GDzina la eneric:venetoclax (ven ET oh klax)
Dzina la Brand: Venclexta, Venclexta Starting Pack

Venetoclax amagwiritsidwa ntchito pochiza matenda a lymphocytic leukemia kapena ang'onoang'ono a lymphocytic leukemia mwa akuluakulu. Venetoclax imagwiritsidwa ntchito yokha kapena kuphatikiza ndi mankhwala ena a khansa pochiza izi.

Venetoclax amagwiritsidwa ntchito limodzi ndi azacitidine, decitabine, kapena cytarabine pochiza matenda oopsa a myeloid leukemia. Kusakaniza kumeneku kumagwiritsidwa ntchito kwa akuluakulu omwe ali ndi zaka 75 kapena kuposerapo, kapena omwe sangathe kugwiritsa ntchito mankhwala amphamvu a chemotherapy chifukwa cha matenda ena.

Nthawi zina Venetoclax imaperekedwa pambuyo poti mankhwala ena alephera.

Venetoclax itha kugwiritsidwanso ntchito pazinthu zomwe sizinalembedwe mu bukhuli lamankhwala.

Kufotokozera

Venetoclax (ABT-199; GDC-0199) ndi yamphamvu kwambiri, yosankha komanso yopezeka pakamwa ya Bcl-2 inhibitor yokhala ndi Ki yosakwana 0.01 nM. Venetoclax imayambitsa autophagy.

Mu Vitro

Venetoclax (ABT-199) imapha mwamphamvu maselo a FL5.12-BCL-2 (EC50 = 4 nM), Venetoclax (ABT-199) imasonyeza ntchito yofooka kwambiri motsutsana ndi maselo a FL5.12-BCL-XL (EC50 = 261 nM). ABT-199 imawonetsanso kusankhidwa kwa ma cell a mammalian two-hybrid assays, pomwe imasokoneza BCL-2-BIM complexes (EC50=3 nM) koma imakhala yocheperako polimbana ndi BCL-XL-BCL-XS (EC50=2.2)μM) kapena MCL-1-NOXA zovuta.

Pambuyo pa mlingo umodzi wapakamwa wa 12.5 mg pa kilogalamu ya kulemera kwa thupi mu xenografts yochokera ku RS4; maselo 11 (ALL), Venetoclax (ABT-199) imayambitsa chotupa chachikulu choletsa kukula (TGImax) cha 47% (P <0.001) ndi kukula kwa chotupa kuchedwa (TGD) kwa 26% (P<0.05)[1].

Chithandizo cha zotupa za xenografted (mouse xenograft model wa T-ALL cell line LOUCY) zotupa ndi Venetoclax (ABT-199) 100 mg/kg kwa masiku 4 zimabweretsa kuchepa kwakukulu kwa leukemic katundu.