Nkọwa

Lenalidomide (CC-5013) bụ ihe sitere na Thalidomide na immunomodulator na-arụ ọrụ ọnụ.Lenalidomide (CC-5013) bụ ligand nke ubiquitin E3 ligase cereblon (CRBN), ọ na-eme ka njedebe nhọrọ na mmebi nke ihe odide lymphoid abụọ, IKZF1 na IKZF3, site na CRBN-CRL4 ubiquitin ligase.Lenalidomide (CC-5013) na-egbochi kpọmkwem uto nke lymphomas B-cell tozuru okè, gụnyere multiple myeloma, ma mee ka IL-2 hapụ mkpụrụ ndụ T.

ndabere

Lenalidomide (nke a makwaara dị ka CC-5013), ihe sitere na thalidomide ọnụ, bụ onye na-ahụ maka antineoplastic na-egosipụta ọrụ antitumor site na usoro dị iche iche, gụnyere ịgbalite usoro ahụ ji alụso ọrịa ọgụ, mgbochi angiogenesis, na mmetụta antineoplastic kpọmkwem.A mụọla ya nke ọma maka ọgwụgwọ nke otutu myeloma na ọrịa myelodysplastic yana ọrịa lymphoproliferative gụnyere ọrịa leukemia lymphocytic na-adịghị ala ala (CLL) na lymphoma na-abụghị Hodgkin.Dị ka nnyocha e mere n'oge na-adịbeghị anya, Lnalidomide na-akwalite ma na-eweghachi ọrụ nke usoro ahụ ji alụso ọrịa ọgụ na ndị ọrịa CLL site n'ime ka mkpụrụ ndụ ihe nketa ego dị na lymphocytes leukemic na-eme ka ahụ dịkwuo mma na mmepụta immunoglobulins, yana imeziwanye ikike nke mkpụrụ ndụ T na mkpụrụ ndụ leukemic iji mepụta synapses na T. lymphocytes.

Ntụaka

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

Na Vitro

Lenalidomide nwere ike na-akpali akpali T cell proliferation na IFN-γ na mmepụta IL-2.E gosiputara Lenalidomide iji gbochie mmepụta nke cytokines pro inflammatory TNF-α, IL-1, IL-6, IL-12 ma bulie mmepụta nke cytokine mgbochi mkpali IL-10 sitere na PBMC mmadụ.Lenalidomide na-ebelata mmepụta nke IL-6 ozugbo yana site na igbochi ọtụtụ mkpụrụ ndụ myeloma (MM) na ụbụrụ ụbụrụ stromal cell (BMSC), nke na-eme ka apoptosis nke mkpụrụ ndụ myeloma dị elu.A na-ahụ mmekọrịta dabere na dose na mgbagwoju CRBN-DDB1 na Thalidomide, Lenalidomide na Pomalidomide, yana ụkpụrụ IC50 nke ~ 30.μM, ~3μM na ~ 3μM, n'otu n'otu, mkpụrụ ndụ okwu CRBN ndị a belatara (U266-CRBN60 na U266-CRBN75) adịghị anabata sel ndị nne na nna na mmetụta antiproliferative Lenalidomide gafee oke nzaghachi dose nke 0.01 ruo 10.μM[3].Lenalidomide, analog nke thalidomide, na-arụ ọrụ dị ka gluu molekụla n'etiti mmadụ E3 ubiquitin ligase cereblon na CKI.α E gosipụtara na-akpalite nbibi na mmebi nke kinase a, si otú a na-eche na ọ na-egbu mkpụrụ ndụ leukemia site na p53 activation.

Nsi nke Lenalidomide doses ruru 15, 22.5, na 45 mg/kg site na IV, IP, na PO ụzọ nchịkwa.Oke solubility n'ime ụgbọ ala dosing PBS anyị, a na-anabata ọgwụ Lenalidomide kacha nke a ga-enweta nke ọma ma ewezuga otu ọnwụ òké (nke ngụkọta dosed anọ) na 15 mg/kg IV dose.N'ụzọ doro anya, ọ dịghị ihe ọ bụla toxicities na-ahụ na ọmụmụ na IV doses nke 15 mg / kg (n = 3) ma ọ bụ 10 mg / kg (n = 45) ma ọ bụ na ihe ọ bụla ọzọ dose larịị site IV, IP, na PO ụzọ.

Nchekwa

Ọdịdị chemical

Data bayoloji emetụtara

Data bayoloji emetụtara