Ibisobanuro

Lenalidomide (CC-5013) ni inkomoko ya Thalidomide hamwe na immunomodulator ikora mu kanwa. Lenalidomide (CC-5013) ni ligand ya ubiquitin E3 ligase cereblon (CRBN), kandi itera guhitamo ahantu hose no gutesha agaciro ibintu bibiri byandikirwa lymphoide, IKZF1 na IKZF3, na CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) ibuza cyane gukura kwa lymphoma B ikuze, harimo na myeloma myinshi, kandi itera IL-2 kurekura selile.

Amavu n'amavuko

Lenalidomide (izwi kandi nka CC-5013), inkomoko yo mu kanwa ya thalidomide, ni antineoplastique yerekana ibikorwa bya antitumor binyuze mu buryo butandukanye, harimo gukora sisitemu y’umubiri, kubuza angiogenezi, hamwe n’ingaruka ziterwa na antineoplastique. Yakozweho ubushakashatsi bwimbitse bwo kuvura syndrome nyinshi ya myeloma na myelodysplastic kimwe n'indwara ya lymphoproliferative harimo na lymphocytike leukemia idakira (CLL) na lymphoma itari Hodgkin. Nk’uko ubushakashatsi buherutse gukorwa bubigaragaza, Lnalidomide iteza imbere kandi ikagarura imikorere y’umubiri ku barwayi ba CLL itera gukabya gukabije kwa molekile zo mu bwoko bwa lymphocytes zo mu bwoko bwa leukemic lymphocytes kugira ngo igarure ubudahangarwa bw’urwenya n’umusemburo wa immunoglobuline ndetse no kunoza ubushobozi bw’uturemangingo T na selile zo mu bwoko bwa leukemic gukora synaps hamwe na T. lymphocytes.

Reba

Ana Pilar Gonzalez-Rodriguez, Angel R. Payer, Andrea Acebes-Huerta, Leticia Hergo-Zapico, Monica Villa-Alvarez, Esther Gonzalez-Garcia, na Segundo Gonzalez. Lenalidomide na lymphocytike idakira. BioMed Ubushakashatsi Mpuzamahanga 2013.

Muri Vitro

Lenalidomide ifite imbaraga mu gukurura T selile ikwirakwizwa na IFN-γ n'umusaruro wa IL-2. Lenalidomide yerekanwe kubuza umusaruro wa cytokine pro inflammatory inflammatory TNF-α, IL-1, IL-6, IL-12 no kuzamura umusaruro wa cytokine anti-inflammatory IL-10 kuva PBMCs zabantu. Lenalidomide igabanya umusaruro wa IL-6 mu buryo butaziguye kandi ikanabuza selile nyinshi za myeloma (MM) hamwe na selile marrow tromal selile (BMSC), ibyo bikaba byongera apoptose ya selile myeloma [2]. Imikoreshereze ishingiye ku mikoreshereze ya CRBN-DDB1 igaragara hamwe na Thalidomide, Lenalidomide na Pomalidomide, hamwe na IC50 indangagaciro za ~ 30μM, ~ 3μM na ~ 3μM.μM [3]. Lenalidomide, igereranya rya thalidomide, ikora nka kole ya molekile hagati yumuntu E3 ubiquitin ligase cereblon na CKIα irerekanwa kugirango itere hose no gutesha agaciro iyi kinase, bityo birashoboka ko yica selile leukemic na p53 activation.

Uburozi bwa Lenalidomide bugera kuri 15, 22.5, na 45 mg / kg ukoresheje inzira ya IV, IP, na PO. Bitewe no kwikemurira mumodoka yacu ya PBS, iyi dosiye ntarengwa ishobora kugerwaho na Lenalidomide yihanganira neza usibye urupfu rwimbeba imwe (ya bane yuzuye) kuri 15 mg / kg IV. Ikigaragara ni uko nta bundi burozi bugaragara mu bushakashatsi kuri dosiye ya IV ya mg / kg 15 (n = 3) cyangwa 10 mg / kg (n = 45) cyangwa ku rundi rwego urwo ari rwo rwose binyuze mu nzira ya IV, IP, na PO.

Ububiko

Imiterere yimiti

Bifitanye isano na Biologiya

Bifitanye isano na Biologiya