Lenalidomide

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Lenalidomide Daawooyinka Oncology Guriga dhexdiisa 31804  


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Sharaxaada

Lenalidomide (CC-5013) waa asal ka soo jeeda Thalidomide iyo immunomodulator afka ah oo firfircoon.Lenalidomide (CC-5013) waa ligand ee ubiquitin E3 ligase cereblon (CRBN), waxayna keentaa xuruufta xulashada iyo hoos u dhigista laba arrimood oo qoraal ah oo lymphoid ah, IKZF1 iyo IKZF3, by CRBN-CRL4 ubiquitin ligase.Lenalidomide (CC-5013) waxay si gaar ah u joojisaa korriinka lymphomas B-cell ee baaluq, oo ay ku jiraan myeloma badan, waxayna keentaa in IL-2 laga sii daayo unugyada T.

Asalkii hore

Lenalidomide (oo sidoo kale loo yaqaan CC-5013), oo ah afka laga qaato thalidomide, waa wakiilka antineoplastic oo soo bandhigaya waxqabadka antitumor iyada oo loo marayo habab kala duwan, oo ay ku jiraan firfircoonida nidaamka difaaca, xakameynta angiogenesis, iyo saameyn toos ah antineoplastic.Waxaa si weyn loo bartay daaweynta myeloma badan iyo myelodysplastic syndrome iyo sidoo kale ciladaha lymphoproliferative oo ay ku jiraan lymphocytic leukemia (CLL) iyo lymphoma non-Hodgkin.Sida laga soo xigtay daraasadihii dhawaa, Lnalidomide wuxuu kor u qaadaa oo dib u soo celiyaa shaqada nidaamka difaaca ee bukaanada CLL iyadoo ay soo jiidanayso xad-dhaaf ah oo ah molecules costimulatory ee leukemic lymphocytes si loo soo celiyo difaaca humoral iyo wax soo saarka immunoglobulins iyo sidoo kale hagaajinta awoodda unugyada T iyo unugyada leukemic si ay u sameeyaan synapses leh T. lymphocytes.

Tixraac

Ana Pilar Gonzalez-Rodriguez, Angel R. Payer, Andrea Acebes-Huerta, Leticia Hergo-Zapico, Monica Villa-Alvarez, Esther Gonzalez-Garcia, iyo Segundo Gonzalez.Lenalidomide iyo leukemia chronic lymphocytic.BioMed Research International 2013.

In Vitro

Lenalidomide waxay awood u leedahay kicinta kororka unugyada T-ga iyo IFN-γ iyo IL-2 wax soo saarka.Lenalidomide ayaa la muujiyay in ay joojiso soo saarista cytokines pro bararka ee TNF-α, IL-1, IL-6, IL-12 iyo kor u qaadida wax soo saarka cytokine anti-bararka IL-10 ee PBMCs aadanaha.Lenalidomide waxay hoos u dhigtaa wax soo saarka IL-6 si toos ah iyo sidoo kale iyada oo la xakameynayo unugyo badan oo myeloma (MM) iyo unugyada dhuuxa lafaha (BMSC), taas oo kordhisa apoptosis ee unugyada myeloma [2].Isdhexgalka qiyaasta-ku-tiirsanaanta ee isku-dhafka CRBN-DDB1 ayaa lagu arkay Thalidomide, Lenalidomide iyo Pomalidomide, oo leh IC50 qiimaha ~ 30μM, ~3μM iyo ~3μM, siday u kala horreeyaan, Unugyadan muujinta CRBN ee la dhimay (U266-CRBN60 iyo U266-CRBN75) way ka yar yihiin jawaab celinta unugyada waalidka ee saamaynta antiproliferative Lenalidomide ee qiyaasta jawaabta qiyaasta ee 0.01 ilaa 10.μM[3].Lenalidomide, analooga thalidomide, wuxuu u shaqeeyaa sida xabagta molecular ee u dhaxaysa bini'aadamka E3 ubiquitin ligase cereblon iyo CKIα waxaa lagu muujiyay in uu keeno meel-ka-baxa iyo hoos u dhigista kinase kan, sidaas awgeed waxay u badan tahay in ay dilaan unugyada leukemic by p53 firfircoonida.

Sunta qiyaasta Lenalidomide ilaa 15, 22.5, iyo 45 mg/kg iyada oo loo sii marayo IV, IP, iyo PO waddooyinka maamulka.Xaddidan milanka ee gaadhiga qiyaasta PBS, qiyaasahan ugu badan ee la heli karo ee Lenalidomide si fiican ayaa loogu dulqaadanayaa marka laga reebo hal dhimasho oo jiir ah (oo ah afar wadarta qiyaasta) ee 15 mg/kg IV qiyaasta.Waxaa xusid mudan, wax sun ah laguma arko daraasadda qiyaasta IV ee 15 mg/kg (n=3) ama 10 mg/kg (n=45) ama heer kasta oo kale oo qiyaas ah iyada oo loo marayo waddooyinka IV, IP, iyo PO.

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Budada

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3 sano
 

4°C

2 sano
Ku milmay

-80°C

6 bilood
 

-20°C

1 bil

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Lenalidomide

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Related Biological Data

Xogta Nafleyda ee La Xidhiidha

Related Biological Data2

SHAHAADADA

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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