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Viracept (Nelfinavir Mesylate) - Summary

 
 



VIRACEPT SUMMARY

VIRACEPT® (nelfinavir mesylate) is an inhibitor of the human immunodeficiency virus type 1 (HIV-1) protease. VIRACEPT Tablets are available for oral administration as a light-blue, capsule-shaped tablet with a clear film coating in 250 mg strength (as nelfinavir-free base) and as a white oval tablet with a clear film coating in 625 mg strength (as nelfinavir-free base).

VIRACEPT in combination with other antiretroviral agents is indicated for the treatment of HIV-1 infection.


See all Viracept indications & dosage >>

NEWS HIGHLIGHTS

Published Studies Related to Viracept (Nelfinavir)

Complex drug interactions of HIV protease inhibitors 1: inactivation, induction, and inhibition of cytochrome P450 3A by ritonavir or nelfinavir. [2011.06]
Conflicting drug-drug interaction (DDI) studies with the HIV protease inhibitors (PIs) suggest net induction or inhibition of intestinal or hepatic CYP3A. As part of a larger DDI study in healthy volunteers, we determined the effect of extended administration of two PIs, ritonavir (RTV) or nelfinavir (NFV), or the induction-positive control rifampin on intestinal and hepatic CYP3A activity as measured by midazolam (MDZ) disposition after a 14-day treatment with the PI in either staggered (MDZ approximately 12 h after PI) or simultaneous (MDZ and PI coadministered) manner...

Influence of CYP2C19 polymorphism on the pharmacokinetics of nelfinavir and its active metabolite. [2009.11]
AIMS: This study reports the pharmacokinetics of nelfinavir, its active metabolite, M8, and active moiety (nelfinavir + M8) in volunteers genotyped for CYP2C19 as extensive metabolizer (*1*1; n = 38), heterozygous poor metabolizer (PM) (*1*2; n = 22) and homozygous PM (*2*2; n = 6)... CONCLUSIONS: Mutation in CYP2C19 increased the systemic exposure of nelfinavir and reduced the exposure of M8. No significant differences were noted among the heterozygous (*1*2) and homozygous (*2*2) PMs. These changes are not considered to be clinically relevant and hence the use of nelfinavir does not require prior assessment of CYP2C19 genotype.

Pharmacokinetic study and comparative bioavailability of two nelfinavir tablet formulations in Iranian healthy volunteers after a low-dose administration. [2009.07]
The objective of this study is to evaluate pharmacokinetic parameters, bioavailability of a potent HIV protease inhibitor, nelfinavir mesylate (NFV), following a single oral administration of 2 tablet formulations. A randomized, 2-way, crossover, bioequivalence study was conducted in 24 healthy male volunteers to compare 2 brands of nelfinavir 250 mg tablets, Nelfabiovir (Bakhtar Bioshimi, Iran) as test and Viracept (Roche, Germany) as reference product...

Effects of standard and supratherapeutic doses of nelfinavir on cardiac repolarization: a thorough QT study. [2009.03]
This was a randomized, 4-way crossover, third-party-blinded study in 68 healthy subjects to assess the effect of nelfinavir on QTc interval...

Significant decrease in nelfinavir systemic exposure after omeprazole coadministration in healthy subjects. [2008.01]
STUDY OBJECTIVES: To assess the effect of omeprazole on the multiple-dose (steady-state) pharmacokinetics and safety of nelfinavir, and to evaluate the safety and tolerability of nelfinavir when administered alone and with omeprazole... CONCLUSION: The observed reduction in the systemic exposure to both nelfinavir and its active metabolite M8 after coadministration with omeprazole could result in loss of virologic control and potential emergence of drug resistance. Hence, omeprazole should not be coadministered to patients taking nelfinavir.

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Clinical Trials Related to Viracept (Nelfinavir)

Safety Of VIRACEPT� 625mg Administered To HIV-Infected Women During Pregnancy [Completed]
This study is an evaluation of the safety of 625 mg formulation when administered to HIV-infected pregnant women from their second trimester through six weeks postpartum. The study will also evaluate the pharmacokinetics of VIRACEPT

Nelfinavir, a Phase I/Phase II Rectal Cancer Study [Completed]
The aim is to study safety and activity of nelfinavir , added to standard chemoradiotherapy in patients with locally advanced rectal cancer. Furthermore analysis of the effect of nelfinavir combined with chemoradiation on tumour tissue will be studied

Nelfinavir and Lenalidomide/Dexamethasone in Progressive Multiple Myeloma [Recruiting]
There is a great need for treatment options in patients with multiple myeloma (MM) after failure of the lenalidomide/dexamethasone regimen as there is no established standard active therapy for these patients. Combining nelfinavir, a drug targeting both the proteasome and PI3K/Akt pathway, with lenalidomide, may restore lenalidomide-sensitivity to the disease as has been shown in vivo for the PI3K/Akt inhibitor perifosine and the proteasome inhibitor bortezomib. Patients expected to be included in the trial are heavily pretreated and might not be candidates for further intensive therapies. The combination of nelfinavir with lenalidomide/dexamethasone offers also to these patients an alternative. Preliminary experiences in another SAKK trial with the combination of bortezomib and nelfinavir are positive with few side effects with nelfinavir doses of up to 1875 mg twice daily (bid). For the phase I part of the trial a starting dose of 1250 mg nelfinavir bid was chosen, since the necessary plasma concentration of nelfinavir will not be reached with lower doses. In case of progression during or after the trial treatment any other lenalidomide- or bortezomib-based chemotherapy combination could be an option for the patient. However, the addition of a chemotherapeutic drug like cyclophosphamide or doxorubicin has known side effects like hematological toxicities, nausea, vomiting and hair loss. The aim of this trial is to demonstrate that the combination of nelfinavir with lenalidomide/dexamethasone is safe (phase I, dose escalation of nelfinavir) and active (phase II). Patients who do not respond to trial medication will stop trial treatment after 4 months of therapy at the latest. If the combination of nelfinavir with lenalidomide/dexamethasone should prove to be safe and efficient in treatment of lenalidomide-refractory MM, this would be the first orally available treatment for these patients and establish a new class of drugs (human immunodeficiency virus (HIV) protease inhibitors) as active antineoplastic agents in MM. In addition this would establish the concept of "re-sensitizing" patients to lenalidomide therapy and demonstrate the effect of nelfinavir on proteasomal degradation and Akt phosphorylation in cancer patients in vivo.

Nelfinavir as Bortezomib-sensitizing Drug in Patients With Proteasome Inhibitor-nonresponsive Myeloma [Recruiting]
Trial objectives: To decide whether the addition of nelfinavir to the approved antimyeloma therapy with bortezomib and dexamethasone has sufficient activity in proteasome inhibitor-resistant myeloma patients to merit further clinical investigation in a prospective controlled trial. Additional research questions: To collect myeloma cell samples from proteasome inhibitor-resistant myeloma patients for the assessment of the biology of proteasome inhibitor resistance and the identification of predictive markers for response to nelfinavir-based antimyeloma therapy.

Nelfinavir for the Treatment of Gammaherpesvirus-Related Tumors [Recruiting]
The goals of this study is to determine if nelfinavir can target Epstein-Barr virus (EBV) and Kaposi sarcoma-associated herpesvirus (KSHV) in patients with certain cancers.

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Reports of Suspected Viracept (Nelfinavir) Side Effects

Maternal Drugs Affecting Foetus (6)Lipodystrophy Acquired (3)Premature Baby (3)Maternal Exposure During Pregnancy (3)Maternal Exposure Timing Unspecified (3)Ileal Atresia (3)Foetal Exposure During Pregnancy (2)Pulmonary Embolism (2)Autoimmune Thyroiditis (2)Live Birth (2)more >>


Page last updated: 2011-12-09

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