Medical use and study of Imatinib

Introduction: In 2001, Imatinib was approved for medical use in the United States. It is used for the treatment of cancer. Specifically, it is introduced for chronic myelogenous leukemia and acute lymphocytic leukemia that are Ph+, certain gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), myelodysplastic syndrome and systemic mastocytosis. 

What is Imatinib?

Imatinib 400 mg is an oral chemotherapy medication. It acts by stopping the Bcr-Abl tyrosine-kinase. This can resist the growth or outcomes in programmed cell death of certain sorts of cancerous cells.

Imatinib is introduced in order to be used for the treatment of patients with chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. In the year of 2006 the FDA extended the approved use to include DFSP (Dermatofibrosarcoma protuberans), (Myelodysplastic/myeloproliferative diseases (MDS/MPD), Aggressive systemic mastocytosis (ASM).

The USFDA has approved imatinib as first-line treatment option for Philadelphia chromosome +Ve CML, both in adults and children. The medication is approved in multiple contexts of Philadelphia chromosome +Ve CML, including following the stem cell transplant, in blast crisis, and also newly diagnosed.

In the year of 2002, the FDA initially granted the approval for the treatment of advanced GIST patients. In the month of February 2012, imatinib was approved for use following the surgical removal of KIT +Ve tumors to help prevent recurrence. This medication is also approved in the treatment of unresectable KIT +Ve GISTs.

In the year of 2006, the FDA granted approval for the treatment of dermatofibrosarcoma protuberans (DFSP) patients. Specifically adults with unresectable, recurrent/metastatic dermatofibrosarcoma protuberans (DFSP). Before approval dermatofibrosarcoma protuberans was considered unresponsive to chemo regimens.

The FDA (Food and Drug Administration) has approved imatinib for use in adult patients with relapsed/refractory Ph+ ALL, myelodysplastic/myeloproliferative diseases associated with platelet-derived growth factor receptor gene rearrangements, aggressive systemic mastocytosis without or an unspecified D816V c-KIT mutation, hypereosinophilic syndrome or chronic eosinophilic leukemia who have the FIP1L1-PDGFRα fusion kinase (CHIC2 allele deletion) or FIP1L1-PDGFRα fusion kinase negative or unspecified, unresectable, recurrent or metastatic dermatofibrosarcoma protuberans. In the month of January 2013, Imatinib was approved for use in children with Ph+ ALL.

To treat progressive plexiform neurofibromas associated with neurofibromatosis type-I, the early research has demonstrated potential for using the c-KIT tyrosine kinase inhibiting properties of imatinib.

How to Take Imatinib?

Imatinib 400 mg comes as a tablet to administer by mouth. It is usually administered through a meal and a large glass of water once/twice daily. Take the pills of imatinib at around the same time(s) each day. Follow the words of your healthcare provider regarding your prescription. 

Price & Storage: The Imatinib price in India is quite reasonable. This medication is available at every WHO-GDP & ISO certified wholesaler at the very best price. Prices usually may vary from generic to innovator drugs. 

Keep imatinib tablets in a cool, dry place, away from the children and direct sunlight. Store it at room temperature. 

Research:

According to a study, imatinib was effective in patients with systemic mastocytosis, including those who had the D816V mutation in c-KIT. Although, since this agent binds to tyrosine kinases when they are not in the active configuration and the D816V mutant of c-KIT is constitutively active, this medication does not block the kinase activity of the D816V mutant of c-KIT. Experience has specified, although, that imatinib is quite less useful in patients with this kind of mutation, and patients with the mutation comprise around 90% of cases of mastocytosis.

Earlier, this oral chemotherapy medication was thought to have a potential role in treatment of pulmonary hypertension. It was known to reduce the smooth muscle hypertrophy as well as hyperplasia of the pulmonary vasculature in a variety of disease processes, including portopulmonary hypertension.

Although, the long-term carried out trial of imatinib in patients with pulmonary arterial hypertension was not successful, and serious and unexpected side effects were frequent. In this six subdural hematomas and 17 deaths reported during or within one month of study completion.

Talking about systemic sclerosis, the medicine has been assessed for potential use in resisting pulmonary fibrosis. In laboratory settings, it is being considered as an experimental agent in order to suppress the platelet-derived growth factor (PDGF) by blocking its receptor (PDGF-Rβ). One of its effects is resisting atherosclerosis in mice either without or with diabetes.

According to mouse animal studies, imatinib and related agents may be effective in treating smallpox, should an outbreak ever occur.

In vitro findings specified that a modified version of imatinib could bind to GSAP. The gamma-secretase activating protein selectively enhances the formation as well as accumulation of the neurotoxic beta-amyloid plaques, which suggests that molecules which target gamma-secretase activating protein and can cross blood–brain barrier are potential therapeutic agents in the treatment of patients with Alzheimer's disease.

According to another study, imatinib may not need to cross the blood–brain barrier in order to be useful at treating Alzheimer's, as the findings specified the formation of beta amyloid may start in the liver. The mice testing indicate that imatinib is effective at decreasing beta-amyloid in the brain. It is unspecified whether the reduction of beta-amyloid is a feasible way of treating Alzheimer's, as an anti beta-amyloid vaccine has been demonstrated to clear the brain of plaques without having any effect on the symptoms of Alzheimer's.

Imatinib's formulation with a cyclodextrin as a carrier to overcome the blood-brain barrier is also currently considered as an experimental medication for reducing and reversing opioid tolerance. Imatinib has demonstrated reversal of tolerance in rats. Imatinib is an experimental medication in treating desmoid tumor or aggressive fibromatosis.

Note: The piece of information provided about "What are the medical uses of Imatinib" in this article is just for informational purposes and is not served as a substitute for the medical treatment, consultation, diagnosis, of an experienced/qualified healthcare professional.