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Combretastatin A-4 Phosphate
Fosbretabulin (also known as combretastatin A-4 phosphate or CA4P) is a microtubule destabilizing experimental drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumours causing central necrosis. It is a derivative of combretastatin. It is formulated as the salts fosbretabulin disodium and fosbretabulin tromethamine. Fosbretabulin is a prodrug. ''In vivo'', it is dephosphorylated to its active metabolite, combretastatin A-4. In July 2007, the pharmaceutical company OXiGENE initiated a 180-patient phase III clinical trial of fosbretabulin in combination with carboplatin for the treatment of anaplastic thyroid cancer. There is currently no fully FDA approved treatment for this form of cancer. By 2017, it had completed multiple clinical trials (e.g. for solid tumours, non-small cell lung cancer) with more in progress. See also * Combretastatin Combretastatin is a dihydrostilbenoid found in '' Combretum caffrum''. As ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vascular-targeting Agent
A vascular-targeting agent (VTA) or vascular disrupting agent (VDA) is a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis. VTAs can be small-molecule or ligand-based. Small-molecule VTAs include: * microtubule destabilizing drugs such as combretastatin A-4 disodium phosphate (CA4P), ZD6126, AVE8062, Oxi 4503 * vadimezan (ASA404) Clinical trials Phase II : ZD6126, CA4P, plinabulin Plinabulin (provisional name BPI-2358, formerly NPI-2358) is a small molecule under development by BeyondSpring Pharmaceuticals, and is in a world-wide Phase 3 clinical trial for non-small cell lung cancer. Plinabulin is being investigated for th ... (NPI-2358) Phase III : DMXAA (ASA404). References {{antineoplastic-drug-stub Cancer treatments Drugs acting on the cardiovascular system ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Combretastatin
Combretastatin is a dihydrostilbenoid found in '' Combretum caffrum''. As a class Combretastatins are a class of natural phenols. A variety of different natural combretastatin molecules are present in the bark of '' Combretum caffrum'', commonly known as South African Bush Willow. Despite having a similar name, combretastatins are unrelated to statins, a family of cholesterol lowering drugs. Natural combretastatins Molecules that fall into the combretastatin family generally share 3 common structural features: a trimethoxy "A"-ring, a "B"-ring containing substituents often at C3' and C4', and ftenan ethene bridge between the two rings which provides necessary structural rigidity. Molecules with such an ethene bridge are also stilbenoids, molecules with a non-ethene bridge are dihydrostilbenoids. Molecules with C3' amino and hydroxyl substituents are very active, and molecules with C4' hydroxyl or methoxy substituents are also cytotoxic. Of the natural products presently kn ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmaceutical Formulation
Pharmaceutical formulation, in pharmaceutics, is the process in which different chemical substances, including the active drug, are combined to produce a final medicinal product. The word ''formulation'' is often used in a way that includes dosage form. Stages and timeline Formulation studies involve developing a preparation of the drug which is both stable and acceptable to the patient. For orally administered drugs, this usually involves incorporating the drug into a tablet or a capsule. It is important to make the distinction that a tablet contains a variety of other potentially inert substances apart from the drug itself, and studies have to be carried out to ensure that the encapsulated drug is compatible with these other substances in a way that does not cause harm, whether direct or indirect. Preformulation involves the characterization of a drug's physical, chemical, and mechanical properties in order to choose what other ingredients (excipients) should be used in the pre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salt (chemistry)
In chemistry, a salt is a chemical compound consisting of an ionic assembly of positively charged cations and negatively charged anions, which results in a compound with no net electric charge. A common example is table salt, with positively charged sodium ions and negatively charged chloride ions. The component ions in a salt compound can be either inorganic, such as chloride (Cl−), or organic, such as acetate (). Each ion can be either monatomic, such as fluoride (F−), or polyatomic, such as sulfate (). Types of salt Salts can be classified in a variety of ways. Salts that produce hydroxide ions when dissolved in water are called ''alkali salts'' and salts that produce hydrogen ions when dissolved in water are called ''acid salts''. ''Neutral salts'' are those salts that are neither acidic nor basic. Zwitterions contain an anionic and a cationic centre in the same molecule, but are not considered salts. Examples of zwitterions are amino acids, many metabolites, peptid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prodrug
A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, salicin is a β-D-glucopyranosid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
In Vivo
Studies that are ''in vivo'' (Latin for "within the living"; often not italicized in English) are those in which the effects of various biological entities are tested on whole, living organisms or cells, usually animals, including humans, and plants, as opposed to a tissue extract or dead organism. This is not to be confused with experiments done ''in vitro'' ("within the glass"), i.e., in a laboratory environment using test tubes, Petri dishes, etc. Examples of investigations ''in vivo'' include: the pathogenesis of disease by comparing the effects of bacterial infection with the effects of purified bacterial toxins; the development of non-antibiotics, antiviral drugs, and new drugs generally; and new surgical procedures. Consequently, animal testing and clinical trials are major elements of ''in vivo'' research. ''In vivo'' testing is often employed over ''in vitro'' because it is better suited for observing the overall effects of an experiment on a living subject. In dr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Active Metabolite
An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide). Certain drugs such as codeine and tramadol have metabolites (morphine and ''O''-desmethyltramadol respectively) that are stronger than the parent drug and in these cases the metabolite may be responsible for much of the therapeutic action of the parent drug. Sometimes, however, metabolites may produce toxic effects and patients must be monitored carefully to ensure they do not build up in the body. This is an issue with some well-known drugs, such as pethidine (meperidine) and dextropropoxyphene. Prodrugs Sometimes drugs are formulated in an inactive form that is designe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Combretastatin A-4
Combretastatin A-4 is a combretastatin and a stilbenoid. It can be isolated from '' Combretum caffrum'', the Eastern Cape South African bushwillow tree or in '' Combretum leprosum'', the mofumbo, a species found in Brazil. Function Tubulin represents a potent target in cancer chemotherapy, given its role in cell division. Combretastatin is a naturally occurring well known tubulin polymerization inhibitor. Combretastatin A-4 comes in two stereoisomers (cis (shown top right), and trans); The cis form binds much better to the 'colchicine' site on tubulin to inhibit polymerization. Derivatives Combretastatin A-4 is the active component of combretastatin A-4 phosphate, a prodrug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis. A large number of synthetic derivatives have been reported, including beta-lactam A beta-lactam (β-lactam) ring is a four-membered lactam. A ''lactam'' is a cyclic amide, and ''beta''-lactams are named so be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carboplatin
Carboplatin, sold under the trade name Paraplatin among others, is a chemotherapy medication used to treat a number of forms of cancer. This includes ovarian cancer, lung cancer, head and neck cancer, brain cancer, and neuroblastoma. It is used by injection into a vein. Side effects generally occur. Common side effects include low blood cell levels, nausea, and electrolyte problems. Other serious side effects include allergic reactions and increased future risk of another cancer. Use during pregnancy may result in harm to the baby. Carboplatin is in the platinum-based antineoplastic family of medications and works by interfering with duplication of DNA. Carboplatin was patented in 1972 and approved for medical use in 1989. It is on the World Health Organization's List of Essential Medicines. Medical uses Carboplatin is used to treat a number of forms of cancer. This includes ovarian cancer, lung cancer, head and neck cancer, brain cancer, and neuroblastoma. It may be used fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anaplastic Thyroid Cancer
Anaplastic thyroid cancer (ATC), also known as anaplastic thyroid carcinoma, is an aggressive form of thyroid cancer characterized by uncontrolled growth of cells in the thyroid gland. This form of cancer generally carries a very poor prognosis due to its aggressive behavior and resistance to cancer treatments. The cells of anaplastic thyroid cancer are highly abnormal and usually no longer resemble the original thyroid cells and have poor differentiation. ATC is an uncommon form of thyroid cancer only accounting for 1-2% of cases, but due to its high mortality, is responsible for 20-50% of deaths from thyroid cancer. The median survival time after diagnosis is three to six months. Some studies report that 10% to 15% survive more than 1 year; 3-year and 5-year survival is very rare. It occurs more commonly in women than in men and is seen most commonly in people ages 40 to 70. Signs and symptoms Anaplastic thyroid cancer typically manifests as a rapidly enlarging neck mass. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Combretastatin
Combretastatin is a dihydrostilbenoid found in '' Combretum caffrum''. As a class Combretastatins are a class of natural phenols. A variety of different natural combretastatin molecules are present in the bark of '' Combretum caffrum'', commonly known as South African Bush Willow. Despite having a similar name, combretastatins are unrelated to statins, a family of cholesterol lowering drugs. Natural combretastatins Molecules that fall into the combretastatin family generally share 3 common structural features: a trimethoxy "A"-ring, a "B"-ring containing substituents often at C3' and C4', and ftenan ethene bridge between the two rings which provides necessary structural rigidity. Molecules with such an ethene bridge are also stilbenoids, molecules with a non-ethene bridge are dihydrostilbenoids. Molecules with C3' amino and hydroxyl substituents are very active, and molecules with C4' hydroxyl or methoxy substituents are also cytotoxic. Of the natural products presently kn ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
