Nelfinavir

567.78

567.78

1533716-785-6

HO3OGH5D7I

747167

DTXSID5035080

C29285

J05AE04|J - Antiinfectives for systemic use

127

5.7

Solid

1.22±0.1 g/cm3(Predicted)

185-186 °C

786.8±60.0 °C(Predicted)

429.7ºC

1.618

H2O: Slightly soluble

Commercially available nelfinavir mesylate tablets and oral powder should be stored at 15-30C.

4.38E-26mmHg at 25°C

D -119.23° (c = 0.26 in methanol)

Oral LD50 is over 5g/kg in rats. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.

Some degree of serum aminotransferase elevation occurs in a high proportion of patients taking nelfinavir containing antiretroviral regimens. Moderate-to severe elevations in serum aminotransferase levels (>5 times the upper limit of normal) are found in only 3% to 10% of patients, although rates may be higher in patients with HIV-HCV coinfection. These elevations are usually asymptomatic and self-limited and can resolve even with continuation of the medication. Clinically apparent acute liver injury due to nelfinavir is rare. The few cases that have been reported have arisen after 1 to 8 weeks of starting nelfinavir, and the pattern of serum enzyme elevations has not been reported, but is likely to have been hepatocellular (Case 1). Signs of hypersensitivity (fever, rash, eosinophilia) can occur as can autoantibody formation but these features are not very prominent. The acute liver injury due to nelfinavir is usually self-limited, but it can be severe, and isolated cases of acute liver failure have been reported to the sponsor, although not in great detail. In HBV or HCV coinfected patients, some instances appear to be due to exacerbation of the underlying chronic liver disease, perhaps as a result of sudden immune reconstitution. Nelfinavir therapy has not been clearly linked to lactic acidosis and acute fatty liver that is reported in association with several nucleoside analogue reverse transcriptase inhibitors used to treat HIV infection.

>98%

Used in combination with other antiviral drugs in the treatment of HIV in both adults and children.|FDA Label|Viracept is indicated in antiretroviral combination treatment of human-immunodeficiency-virus (HIV-1)-infected adults, adolescents and children of three years of age and older.In protease-inhibitor (PI)-experienced patients, the choice of nelfinavir should be based on individual viral resistance testing and treatment history.

Nelfinavir is an antiretroviral protease inhibitor used in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Nelfinavir can cause transient and usually asymptomatic elevations in serum aminotransferase levels and is a rare cause of clinically apparent, acute liver injury. In HBV or HCV coinfected patients, hepatic injury during antiretroviral therapy that includes nelfinavir may be a result of exacerbation of the underlying chronic hepatitis B or C, rather than a direct effect of the medication.

Antiviral Agents

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.

Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly. (See all compounds classified as HIV Protease Inhibitors.)

Well absorbed following oral administration.|The terminal half-life in plasma was typically 3.5 to 5 hours. The majority (87%) of an oral 750 mg dose containing 14C-nelfinavir was recovered in the feces; fecal radioactivity consisted of numerous oxidative metabolites (78%) and unchanged nelfinavir (22%). Only 1–2% of the dose was recovered in urine, of which unchanged nelfinavir was the major component.|2 to 7 L/kg

Primarily hepatic via cytochrome P450 (CYP450) enzymes. CYP3A and CYP2C19 appear to be the predominant enzymes that metabolize nelfinavir in humans. One major and several minor metabolites are found in plasma; the major oxidative metabolite has in vitro antiviral activity comparable to that of the parent drug.|Nelfinavir has known human metabolites that include 3,4-Dihydroxynelfinavir and Nelfinavir hydroxyl-t- butylamide.

3.5 - 5 hours

Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

AG 1343

Human drugs -> Viracept -> EMA Drug Category|Antivirals for systemic use -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients