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에베로리무스

에베로리무스
에베로리무스 구조식 이미지
카스 번호:
159351-69-6
한글명:
에베로리무스
동의어(한글):
에베로리무스
상품명:
Everolimus
동의어(영문):
SDZRAD;Certica;RAD-001;Certican;Zortress;Afinitor;Everolimus;CERTICAN(R);EveroliMus API;Everolimus powder
CBNumber:
CB9502411
분자식:
C53H83NO14
포뮬러 무게:
958.232
MOL 파일:
159351-69-6.mol

에베로리무스 속성

녹는점
NA
끓는 점
998.7±75.0 °C(Predicted)
밀도
1.18±0.1 g/cm3(Predicted)
인화점
2℃
저장 조건
−20°C
산도 계수 (pKa)
10.40±0.70(Predicted)
수용성
Soluble in dimethysulfoxide,ethanol and chloroform. Slightly soluble in water.
안정성
Hygroscopic
InChIKey
HKVAMNSJSFKALM-GKUWKFKPSA-N
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 T,Xn,F
위험 카페고리 넘버 48/25-36-20/21/22-11
안전지침서 45-36/37-26-16
유엔번호(UN No.) UN 1648 3 / PGII
WGK 독일 2
F 고인화성물질 10
HS 번호 29349990
그림문자(GHS):
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H225 고인화성 액체 및 증기 인화성 액체 구분 2 위험 P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 P264, P280, P305+P351+P338,P337+P313P
H372 장기간 또는 반복 노출되면 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴 특정 표적장기 독성 - 반복 노출 구분 1 위험 P260, P264, P270, P314, P501
예방조치문구:
P210 열·스파크·화염·고열로부터 멀리하시오 - 금연 하시오.
P260 분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P314 불편함을 느끼면 의학적인 조치·조언을 구하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

에베로리무스 C화학적 특성, 용도, 생산

용도

에베로 리무스는 신호 전달 억제제라고하는 치료 유형입니다. 신호 전달 저해제는 세포 내에서 신호가 성장하고 분열되도록하는 신호를 차단합니다.에버 롤리 무스는 mTOR라는 특정 단백질을 제대로 작동시키지 못하도록 막습니다. mTOR는 암세포가 자라는 다른 단백질을 조절합니다. 따라서 는 암의 성장을 막는데 도움이됩니다.
 

독성

에베로 리무스를 복용하면 박테리아, 바이러스 및 곰팡이에 의한 감염을 막을 수있는 능력이 떨어지고 심각한 또는 생명을 위협하는 감염 위험을 높일 수 있습니다.

개요

Everolimus, an oral immunosuppressant for the treatment of kidney and heart transplant rejection, is the 40-O-(2-hydroxyethyl) derivative of rapamycin. It has immunosuppressive properties similar to those of rapamycin, but with improved pharmacokinetic profile. In addition, the 40-O-(2-hydroxyethyl) group alters the physico-chemical properties of the macrolide to allow galenic formulation. Everolimus is prepared in a two-step semisynthesis starting from rapamycin, by alkylation of the 40-hydroxyl group with t-butyldimethylsilyloxyethyl triflate and subsequent cleavage of the silyl protecting group. Everolimus, like rapamycin, is a proliferation signal inhibitor that exerts its immunosuppressive effect by inhibiting the activation of p70 S6 kinase, thereby blocking growth factor-driven proliferation of T cells, B cells and vascular smooth muscle cells, and arresting cell cycle at the G1 phase. Inhibition of p70 S6 kinase activation by everolimus and rapamycin is mediated by their binding to FKBP12 (FK506 binding-protein 12). Everolimus inhibits FK506 binding to FKBP12 with an IC50 of 1.8–2.6 nM, and it is about 3- to 5-fold less potent than rapamycin (IC50=0.4–0.9 nM). The in vitro immunosuppressive activity of everolimus is also slightly less than that of rapamycin as demonstrated in a mixed lymphocyte reaction (MLR) assay (IC50=0.2–1.6 nM versus 0.07–0.5 nM, respectively) and in antigen-specific human helper T-cell clones (IC50=0.05–0.17nM versus 0.014–0.37nM, respectively). However, the in vivo immunosuppressive activity of oral everolimus 1–5 mg/ kg/day is similar to that of rapamycin at equivalent doses in rat models of renal or cardiac transplantation, localized graft-versus-host disease, and autoimmune glomerulonephritis. The recommended dosage of everolimus is 0.75 mg twice daily, and it is used in combination with cyclosporine microemulsion and corticosteroids. Following oral dosing, the peak concentration (Cmax) of everolimus is estimated between 1.5 to 2 hours, and steady state is achieved within 4 days. The terminal elimination half-life is 21 to 35 hours. By comparison, rapamycin has a longer elimination half-life (60 hours) and longer time to reach steady state (7 to 14 days). Consequently, rapamycin treatment requires a large loading dose, followed by once daily maintenance dose, whereas everolimus is administered twice daily but without the need of a loading dose. Everolimus is extensively metabolized, primarily by CYP3A4. Approximately 80% of the dose is excreted in the feces and about 5% in the urine. In clinical trials with adult cardiac transplant recipients, oral everolimus 0.75 or 1.5 mg twice daily significantly reduced the incidence of efficacy failure as well as cardiac allograft vasculopathy (CAV) up to 2 years after transplantation as compared with azathioprene 1–3 mg/kg/day. However, graft and patient survival rates at 1 year were similar in patients receiving everolimus and azathioprene. In trials involving renal transplant recipients, the combined incidence of biopsy-confirmed acute rejection, graft loss, death, or loss to follow-up was similar in patients receiving everolimus 1.5 or 3 mg/day or mycophenolate mofetil 2 g/day up to 3 years after transplantation. Everolimus was well tolerated in transplant patients. The incidence of viral infection including cytomegalovirus (CMV) was reduced in comparison to azathioprene and mycophenolate mofetil, but bacterial infections were more frequent. Main adverse events associated with everolimus were thrombocytopenia, leucopenia, and elevated serum lipids and creatinine.

화학적 성질

Off White Solid

Originator

Novartis (Switzerland)

용도

Macrolide immunosuppressant; derivative of Rapamycin. Inhibits cytokine-mediated lymphocyte proliferation

용도

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM

용도

Everolimus Macrolide immunosuppressant; Everolimus is a derivative of Rapamycin. Everolimus inhibits cytokine-mediated lymphocyte proliferation.

용도

Everolimus is a semi-synthetic macrocyclic lactone prepared from rapamycin by selective alkylation of the 42-hydroxy group with a silyl-protected hydroxyethyl triflate moiety, followed by addition of an ethylhydroxy moiety to provide greater stability and bioavailability. Like all tacrolimus analogues, everolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. Everolimus is extensively cited in the literature with over 2,000 citations.

정의

ChEBI: A macrocyclic lactone that is rapamycin in which the hydroxy group attached to the cyclohexyl moiety has been converted to the corresponding 2-hydroxyethyl ether. It is an immunosuppressant and antineoplastic agent.

상표명

Certican

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