Gaha eneric:venetoclax (ven ET oh klax)
Aha ika: Venclexta, ngwugwu mmalite Venclexta

A na-eji Venetoclax agwọ ọrịa leukemia lymphocytic na-adịghị ala ala ma ọ bụ obere leukemia lymphocytic na ndị okenye. A na-eji Venetoclax naanị ma ọ bụ jikọtara ya na ọgwụ ọrịa kansa ndị ọzọ iji gwọọ ọnọdụ ndị a.

A na-eji Venetoclax yana azacitidine, decitabine, ma ọ bụ cytarabine na-agwọ ọrịa leukemia myeloid buru ibu. Ngwakọta a bụ maka ndị okenye gbara afọ 75 ma ọ bụ karịa, ma ọ bụ ndị enweghị ike iji kemoterapi ọkọlọtọ n'ihi ọnọdụ ahụike ndị ọzọ.

A na-enye Venetoclax mgbe ụfọdụ mgbe ọgwụgwọ ndị ọzọ daa.

Enwere ike iji Venetoclax mee ihe maka ebumnuche edepụtaghị na ntuziaka ọgwụ a.

Nkọwa

Venetoclax (ABT-199; GDC-0199) bụ ike dị ukwuu, nhọrọ na ọnụ na-egbochi ihe mgbochi Bcl-2 nwere Ki nke na-erughị 0.01 nM. Venetoclax na-ebute autophagy.

Na Vitro

Venetoclax (ABT-199) na-egbusi mkpụrụ ndụ FL5.12-BCL-2 (EC50 = 4 nM), Venetoclax (ABT-199) na-egosi ọrụ siri ike megide sel FL5.12-BCL-XL (EC50 = 261 nM). ABT-199 na-egosikwa selectivity na cellular mammalian ngwakọ ngwakọ abụọ, ebe ọ na-akpaghasị ogige BCL-2-BIM (EC50 = 3 nM) mana ọ naghị adị irè megide BCL-XL-BCL-XS (EC50=2.2).μM) ma ọ bụ MCL-1-NOXA.

Mgbe otu ọnụọgụ ọnụ nke 12.5 mg kwa kilogram nke ịdị arọ ahụ dị na xenografts sitere na RS4; sel 11 (ALL), Venetoclax (ABT-199) na-ebute oke mgbochi uto tumor (TGImax) nke 47% (P <0.001) na uto tumor. igbu oge (TGD) nke 26% (P<0.05)[1].

Ọgwụgwọ nke xenograft guzobere (ụdị xenograft òké nke T-ALL cell line LOUCY) etuto nwere Venetoclax (ABT-199) 100 mg / kg maka ụbọchị 4 na-ebute mbelata dị ukwuu nke ibu leukemic.