GIzina rifite ingufu:venetoclax (ven ET oh klax)
Izina ry'ikirango: Venclexta, Venclexta Gutangira

Venetoclax ikoreshwa mu kuvura indwara ya lymphocytike idakira cyangwa lymphocytike leukemia nto ku bantu bakuru. Venetoclax ikoreshwa wenyine cyangwa ifatanije nindi miti ya kanseri kugirango ivure ibi bihe.

Venetoclax ikoreshwa ifatanije na azacitidine, decitabine, cyangwa cytarabine mu kuvura indwara ya myeloid ikaze. Uku guhuriza hamwe gukoreshwa kubakuze bafite imyaka 75 cyangwa irenga, cyangwa badashobora gukoresha chimiotherapie isanzwe kubera ubundi buzima bwubuvuzi.

Venetoclax rimwe na rimwe itangwa nyuma yandi miti yananiwe.

Venetoclax irashobora kandi gukoreshwa mubikorwa bitanditswe muriki gitabo cyimiti.

Ibisobanuro

Venetoclax (ABT-199; GDC-0199) ni imbaraga zikomeye, zitoranya kandi zikoreshwa mu kanwa bioavailable Bcl-2 inhibitor hamwe na Ki iri munsi ya 0.01 nM. Venetoclax itera autophagy.

Muri Vitro

Venetoclax (ABT-199) yica cyane selile FL5.12-BCL-2 (EC50 = 4 nM), Venetoclax (ABT-199) yerekana ibikorwa bidakomeye cyane kurwanya selile FL5.12-BCL-XL (EC50 = 261 nM). ABT-199 irerekana kandi guhitamo mubikoko by’inyamabere ebyiri-bivangavanze, aho bihungabanya inganda za BCL-2-BIM (EC50 = 3 nM) ariko ntibikora neza kurwanya BCL-XL-BCL-XS (EC50 = 2.2μM) cyangwa MCL-1-NOXA.

Nyuma yo kunywa umunwa umwe wa 12.5 mg kuri kg ibiro byumubiri mubishushanyo mbonera byakomotse kuri RS4; selile 11 (BYOSE), Venetoclax (ABT-199) itera ikura ryinshi ryikibyimba (TGImax) cya 47% (P <0.001) no gukura kwikibyimba gutinda (TGD) ya 26% (P <0.05) [1].

Kuvura ibishushanyo mbonera byashizweho (imbeba ya xenograft yerekana ibibyimba bya T-ALL umurongo wa selile LOUCY) hamwe na Venetoclax (ABT-199) 100 mg / kg muminsi 4 bivamo kugabanya cyane umutwaro wa leukemic.