Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  API >  Synthetic Anti-infective Drugs >  Antiviral drugs >  NELFINAVIR

NELFINAVIR

Basic information Safety Supplier Related

NELFINAVIR Basic information

Product Name:
NELFINAVIR
Synonyms:
  • Nelfinavir Regeoisomer
  • N-tert-butyl-2-[2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)-oxomethyl]amino]-4-(phenylthio)butyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide
  • AG 1341; AG-1341; AG1341
  • 3-isoquinolinecarboxamide,n-(1,1-dimethylethyl)decahydro-2-(2-hydroxy-3-((3-hy
  • 8a-beta))-a-bet
  • nefinavir
  • NELFINAVIR
  • (3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide
CAS:
159989-64-7
MF:
C32H45N3O4S
MW:
567.78
EINECS:
1533716-785-6
Product Categories:
  • peptides
Mol File:
159989-64-7.mol
More
Less

NELFINAVIR Chemical Properties

Melting point:
185-186 °C
alpha 
D -119.23° (c = 0.26 in methanol)
Boiling point:
786.8±60.0 °C(Predicted)
Density 
1.22±0.1 g/cm3(Predicted)
pka
pKa1 6.0; pKa2 11.06(at 25℃)
Water Solubility 
7g/L(temperature not stated)
More
Less

NELFINAVIR Usage And Synthesis

Uses

Antiviral.

Definition

ChEBI: An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.

Indications

Nelfinavir (Viracept) is probably the most commonly used protease inhibitor because of its low incidence of serious adverse effects. Its most common side effects are diarrhea and flatulence; these may resolve with continued use. In addition to the drugs contraindicated for use with all protease inhibitors, amiodarone, rifampin, and quinidine are contraindicated in patients taking nelfinavir.

brand name

Viracept (Agouron).

Antimicrobial activity

Nelfinavir inhibits HIV-1 and HIV-2 proteases. Bioavailability is affected to only a limited degree by combination with lowdose ritonavir.

Acquired resistance

Resistance is most frequently selected through a D30N mutation in the HIV protease. An L90M mutation also confers resistance.

Pharmaceutical Applications

A synthetic chemical formulated as the mesylate for oral administration.

Pharmacokinetics

Oral absorption: c. 70–80% (with food)
Cmax 750 mg thrice daily: c. 3–4 mg/L
1250 mg twice daily: c. 4 mg/L
Cmin 750 mg thrice daily: c. 1–3 mg/L
1250 mg twice daily: c. 0.7–2.2 mg/L
Plasma half-life: c. 3.5 h
Volume of distribution: c. 2–7 L/kg
Plasma protein binding: >98%
Absorption and distribution
Food improves the bioavailability and the drug should be administered with a light meal. The semen:plasma ratio is 0.07. It is distributed into breast milk.
Metabolism and excretion
One major and several minor oxidative metabolites are found in plasma. Most of an oral dose is recovered in feces as unchanged drug (22%) and metabolites (78%). The remainder is recovered in urine, mainly unchanged.
An increase in the area under the time–concentration curve (AUC) has been observed in patients with hepatic impairment, but specific dose recommendations have not been made.

Clinical Use

Treatment of HIV infection (in combination with other antiretroviral drugs)

Side effects

The most common adverse effect is diarrhea of mild to moderate severity. Other side effects include nausea, fatigue, vomiting and headache. It is associated with less dyslipidemia in comparison with ritonavir-boosted protease inhibitors.

Metabolism

Following oral administration, nelfinavir peak levels in plasma ranged from 0.34 mg/mL (10 mg/kg in the dog) to 1.7 mg/mL (50 mg/kg in the rat). In the dog, nelfinavir was slowly absorbed, and bioavailability was 47%. The drug appeared to be metabolized in the liver, and the major excretory route was in feces.

NELFINAVIRSupplier

Chembest Research Laboratories Limited
Tel
021-20908456-
Email
sales@BioChemBest.com
LGM Pharma
Tel
1-(800)-881-8210
Email
inquiries@lgmpharma.com
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202- ; ;
Email
jerry.ma@hanhonggroup.com;jerry.ma@hanhonggroup.com;jerry.ma@hanhonggroup.com
China DongFan Chemical Co.,LTD
Tel
86-0571-85151182
Email
sales@dongfan-chem.com
Hangzhou Yuhao Chemical Technology Co., Ltd
Tel
0571-82693216
Email
info@yuhaochemical.com