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 otutu 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 [2]. 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 egosiputara iji kpalite nbibi na mmebi nke kinase a, si otú a na-eche na ọ na-egbu mkpụrụ ndụ leukemic site na p53 activation.

Nsi nke Lenalidomide doses ruo 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 oke Lenalidomide doses a 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