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QuickView for Nelfinavir (compound)


PubChem
Name: Nelfinavir
PubChem Compound ID: 10578931
Description: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
Molecular formula: C32H45N3O4S
Molecular weight: 567.784 g/mol
DrugBank
Identification
Name: Nelfinavir
Name (isomeric): DB00220
Drug Type: small molecule
Description: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
Synonyms:
Nelfinavir mesylate; NLF; 1UN; AG1343; NFV
Brand: Viracept
Category: HIV Protease Inhibitors, Anti-HIV Agents
CAS number: 159989-64-7
Pharmacology
Indication: Used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
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 ...
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Mechanism of Action: Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Absorption: Well absorbed following oral administration.
Protein binding: >98%
Biotransformation: 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.
Route of elimination: 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.
Half Life: 3.5 - 5 hours
Toxicity: Oral LD50 is over 5g/kg in rats. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.
Affected organisms: Human Immunodeficiency Virus
Interactions
Food interaction:
Food significantly increases absorption (2 to 3 times).
Take with food.
Drug interaction:
ClorazepateThe protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, clorazepate.
ErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinib
DiazepamThe protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, diazepam.
St. John's WortSt. John's Wort decreases the effect of indinavir
TelithromycinNelfinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
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