GIgama le-eneric:i-venetoclax (ven ET oh klax)
I gama le-brand: Venclexta, Venclexta Starting Pack

I-Venetoclax isetshenziselwa ukwelapha i-lymphocytic leukemia engapheli noma i-lymphocytic leukemia encane kubantu abadala. I-Venetoclax isetshenziswa iyodwa noma ihlanganiswe neminye imithi yomdlavuza ukwelapha lezi zimo.

I-Venetoclax isetshenziswa ngokuhambisana ne-azacitidine, i-decitabine, noma i-cytarabine ukwelapha i-acute myeloid leukemia. Le nhlanganisela isetshenziselwa abantu abadala abaneminyaka engu-75 noma ngaphezulu, noma abangakwazi ukusebenzisa ukwelashwa ngamakhemikhali okujwayelekile ngenxa yezinye izimo zezokwelapha.

I-Venetoclax ngezinye izikhathi inikezwa ngemva kokuba ezinye izindlela zokwelapha zehlulekile.

I-Venetoclax ingase isetshenziselwe izinjongo ezingabaliwe kulo mhlahlandlela wemithi.

Incazelo

I-Venetoclax (ABT-199; GDC-0199) iyi-Bcl-2 inhibitor enamandla kakhulu, ekhethayo futhi etholakala ngomlomo ene-Ki engaphansi kuka-0.01 nM. I-Venetoclax idala i-autophagy.

Ku-Vitro

I-Venetoclax (ABT-199) ibulala ngokunamandla amaseli e-FL5.12-BCL-2 (EC50=4 nM), i-Venetoclax (ABT-199) ibonisa umsebenzi obuthakathaka kakhulu ngokumelene namaseli e-FL5.12-BCL-XL (EC50=261 nM). I-ABT-199 iphinda ibonise ukukhetha ekuhlolweni kwe-hybrid yezilwane ezincelisayo ezimbili, lapho iphazamisa izakhiwo ze-BCL-2-BIM (EC50=3 nM) kodwa ingasebenzi kahle kakhulu ku-BCL-XL-BCL-XS (EC50=2.2)μM) noma i-MCL-1-NOXA complexes.

Ngemuva komthamo owodwa womlomo we-12.5 mg ngekhilogremu ngayinye yesisindo somzimba kuma-xenografts atholakala ku-RS4; amaseli ayi-11 (ALL), i-Venetoclax (ABT-199) ibangela ukuvimbela ukukhula kwesimila okukhulu (TGImax) kwama-47% (P<0.001) nokukhula kwesimila ukubambezeleka (TGD) kokungu-26% (P<0.05)[1].

Ukwelashwa kwe-xenografted eqinisekisiwe (imodeli ye-xenograft yegundane ye-T-ALL cell line LOUCY) izimila nge-Venetoclax (ABT-199) 100 mg/kg izinsuku ezingu-4 kuphumela ekuncipheni okukhulu komthwalo we-leukemic.