nelfinavir
American Heritage Dictionary:
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nel·fin·a·vir
(nĕl-fĭn'ə-vîr) 
n.
A protease-inhibiting drug usually used in combination with other drugs to suppress the replication of HIV.
n.
A protease-inhibiting drug usually used in combination with other drugs to suppress the replication of HIV.
[nelfi-, of unknown origin + -navir, protease inhibitor suff. (from SAQUINAVIR).]
Drug Info:
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Nelfinavir
Brand names: Viracept®
Chemical formula:
- Drug Forms:
- Nelfinavir Mesylate Oral tablet (below)
- Nelfinavir Mesylate Oral suspension
Nelfinavir Mesylate Oral tablet
What is this medicine?
NELFINAVIR (nel FIN a veer) is an antiretroviral medicine. It is used with other medicines to treat HIV. This medicine is not a cure for HIV. It will not stop the spread of HIV to others.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•diabetes
•hemophilia
•liver disease
•an unusual or allergic reaction to nelfinavir, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take this medicine with food. If you cannot swallow the tablets you can dissolve them in water. Put the tablets in a small amount of water. Stir until the tablets dissolve and drink all of the solution immediately. Rinse the glass and drink the rinse to get the full dose. Take your medicine at regular intervals. Do not take your medicine more often than directed. For your anti-HIV therapy to work as well as possible, take each dose exactly as prescribed. Do not skip doses or stop your medicine even if you feel better. Skipping doses may make the HIV virus resistant to this medicine and other medicines. Do not stop taking except on your doctor's advice.
Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 2 years old for selected conditions, precautions do apply.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
Do not take this medicine with any of the following medications:
•amiodarone
•cisapride
•dofetilide
•eplerenone
•lovastatin
•medicines for headaches like dihydroergotamine, ergonovine, ergotamine, methylergonovine
•midazolam
•omeprazole
•pimozide
•quinidine
•ranolazine
•red yeast rice
•rifampin
•rifapentine
•simvastatin
•St. John's wort
•triazolam
This medicine may also interact with the following medications:
•azithromycin
•birth control pills or patch
•cyclosporine
•fluticasone
•medicines for cholesterol like atorvastatin, fluvastatin, rosuvastin
•medicines for erectile dysfunction like sildenafil
•medicines for seizures
•methadone
•other medicines for HIV
•rifabutin
•sirolimus
•tacrolimus
•trazodone
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular check ups. Discuss any new symptoms with your doctor. You will need to have important blood work done while on this medicine.
HIV is spread to others through sexual or blood contact. Talk to your doctor about how to stop the spread of HIV.
Birth control pills may not work properly while you are taking this medicine. Talk to your doctor about using an extra method of birth control. Women who can still have children must use a reliable form of barrier contraception, like a condom or diaphragm.
This medicine may affect blood sugar levels. If you have diabetes, check with your doctor or health care professional before you change your diet or the dose of your diabetic medicine.
This medicine contains a chemical that may increase your risk of cancer. Pregnant women and children may need to use a different HIV medicine. Women should inform their doctor if they wish to become pregnant or think they might be pregnant. Talk to your health care professional or pharmacist for more information.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing difficulty
•fever
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•diarrhea
•increased hunger or thirst
•increased urination
•nausea, vomiting
•skin rash
•stomach upset, gas
•unusually weak or tired
•weight gain around waist, back, or thinning of face, arms, legs
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
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nelfinavir
A protease inhibitor (see antiviral drugs) that is used in combination with other antiretroviral drugs for the treatment of HIV infection. It is available, on prescription only, as tablets.
Side effects:
include diarrhoea, flatulence, nausea, rashes, reduced white-blood-cell count, and hepatitis.
Precautions:
nelfinavir should not be taken by women who are breastfeeding. It should be used with caution in people with kidney or liver disease, haemophilia, or diabetes and in pregnant women.
Interactions with other drugs:
nelfinavir is a potent inhibitor of several enzyme systems in the liver that are involved in metabolizing drugs; it therefore has the potential to interact with many drugs. A doctor should be consulted before taking nelfinavir with any other drug.
Proprietary preparation:
Viracept.
| nelarabine, nefopam, nedocromil sodium | |
| neomycin sulphate, neostigmine, nepafenac |
Wikipedia on Answers.com:
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Nelfinavir
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| Systematic (IUPAC) name | |
| (3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylphenyl)formamido]-4-(phenylsulfanyl)butyl]-decahydroisoquinoline-3-carboxamide | |
| Clinical data | |
| Trade names | Viracept |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a697034 |
| Licence data | US FDA:link |
| Pregnancy cat. | B (US) |
| Legal status | ℞-only (US) |
| Routes | oral |
| 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 |
| Identifiers | |
| CAS number | 159989-64-7  |
| ATC code | J05AE04 |
| PubChem | CID 64143 |
| DrugBank | DB00220 |
| ChemSpider | 57718 |
| UNII | HO3OGH5D7I |
| KEGG | D08259 |
| ChEMBL | CHEMBL1159655  |
| NIAID ChemDB | 028590 |
| Chemical data | |
| Formula | C32H45N3O4S |
| Mol. mass | 567.784 g/mol |
| SMILES | eMolecules & PubChem |
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| Physical data | |
| Melt. point | 349.94 °C (662 °F) |
 (what is this?) (verify) |
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Nelfinavir (brand name 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 mesylate (Viracept, formally AG1343) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.[1]
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Contents
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History
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This section needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (April 2011) |
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 and elsewhere by ViiV Healthcare.
The U.S. Food and Drug Administration (FDA) approved it for therapeutic use on March 14, 1997,[citation needed] making it the twelfth[citation needed] approved antiretroviral. The initial product launched proved to be the largest[citation needed] "biotech launch" in the history of the pharmaceutical industry, achieving first full year sales exceeding $US335M.[citation needed] Agouron's patent on the drug will expire in 2014.[citation needed]
On the 6 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 some batches may have been contaminated with potentially cancer-causing chemicals.
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.
Mode of action
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This unreferenced section requires citations to ensure verifiability. |
Nelfinavir is a protease inhibitor: it inhibits HIV-1 and HIV-2 proteases. This protease[which?] is an enzyme which splits viral protein molecules into smaller fragments, and it is vital to both the replication of the virus within the cell, and also to the release of mature viral particles from an infected cell. Though this mode of action[clarification needed] is common to all protease inhibitors, the precise mode of binding of Nelfinavir to the enzyme may be sufficiently unique to reduce cross-resistance[clarification needed] between it and other PIs. Also, not all PIs inhibit both HIV-1 and HIV-2 proteases.
Toxicity
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This unreferenced section requires citations to ensure verifiability. |
Nelfinavir can produce a range of adverse side effects. Flatulence, diarrhea or abdominal pain are common (i.e. experienced by more than one in one hundred patients). Fatigue, urination, rash, mouth ulcers or hepatitis are less frequent effects (experienced by one in one thousand to one in one hundred patients). Nephrolithiasis, arthralgia, Leukopenia, pancreatitis or allergic reactions may occur, but are rare (less than one in one thousand patients) .
Potential anti-cancer activity
Nelfinavir were under investigation, in 2009, for potential use as an anti-cancer agent.[3] When applied to cancer cells in culture (in vitro), it can inhibit the growth of a variety cancer types and can trigger cell death (apoptosis). [4] When Nelfinavir was given to laboratory mice with tumors of the prostate or of the brain, it could suppress tumor growth in these animals. [5][6] In vitro tests showed it may work well with sorafenib[7]
In the United States, several clinical trials were conducted in 2008 that sought to verify whether nelfinavir is effective as a cancer therapeutic agent in humans.[8] In some of these trials, nelfinavir was used alone in monotherapy fashion, whereas in others it was combined with other modes of cancer therapy, such as well-established chemotherapeutic agents or radiation therapy.
Good phase I results were obtained for locally advanced pancreatic cancer.[9]
In the UK, in 2010, a phase I trial (of nelfinavir with radiotherapy), on patients with inoperable cancer, showed a doubling of survival times, and six patients had tumor regression to the extent that they became operable.[10]
Interactions
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This unreferenced section requires citations to ensure verifiability. |
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.
See also
References
- ^ Zhang KE, Wu E, Patick AK, et al. (April 2001). "Circulating metabolites of the human immunodeficiency virus protease inhibitor nelfinavir in humans: structural identification, levels in plasma, and antiviral activities". Antimicrob. Agents Chemother. 45 (4): 1086–93. DOI:10.1128/AAC.45.4.1086-1093.2001. PMC 90428. PMID 11257019. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=90428.
- ^ Press release from the European Medicines Agency regarding possible genotoxic ethyl mesylate contamination
- ^ Chow WA, Jiang C, Guan M (2009). "Anti-HIV drugs for cancer therapeutics: back to the future?". Lancet Oncol 10 (1): 61–71. DOI:10.1016/S1470-2045(08)70334-6. PMID 19111246.
- ^ Gills, JJ; Lopiccolo, J; Tsurutani, J; Shoemaker, RH; Best, CJM; Abu-Asab, MS; Borojerdi, J; Warfel, NA et al. (September 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 : an Official Journal of the American Association for Cancer Research 13 (17): 5183–94. DOI:10.1158/1078-0432.CCR-07-0161. PMID 17785575. http://clincancerres.aacrjournals.org/content/13/17/5183.full.pdf+html.
- ^ Pyrko, P.; Kardosh, A; Wang, W; Xiong, W; Schönthal, AH; Chen, TC (2007). "HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma death by triggering endoplasmic reticulum stress". Cancer Research 67 (22): 10920–10928. DOI:10.1158/0008-5472.CAN-07-0796. PMID 18006837.
- ^ Yang, Y; Ikezoe, T; Takeuchi, T; Adachi, Y; Ohtsuki, Y; Takeuchi, S; Koeffler, HP; Taguchi, H (July 2005). "HIV-1 protease inhibitor induces growth arrest and apoptosis of human prostate cancer LNCaP cells in vitro and in vivo in conjunction with blockade of androgen receptor STAT3 and AKT signaling". Cancer Science 96 (7): 425–33. DOI:10.1111/j.1349-7006.2005.00063.x. PMID 16053514.
- ^ Brüning, A; Burger, P; Vogel, M; Gingelmaier, A; Friese, K; Burges, A (October 2010). "Nelfinavir induces mitochondria protection by ERK1/2-mediated mcl-1 stabilization that can be overcome by sorafenib". Investigational New Drugs 28 (5): 535–42. DOI:10.1007/s10637-009-9281-1. PMID 19554262.
- ^ http://clinicaltrials.gov/ct2/results?term=Nelfinavir+cancer
- ^ Brunner, TB; Geiger, M; Grabenbauer, GG; Lang-Welzenbach, M; Mantoni, TS; Cavallaro, A; Sauer, R; Hohenberger, W et al. (June 2008). "Phase I trial of the human immunodeficiency virus protease inhibitor nelfinavir and chemoradiation for locally advanced pancreatic cancer". Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology 26 (16): 2699–706. DOI:10.1200/JCO.2007.15.2355. PMID 18509182. http://jco.ascopubs.org/content/26/16/2699.full.pdf.
- ^ "'Last year, I was dying of cancer. Now I might be cured'". The Sunday Telegraph. 28 November 2010. http://www.telegraph.co.uk/news/telegraphchristmasappeal/8164996/Telegraph-Christmas-Appeal-Last-year-I-was-dying-of-cancer.-Now-I-might-be-cured.html.
- Pai, VB; Nahata, MC (March 1999). "Nelfinavir mesylate: a protease inhibitor". The Annals of Pharmacotherapy 33 (3): 325–39. DOI:10.1345/aph.18089. PMID 10200859.
- Bardsley-Elliot, A; Plosker, GL (March 2000). "Nelfinavir: an update on its use in HIV infection". Drugs 59 (3): 581–620. DOI:10.2165/00003495-200059030-00014. PMID 10776836.
- Actual photo of Nelfinavir and further Nelfinavir information
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American Heritage Dictionary
The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.
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Oxford A-Z of Medicinal Drugs
Market University Press. © 2000, 2003, 2010 An A-Z of Medicinal Drugs. All rights reserved.
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