GMagaca tamarta:Venetoclax (ven ET oh klax)
Magaca Summada: Venclexta, Xidhmada Bilowga Venclexta

Venetoclax waxaa loo isticmaalaa in lagu daweeyo leukemia lymphocytic raaga ama leukemia yar oo leukemia ee dadka waaweyn. Venetoclax waxaa loo isticmaalaa kaligiis ama lagu daro daawooyinka kale ee kansarka si loo daaweeyo xaaladahan.

Venetoclax waxaa loo isticmaalaa in lagu daro azacitidine, decitabine, ama cytarabine si loo daaweeyo leukemia myeloid ba'an. Isku dhafkan waxaa loogu talagalay dadka waaweyn ee jira 75 sano ama ka weyn, ama aan isticmaali karin kiimoterabiga caadiga ah xaalado kale oo caafimaad dartood.

Venetoclax ayaa mararka qaarkood la bixiyaa ka dib markii daawaynta kale ay fashilanto.

Venetoclax waxa kale oo loo isticmaali karaa ujeedooyin aan lagu xusin hagaha daawaynta.

Sharaxaada

Venetoclax (ABT-199; GDC-0199) waa mid aad u awood badan, door ah oo afka laga heli karo Bcl-2 inhibitor oo leh Ki ka yar 0.01 nM. Venetoclax waxay keentaa autophagy.

In Vitro

Venetoclax (ABT-199) waxay si xoog leh u dishaa unugyada FL5.12-BCL-2 (EC50=4 nM), Venetoclax (ABT-199) waxay muujinaysaa waxqabad aad u daciif ah oo ka dhan ah unugyada FL5.12-BCL-XL (EC50=261 nM). ABT-199 waxa kale oo ay ku tusinaysaa xulashada naasleyda gacanta ee laba-isku-dhafan, halkaas oo ay carqaladayso dhismayaasha BCL-2-BIM (EC50=3 nM) laakiin aad bay waxtar uga yar tahay BCL-XL-BCL-XS (EC50=2.2).μM) ama dhismayaasha MCL-1-NOXA.

Ka dib hal dose oo afka ah oo ah 12.5 mg halkii kg miisaanka jirka ee xenografts oo laga soo qaatay RS4; 11 unug (ALL), Venetoclax (ABT-199) waxay sababtaa xannibaadda koritaanka ugu badan ee burooyinka (TGImax) ee 47% (P <0.001) iyo koritaanka burooyinka daahitaanka (TGD) ee 26% (P<0.05)[1].

Daawaynta xenografted la aasaasay (qaab mouse xenograft ah oo ah T-ALL cell line LOUCY) burooyinka leh Venetoclax (ABT-199) 100 mg/kg ee maalmaha 4 waxay keenaysaa hoos u dhac weyn oo ah culeyska leukemic.