Name: | Nelfinavir |
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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 |
Name: | Nelfinavir |
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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
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Brand: | Viracept |
Category: | HIV Protease Inhibitors, Anti-HIV Agents |
CAS number: | 159989-64-7 |
Indication: | Used in combination with other antiviral drugs in the treatment of HIV in both adults and children. |
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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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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.
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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 |
Food interaction: |
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Drug interaction: |
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UniProt ID: | O90777 | ||||||||
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Gene: | HIV-1 protease | ||||||||
Actions: | inhibitor | ||||||||
References: |
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UniProt ID: | P20813 | |||
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Gene: | CYP2B6 | |||
Actions: | inhibitor | |||
References: |
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UniProt ID: | P33261 | |||
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Gene: | CYP2C19 | |||
Actions: | substrate, inhibitor | |||
References: |
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UniProt ID: | P08684 | |||
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Gene: | CYP3A4 | |||
Actions: | substrate, inhibitor | |||
References: |
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UniProt ID: | P24462 | ||
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Gene: | CYP3A7 | ||
Actions: | substrate, inhibitor | ||
References: |
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UniProt ID: | P20815 | |||
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Gene: | CYP3A5 | |||
Actions: | substrate, inhibitor | |||
References: |
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UniProt ID: | P05177 | |
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Gene: | CYP1A2 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P11712 | |
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Gene: | CYP2C9 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P10635 | |
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Gene: | CYP2D6 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P08183 | ||||
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Gene: | ABCB1 | ||||
Actions: | substrate, inhibitor, inducer | ||||
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UniProt ID: | O15245 | |
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Gene: | SLC22A1 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P46721 | |
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Gene: | SLCO1A2 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | Q9UNQ0 | |
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Gene: | ABCG2 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | Q9Y6L6 | |
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Gene: | SLCO1B1 | |
Actions: | inhibitor | |
References: |
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