Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
용해도
수용액(약간 용해됨), DMF(약간 용해됨)
물리적 상태
고체
물리적 상태
단단한 모양
색상
흰색에서 황백색까지
BCS Class
2
안전
위험 및 안전 성명
위험 및 사전주의 사항 (GHS)
그림문자(GHS):
신호 어:
Warning
유해·위험 문구:
암호
유해·위험 문구
위험 등급
범주
신호 어
그림 문자
P- 코드
H315
피부에 자극을 일으킴
피부부식성 또는 자극성물질
구분 2
경고
P264, P280, P302+P352, P321,P332+P313, P362
H361
태아 또는 생식능력에 손상을 일으킬 것으로 의심됨
생식독성 물질
구분 2
경고
P201, P202, P281, P308+P313, P405,P501
예방조치문구:
P201
사용 전 취급 설명서를 확보하시오.
P202
모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.
P264
취급 후에는 손을 철저히 씻으시오.
P264
취급 후에는 손을 철저히 씻으시오.
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P281
요구되는 개인 보호구를 착용하시오
P302+P352
피부에 묻으면 다량의 물로 씻으시오.
P308+P313
노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.
P321
(…) 처치를 하시오.
P332+P313
피부 자극이 생기면 의학적인 조치· 조언을 구하시오.
P362
오염된 의복을 벗고 세척 후에 재사용하기
P405
밀봉하여 저장하시오.
P501
...에 내용물 / 용기를 폐기 하시오.
NFPA 704
0
1
0
포삼프레나비어 C화학적 특성, 용도, 생산
개요
Fosamprenavir, a prodrug of the HIV protease inhibitor amprenavir, is indicated for the
oral treatment of HIV infection in adults in combination with other antiretroviral agents.
Although amprenavir has excellent antiviral potency and good tolerability, its watersolubility
is poor (0.04 mg/ml). As a result, the formulation of the agent includes a high
percentage of organic excipients to facilitate gastric dissolution, which limits the amount
of active drug that can be formulated per capsule. Fosamprenavir is a highly soluble
phosphate ester of amprenavir. It allows more convenient dosing and reduction in pill
counts as compared to amprenavir. Fosamprenavir is readily prepared in two steps
starting from a key intermediate used in the synthesis of amprenavir, by phosphorylating
a hydroxyl group and subsequently reducing a p-nitrophenyl to a p-aminophenyl group.
Fosamprenavir has little or no antiviral activity in vitro. After oral administration, it is
rapidly and almost completely hydrolyzed by phosphatases in the gut epithelium to
amprenavir prior to reaching systemic circulation. The time to reach peak plasma
concentration of amprenavir is approximately 2.5 h and the plasma elimination half-life
is approximately 7.7 h. Amprenavir is metabolized in the liver by CYP3A4 and ＞90% of
the dose is excreted as metabolites in urine and feces. In most patients, fosamprenavir is
administered at daily doses of 700–1400 mg in conjunction with ritonavir. Monotherapy
with fosamprenavir is only recommended in antiretroviral therapy-na?ve patients and the
dosing regimen is 1400 mg twice daily. The most common adverse events experienced
with fosamprenavir are diarrhea, nausea, vomiting, headache and rash.
화학적 성질
White Microcrystalline Needles
일반 설명
Fosamprenavir is used in combination with otherHIV drugs in adult patients. Like the other PIs, this compoundis a prodrug that produces the active drug uponhydrolysis. In this case, the active drug is amprenavir, apeptidomimetic transition state inhibitor. Fosamprenaviris typically administered in combination with RTinhibitors.
Clinical Use
Fosamprenavir calcium has been approved for the treatment of HIV in adults when used in combination
with other anti-HIV drugs. It is a prodrug that, on hydrolysis by serum phosphatases, gives rise to
amprenavir, which is a peptidomimetic transition-state inhibitor that targets HIV-1 protease and reduces
the viral replication and, thus, the infectiousness of HIV-1. It is commonly administered in combination
with RT inhibitors to produce excellent efficacy in patients with AIDS. The drug is administered as two
700 mg tablets twice daily or, in combination with ritonavir, can be given as two 700 mg tables once daily
or one 700 mg tablet twice daily. As a result, formaprenavir lowers the "pill burden" in patients with AIDS.
