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Encyclopedia > Nelfinavir
Nelfinavir
Systematic (IUPAC) name
2-[2-hydroxy-3-(3-hydroxy-2-methyl-benzoyl) amino-4-phenylsulfanyl-butyl] -N-tert-butyl- 1,2,3,4,4a,5,6,7,8,8a- decahydroisoquinoline-3-carboxamide
Identifiers
CAS number 159989-64-7
ATC code J05AE04
PubChem 64143
DrugBank APRD00003
Chemical data
Formula C32H45N3O4S 
Mol. mass 567.784 g/mol
Physical data
Melt. point 349.94 °C (662 °F)
Pharmacokinetic data
Bioavailability Uncertain; improved by taking with food
Protein binding >98%
Metabolism Hepatic metabolism by CYP450 incl. CYP3A4
Half life 3.5 - 5 hours
Excretion Metabolites eliminated in faeces
Therapeutic considerations
Pregnancy cat.

? Image File history File links Nelfinavir. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... This article is about the chemistry of hydrogen. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, symbol, number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, period, block 16, 2, p Appearance colorless (gas) pale blue (liquid) Standard atomic weight 15. ... This article is about the chemical element. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... The melting point of a crystalline solid is the temperature range at which it changes state from solid to liquid. ... 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 pharmacokinetic properties of drugs. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The biological half-life of a substance is the time required for half of that substance to be removed from an organism by either a physical or a chemical process. ... The kidneys are important excretory organs in vertebrates. ... 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. ...

Legal status
Routes  ?

Nelfinavir (Viracept®) is an antiretroviral drug used in the treatment of the human immunodeficiency virus (HIV). Nelfinavir belongs to the class of drugs known as protease inhibitors (PIs) and like other PIs is generally used in combination with other antiretroviral drugs. Nelfinavir is presented as the mesilate (mesylate) ester prodrug. The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... 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. ... HAART redirects here. ... The human immunodeficiency virus (HIV) is a frequently mutating retrovirus that attacks the human immune system and which has been shown to cause acquired immune deficiency syndrome (AIDS). ... Protease inhibitors are a class of medication used to treat or prevent viral infections. ... For other uses, see Ester (disambiguation). ... A prodrug is a pharmacological substance (drug) which is administered in an inactive (or significantly less active) form. ...


Nelfinavir mesylate (Viracept, formally AG1343) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2nM) and is being widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. Nelfinavir mesylate contains the Castor oil derivative Cremophor EL.[1] HIV-1 protease is an aspartyl protease that is essential for the life-cycle of HIV. Inhibition of this protease prevents maturation of HIV particles. ... Species Human immunodeficiency virus 1 Human immunodeficiency virus 2 Human immunodeficiency virus (HIV) is a retrovirus that causes acquired immunodeficiency syndrome (AIDS, a condition in humans in which the immune system begins to fail, leading to life-threatening opportunistic infections). ... Castor oil is a vegetable oil obtained from the castor bean (technically castor seed as the castor plant, Ricinus communis, is not a member of the bean family). ... Cremophor EL is polyethoxylated castor oil. ...

Contents

History

Nelfinavir was developed by Agouron Pharmaceuticals as part of a joint venture with Japan Tobacco. Agouron Pharmaceuticals was acquired by Warner Lambert in 1999 and is now a subsidiary of Pfizer. It is marketed in Europe by Hoffman-La Roche. The Food and Drug Administration approved it for therapeutic use on March 14, 1997, making it the twelfth approved antiretroviral. It never secured a large market share and newer PIs are generally preferred for first-line therapy. Hoffmann-La Roche, Ltd. ... “FDA” redirects here. ... is the 73rd day of the year (74th in leap years) in the Gregorian calendar. ... For the band, see 1997 (band). ...


Agouron's patent on the drug will expire in 2014. For other uses, see Patent (disambiguation). ...


On the 6th June 2007 both the Medicines and Healthcare products Regulatory Agency and the European Medicines Agency[2] put out an alert requesting the recall of any of the drug in circulation because of fears that batches of the therapy may have been contaminated with potentially cancer-causing chemicals The logo of the MHRA. The Medicines and Healthcare products Regulatory Agency (MHRA) is the UK government agency which is responsible for ensuring that medicines and medical devices work and are acceptably safe. ... The European Medicines Agency (EMEA) is a European agency for the evaluation of medicinal products. ...


Nelfinavir is currently under investigation for potential repositioning as an anti-cancer agent. When applied to cancer cells in culture, both apoptotic and non-apoptotic cell death is observed. However, there is no evidence that Nelfinavir actually targets cancer cells within a native tumor in a person. [3]


Pharmacology

Nelfinavir should be taken with food. The bioavailability of Nelfinavir is increased 2.5 to 5 times when taken with food.[citation needed] Taking the drug with food also decreases the risk of diarrhea as a side effect. 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 διάρροια; literally meaning through-flowing). Acute infectious diarrhea is a common cause...


Mode of action

Nelfinavir is a protease inhibitor: it inhibits HIV-1 and HIV-2 proteases. This protease is an enzyme which cleaves viral protein molecules into smaller fragments, and it is vital for both the replication of the virus within the cell and also the release of mature viral particles from an infected cell. Though this mode of action is common to all protease inhibitors, the precise mode of binding of nelfinavir to the enzyme may be sufficiently unique to reduce cross-resistance between it and other PIs. Also, not all PIs inhibit both HIV-1 and HIV-2 proteases. Protease inhibitors are a class of medication used to treat or prevent viral infections. ... HIV-1 protease is an aspartyl protease that is essential for the life-cycle of HIV. Inhibition of this protease prevents maturation of HIV particles. ...


Toxicity

Nelfinavir can produce a range of adverse effects. Common (experienced by more than one in one hundred patients; greater than 1%) are flatulence, diarrhea or abdominal pain. Infrequent (experienced by one in one thousand to one in one hundred patients; 0.01 - 0.1%) adverse effects are fatigue, urination, rash, mouth ulcers or hepatitis. Rarely (less than one in one thousand patients; under 0.01%) nephrolithiasis, arthralgia, Leukopenia, pancreatitis or allergic reactions may occur. 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 διάρροια; literally meaning through-flowing). Acute infectious diarrhea is a common cause... A rash is a change in skin which affects its color, appearance, or texture. ... Mouth ulcer on the lower lip A mouth ulcer (from Latin ulcus) is the name for the appearance of an open sore inside the mouth caused by a break in the mucous membrane or the epithelium on the lips or surrounding the mouth. ... Hepatitis (plural hepatitides) implies injury to liver characterised by presence of inflammatory cells in the liver tissue. ... Kidney stones are solid accretions (crystals) of dissolved minerals in urine found inside the kidneys or ureters. ... This article does not cite any references or sources. ... Leukopenia or leukocytopenia refers to a decrease in the number of circulating white blood cells (leukocytes) in the blood. ... Pancreatitis is inflammation of the pancreas. ... Allergy is an abnormal reaction to a substance foreign to the body that is acquired, predictable and rapid. ...


Interactions

Nelfinavir's interaction profile is similar to that of other protease inhibitors. Most interactions occur at the level of the Cytochrome P450 isozymes 3A4 and CYP2C19, by which nelfinavir is metabolised. HAART redirects here. ... Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ... Cytochrome P450 2C19 (abbreviated CYP2C19), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. ...


See also

HIV-1 protease is an aspartyl protease that is essential for the life-cycle of HIV. Inhibition of this protease prevents maturation of HIV particles. ... Cremophor EL is polyethoxylated castor oil. ... Castor oil is a vegetable oil obtained from the castor bean (technically castor seed as the castor plant, Ricinus communis, is not a member of the bean family). ...

References

  1. ^ Circulating metabolites of the Human Immunodeficiency Virus Protese Inhibitor Nelfinavir in Humans:. PubMed. Retrieved on 2007-01-07.
  2. ^ Press release from the European Medicines Agency regarding possible genotoxic ethyl mesylate contamination
  3. ^ J.J. Gills et al. (2007). "Nelfinavir, A Lead HIV Protease Inhibitor, Is a Broad-Spectrum, Anticancer Agent that Induces Endoplasmic Reticulum Stress, Autophagy, and Apoptosis In vitro and In vivo". Clinical Cancer Research 13: 5183-5194. 

Pai VB, Nahata MC. Nelfinavir mesylate: a protease inhibitor. Ann Pharmacother 1999; 33: 325–39. Year 2007 (MMVII) is the current year, a common year starting on Monday of the Gregorian calendar and the AD/CE era in the 21st century. ... is the 7th day of the year in the Gregorian calendar. ... The European Medicines Agency (EMEA) is a European agency for the evaluation of medicinal products. ...


Bardsley-Elliot A, Plosker GL. Nelfinavir: an update on its use in HIV infection. Drugs 2000; 59: 581–620.


  Results from FactBites:
 
Viracept Online, Description, Chemistry, Ingredients - Nelfinavir Mesylate - RxList Monographs (788 words)
(nelfinavir mesylate) is an inhibitor of the human immunodeficiency virus (HIV) protease.
Nelfinavir mesylate is a white to off-white amorphous powder, slightly soluble in water at pH
The overall incidence of the D30N mutation in the viral protease of evaluable isolates (n=157) from patients receiving nelfinavir monotherapy or nelfinavir in combination with zidovudine and lamivudine or stavudine was 54.8%.
Nelfinavir (607 words)
The effect of nelfinavir on the clinical progression of HIV infection, including the effect on the incidence of opportunistic infections or on overall survival, remains to be established.
Nelfinavir is one of a class of drugs called protease (pro' tee ace) inhibitors, which slow the spread of HIV infection in the body.
Nelfinavir is not a cure and does not prevent the spread of HIV infection to other people, so use precautions to avoid the spread of this infection.
  More results at FactBites »

 
 

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