GIgama lamandla:venetoclax (ven ET oh klax)
Igama lebrand: IVenclexta, iVenclexta yokuQalisa iPakethi

I-Venetoclax isetyenziselwa ukunyanga i-lymphocytic leukemia engapheliyo okanye i-lymphocytic leukemia encinci kubantu abadala.IVenetoclax isetyenziswa yodwa okanye idityaniswe namanye amayeza omhlaza ukunyanga ezi meko.

I-Venetoclax isetyenziselwa ukudibanisa ne-azacitidine, i-decitabine, okanye i-cytarabine ukunyanga i-acute myeloid leukemia.Le ndibaniselwano isetyenziselwa abantu abadala abaneminyaka engama-75 nangaphezulu, okanye abangakwaziyo ukusebenzisa ichemotherapy eqhelekileyo ngenxa yezinye iimeko zonyango.

I-Venetoclax ngamanye amaxesha inikezelwa emva kokuba olunye unyango luhlulekile.

I-Venetoclax ingasetyenziselwa iinjongo ezingadweliswanga kwesi sikhokelo samayeza.

Inkcazo

I-Venetoclax (ABT-199; GDC-0199) inamandla kakhulu, ikhethiweyo kunye ne-Bcl-2 inhibitor ye-bioavailable ngomlomo kunye ne-Ki engaphantsi kwe-0.01 nM.I-Venetoclax yenza i-autophagy.

I-In vitro

I-Venetoclax (ABT-199) ibulala ngokunamandla iiseli ze-FL5.12-BCL-2 (EC50 = 4 nM), i-Venetoclax (ABT-199) ibonisa umsebenzi obuthathaka kakhulu kwiiseli ze-FL5.12-BCL-XL (EC50 = 261 nM).I-ABT-199 iphinda ibonise ukukhetha kwiimvavanyo ze-mammalian ezimbini ze-hybridi zeselula, apho ziphazamisa ii-BCL-2-BIM complexes (EC50 = 3 nM) kodwa zingasebenzi kakhulu kwi-BCL-XL-BCL-XS (EC50 = 2.2)μM) okanye i-MCL-1-NOXA complexes.

Emva komthamo omnye womlomo we-12.5 mg ngekhilogram ubunzima bomzimba kwi-xenografts evela kwi-RS4; iiseli ze-11 (ALL), i-Venetoclax (ABT-199) ibangela inhibition enkulu yokukhula kwe-tumor (TGImax) ye-47% (P <0.001) kunye nokukhula kwe-tumor ukukhula kwe-tumor. ukulibaziseka (TGD) kwe-26% (P <0.05) [1].

Unyango lwe-xenografted esekelwe (imodeli ye-mouse xenograft ye-T-ALL line line LOUCY) i-tumor kunye ne-Venetoclax (ABT-199) i-100 mg / kg kwiintsuku ze-4 iphumela ekunciphiseni okukhulu komthwalo we-leukemic.