넬피나비어

한글명:넬피나비어

카스 번호159989-64-7

상품명:NELFINAVIR

CBNumberCB8213806

분자식C32H45N3O4S

포뮬러 무게567.78

MOL 파일159989-64-7.mol

동의어(한글)

넬피나비어

화학적 성질

녹는점	185-186 °C
끓는 점	786.8±60.0 °C(Predicted)
알파	D -119.23° (c = 0.26 in methanol)
밀도	1.22±0.1 g/cm3(Predicted)
저장 조건	under inert gas (nitrogen or Argon) at 2–8 °C
용해도	≥ 20.45mg/mL in Ethanol
물리적 상태	가루
산도 계수 (pKa)	pKa1 6.0; pKa2 11.06(at 25℃)
색상	White to off-white
수용성	7g/L(온도는 명시되지 않음)

위험 및 안전 성명

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

그림문자(GHS)

넬피나비어 화학적 특성, 용도, 생산

용도
Antiviral.
정의
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.
Antimicrobial activity
Nelfinavir inhibits HIV-1 and HIV-2 proteases. Bioavailability is affected to only a limited degree by combination with lowdose ritonavir.
원료
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)
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)
부작용
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.
신진 대사
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.

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