that has a signaling effect in the organism and can thus transmit information from one cell to another. The molecule binds to a receptor for which the substance has the correct fit: the VEGF-R. The binding of VEGF to its receptor is a process known as “signaling”. The binding of VEGF to its receptor triggers a reaction in the cell to which this receptor belongs. Physicians distinguish between different forms of VEGF and the corresponding receptors. So far, six variants of the signal molecule and three different receptors have been identified, which cannot react with each other at will. VEGF-A in particular, which appears to bind only to receptors 1 and 2, may be linked to cancer and is therefore of great interest to researchers. A 2000 study by Wood and colleagues concluded vatalanib acted primarily against VEGF-R1 and VEGF-R2.

Medical application and use

Medical researchers are developing vatalanib for possible future use in the treatment of certain cancers. A study by Dragovich and colleagues looked at the use of vatalanib as a second-line therapy for pancreatic adenocarcinoma. Adenocarcinoma is a specific type of cancer that can arise from glandular tissue. In this case, the tumor grows from epithelial cell tissue. Pancreatic or pancreatic cancer appears to be due to changes in certain counterparts that stimulate the growth of the cells, causing the tumor to develop. Chemotherapy may be considered as treatment, which was the case in the study by Dragovich and colleagues in the first phase of therapy. However, some patients do not respond to the drug administered in this process and the treatment does not lead to a sufficient result. It was precisely this group that Dragovich and the rest of the research group focused on. The patients received oral vatalanib twice daily during the second phase of therapy, gradually increasing the dose up to 1500 mg and then holding it constant at 750 mg. After six months, the researchers compared their patients with previous pancreatic cancer patients and found the survival rate to be quite favorable for this type of cancer, at around 30%. However, the physicians were not able to establish a direct link between the intake of vatalanib and VEGF-R. The findings are therefore inconclusive. Thus, the findings are inconclusive. Another study by Roodhart and Voest found no improvement in survival but did find an improvement in progression-free survival (the time between starting treatment and disease progression).

Risks and side effects

Overall, researchers such as Dragovich and colleagues and Wood et al describe vatalanib as well tolerated. The former group of researchers documented fatigue, hypertension, abdominal (stomach) pain, and irregularities in liver function tests as the most common side effects.Other sources also report diarrhea, vomiting, other digestive symptoms and dizziness. Because vatalanib is not yet commercially available and some research is still needed, the risks and side effects also have not been conclusively researched; these include possible long-term effects.