NELFINAVIR

Bezeichnung:NELFINAVIR

CAS-Nr159989-64-7

Englisch Name:NELFINAVIR

CBNumberCB8213806

SummenformelC32H45N3O4S

Molgewicht567.78

MOL-Datei159989-64-7.mol

NELFINAVIR physikalisch-chemischer Eigenschaften

Schmelzpunkt	185-186 °C
Siedepunkt	786.8±60.0 °C(Predicted)
alpha	D -119.23° (c = 0.26 in methanol)
Dichte	1.22±0.1 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2–8 °C
Löslichkeit	≥ 20.45mg/mL in Ethanol
Aggregatzustand	Powder
pka	pKa1 6.0; pKa2 11.06(at 25℃)
Farbe	White to off-white
Wasserlöslichkeit	7g/L(temperature not stated)

Sicherheit

Toxizität

rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998.

Gefahreninformationscode (GHS)

NELFINAVIR Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
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.
Trademarks
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.
Pharmazeutische Anwendungen
A synthetic chemical formulated as the mesylate for oral administration.
Pharmakokinetik
Oral absorption: c. 70–80% (with food)
C_max 750 mg thrice daily: c. 3–4 mg/L
1250 mg twice daily: c. 4 mg/L
C_min 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)
Nebenwirkungen
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.
Stoffwechsel
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.

NELFINAVIR Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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