Bayani

Lenalidomide (CC-5013) ya samo asali ne daga Thalidomide da kuma immunomodulator na baka.Lenalidomide (CC-5013) shine ligand na ubiquitin E3 ligase cereblon (CRBN), kuma yana haifar da zaɓaɓɓen wuri da kuma lalata abubuwan rubutun lymphoid guda biyu, IKZF1 da IKZF3, ta CRBN-CRL4 ubiquitin ligase.Lenalidomide (CC-5013) musamman yana hana haɓakar ƙwayoyin lymphomas B-cell balagagge, ciki har da myeloma mai yawa, kuma yana haifar da sakin IL-2 daga ƙwayoyin T.

Fage

Lenalidomide (wanda kuma aka sani da CC-5013), wani nau'i na thalidomide na baka, wakili ne na antineoplastic wanda ke nuna ayyukan antitumor ta hanyoyi daban-daban, ciki har da kunna tsarin rigakafi, hana angiogenesis, da tasirin antineoplastic kai tsaye.An yi nazari da yawa don maganin myeloma da yawa da ciwon myelodysplastic da kuma cututtuka na lymphoproliferative ciki har da cutar sankarar lymphocytic na yau da kullum (CLL) da lymphoma ba Hodgkin.Dangane da binciken da aka yi kwanan nan, Lnalidomide yana haɓakawa da dawo da aikin tsarin garkuwar jiki a cikin marasa lafiya na CLL ta hanyar haifar da wuce gona da iri na ƙwayoyin cuta a cikin ƙwayoyin lymphocytes na leukemic don dawo da rigakafin humoral da samar da immunoglobulins da haɓaka ikon ƙwayoyin T da ƙwayoyin leukemic don samar da synapses tare da T. lymphocytes.

Magana

Ana Pilar Gonzalez-Rodriguez, Angel R. Payer, Andrea Acebes-Huerta, Leticia Hergo-Zapico, Monica Villa-Alvarez, Esther Gonzalez-Garcia, da Segundo Gonzalez.Lenalidomide da na kullum lymphocytic cutar sankarar bargo.BioMed Research International 2013.

A cikin Vitro

Lenalidomide yana da ƙarfi a cikin haɓaka haɓakar ƙwayoyin T da IFN-γ da IL-2 samarwa.An nuna Lenalidomide don hana samar da pro-inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 da haɓaka samar da cytokine anti-inflammatory IL-10 daga PBMCs na mutum.Lenalidomide yana raguwa da samar da IL-6 kai tsaye kuma ta hanyar hana ƙwayoyin myeloma (MM) da yawa da kuma hulɗar sel stromal sel (BMSC), wanda ke haɓaka apoptosis na ƙwayoyin myeloma [2].Ana lura da hulɗar dogaro da kashi tare da hadaddun CRBN-DDB1 tare da Thalidomide, Lenalidomide da Pomalidomide, tare da ƙimar IC50 na ~30μM, ~3μM da ~ 3μM, bi da bi, Waɗannan ƙananan ƙwayoyin maganganu na CRBN (U266-CRBN60 da U266-CRBN75) ba su da ƙarfi fiye da sel na iyaye zuwa tasirin antiproliferative Lenalidomide a cikin kewayon amsa-kashi na 0.01 zuwa 10.μM[3].Lenalidomide, analog na thalidomide, yana aiki azaman manne kwayoyin halitta tsakanin ɗan adam E3 ubiquitin ligase cereblon da CKIα an nuna shi don haifar da haɓakawa da lalata wannan kinase, don haka mai yiwuwa kashe kwayoyin cutar leukemia ta hanyar kunna p53.

Gubar Lenalidomide allurai har zuwa 15, 22.5, da 45 mg/kg ta hanyar IV, IP, da PO hanyoyin gudanarwa.Iyakance ta hanyar solubility a cikin abin hawan mu na PBS, waɗannan matsakaicin iyakar adadin Lenalidomide ana iya jurewa da kyau ban da mutuwar linzamin kwamfuta ɗaya (na jimlar adadin kashi huɗu) a kashi 15 mg/kg IV.Musamman, ba a lura da wasu abubuwan guba ba a cikin binciken a allurai na IV na 15 mg / kg (n = 3) ko 10 mg / kg (n = 45) ko a kowane matakin kashi ta hanyar IV, IP, da PO.

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