NationMaster - Encyclopedia: Methotrexate

Methotrexate (rINN) (IPA: [mɛθəˈtrɛkseɪt]), abbreviated MTX and formerly known as amethopterin, is an antimetabolite and antifolate drug used in treatment of cancer and autoimmune diseases. It acts by inhibiting the metabolism of folic acid. Methotrexate replaced the more powerful and toxic antifolate aminopterin, and the two should not be confused with each other. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... Intramuscular injection is an injection of a substance directly into a muscle. ... The subcutis is the layer of tissue directly underlying the cutis. ... Intrathecal: Delivered into the spinal canal (intrathecal space surrounding the spinal cord), as in a spinal anaesthesia. ... An International Nonproprietary Name (INN) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization. ... Articles with similar titles include the NATO phonetic alphabet, which has also informally been called the â€œInternational Phonetic Alphabetâ€. For information on how to read IPA transcriptions of English words, see IPA chart for English. ... An antimetabolite is a chemical with a similar structure to a substance (a metabolite) required for normal biochemical reactions, yet different enough to interfere with the normal functions of cells, including cell division. ... Cancer is a class of diseases or disorders characterized by uncontrolled division of cells and the ability of these to spread, either by direct growth into adjacent tissue through invasion, or by implantation into distant sites by metastasis (where cancer cells are transported through the bloodstream or lymphatic system). ... Autoimmune diseases arise from an overactive immune response of the body against substances and tissues normally present in the body. ... Folic acid and folate (the anion form) are forms of the water-soluble Vitamin B9. ... Aminopterin (4-aminopteroic acid), a 4-amino analog of folic acid, is an antineoplastic drug with immunosuppressive properties used in chemotherapy. ...

History

Methotrexate originated in the 1940s when Sidney Farber at Children's Hospital Boston was testing the effects of folic acid on cancer. This inspired chemists at the drug company Lederle to start looking for antimetabolites resembling folate. The result was methotrexate, which was developed in 1948 by Yellapragada Subbarao from Lederle. Methotrexate gained Food and Drug Administration (FDA) approval as an oncology drug in 1953. Dr Sydney Farber, after whom the Dana-Farber Cancer Institute is named Sidney Farber was a pediatric pathologist. ... Childrens Hospital Boston is a hospital located in Boston, Massachusetts, USA, adjacent to Brigham and Womens Hospital and Harvard Medical School. ... Folic acid and folate (the anion form) are forms of the water-soluble Vitamin B9. ... Yellapragada Subbarao (Subba Row or Subba Rao) (January 12, 1895-August 1948) born to a very poor family in South India, he remains in the views of many the most notable medical scientist to emerge from India. ... hi â€œFDAâ€ redirects here. ...

Uses

In chemotherapy

Methotrexate was originally used, as part of combination chemotherapy regimens, to treat many kinds of cancers. It is still the mainstay for the treatment of many neoplastic disorders including acute lymphoblastic leukemia. Cancer is a class of diseases or disorders characterized by uncontrolled division of cells and the ability of these to spread, either by direct growth into adjacent tissue through invasion, or by implantation into distant sites by metastasis (where cancer cells are transported through the bloodstream or lymphatic system). ... Neoplasia (literally: new growth) is sudden and abnormal growth in a tissue or organ. ... Acute lymphoblastic leukemia (ALL), also known as acute lymphocytic leukemia, is a form of leukemia, characterised by the overproduction and continuous multiplication of malignant and immature white blood cells (also known as lymphoblasts) in the bone marrow. ...

Other uses

More recently it has come into use as a treatment for some autoimmune diseases, including ankylosing spondylitis, Crohn's disease, psoriasis, psoriatic arthritis, and rheumatoid arthritis (see disease-modifying antirheumatic drugs). A parallel use with TNFα blockers as infliximab or etanercept has been shown to markedly improve symptoms.^[1] Autoimmune diseases arise from an overactive immune response of the body against substances and tissues normally present in the body. ... Crohns disease (also known as regional enteritis) is a chronic, episodic, inflammatory condition of the gastrointestinal tract characterized by transmural inflammation (affecting the entire wall of the involved bowel) and skip lesions (areas of inflammation with areas of normal lining between). ... Psoriatic arthritis (or Arthropathic psoriasis) is a type of inflammatory arthritis that affects around 20% of people suffering from the chronic skin condition Psoriasis. ... Rheumatoid arthritis (RA) is traditionally considered a chronic, inflammatory autoimmune disorder that causes the immune system to attack the joints. ... Disease-modifying antirheumatic drugs is a category of drugs used in many autoimmune diseases to slow down disease progression. ... In medicine, tumor necrosis factor alpha (TNFα, cachexin or cachectin) is an important cytokine involved in systemic inflammation and the acute phase response. ... Infliximab (brand name RemicadeÂ®) is a drug used to treat auto-immune disorders. ... Etanercept (EnbrelÂ®, co-marketed by Amgen and Wyeth) is a human recombinant, soluble tumor necrosis factor-alpha (TNFÎ±) receptor. ...

Although not indicated for this use, methotrexate is also sometimes used (generally in combination with misoprostol) to terminate early pregnancies, particularly ectopic pregnancies. Misoprostol is a drug that is United States Food and Drug Administration (FDA)-approved for the treatment and prevention of stomach ulcers. ... This article is about human pregnancy in biological females. ...

Pharmacokinetics

Methotrexate is a weak dicarboxylic acid with pKa 4.8 and 5.5, and thus it is mostly ionized at physiologic pH. Oral absorption is saturatable and thus dose-dependent, with doses less than 40mg/M2 having 42% bioavailability and doses greater than 40mg/M2 only 18%. Mean oral bioavailability is 33% (13-76% range), and there is no clear benefit to subdividing an oral dose. Mean intramuscular bioavailability is 76%. The acid dissociation constant (Ka), also known as the acidity constant or the acid-ionization constant, is a specific equilibrium constant for the reaction of an acid with its conjugate base in aqueous solution [1]. // When an acid dissolves in water, it partly dissociates forming hydronium ions and its conjugate... Ionization is the physical process of converting an atom or molecule into an ion by changing the difference between the number of protons and electrons. ...

Methotrexate is metabolized by intestinal bacteria to the inactive metabolite 4-amino-4-deoxy-N-methylpteroic acid (DAMPA) and accounts for less than 5% loss of the oral dose.

Factors that decrease absorption include food, oral non-absorbable antibiotics (e.g. vancomycin, neomycin, and bacitracin), and more rapid transit through the Gastrointestinal (GI) tract such as diarrhea, while slower transit time in the GI tract from constipation will increase absorption.

Administration

It can be taken orally or administered by injection (subcutaneous, intramuscular, intravenous or intrathecal). Although daily preparations are occasionally used, most patients take weekly doses, which decreases the risk of certain side-effects. Intramuscular injection is an injection of a substance directly into a muscle. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... Intrathecal: Delivered into the spinal canal (intrathecal space surrounding the spinal cord), as in a spinal anaesthesia. ...

Adverse effects

Possible side effects can include anemia, neutropenia, increased risk of bruising, nausea and vomiting, dermatitis and diarrhea. A small percentage of patients develop hepatitis, and there is an increased risk of pulmonary fibrosis. This article discusses the medical condition. ... Neutropenia (or neutropaenia, adjective neutrop(a)enic) is a hematological disorder characterized by an abnormally low number of neutrophil granulocytes (a type of white blood cell). ... A bruise or contusion or ecchymoses is a kind of injury, usually caused by blunt impact, in which the capillaries are damaged, allowing blood to seep into the surrounding tissue. ... For other uses, see Nausea (disambiguation). ... Vomiting (also throwing up or emesis) is the forceful expulsion of the contents of ones stomach through the mouth and sometimes the nose. ... Dermatitis is a blanket term literally meaning inflammation of the skin. It is usually used to refer to eczema, which is also known as Dermatitis eczema. ... Types 5-7 on the Bristol Stool Chart are often associated with diarrhea Diarrhea (in American English) or diarrhoea (in British English) is a condition in which the sufferer has frequent watery, loose bowel movements (from the Greek word Î´Î¹Î¬ÏÏÎ¿Î¹Î±; literally meaning through-flowing). Acute infectious diarrhea is a common cause... Hepatitis (plural hepatitides) implies injury to liver characterised by presence of inflammatory cells in the liver tissue. ... Diffuse parenchymal lung disease (DPLD), also known as interstitial lung disease, refers to a group of lung diseases, affecting the alveolar epithelium, pulmonary capillary endothelium, basement membrane, perivascular and perilymphatic tissues. ...

The higher doses of methotrexate often used in cancer chemotherapy can cause toxic effects to the rapidly-dividing cells of bone marrow and gastrointestinal mucosa. The resulting myelosuppression and mucositis are often prevented (termed methotrexate "rescue") by using folinic acid supplements (not to be confused with folic acid). This article does not cite any references or sources. ... For the Physics term GUT, please refer to Grand unification theory The gastrointestinal or digestive tract, also referred to as the GI tract or the alimentary canal or the gut, is the system of organs within multicellular animals which takes in food, digests it to extract energy and nutrients, and... The mucous membranes (or mucosa) are linings of ectodermic origin, covered in epithelium, that line various body cavities and internal organs. ... Mucositis is the painful inflammation and ulceration of the mucous membranes lining the digestive tract. ... Folinic acid (INN) or leucovorin (USAN), generally administered as calcium folinate (or leucovorin calcium), is an adjuvant used in cancer chemotherapy involving the drug methotrexate. ... Folic acid and folate (the anion form) are forms of the water-soluble Vitamin B9. ...

Methotrexate is a highly teratogenic drug and categorized in Pregnancy Category X by the FDA. Women must not take the drug during pregnancy, if there is a risk of becoming pregnant, or if they are breastfeeding. Men who are trying to get their partner pregnant must also not take the drug. To engage in any of these activities (after discontinuing the drug), women must wait until the end of a full ovulation cycle and men must wait three months. Teratogenesis is a medical term from the Greek, literally meaning monster making. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...

There is a risk of a severe adverse reaction if penicillin is prescribed alongside methotrexate. For the Japanese rock band, see Penicillin (band). ...

Interestingly, there have also been some reports of central nervous system reactions to methotrexate especially when given via the intrathecal route which include myelopathies and leucoencephalopathies.

Mode of action

Methotrexate competitively and reversibly inhibits dihydrofolate reductase (DHFR), an enzyme that is part of the folate synthesis metabolic pathway. The affinity of methotrexate for DHFR is about one thousand-fold that of folate for DHFR. Dihydrofolate reductase catalyses the conversion of dihydrofolate to the active tetrahydrofolate. Folic acid is needed for the de novo synthesis of the nucleoside thymidine, required for DNA synthesis. Methotrexate, therefore, inhibits the synthesis of DNA, RNA, thymidylates, and proteins. Categories: Biochemistry stubs | EC 1. ... Ribbon diagram of the enzyme TIM, surrounded by the space-filling model of the protein. ... Folic acid (the anion form is called folate) is a B-complex vitamin (once called vitamin M) that is important in preventing neural tube defects (NTDs) in the developing human fetus. ... Dihydrofolic acid is a folic acid derivative acted upon by dihydrofolate reductase. ... To meet Wikipedias quality standards, this articles references may require cleanup. ... Nucleosides are glycosylamines made by attaching a nucleobase (often reffered to simply as bases) to a ribose ring. ... The chemical structure of deoxythymidine Thymidine (more precisely called deoxythymidine can also be labelled deoxyribosylthymine, and thymine deoxyriboside) is a chemical compound, more precisely a pyrimidine deoxynucleoside. ... DNA replication. ... The structure of part of a DNA double helix Deoxyribonucleic acid, or DNA, is a nucleic acid molecule that contains the genetic instructions used in the development and functioning of all known living organisms. ... Ribonucleic acid or RNA is a nucleic acid polymer consisting of nucleotide monomers that plays several important roles in the processes that translate genetic information from deoxyribonucleic acid (DNA) into protein products; RNA acts as a messenger between DNA and the protein synthesis complexes known as ribosomes, forms vital portions... A representation of the 3D structure of myoglobin, showing coloured alpha helices. ...

Methotrexate acts specifically during DNA and RNA synthesis, and thus it is cytotoxic during the S-phase of the cell cycle. Logically, it therefore has a greater toxic effect on rapidly dividing cells (such as malignant and myeloid cells, and GI & oral mucosa), which replicate their DNA more frequently, and thus inhibits the growth and proliferation of these non-cancerous cells as well causing side effects listed above. The cell cycle, or cell-division cycle, is the series of events that take place in a eukaryotic cell leading to its replication. ... In medicine, malignant is a clinical term that means to be severe and become progressively worse, as in malignant hypertension. ... Myeloid cells is a subsummating term for all hemopoietic cells except the lymphoid ones (T-cells, B-cells, NK-cells, dendritic cells). ...

Lower doses of methotrexate have been shown to be very effective for the management of rheumatoid arthritis and psoriasis. In these cases inhibition of dihydrofolate reductase (DHFR) is not thought to be the main mechanism, rather the inhibition of enzymes involved in purine metabolism, leading to accumulation of adenosine, or the inhibition of T cell activation and suppression of intercellular adhesion molecule expression by T cells.^[2] Rheumatoid arthritis (RA) is traditionally considered a chronic, inflammatory autoimmune disorder that causes the immune system to attack the joints. ... Categories: Biochemistry stubs | EC 1. ... Ribbon diagram of the enzyme TIM, surrounded by the space-filling model of the protein. ... Adenosine is a nucleoside comprised of adenine attached to a ribose (ribofuranose) moiety via a Î²-N9-glycosidic bond. ... T cells are a subset of lymphocytes that play a large role in the immune response. ... Intercellular adhesion molecules (ICAMs) are molecules that promote adhesion between cells. ... T cells are a subset of lymphocytes that play a large role in the immune response. ...

References

External links

Categories: Chemotherapeutic agents | Immunosuppressive agents | Dihydrofolate reductase inhibitors Chemotherapy is the use of chemical substances to treat disease. ... A section of the Anatomical Therapeutic Chemical Classification System. ... An alkylating antineoplastic agent is an alkylating agent that attaches an alkyl group to DNA. Since cancer cells generally divide more rapidly than do healthy cells they are more sensitive to DNA damage, and alkylating agents are used clinically to treat a variety of tumours. ... The nitrogen mustards are cytotoxic chemotherapy agents similar to mustard gas. ... Chlorambucil (marketed as Leukeran by GlaxoSmithKline) is a chemotherapy drug that has been mainly used in the treatment of chronic lymphocytic leukemia. ... Mechloretamine: chemical structure Mechlorethamine also known as nitrogen mustard and HN2 and sold under the brand name Mustargen, is the first anticancer drug to be widely used clinically. ... Cyclophosphamide (the generic name for Cytoxan, Neosar) is a nitrogen mustard alkylating agent, used to treat various types of cancer and some autoimmune disorders. ... Ifosfamide (MitoxanaÂ®) Ifosfamide (pronounced i fos fa mide) is chemotherapy that is given as a treatment for many different types of cancer. ... Melphalan hydrochloride ( AlkeranÂ®) is a chemotherapy drug belonging to the class of nitrogen mustard alkylating agents. ... Urea streptozotocin ENU Nitrosourea compounds are compounds that include a nitroso (R-NO) group and a urea. ... Carmustine is an nitrosourea compound used as an alkylating agent in chemotherapy. ... Fotemustine is a nitrosourea alkylating agent. ... Lomustine (or CCNU) is an alkylating nitrosourea compound used in chemotherapy. ... Streptozotocin (STZ, Zanosar) is a drug used in treating cancer of the pancreas. ... General Name, Symbol, Number platinum, Pt, 78 Chemical series transition metals Group, Period, Block 10, 6, d Appearance grayish white Standard atomic weight 195. ... Carboplatin is a chemotherapy drug used against some forms of cancer. ... Cisplatin, cisplatinum or cis-diamminedichloroplatinum(II) (CDDP) is a platinum-based chemotherapy drug used to treat various types of cancers, including sarcomas, some carcinomas (e. ... Oxaliplatin is a platinum-based chemotherapy drug in the same family as cisplatin and carboplatin. ... There are very few or no other articles that link to this one. ... Busulfan is a chemotherapy drug that is an alkylating agent (slows the growth of cancer cells). ... Dacarbazine (da-KAR-ba-zeen) (brand names DTIC, DTIC-Dome; also known as DIC or Imidazole Carboxamide) is an antineoplastic chemotherapy drug used in the treatment of various cancers, among them malignant melanoma (a form of skin cancer which can spread to other parts of the body). ... Procarbazine (MatulaneÂ® (US), Natulan (Canada)) is an antineoplastic chemotherapy drug for the treatment of Hodgkins lymphoma and certain brain cancers (such as Glioblastoma multiforme). ... Temozolomide (brand name TemodarÂ® Schering-Plough Corporation) is an oral alkylating agent used for the treatment of refractory anaplastic astrocytoma -- a type of cancerous brain tumor. ... N,NN-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group, now in use for over 50 years. ... Uracil mustard or uramustine is a chemotherapy drug which belongs to the class of alkylating agents. ... An antimetabolite is a chemical with a similar structure to a substance (a metabolite) required for normal biochemical reactions, yet different enough to interfere with the normal functions of cells, including cell division. ... Folic acid and folate (the anion form) are forms of the water-soluble Vitamin B9. ... Aminopterin (4-aminopteroic acid), a 4-amino analog of folic acid, is an antineoplastic drug with immunosuppressive properties used in chemotherapy. ... Pemetrexed chemical structure Pemetrexed (brand name Alimta) is a chemotherapy drug. ... Raltitrexed (brand name TomudexÂ®) is a chemotherapy drug manufactured AstraZeneca Company, is an antimetabolite used in chemotherapy. ... Purine is a heterocyclic aromatic organic compound, consisting of a pyrimidine ring fused to an imidazole ring. ... Cladribine is a drug used to treat hairy cell leukemia (leukemic reticuloendotheliosis). ... Clofarabine: chemical structure Clofarabine is a substance that is being studied in the treatment of cancer. ... Fludarabine is a chemotherapy drug used in the firstline treatment of chronic lymphocytic leukemia. ... Mercaptopurine: chemical structure Mercaptopurine (also called 6-MP or by its brand name PurinetholÂ®) is an immunosuppressive drug used to treat leukemia. ... Pentostatin (Deoxycoformycin) is an anticancer chemotherapeutic drug. ... Tioguanine (INN), formerly Thioguanine (BAN), is a drug that is used in the treatment of cancer. ... Pyrimidine is a heterocyclic aromatic organic compound similar to benzene and pyridine, containing two nitrogen atoms at positions 1 and 3 of the six-member ring [1]. It is isomeric with two other forms of diazine. ... Capecitabine (INN) (IPA: ) is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers. ... Cytarabine is a shortened form of cytosine arabinoside, a commonly used chemotherapy agent used mainly in the treatment of leukemia and non-Hodgkin lymphoma. ... Fluorouracil (5-FU) is a drug that is used in the treatment of cancer. ... Floxuridine is an oncology drug that belongs to the class known as antimetabolites. ... Gemcitabine is a nucleoside used as chemotherapy. ... These poisons disrupt cellular reproduction by affecting the protein threads which connect the centromere regions of chromosomes, known as spindles. ... A mitotic inhibitor is a type of drug used mainly to treat cancer. ... The taxanes are NOT alkaloids (not every molecule coming from a plant and bearing a nitrogen is an alkaloid!). They are diterpenes produced by the plants of the genus Taxus (yews). ... Docetaxel chemical structure Docetaxel is a chemotherapy drug used in the treatment of cancer. ... Paclitaxel is a drug used in the treatment of cancer. ... Vinca is Vinca, a botanical genus; see Periwinkle (plant). ... Vinblastine stick molecular model Vinblastine is an anti-mitotic drug used to treat certain kinds of cancer, including Hodgkins lymphoma, non-small cell lung cancer, breast cancer and testicular cancer. ... Vincristine (OncovinÂ®) is a vinca alkaloid from the Madagascar periwinkle (Catharanthus roseus, formerly Vinca rosea and hence its name). ... Vindesine is a vinca alkaloid used in chemotherapy. ... Vinorelbine (Navelbine) is a chemotherapy drug that is given as a treatment for some types of cancer including breast cancer and non-small-cell lung cancer. ... herbs that have the specific action of inhibiting and combating the development of tumors. ... Anthracycline - Wikipedia, the free encyclopedia /**/ @import /skins-1. ... Daunorubicin or daunomycin (daunomycin cerubidine) is chemotherapy of the anthracycline family that is given as a treatment for some types of cancer. ... Doxorubicin or AdriamycinÂ® or hydroxyldaunorubicin is a DNA-interacting drug widely used in chemotherapy. ... Epirubicin (marketed by Pfizer under the trade name EllenceÂ®) is an anthracycline drug used for chemotherapy. ... Idarubicin chemical structure Idarubicin or 4-demethoxydaunorubicin is an anthracycline drug that is used in the treatment of cancer. ... Mitoxantrone belongs to the general group of medicines known as antineoplastics, specifically the anthracycline class. ... Valrubicin chemical structure Valrubicin (N-trifluoroacetyladriamycin-14-valerate, ValstarÂ®) is a chemotherapy drug used to treat bladder cancer. ... Streptomyces is a genus of Actinobacteria. ... Actinomycin is any of a class of polypeptide antibiotics isolated from soil bacteria of the genus Streptomyces. ... Bleomycin is an anti-cancer agent. ... Mitomycin or mitomycin C is a form of chemotherapy given intravenously to treat upper gastro-intestinal (e. ... Plicamycin (INN, also known as mithramycin; trade name Mithracin) is an antineoplastic antibiotic produced by Streptomyces plicatus. ... Hydroxyurea chemical structure Hydroxyurea or hydroxycarbamide (rINN), (brand names include HydreaÂ®) is an antineoplastic drug used in hematological malignancies. ... Topoisomerase inhibitors are chemotherapy agents designed to interfere with the action of topoisomerase enzymes (topoisomerase I and II), which are enzymes that control the changes in DNA structure by catalyzing the breaking and rejoining of the phosphodiester backbone of DNA strands during the normal cell cycle. ... Species Camptotheca acuminata - Happy tree Camptotheca lowreyana The Happy tree, Camptotheca acuminata, is a medium-sized deciduous tree native to central China, usually included in the tupelo family Nyssaceae, but sometimes included (with the tupelos) in the dogwood family Cornaceae. ... Camptothecin is a plant secondary metabolite used as an anti-cancer drug that damages DNA, leading to the destruction of the cell. ... Topotecan (HycamtinÂ®) is a chemotherapy agent that is a topoisomerase 1 inhibitor. ... Irinotecan is a chemotherapy agent that is a topoisomerase 1 inhibitor. ... Binomial name Podophyllum peltatum L. The American Mayapple (Podophyllum peltatum) is a herbaceous perennial plant in the family Berberidaceae, native to the eastern part of North America. ... Etoposide phosphate (EposinÂ®, EtopophosÂ®, VepesidÂ®, VP-16Â®) is an inhibitor of the enzyme topoisomerase II. It is used as a form of chemotherapy for malignancies such as lung cancer, testicular cancer, lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme. ... Teniposide is a prescribed medication mainly used to treat childhood acute lymphocytic leukemia. ... Cancer Immunotherapy is the use of monoclonal antibodies (-mab) to specifically target cells. ... // Monoclonal antibodies (mAb) are antibodies that are identical because they were produced by one type of immune cell and are all clones of a single parent cell. ... Alemtuzumab (marketed as Campath or Campath-1H) is a monoclonal antibody used in the treatment of chronic lymphocytic leukemia (CLL) and T-cell lymphoma. ... Bevacizumab (trade name Avastin) is a monoclonal antibody against vascular endothelial growth factor. ... Cetuximab (Erbitux®) is a chimeric monoclonal antibody given by intravenous injection for treatment of colorectal cancer. ... Gemtuzumab ozogamicin (marketed as Mylotarg) is a monoclonal antibody used to treat acute myelogenous leukemia. ... It is proposed that this article be deleted, because of the following concern: No references or indication of notability. ... Rituximab, sold under the trade names RituxanÂ® and MabTheraÂ®, is a monoclonal antibody used in the treatment of B cell non-Hodgkins lymphoma, B cell leukemia, and some autoimmune disorders. ... Tositumomab is a monoclonal antibody. ... Trastuzumab (more commonly known under the trade name Herceptin) is a humanized monoclonal antibody that acts on the HER2/neu (erbB2) receptor. ... A photosensitizer is a chemical compound, used in the Photodynamic Therapy of cancers, that can be excited by light of a specific wavelength. ... D-Aminolevulinic acid (dALA or Î´-ALA) is the first compound in the porphyrin synthesis pathway. ... Methyl aminolevulinate is a sensitizer used in photodynamic/radiation therapy. ... Porfimer is a sensitizer used in photodynamic/Radiation therapy. ... Verteporfin, otherwise known as benzoporphyrin derivative (VisudyneÂ®), is a medication used in conjunction with laser treatment to eliminate the abnormal blood vessels in the eye associated with conditions such as the wet form of macular degeneration. ... Tyrosine kinases are a subclass of protein kinase, see there for the principles of protein phosphorylation A tyrosine kinase (EC 2. ... A protein kinase inhibitor is a type of enzyme inhibitor which specifically blocks the action of protein kinase. ... Dasatinib is a drug produced by Bristol-Myers Squibb and sold under the trade name SprycelÂ®. Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinases inhibitor approved for use in patients with chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). ... Erlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. ... Gefitinib is a new drug used in the treatment of certain types of cancer. ... Imatinib is a drug used to treat certain types of cancer. ... Lapatinib (INN) or lapatinib ditosylate (USAN), also known as GW572016, is an anti-cancer drug developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung cancer. ... Sorafenib (rINN), marketed as Nexavar by Bayer, is a drug approved for the treatment of advanced renal cell carcinoma (primary kidney cancer). ... Sunitinib (marketed as Sutent, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. ... The Retinoids are a class of chemical compounds that are related chemically to vitamin A. Retinoids are used in medicine, primarily due to the way they regulate epithelial cell growth. ... Alitretinoin is an antineoplastic agent. ... Tretinoin is the acid form of vitamin A and so also known as all-trans retinoic acid or ATRA. It is a drug commonly used to treat acne vulgaris and keratosis pilaris. ... Altretamine (also hexalen) is a drug that is used to treat ovarian cancer. ... Amsacrine is an antineoplastic agent. ... Anagrelide (AgrylinÂ®/XagridÂ®, Shire) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). ... R-phrases , , , S-phrases , , , Supplementary data page Structure and properties n, Îµr, etc. ... Asparaginase (EC 3. ... Pegaspargase is an antineoplastic agent. ... Bexarotene is an antineoplastic agent. ... Bortezomib (VelcadeTM) is a first-in-class proteasome inhibitor. ... Denileukin diftitox is an antineoplastic agent. ... Estramustine (EmcytÂ®) is a chemotherapy agent used to treat prostate cancer. ... Masoprocol is an antineoplastic agent. ... Mitotane is a substance used for the rare disease adrenocortical carcinoma. ... For a list of immunosuppressive drugs, see the transplant rejection page. ... A section of the Anatomical Therapeutic Chemical Classification System. ... // Monoclonal antibodies (mAb) are antibodies that are identical because they were produced by one type of immune cell and are all clones of a single parent cell. ... Tumor necrosis factor (TNF) promotes the inflammatory response, which in turn causes many of the clinical problems associated with autoimmune disorders such as rheumatoid arthritis, ankylosing spondylitis, Crohns disease, psoriasis and refractory asthma. ... Infliximab (brand name RemicadeÂ®) is a drug used to treat auto-immune disorders. ... Adalimumab (HumiraÂ®) is the third TNF antagonist (after infliximab and etanercept) to be approved in the US. Like infliximab and etanercept, adalimumab binds to TNFÎ±, preventing it from activating TNF receptors; adalimumab was constructed from a fully human monoclonal antibody, while infliximab is a mouse-human chimeric antibody and etanercept... The introduction to this article provides insufficient context for those unfamiliar with the subject matter. ... Afelimomab (also known as Fab 2) is a anti-TNF-Î± monoclonal antibody. ... Anrulizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat asthma. ... Aselizumab is an immunosuppressive drug. ... Atlizumab is a humanized monoclonal antibody and which its used as an immunosuppressive drug. ... Atorolimumab is an immunosuppressive drug. ... Azulizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat Type 1 diabetes. ... Balizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug to treat HIV/AIDS. Categories: | | ... Basiliximab (Simulect) is a chimeric mouse-human monoclonal antibody to the IL-2RÎ± receptor of T cells. ... Belimumab (marketed under the trade name LymphoStat-B), is a human monoclonal antibody which its used to inhibit TNFÎ±. Categories: | ... Belizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug to treat HIV/AIDS. Categories: | | ... Bertilimumab is a human monoclonal antibody and which its used to treat severe allergic disorders. ... Cedelizumab is an immunosuppressive drug. ... Citilimumab is an immunosuppressive drug. ... Clenoliximab is an immunosuppressive drug. ... Daclizumab (Zenapax) is a murine-human chimaerised monoclonal antibody to the IL-2Rα receptor of T cells. ... Destilimumab is a human monoclonal antibody and which it is used as an immunosuppressive drug. ... Doraglizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat Type 1 diabetes. ... Dorlimomab aritox is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Dorlixizumab is a chimeric/humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Dorlizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat Type 1 diabetes. ... Drinalizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat Type 1 diabetes. ... Durlizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat Type 1 diabetes. ... Eculizumab is a monoclonal antibody directed against the complement protein C5. ... Efalizumab (RaptivaÂ®, Genentech) is a medication used to treat psoriasis. ... Elsilimomab is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Erlizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Faralimomab is a mouse monoclonal antibody which its an immunosuppressive drug. ... Fontolizumab (marketed under the trade name HuZAFâ„¢) is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Galiximab is a chimeric monoclonal antibody which its used as an immunosuppressive drug. ... This article does not cite any references or sources. ... Gavilimomab is a mouse monoclonal antibody (also known as ABX-CBL) is an immunosuppresive drug. ... Golimumab is a human monoclonal antibody which its used as an immunosuppressive drug. ... Gomiliximab is a chimeric monoclonal antibody which its used as an immunosuppressive drug. ... Hylizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug. ... This article does not cite any references or sources. ... Inolimomab is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Ipilimumab (also known as MDX-010) is a human monoclonal antibody being developed by Bristol-Myers Squibb and Medarex which is used as a drug to activate the immune system. ... Keliximab is a chimeric monoclonal antibody which its used as an immunosuppressive drug. ... Lebrilizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat asthma. ... Lerdelimumab is a human monoclonal antibody which its used as an immunosuppressive drug. ... Lucalizumab is a humanized monoclonal antibody which it is used as an immunosuppressive drug. ... Lumiliximab is a chimeric monoclonal antibody which its used as an immunosuppressive drug. ... Maslimomab is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Mepolizumab is a humanized monoclonal antibody and which its used an immunosuppressive drug. ... Metelimumab is a human monoclonal antibody which its used as an immunosuppressive drug. ... Morolimumab is an immunosuppresive drug. ... Muromonab-CD3 (generic name) is a monoclonal antibody (mAb), also known as Orthoclone OKT3 (Brand name). ... Natalizumab is a drug co-marketed by Biogen Idec and Ã‰lan as Tysabri. ... Nerelimomab is a mouse monoclonal antibody and which its used as an immunosuppressive drug. ... Ocrelizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Odulimomab is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Omalizumab (marketed under the name XolairÂ®) is a monoclonal antibody made by Genentech / Novartis and used mainly in allergy-related asthma therapy, with the purpose of reducing allergic hypersensitivity. ... Oteliximab is a chimeric monoclonal antibody and which it is used as an immunosuppressive drug. ... Otelixizumab is a chimeric/humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Pascolizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Pexelizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Reslizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Rovelizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Ruplizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Siplizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Talizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Teglizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Telimomab aritox is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Teneliximab is a chimeric monoclonal antibody which its used as an immunosuppressive drug. ... This article does not cite any references or sources. ... Tilolizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Tocilizumab (marketed under the trade name Actemraâ„¢) is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Toralizumab is a humanized monoclonal antibody which its used as an immunosuppressive drug. ... Tralizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Treglizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Trelizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Trilizumab is a humanized monoclonal antibody which is used as an immunosuppresive drug. ... Ubrelizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug and it is used to treat severe asthma. ... Vapaliximab is a chimeric monoclonal antibody which its used as an immunosuppressive drug. ... Vepalimomab is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Visilizumab (marketed under the trade name NuvionÂ® by PDL BioPharma Inc. ... Xalizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Zanolimumab (marketed under the trade name HuMax-CD4) is a human monoclonal antibody which its used as an immunosuppressive drug. ... Ziralimumab is a human monoclonal antibody which its used as an immunosuppressive drug. ... Zolimomab aritox is a mouse monoclonal antibody which its used as an immunosuppressive drug. ... Zulizumab is a humanized monoclonal antibody which it is used as an immunosuppresive drug. ... Everolimus is a new mTOR inhibitor drug used as an immunosuppressant to prevent rejection of organ transplants. ... // Chemical Designation Common references are: (+-)-15-Deoxyspergualin, 1-Amino-19-guanidino-11-hydroxy-4,9,12-triazanonadecane-10,13-dione, 15-Deoxyspergualin, 15-Deoxyspergualin Hydrochloride, 7-{(Aminoiminomethyl)amino]-N-[2-[[4-[(3-aminopropyl)amino]butyl]amino]-1-hydroxy-2-oxoethyl]heptanamide, Gusperimus (Trihydrochloride), N-[[[4-[(3-Aminopropyl)amino]-butyl]carbamoyl... Pimecrolimus is an immunomodulating agent used in the treatment of atopic dermatitis. ... Sirolimus is a relatively new immunosuppressant drug used to prevent rejection in organ transplantation, and is especially useful in kidney transplants. ... Tacrolimus (also FK-506 or Fujimycin) is a 23-membered macrolide lactone discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. ... A fusion protein is a protein created through genetic engineering from two or more proteins/peptides. ... Abatacept (Orencia) is a first-generation hybrid protein composed of an immunoglobulin and CTLA-4, which is a molecule crucial for T-cell costimulation. ... Alefacept is a genetically engineered immunosuppressive drug sold under the brand name Amevive in Canada and the United States. ... Belatacept is a hybrid protein composed of an immunoglobulin, and CTLA 4, which is a molecule crucial for T-cell costimulation, selectively blocking the process of T-cell activation. ... Tumor necrosis factor (TNF) promotes the inflammatory response, which in turn causes many of the clinical problems associated with autoimmune disorders such as rheumatoid arthritis, ankylosing spondylitis, Crohns disease, psoriasis and refractory asthma. ... Etanercept (EnbrelÂ®, co-marketed by Amgen and Wyeth) is a human recombinant, soluble tumor necrosis factor-alpha (TNFÎ±) receptor. ... // Basic chemical, pharmacological and marketing data Anakinra is an IL-1 receptor antagonist. ... Azathioprine is a chemotherapy drug, now rarely used for chemotherapy but more for immunosuppression in organ transplantation, autoimmune disease such as rheumatoid arthritis or inflammatory bowel disease such as Crohns disease. ... Ciclosporin (INN), cyclosporine or cyclosporin (former BAN), is an immunosuppressant drug. ... // Basic Chemical, Pharmacological, and Marketing Data Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD class of drugs, which are chemically and pharmacologically very heterogen. ... Mycophenolic acid (INN) (IPA: ) or mycophenolate is an immunosuppressant drug used to prevent rejection in organ transplantation. ... This article is about the drug. ...

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