I-Lisaftoclax (APG-2575) Ithola Ukuvunyelwa Kokuqala Okunemibandela KwaseShayina Kwe-CLL/SLL, Okuphawula Ingqophamlando Yomhlaba Wonke Ekwelashweni Kwe-Bcl-2 Inhibitor

Muva nje, i-Ascentage Pharma imemezele ukuthi i-Bcl-2 selective inhibitor lisaftoclax (APG-2575) yayo entsha ivunyelwe yi-National Medical Products Administration (NMPA) yaseShayina yokwelapha iziguli ezindala ezine-chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) ezake zathola okungenani ukwelashwa okukodwa okuhleliwe okuhlanganisa ne-Bruton's tyrosine kinase (BTK) inhibitors, okwenza i-lisaftoclax ibe yi-Bcl-2 inhibitor yokuqala ethola imvume enemibandela kanye nemvume yokumaketha yokwelapha iziguli ezine-CLL/SLL eShayina, kanye ne-Bcl-2 inhibitor yesibili evunyelwe emhlabeni jikelele.

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I-Lisaftoclax iyisidakamizwa esisha esikhethekile, esinikezwa ngomlomo esinomuthi omncane we-Bcl-2 okhethiwe owakhiwe yi-Ascntage Pharma ukuze welaphe iziguli ezine-malignancies ngokuvimbela ngokukhetha iphrotheni yokulwa ne-apoptotic i-Bcl-2 bese kubuyiselwa inqubo evamile ye-apoptosis kumaseli omdlavuza. Ezivivinyweni zemitholampilo, i-lisaftoclax ibonise amandla amakhulu okwelapha kuma-malignancies amaningi e-hematologic kanye nama-tumors aqinile, ikakhulukazi ku-CLL/SLL, kokubili njengokwelashwa okukodwa kanye nokuhlanganiswa.

Lokhu kuvunywa kusekelwe emiphumeleni evela ocwaningweni olubalulekile lweSigaba II sokubhalisa (APG2575CC201) olwaklanyelwe ukuhlola ukusebenza kahle kanye nokuphepha kwe-lisaftoclax monotherapy ezigulini ezine-CLL/SLL ephinde yabuya noma engaphenduli, kanye nesilinganiso sokuphendula esiphelele (ORR) njengephuzu eliyinhloko. I-Lisaftoclax ibonise ukusebenza kahle okunamandla kanye ne-ORR ehlangabezana nephuzu elibekiwe kusengaphambili ezigulini ezelaphe ngaphambilini ngama-BTK inhibitors kanye/noma i-immunochemotherapy. Ngaphezu kwalokho, i-lisaftoclax ibonise iphrofayili yokuphepha enhle engenaso isifo se-tumor-lysis (TLS) esenzeka ngesikhathi socwaningo, ukwanda okuphansi kobuthi be-hematologic okwakungalawuleka, kanye nokwanda okuphansi kobuthi obungebona be-hematologic okwakuyibanga 1-2.

I-CLL/SLL iyisifo esibangelwa yi-hematologic cancer esibangelwa ama-neoplasms e-B-cell avuthiwe. Ithinta kakhulu abantu asebekhulile abanezifo ezintsha ezingaphezu kuka-100,000 ezibikwa emhlabeni wonke minyaka yonke1. E-China, lapho izinga lokwanda kwe-CLL/SLL liphansi kunelamazwe asentshonalanga, lesi sifo senzeka ngesivinini esikhuphuka ngokushesha, ngeminyaka emincane yokuqala kanye nolaka oluphezulu2. Njengendlela yamanje eyinhloko yokwelashwa kokuqala kwe-CLL/SLL, ama-inhibitors e-BTK athuthukise kakhulu imiphumela yokwelashwa kweziguli. Kodwa-ke, ama-inhibitors e-BTK asabhekene nezinkinga ezahlukahlukene ezifana nekhono elilinganiselwe lokudala izimpendulo ezijulile, ingozi ephezulu yokubuyela emuva ekwelashweni kwesikhathi esiphakathi nesikhathi eside, ubuthi kanye nokungabekezeleleki okuhambisana nokwelashwa isikhathi eside; ngakho-ke, isidingo sezinketho zokwelapha eziphephile nezisebenza kahle kakhulu zeziguli ezine-CLL/SLL.

Ukwethulwa kwama-inhibitors e-Bcl-2 kuye kwashintsha kakhulu ukwelashwa kwe-CLL/SLL. I-apoptosis suppressor factor i-Bcl-2, evame ukuvela kakhulu ezinhlotsheni ezahlukene ze-hematologic monicancies, ikakhulukazi i-CLL/SLL, iyindlela ebalulekile lapho amaseli esimila egwema khona i-apoptosis. Kodwa-ke, ukutholakala kwe-Bcl-2 inhibitor njengenhloso yokwelapha kuyinselele kakhulu ngoba indlela esebenza ngayo isekelwe ekusebenzisaneni kwamaprotheni-protein (PPI). I-interface yokubopha ye-Bcl-2 inkulu kakhulu, okwenza kube nzima ngama-inhibitors amancane ukuba aveze imiphumela yokuvimba. Ngaphezu kwalokho, iphrotheni ye-Bcl-2 itholakala kwi-mitochondria, enesakhiwo se-membrane ephindwe kabili, ingenye yezingxenye zeseli eziyinkimbinkimbi kakhulu futhi eziyinselele njengoba idinga ukuthi imithi ingene kuqala ku-membrane yeseli ngaphambi kokuba isebenze ku-membrane ye-mitochondrial. Ngaphambi kwalokhu, akukho inhibitor ye-Bcl-2 eyayivunyelwe ukwelashwa kwe-CLL/SLL eShayina. Lokhu kuvunyelwa kwe-lisaftoclax kugcwalisa igebe lokwelashwa ku-CLL/SLL, okuletha ithemba elisha ezigulini eziningi ezweni.

Njengamanje, kusenezivivinyo eziningi zemitholampilo zobuchwepheshe obusha bokulwa nomdlavuza eShayina ezifuna iziguli. Ukubonisana ngemithi emisha kanye nobuchwepheshe, ungaxhumana noMnyango Wezizwe Ngezizwe Wesibhedlela iBeijing South Region Oncology.

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Isikhathi sokuthunyelwe: Julayi-15-2025