China Lenalidomide opanga ndi ogulitsa

Lenalidomide

Kufotokozera Kwachidule:

Dzina la API	Chizindikiro	Kufotokozera	US DMF	EU DMF	CEP
Lenalidomide	Oncology mankhwala	M'nyumba	31804	√

Titumizireni imelo

Tsatanetsatane wa Zamalonda

Zolemba Zamalonda

PRODUCT DETAIL

Kufotokozera

Lenalidomide (CC-5013) ndi chochokera ku Thalidomide ndi pakamwa yogwira immunomodulator. Lenalidomide (CC-5013) ndi ligand ya ubiquitin E3 ligase cereblon (CRBN), ndipo imayambitsa kusankha kokhazikika komanso kuwonongeka kwa zinthu ziwiri zolembera za lymphoid, IKZF1 ndi IKZF3, ndi CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) makamaka imalepheretsa kukula kwa B-cell lymphomas okhwima, kuphatikizapo angapo myeloma, ndipo imapangitsa kuti IL-2 itulutsidwe ku T cell.

Mbiri

Lenalidomide (yomwe imadziwikanso kuti CC-5013), yochokera pakamwa ya thalidomide, ndi antitineoplastic agent yomwe imasonyeza ntchito ya antitumor pogwiritsa ntchito njira zosiyanasiyana, kuphatikizapo chitetezo cha mthupi, angiogenesis inhibition, ndi zotsatira za antineoplastic mwachindunji. Zaphunziridwa kwambiri pochiza matenda ambiri a myeloma ndi myelodysplastic komanso matenda a lymphoproliferative kuphatikizapo chronic lymphocytic leukemia (CLL) ndi non-Hodgkin lymphoma. Malinga ndi kafukufuku waposachedwa, Lnalidomide imalimbikitsa ndikubwezeretsa chitetezo cham'thupi mwa odwala CLL mwa kuchititsa kuti ma molekyulu a costimulatory adziwike mu leukemic lymphocytes kuti abwezeretse chitetezo chamthupi komanso kupanga ma immunoglobulins komanso kupititsa patsogolo luso la ma T cell ndi leukemic cell kupanga ma synapses ndi T. ma lymphocytes.

Buku

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

Mu Vitro

Lenalidomide ndi yamphamvu polimbikitsa kuchuluka kwa T cell ndi IFN-γ ndi kupanga IL-2. Lenalidomide yasonyezedwa kuti imalepheretsa kupanga ma pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 ndikukweza kupanga anti-inflammatory cytokine IL-10 kuchokera ku PBMC zaumunthu. Lenalidomide imachepetsa kupanga IL-6 mwachindunji komanso poletsa ma cell angapo a myeloma (MM) ndi ma cell marrow stromal cell (BMSC), omwe amawonjezera apoptosis ya maselo a myeloma [2]. Kugwirizana kodalira mlingo ndi CRBN-DDB1 zovuta zimawonedwa ndi Thalidomide, Lenalidomide ndi Pomalidomide, ndi IC50 values of ~30μm, ~3μM ndi ~3μM, motero, Maselo ochepetsetsa a CRBN (U266-CRBN60 ndi U266-CRBN75) samvera kwambiri kusiyana ndi maselo a makolo ku zotsatira za antiproliferative Lenalidomide kudutsa mlingo-mayankhidwe osiyanasiyana a 0.01 mpaka 10μM[3]. Lenalidomide, analogi ya thalidomide, imagwira ntchito ngati guluu molekyulu pakati pa E3 ubiquitin ligase cereblon ndi CKI.α akuwonetsedwa kuti apangitse kufalikira ndi kuwonongeka kwa kinase iyi, motero kupha maselo a leukemic ndi p53 activation.

Kawopsedwe wa Mlingo wa Lenalidomide mpaka 15, 22.5, ndi 45 mg/kg kudzera munjira za IV, IP, ndi PO. Zochepa chifukwa cha kusungunuka mu galimoto yathu ya PBS, Mlingo wopambana wa Lenalidomide uwu umaloledwa bwino kupatula kufa kwa mbewa imodzi (yomwe ili ndi mlingo umodzi) pa mlingo wa 15 mg/kg IV. Makamaka, palibe poizoni wina yemwe amawonedwa mu kafukufuku wa IV Mlingo wa 15 mg/kg (n=3) kapena 10 mg/kg (n=45) kapena pamlingo wina uliwonse kudzera munjira za IV, IP, ndi PO.

Kusungirako