Generic Zita:venetoclax (ven ET oh klax)
Zita reBrand: Venclexta, Venclexta Kutanga Pack

Venetoclax inoshandiswa kurapa chronic lymphocytic leukemia kana diki lymphocytic leukemia muvakuru. Venetoclax inoshandiswa yoga kana musanganiswa nemimwe mishonga yegomarara kurapa mamiriro aya.

Venetoclax inoshandiswa pamwe chete neazacitidine, decitabine, kana cytarabine kurapa acute myeloid leukemia. Musanganiswa uyu ndewekushandiswa kune vanhu vakuru vane makore makumi manomwe nemashanu kana kupfuura, kana vasingakwanise kushandisa yakajairwa chemotherapy nekuda kwemamwe mamiriro ekurapa.

Venetoclax dzimwe nguva inopiwa mushure mokunge mamwe marapirwo akundikana.

Venetoclax inogonawo kushandiswa kune zvinangwa zvisina kunyorwa mugwaro remishonga.

Tsanangudzo

Venetoclax (ABT-199; GDC-0199) ine simba zvakanyanya, inosarudza uye inoramwa bioavailable Bcl-2 inhibitor ine Ki isingasviki 0.01 nM. Venetoclax inokonzera autophagy.

In Vitro

Venetoclax (ABT-199) inouraya zvine simba FL5.12-BCL-2 masero (EC50 = 4 nM), Venetoclax (ABT-199) inoratidza basa risina simba rinopesana neFL5.12-BCL-XL masero (EC50 = 261 nM). ABT-199 inoratidzawo kusarudza mumasero mammalian maviri-hybrid assays, apo inokanganisa BCL-2-BIM complexes (EC50=3 nM) asi isinganyanyi kushanda paBCL-XL-BCL-XS (EC50=2.2)μM) kana MCL-1-NOXA yakaoma.

Mushure meyero imwechete yemuromo ye12.5 mg pakg uremu hwemuviri mune xenografts inotorwa kubva kuRS4; 11 masero (ALL), Venetoclax (ABT-199) inokonzera maximal bundu kukura inhibition (TGImax) ye47% (P <0.001) uye bundu kukura kunonoka (TGD) kwe26% (P <0.05)[1].

Kurapa kwezvakagadzirwa xenografted (a mouse xenograft model yeT-ALL cell line LOUCY) mapundu ane Venetoclax (ABT-199) 100 mg/kg kwemazuva 4 anokonzera kuderedzwa kukuru kwemutoro weleukemic.