Mycophenolic acid

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Mycophenolic acid

Mycophenolic acid (INN

International Nonproprietary Name

An International Nonproprietary Name is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization ....
) or mycophenolate is an immunosuppressant

Immunosuppression

Immunosuppression involves an act that reduces the activation or efficacy of the immune system. Some portions of the immune system itself have immuno-suppressive effects on other parts of the immune system, and immunosuppression may occur as an adverse reaction to treatment of other conditions....
drug used to prevent rejection

Transplant rejection

Transplant rejection occurs when a Organ transplant organ or tissue is not accepted by the body of the transplant recipient. This is explained by the concept that the immune system of the recipient attacks the transplanted organ or tissue....
in organ transplant

Organ transplant

Organ transplant is the moving of an organ from one body to another , for the purpose of replacing the recipient's damaged or failing organ with a working one from the donor site....
ation. It was initially marketed as the prodrug

Prodrug

A prodrug is a Pharmacology substance that is administered in an inactive form. Once administered, the prodrug is drug metabolism in vivo into an active metabolite....
mycophenolate mofetil (abbreviated MMF) to improve oral bioavailability

Bioavailability

In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetics properties of medication....
. More recently, the salt mycophenolate sodium has also been introduced. Mycophenolic acid is commonly marketed under the trade names CellCept (mycophenolate mofetil; Roche

Hoffmann-La Roche

F. Hoffmann?La Roche, Ltd. is a Switzerland global health-care company that operates world-wide under two divisions: Pharmaceutical companys and Roche Diagnostics....
) and Myfortic (mycophenolate sodium; Novartis

Novartis

Novartis International AG is a multinational corporation pharmaceutical company based in Basel, Switzerland that manufactures drugs such as clozapine , diclofenac , carbamazepine , valsartan , imatinib mesylate , ciclosporin , letrozole , methylphenidate , terbinafine , and others....
).

phenolate is derived from the fungus Penicillium stoloniferum
Penicillium

Penicillium is a genus of ascomyceteous fungi that includes:*Penicillium bilaiae, which is an agricultural inoculant.*Penicillium camemberti, which is used in the production of Camembert and Brie cheese cheeses....
.

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Mycophenolic acid (INN

International Nonproprietary Name

Immunosuppression

Transplant rejection

Organ transplant

Prodrug

Bioavailability

Hoffmann-La Roche

Novartis

Pharmacokinetics/pharmacology

Mycophenolate is derived from the fungus Penicillium stoloniferum
Penicillium

Penicillium is a genus of ascomyceteous fungi that includes:*Penicillium bilaiae, which is an agricultural inoculant.*Penicillium camemberti, which is used in the production of Camembert and Brie cheese cheeses....
. Mycophenolate mofetil is metabolised in the liver

Liver

The liver is a vital organ present in vertebrates and some other animals; it has a wide range of functions, a few of which are detoxification, protein synthesis, and production of biochemicals necessary for digestion....
to the active moiety mycophenolic acid. It inhibits inosine monophosphate dehydrogenase, the enzyme

Enzyme

Enzymes are biomolecules that catalysis chemical reactions. Almost all enzymes are proteins. In enzymatic reactions, the molecules at the beginning of the process are called Substrate , and the enzyme converts them into different molecules, the products....
that controls the rate of synthesis of guanine monophosphate in the de novo
De novo synthesis

De novo is a Latin phrase, meaning "from the new," anew, or from the beginning. De novo synthesis refers to the synthesis of complex molecules from simple molecules such as sugars or amino acids, as opposed to their being recycled after partial degradation....
pathway of purine

Purine

Purine is a heterocyclic compound aromatic organic compound, consisting of a pyrimidine ring fused to an imidazole ring. Purines, including substituted purines and their tautomers, are the most widely distributed kind of nitrogen-containing heterocycle in nature....
synthesis used in the proliferation of B and T lymphocytes.

Mycophenolate is potent and can be used in place of the older anti-proliferative azathioprine

Azathioprine

Azathioprine is an immunosuppressant used in organ transplantation, autoimmune disease such as rheumatoid arthritis and pemphigus or inflammatory bowel disease such as Crohn's disease and ulcerative colitis as well as multiple sclerosis....
. It is usually used as part of a three compound regimen of immunosuppressants, also including a calcineurin inhibitor (cyclosporin or tacrolimus

Tacrolimus

Tacrolimus is an immunosuppression medication whose main use is after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ Transplant rejection....
) and prednisolone

Prednisolone

Prednisolone is the active metabolite of prednisone....
.

Clinical use

Indications

In general, mycophenolate is used for the prevention of organ transplant

Organ transplant

Organ transplant is the moving of an organ from one body to another , for the purpose of replacing the recipient's damaged or failing organ with a working one from the donor site....
rejection

Transplant rejection

Kidney transplantation

Kidney transplantation or renal transplantation is the organ transplant of a kidney in a patient with end-stage renal disease. Kidney transplantation is typically classified as deceased-donor or living-donor transplantation depending on the source of the recipient organ....
rejection in children >2 years; whereas mycophenolate sodium is indicated for the prevention of renal transplant rejection in adults. Mycophenolate sodium has also been used for the prevention of rejection in liver

Liver transplantation

Liver transplantation or hepatic transplantation is the replacement of a diseased liver with a healthy liver allograft. The most commonly used technique is orthotopic transplantation, in which the native liver is removed and the donor organ is placed in the same anatomic location as the original liver....
, heart

Heart transplantation

HistoryThe first heart transplant involving a human was carried out by a team led by Dr James D Hardy on the of 23 of January 1964 at the University of Mississippi Medical Center, when the heart of a chimpanzee was transplanted into the chest of a dying man....
, and/or lung transplant

Lung transplantation

Lung transplantation is a surgical procedure in which a patient's diseased lungs are partially or totally replaced by lungs which come from a donor....
s in children >2 years.

An immunosuppressant that has drastically decreased the incidence of acute rejection in solid transplant recipients, mycophenolate is increasingly utilized as a steroid sparing treatment in immune-mediated disorders including immunoglobulin A nephropathy, small vessel vasculitides, and psoriasis

Psoriasis

Psoriasis is a chronic, non-contagious autoimmune disease which affects the skin and joints. It commonly causes red scaly patches to appear on the skin....
.

Its increasing application in treating lupus nephritis

Lupus nephritis

Lupus nephritis is an inflammation of the kidney caused by systemic lupus erythematosus , a disease of the immune system. Apart from the kidneys, SLE can also damage the skin, joints, nervous system and virtually any organ or system in the body....
has demonstrated more frequent complete response and less frequent complications compared to cyclophosphamide bolus therapy, a regimen with risk of bone marrow suppression, infertility, and malignancy. Further work addressing maintenance therapy demonstrated mycophenolate superior to cyclophosphamide

Cyclophosphamide

Cyclophosphamide , also known as cytophosphane, is a nitrogen mustard alkylating antineoplastic agent, from the oxazophorines group. It is used to treat various types of cancer and some autoimmune disorders....
, again in terms of response and side-effects. Walsh et al. even propose that mycophenolate should be considered as a first-line induction therapy for treatment of lupus nephritis in patients without renal dysfunction, suggesting that mycophenolate will be encountered more frequently in medical practice.

Adverse effects

Common adverse drug reaction

Adverse drug reaction

An adverse drug reaction or adverse drug event is an expression that describes the unwanted, negative consequences associated with the use of given medications....
s (=1% of patients) associated with mycophenolate therapy include diarrhea, nausea, vomiting, infections, leukopenia

Leukopenia

Leukopenia is a decrease in the number of circulating white blood cells in the blood. As the principal function of white cells is to combat infection, a decrease in the number of these cells can place patients at increased risk for infection....
, and/or anemia

Anemia

Anemia or an?mia/anaemia is defined as a qualitative or quantitative deficiency of hemoglobin, a protein found inside red blood cells ....
. Mycophenolate sodium is also commonly associated with fatigue, headache, and/or cough. Intravenous (IV) administration of mycophenolate mofetil is also commonly associated with thrombophlebitis

Thrombophlebitis

Thrombophlebitis is phlebitis related to a blood clot or thrombus. When it occurs repeatedly in different locations, it is known as "Thrombophlebitis migrans" or "migrating thrombophlebitis"....
and thrombosis

Thrombosis

Thrombosis is the formation of a blood clot inside a blood vessel, obstructing the flow of blood through the circulatory system. When a blood vessel is injured, the body uses platelets and fibrin to form a blood clot, because the first step in repairing it is to prevent loss of blood....
. Infrequent adverse effects (0.1–1% of patients) include esophagitis

Esophagitis

Esophagitis is inflammation of the esophagus....
, gastritis

Gastritis

Gastritis is an inflammation of the lining of the stomach, and has many possible causes. The main acute causes are excessive alcohol consumption or prolonged use of nonsteroidal anti-inflammatory drugs such as aspirin or ibuprofen....
, gastrointestinal tract

Gastrointestinal tract

The digestive tract is the system of Organ s within multicellular animals that takes in food, digestion it to extract energy and nutrients, and expels the remaining waste....
hemorrhage, and/or invasive cytomegalovirus

Cytomegalovirus

Cytomegalovirus is a Virus genus of the Herpesviridae group: in humans it is commonly known as HCMV or Human Herpesvirus 5 . CMV belongs to the Betaherpesvirinae subfamily of Herpesviridae, which also includes Roseolovirus....
(CMV) infection.

"Novartis and FDA informed healthcare professionals and patients that use of mycophenolic acid (Myfortic Delayed- Release Tablets) during pregnancy is associated with increased risks of pregnancy loss and congenital malformations. The pregnancy category for Myfortic has been changed to Category D (Positive evidence of fetal risk). This change is a result of postmarketing data from the United States National Transplantation Pregnancy Registry and additional postmarketing data collected in women exposed to systemic mycophenolate mofetil (MMF) during pregnancy. MMF is converted to the active ingredient in Myfortic, following oral or intravenous administration.

"A patient who is planning a pregnancy should not use Myfortic unless she cannot be successfully treated with other immunosuppressant drugs. Healthcare professionals should discuss the risks and benefits of Myfortic as well as alternative immunosuppressant therapy with the patient. Female patients of childbearing potential must receive contraceptive counseling and must use effective contraception while taking Myfortic. Myfortic is indicated for the prophylaxis of organ rejection in patients receiving allogeneic renal transplants, administered in combination with cyclosporine and corticosteroids". http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a601081.html, http://www.fda.gov/medwatch/safety/2007/safety07.htm#Myfortic, http://www.fda.gov/medwatch/safety/2007/Myfortic_DHCP_Letter.pdf and http://www.fda.gov/medwatch/safety/2007/MyforticPIfinal_Oct07.pdf.

The U.S. Food and Drug Administration (FDA) has added a list of warnings to the organ transplant drug stating that they can cause miscarriages and birth defects when used by pregnant women. In addition the FDA is investigating 16 patients that developed a rare neurological disease while taking the drug. The neurological condition known as progressive multifocal leukoencephalopathy

Progressive multifocal leukoencephalopathy

Progressive multifocal leukoencephalopathy , also known as progressive multifocal leukoencephalitis, is a rare and usually fatal virus disease that is characterized by progressive damage or inflammation of the white matter of the brain at multiple locations ....
attacks the brain and central nervous system and is usually fatal.

Comparison to other agents

Compared with azathioprine it is more lymphocyte

Lymphocyte

A lymphocyte is a type of white blood cell in the vertebrate immune system.By their appearance under the light microscope, there are two broad categories of lymphocytes, namely the large granular lymphocytes and the small lymphocytes....
-specific and is associated with less bone marrow suppression

Bone marrow suppression

Bone marrow suppression or myelotoxicity is a serious side-effect of chemotherapy and certain drugs affecting the immune system such as azathioprine....
, fewer opportunistic infection

Opportunistic infection

An opportunistic infection is an infection caused by pathogens that usually do not cause disease in a healthy immune system. A Immunodeficiency, however, presents an "opportunity" for the pathogen to infect....
s and lower incidence of acute rejection. The exact role of mycophenolate vs azathioprine has yet to be conclusively established, but many centers use it in place of azathioprine for high-risk patients, or patients that have already experienced an episode of acute rejection. In long-term immunosuppression, it may be used to avoid calcineurin inhibitors

Immunosuppressive drug

Immunosuppressive drugs or immunosuppressive agents are medication that inhibit or prevent activity of the immune system. They are used in immunosuppression to:...
or steroids.

Potential future uses

Mycophenolate mofetil is beginning to be used in the management of auto-immune disorders such as idiopathic thrombocytopenic purpura

Idiopathic thrombocytopenic purpura

Idiopathic thrombocytopenic purpura is the condition of having a low platelet platelet count of no known cause . As most causes appear to be related to antibody against platelets, it is also known as immune thrombocytopenic purpura or immune-mediated thrombocytopenic purpura....
(ITP), systemic lupus erythematosus

Systemic lupus erythematosus

Systemic lupus erythematosus is a chronic Autoimmunity connective tissue disease that can affect any part of the body. As occurs in other autoimmune diseases, the immune system attacks the body?s cells and tissue, resulting in inflammation and tissue damage....
(SLE), and pemphigus

Pemphigus

Pemphigus is a rare group of autoimmune blistering diseases that affect the skin and mucous membranes.In pemphigus, autoantibody form against desmoglein....
vulgaris (PV) with success for some patients.

It is also currently being used as a long-term therapy for maintaining remission of C-ANCA positive (Wegener's) granulomatosis. A combination of mycophenolate and ribavirin

Ribavirin

Ribavirin is an anti-viral drug indicated for severe Human respiratory syncytial virus infection , hepatitis C infection and other viral infections....
has been found to stop infection by and replication

Viral replication

Viral replication is the term used by virologists to describe the formation of biological viruses during the infection process in the target host cells....
of dengue virus in vitro
In vitro

In vitro refers to the technique of performing a given procedure in a controlled environment outside of a living organism. Some may argue that in vitro refers to a process that is created in a "test tube"; however, Robert Kail and John Cavanaugh on page 58 in the 4th edition of Human Development: A Life-Span View cite that in fact th...
.

Footnotes

External links

– information from USP DI Advice for the Patient