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What is Imatib used for?

Imatib tablets 100mg are used to treat cancers in which there is a similar genetic abnormality resulting in loss of control of cell growth.

Leukaemia is a cancer of the white blood cell that develops in the bone marrow.  Several types of leukaemia are classified by the speed at which they grow; being acute if they are fast growing or chronic if they are slow growing.  Classification for leukaemia also depends on the type of cell affected; lymphoblastic leukaemia develops from the lymphocytic cells, which form the white cells of the immune system; or myeloid leukaemia, which develops from the myelogenous cells that form the red blood cells, white cells and platelets.  Imatib tablets 100mg are used to treat adults and children with chronic myeloid leukaemia (CML) that is newly diagnosed or after failure of interferon therapy; also newly diagnosed acute lymphoblastic leukaemia (ALL) in adults and children in combination with chemotherapy or as monotherapy in adults with relapsed or refractory (difficult to treat) ALL. CML and ALL are positive for the Philadelphia chromosome, which is a specific chromosomal abnormality that results in uncontrolled growth of white blood cells.

Myelodysplastic/myeloproliferative diseases are blood cancers caused by either over-production or abnormal development of bone marrow myeloid cells.  Imatib tablets 100mg online are used to treat some of these cancers associated with gene re-arrangements in the platelet-derived growth factor receptor (PDGFR) gene.  Imatib tablets 100mg are also used to treat aggressive systemic mastocytosis (SM), in which mast cells, a type of white blood cell, accumulate and grow in several organs in an uncontrolled manner and also become more active by releasing granules containing inflammatory mediators and chemicals that can have serious effects, including loss of organ function and changes in blood pressure.  SM is a rare clonal bone marrow disorder where the cancer cells develop from a single abnormal myeloid bone marrow cell with a gene mutation resulting in the over-activation of the receptor for mast cell growth factor (KIT).  However, not all SM cancers have this mutation and Imatib tablets 100mg are used to treat SM where this mutation has not been identified.

Hypereosinophilic syndrome (HES) and chronic eosinophilic leukaemia (CEL) are also rare myeloproliferative blood cancers characterised by high numbers of eosinophils, which are white cells that originate in the bone marrow and are important in the inflammation process and the fight against infection.  HES and CEL can cause multiple organ damage and are associated with a mutation in the FIP1L1/PDGFRA gene leading to an abnormal receptor for a specific growth factor and loss of regulation of cell growth in these cancers.  Imatib tablets 100mg can be effective in HES and CEL with or without this genetic abnormality.

Dermatofibrosarcoma protuberans (DFSP) is a rare sarcoma type of cancer that develops in the middle dermal layer of the skin and penetrates deep into the lower layers of the skin.  It is another cancer caused by a genetic abnormality in a growth factor receptor gene, in this case PDGFRA which results in cells that that are continually stimulated to grow and differentiation.  Imatib tablets 100mg are used to treat unresectable, recurrent and/or metastatic DFSP.

Gastrointestinal stromal tumour (GIST) is a rare form of sarcoma that develops usually in the stomach from the supporting stromal tissue.  Most GISTs have a mutation in the mast cell growth factor receptor gene (c-kit CD117).  Imatib tablets 100mg are used to treat unresectable (untreatable) and/or metastatic malignant GIST that are Kit positive.

All these cancers are the result of loss of normal control in cell growth and enhanced cell survival due to a mutation in a gene coding for a specific growth factor cell surface receptor.  Imatib 100 works in a similar way to inhibit the abnormal signals that result in uncontrolled growth of these cancers.

How does Imatib work?

Imatib tablets 100mg contain imatinib, a tyrosine kinase (TK) inhibitor that blocks the activity of several different TKs.  These TKs are cell surface receptors for many cellular messengers including growth factors.  Tyrosine kinase is an enzyme that phosphorylates a protein inside a cell, which is the way many cell processes are regulated and is the first step in a complex cell signalling pathway involved in cell proliferation and survival.  Normally activation of these TK receptors is regulated and therefore, cell proliferation is controlled and programmed cell death (apoptosis) takes place. Imatib 100mg use and dosage However, over production or over stimulation of this enzyme receptor causes loss of control of cell growth resulting in enhanced cell proliferation, arrest in cell differentiation (when a simple cell becomes specialised for a particular function) and resistance to cell death.  This is a common mechanism found in several cancers.  These abnormal enzymes are usually a product of a genetic mutation resulting in the formation of an oncogene, which is a gene that has the potential to cause cancer.  The abnormality can result from overproduction or constitutive activation of the respective TK involved.  The Philadelphia chromosome is a chromosome abnormality caused by exchange of genetic material between chromosomes 9 and 22 resulting in a truncated chromosome 22 containing the proto- oncogene Bcr-Abl11.  A proto-oncogene is a gene that can cause normal cells to become tumour cells when mutated to become an oncogene.  They usually code for proteins that stimulate cell division, inhibit cell differentiation and halt cell death, such as TK.  The Bcr-Abl1 proto-oncogene results in constantly activated or turned on (constitutively activated) TK.  It can be expressed in a single leukemic stem cell in the bone marrow, which results in enhanced activity of TK and clonal expansion of the abnormal cell that develops into leukaemia.  Imatinib in Imatib tablets 100mg inhibits the activity of this abnormal Bcr-Abl1 protein TK in both CML and ALL, thereby preventing growth of the cancer cells without affecting growth of normal cells2.  Imatinib in Imatib tablets 100mg also inhibit TKs for other growth factors that cause cancers. These include the abnormal TK receptor for platelet-derived growth factor A and B (PDGFRA and PDGFRB) that are caused by gene rearrangements and are found in systemic mastocytosis (SM), chronic eosinophilic leukaemia (CEL), dermatofibrosarcoma protuberans (DFSP) and some cases of chronic myeloid leukaemia (CML)3, 4, 5.  Another abnormal TK that Imatinib in Imatib tablets 100mg targets is the receptor for mast cell growth factor (KIT) caused by c-kit an oncogene found in gastrointestinal stromal tumour (GIST) and most cases of aggressive systemic mastocytosis (SM)6, 7.  Imatinib in Imatib tablets 100mg inhibits the action of these various abnormal TKs that are known to be involved in the development of several cancers, thereby blocking uncontrolled cell proliferation, restoring normal cell differentiation and apoptosis.  This action of Imatinib in Imatib 100 is effective in reducing the growth of susceptible cancers, while having no effect on the growth of normal cells.

What does Imatib contain?

Imatib tablets 100mg contain the active ingredient imatinib, a tyrosine kinase (TK) inhibitor that is used to treat a variety of cancers caused by abnormal TK activity or structure.

Treating cancer with Imatib

Imatib tablets 100mg are used to treat a variety of cancers that are caused by a gene mutation resulting in loss of normal control of cell growth.  These include chronic myeloid leukaemia (CML), acute lymphoblastic leukaemia (ALL), myelodysplastic/myeloproliferative diseases (bone marrow cancers); aggressive systemic mastocytosis (SM), cancer of mast cells (white blood cells); metastatic malignant gastrointestinal stromal cancer (GIST) (a rare stomach cancer); hypereosinophilic syndrome (HES) and chronic eosinophilic leukaemia (CEL) (white blood cell cancers) and dermatofibrosarcoma protuberans (DFSP) (a rare skin cancer).  Each of these cancers is characterised by a gene mutation resulting in an abnormality in a specific tyrosine kinase (TK), which is an enzyme that is also a receptor for many growth factors in many cells.  Activation of the TKs is the first step in a complex cell signalling pathway involved in cell proliferation and survival; activation of TK is normally regulated and therefore, cell proliferation is controlled and programmed cell death (apoptosis) takes place.  However, over production or over stimulation of this enzyme receptor causes loss of control of cell growth resulting in enhanced cell proliferation, arrest in cell differentiation (when a simple cell becomes specialised for a particular function) and resistance to cell death.  Imatib tablets 100mg contain imatinib, a tyrosine kinase (TK) inhibitor that can block the activity of several different TKs, thereby blocking uncontrolled cell proliferation, restoring normal cell differentiation and apoptosis.  This action of Imatinib in Imatib 100 is effective in reducing the growth of susceptible cancers, while having no effect on the growth of normal cells.

What are the side effects of Imatib?

The most commonly reported side effects when taking Imatib tablets 100mg include: nausea, vomiting, diarrhoea, dyspepsia (heartburn), abdominal pain, fatigue, myalgia, asthenia (weakness) muscle pain (myalgia), muscle cramps, joint pain (arthralgia), bone pain, dermatitis, eczema rash, anorexia, weight increase, insomnia, headache, general oedema (fluid retention), swelling around the eye and around the eyelid, increased lacrimation (tear production), conjunctival haemorrhage (red eye or small bleed behind the conjunctiva of the eye), conjunctivitis (eye infection and inflammation), dry eye, blurred vision, flushing, haemorrhage, dyspnoea (difficulty breathing), epistaxis (nosebleed), cough,

When should Imatib not be used?

You should not use Imatib tablets 100mg if you:

  • are allergic to imatinib or any ingredients in Imatib
  • are pregnant or are breastfeeding
  • have kidney or liver disease
  • have heart disease or are at risk of heart failure
  • have had hepatitis B infection, as the virus may become reactivated
  • have had your thyroid removed and are receiving thyroid hormone replacement, as your thyroid hormone levels may fall (hypothyroidism)
  • are taking medicines that interact with Imatib 100mg, including, antibiotics like erythromycin, clarithromycin and rifampin, antifungals like ketoconazole and itraconazole, antivirals like ritonavir and ritonavir for HIV, antiepileptics like carbamazepine and phenytoin, the steroid dexamethasone statins for high cholesterol, calcium channel blockers for high blood pressure, warfarin for heart disease, the immunosuppressive cyclosporine, the analgesic acetaminophen and paracetamol

What medications interact with Imatib?

Several medications interact with Imatib tablets 100mg and should either not be taken while you are taking Imatib or only after discussion and instruction from your doctor:

Drugs that cause a serious reaction with Imatib: the analgesics acetaminophen and paracetamol

Drugs that affect Imatib: antibiotics like erythromycin, clarithromycin and rifampin, antifungals like ketoconazole and itraconazole, antivirals like ritonavir and ritonavir for HIV, antiepileptics like carbamazepine and phenytoin, the steroid dexamethasone

Drugs that are affected by Imatib: statins for high cholesterol, calcium channel blockers for high blood pressure, warfarin for heart disease, the immunosuppressive cyclosporine, the analgesics acetaminophen and paracetamol

How should Imatib be taken?

You should take your Imatib tablets 100mg once daily swallowed whole with a glass of water and with food.  The dose you take and for how long depends on what you are being treated for and your doctor’s recommendation.  You should continue to take your Imatib 100 for as long as you are benefiting from treatment and not having severe side effects, as recommended by your doctor.


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