My Cart

0 Item(s): $0.00

You have no items in your shopping cart.

Nelfinavir Mesylate

Nelfinavir Mesylate


Nelfinavir was developed by Agouron Pharmaceuticals as part of a joint venture with Eli Lilly and Company. 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 expired in 2014.

On the 6 June 2007, both the Medicines and Healthcare products Regulatory Agency and the European Medicines Agency 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.

Uses for Nelfinavir Mesylate

Treatment of HIV-1 infection in adults, adolescents, and pediatric patients ≥2 years of age; usually used in conjunction with 2 HIV nucleoside reverse transcriptase inhibitors (NRTIs).1

Experts state nelfinavir not recommended for initial treatment regimens in antiretroviral-naive adults and adolescents because of inferior virologic efficacy and high incidence of diarrhea.200

For initial treatment in antiretroviral-naive pediatric patients, experts state nelfinavir in conjunction with 2 NRTIs can be considered in children ≥2 years of age, but only in special circumstances when preferred or alternative regimens cannot be used.201 Safety and efficacy not established in those <2 years of age,1 and not recommended in this age group because of insufficient data.201

Potential anti-cancer activity

Since 2009, nelfinavir has been under investigation for potential use as an anti-cancer agent.[8] When applied to cancer cells in culture (in vitro), it can inhibit the growth of a variety of cancer types and can trigger cell death (apoptosis).[9] When Nelfinavir was given to laboratory mice with tumors of the prostate or of the brain, it could suppress tumor growth in these animals.[10][11] At the cellular level, nelfinavir exerts multiple effects to inhibit cancer growth; the two main ones appear to be inhibition of the Akt/PKB signaling pathway and activation of endoplasmic reticulum stress with subsequent unfolded protein response.[12]

In the United States, about three dozen clinical trials are being conducted (or have been completed) in order to determine whether nelfinavir is effective as a cancer therapeutic agent in humans.[13] In some of these trials, nelfinavir is used alone in monotherapy fashion, whereas in others it is combined with other modes of cancer therapy, such as well-established chemotherapeutic agents or radiation therapy.


Concomitant use with drugs highly dependent on CYP3A for metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events (e.g., alfuzosin, amiodarone, cisapride, ergot alkaloids, oral midazolam, pimozide, quinidine, sildenafil used for treatment of pulmonary arterial hypertension [PAH], triazolam).1 Concomitant use with drugs that may decrease nelfinavir concentrations (e.g., rifampin, St. John’s wort [Hypericum perforatum].1 (See Specific Drugs under Interactions.

Pediatric Use

Safety and efficacy not established in infants and children <2 years of age.1 Some data collected in this age group, but reliably effective dosage not established.1 Some evidence that those <2 years of age have a lower response rate than older children.1

Consider that use of nelfinavir in children is associated with highly variable drug exposure.1 (See Pharmacokinetics.)

Use of nelfinavir in children 2–13 years of age supported by evidence from adequate and well-controlled studies in adults and pharmacokinetic and clinical studies supporting activity in pediatric patients.1 80 124 126 127 152 153 161 201 213 Diarrhea reported less frequently in children than in adults.80 124