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Nelfinavir
drug data and news
Nelfinavir drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Nelfinavir | ||
| Brand Names/Synonyms | 1UN; AG1346; NELFINAVIR MESYLATE AG1343; NFV; NLF; Nelfinavir; Nelfinavir Mesylate; Nelfinavir [Inn:Ban]; Viracept | ||
| Indication | For the treatment of HIV infection. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Nelfinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs. | ||
| Mechanism Of Action | Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. | ||
| Nelfinavir News (When available) |
CROI: Saquinavir-based combination prevents mother-to-child HIV ... Feb 22, 2006 Restoration of CD4 T-cells limited in children starting HIV ... Mar 2, 2006 CROI: Studies begin to identify genes linked to metabolic and body ... Feb 26, 2006 US, Brazil Dispute Patent Protection Feb 24, 2006 CROI: Study reveals widespread misunderstandings about post ... Feb 10, 2006 Gilead Sciences Welcomes Guidance From Nice On Treatment Of ... Feb 22, 2006 Adolescents Adherence to HIV Regimens Falls Short of Optimal ... Feb 7, 2006 Impaired Glucose Tolerance Frequent Among HIV-Infected Pregnant ... Feb 10, 2006 Schering-Plough Presents Vicriviroc Clinical Study Results at 13th ... Feb 10, 2006 Multi-component drug delivery system: An emerging trend Feb 8, 2006 Multi-component drug delivery system: An emerging trend Feb 8, 2006 Adolescents Adherence to HIV Regimens Falls Short of Optimal ... Feb 7, 2006 Roche to share know-how in making protease inhibitors with poorest ... Jan 13, 2006 Most people given non-occupational PEP fully adhere to their ... Jan 19, 2006 FDA Approves EMEND(R) (aprepitant), in Combination with Other ... Jan 11, 2006 HIV Drug Resistance Linked to Viral Fitness Jan 12, 2006 Procyon reports new data for its lead HIV protease inhibitor, PPL ... Nov 16, 2005 Drugs, not host or immune system, create conditions for fat loss Nov 15, 2005 Once-daily boosted saquinavir has low blood levels when used with ... Nov 11, 2005 UK HIV patients have high levels of primary drug resistance Nov 18, 2005 Patients switching from other PIs to unboosted atazanavir maintain ... Nov 22, 2005 Shortage of antiretroviral drugs in Ghana No cause for alarm ... ... Oct 21, 2005 Switch to Atazanavir Normalizes Aberrant Cholesterol Values ... Oct 13, 2005 This week in the medical journals Sep 29, 2005 HCV/HIV coinfection guidelines may lead to unnecessarily premature ... Sep 26, 2005 Nonoccupational HIV Postexposure Prophylaxis—Reply Oct 5, 2005 This week in the medical journals Sep 29, 2005 New ways to fight AIDS in Brazil Sep 28, 2005 Discordant CD4 increase of 25 cells/mm 3 confers clinical benefit ... Sep 26, 2005 HIV Drug Boosts Immune System Sharply Sep 23, 2005 Antiretroviral therapy enhances production of new T-cells ... Sep 8, 2005 Genetic test can help predict who will develop hyperbilirubinaemia Sep 13, 2005 Antiretroviral therapy enhances production of new T-cells ... 08 Sep 2005 In this thing together Sep 1, 2005 Drug interactions with the pill Aug 31, 2005 Brazil advised to break patent on AIDS drugs Aug 23, 2005 IAS: Study in Côte d’Ivoire describes factors associated with ... Aug 3, 2005 Newest HIV drugs should be used with FUZEON(R Jul 27, 2005 IAS: Have we prematurely discarded triple NRTI regimens? Jul 27, 2005 Brazil pact on AIDS drugs lauded Jul 11, 2005 | ||
| Dosage Forms | Tablets, Oral powder | ||
| Drug_Category | Anti-HIV Agents; HIV Protease Inhibitors; ATC:J05AE04 | ||
| Absorption | Well absorbed | ||
| Interactions | DRUG INTERACTIONS Nelfinavir is an inhibitor of CYP3A (cytochrome P450 3A). Coadministration of VIRACEPT and drugs primarily metabolized by CYP3A (e.g., dihydropyridine calcium channel blockers) may result in increased plasma concentrations of the other drug that could increase or prolong both its therapeutic and adverse effects. Nelfinavir is metabolized in proof by C.P.A. Coadministration of VIRACEPT and drugs that induce CYP3A may decrease nelfinavir plasma concentrations and reduce its therapeutic effect. Coadministration of VIRACEPT and drugs that inhibit CYP3A may increase nelfinavir plasma concentrations. Based on known metabolic profiles, clinically significant drug interactions are not expected between VIRACEPT and dapsone, trimethoprim/sulfamethoxazole, clarithromycin, erythromycin, itraconazole or fluconazole. Drugs That Should Not Be Coadministered With VIRACEPT Antiarrhythmics: amiodarone, quinidine Antihistamines: astemizole, terfenadine Antimigraine: ergot derivatives Antimycobacterial agents: rifampin Benzodiazepines midazolam, triazolam GI motility agents: cisapride Drugs Which Require a Dose Reduction When Coadminstered With VIRACEPT Antimycobacterial agents: rifabutin Other Potentially Clinically Significant Drug Interactions With VIRACEPT* Anticonvulsants: carbamazepine, phenobarbital, phenytoin May decrease nelfinavir plasma concentrations** Anti-HIV protease inhibitors: indinavir, ritonavir May increase nelfinavir plasma concentrations Oral contraceptives: ethinyl estradiol, norethindrone Plasma concentrations may be decreased by VIRACEPT * This table is not all inclusive ** VIRACEPT may not be effective due to decreased nelfinavir plasma concentrations in patients taking these agents concomitantly Antihistamines Terfenadine: Administration of terfenadine with VIRACEPT resulted in the appearance of unchanged terfenadine in plasma; therefore, VIRACEPT should not be administered concurrently with terfenadine because of the potential for serious and/or life-threatening cardiac arrhythmias. Because a similar interaction is likely, VIRACEPT should also not be administered concurrently with astemizole. Anti-HIV Protease Inhibitors Indinavir: Coadministration of indinavir with VIRACEPT resulted in an 83% increase in nelfinavir plasma AUC and a 51% increase in indinavir plasma A.C. Currently, there are no safety and efficacy data available from the use of this combination. Ritonavir: Coadministration of ritonavir with VIRACEPT resulted in a 152% increase in nelfinavir plasma AUC and very little change in ritonavir plasma A.C. Currently, there are no safety and efficacy data available from the use of this combination. Saquinavir: Coadministration of saquinavir (using an experimental soft-gelatin capsule formulation of saquinavir 1200mg) with VIRACEPT resulted in an 18% increase in nelfinavir plasma AUC and a 4-fold increase in saquinavir plasma A.C. If used in combination with saquinavir hard gelatin capsules at the recommended dose of 600 mg tid, no dose adjustments are needed. Currently, there are no safety and efficacy data available from the use of this combination. Antifungal Agents Ketoconazole: Coadministration of ketoconazole with VIRACEPT resulted in a 35% increase in nelfinavir plasma A.C. This change was not considered clinically significant and no dose adjustment is needed when ketoconazole and VIRACEPT are coadministered. Anti-HIV Reverse Transcriptase Inhibitors Didanosine: It is recommended that didanosine be administered on an empty stomach; therefore, nelfinavir should be administered (with food) one hour after or more than two hours before didanosine. Zidovudine: Coadministration of zidovudine and lamivudine with VIRACEPT resulted in a 35% decrease in zidovudine plasma A.C. A dose adjustment is not needed when zidovudine is administered with VIRACEPT. Little or no change in the pharmacokinetics of either drug was observed when VIRACEPT was coadministered with lamivudine or stavudine. Antimycobacterial Agents Rifabutin: Coadministration of rifabutin and VIRACEPT resulted in a 32% decrease in nelfinavir plasma AUC and a 207% increase in rifabutin plasma A.C. It is recommended that the dose of rifabutin be reduced to one-half the usual dose when administered with VIRACEPT. Rifampin: Coadministration of rifampin and VIRACEPT resulted in an 82% decrease in nelfinavir plasma A.C. VIRACEPT and rifampin should not be coadministered. Oral Contraceptives Ethinyl Estradiol and Norethindrone: Coadministration of VIRACEPT with OVCON-35 resulted in a 47% decrease in ethinyl estradiol and an 18% decrease in norethindrone plasma concentrations. Alternate or additional contraceptive measures should be used during therapy with VIRACEPT | ||
| Toxicity | LD50 >5g/kg (rat). Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin | ||
| Organisms Affected | Human immunodeficiency virus | ||
| Chemical 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 | ||
| Chemical Formula | C32H45N3O4S | ||
| Molecular Weight | 567.784 g/mol | ||
| Smiles String | CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O | ||
| Melting Point | 349.84 °C | ||
| Water Solubility | Slightly soluble | ||
| State | White to off-white amorphous powder | ||
| LogP/Hphobicity | 5.247 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Primarily hepatic via CYP450 enzymes. | ||
| Half Life | 3.5 - 5 hours | ||
| Protein Binding [%] | >98% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Nelfinavir.html http://www.rxlist.com/cgi/generic2/nelfin.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00003 | ||
| CAS Registry Number | 159989-64-7 | ||
| KEGG Compound ID | C07257 | ||
| PubChem ID | SID:206971 | ||
| PharmGKB ID | Not Available | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2248761 |
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