Ngomhlaka-15 kuMbasa 2025, i-InnoCare Pharma yamemezela ukuthi i-Center for Drug Evaluation (CDE) ye-China National Medical Products Administration (NMPA) yamukele isicelo esisha semithi (NDA) sesizukulwane sayo esisha se-pan-TRK inhibitor zurletrectinib (ICP-723) yokwelapha iziguli ezindala nentsha (ezineminyaka engu-12 kuya kwengu-18 ubudala) ezinezimila eziqinile ezithinta ukuhlanganiswa kwezakhi zofuzo ze-NTRK.
Izakhi zofuzo ze-NTRK fusion zenzeka ezinhlotsheni ezahlukene zezimila zabantu abadala kanye nezingane. Kwezinye izimila ezingavamile, njenge-salivary gland carcinoma, umdlavuza webele oyimfihlo, kanye ne-infantile fibrosarcoma, izinga lokuhlanganiswa kwezakhi zofuzo ze-NTRK lidlula u-90%[1]. Kulinganiselwa ukuthi kunezimo ezintsha ezingaba ngu-6,500 zezimila eziqinile ze-NTRK fusion-positive ezitholakalayo, eShayina njalo ngonyaka. Kunezidingo zezokwelapha ezingahlangatshezwanga kakhulu kule ndawo ngenxa yokuntuleka kwezinketho zokwelapha ezisebenzayo.
I-Zurletrectinib iyi-TRK inhibitor entsha esanda kuthuthukiswa ebonise ukusebenza ngokumelene ne-TRK WT kanye nama-mutant kinases.
I-British Journal of Cancer, eyingxenye yephephabhuku lesayensi elihamba phambili i-Nature, ishicilele iphepha elinesihloko esithi “I-Zurletrectinib iyisivimbeli se-TRK sesizukulwane esilandelayo esinomsebenzi oqinile wangaphakathi kwekhanda ngokumelene nezimila ze-NTRK fusion-positive ezimelana ngqo nezidakamizwa zesizukulwane sokuqala”. Leli phephabhuku liphethe ngokuthi i-zurletrectinib iyisivimbeli se-TRK sesizukulwane esilandelayo esisha, esinamandla kakhulu esinokungena okuphezulu kobuchopho emzimbeni kanye nomsebenzi oqinile wangaphakathi kwekhanda kunezinye izidakamizwa zesizukulwane esilandelayo.
Leli phepha liveze ukuthi i-zurletrectinib ibonise amandla aqinile ngokumelene ne-TRKA, TRKB, kanye ne-TRKC WT kinases, kanye nokuguqulwa kokumelana okutholiwe kwe-TRKA G595R kanye ne-TRKA G667C. I-Zurletrectinib yayisebenza kakhulu kunezinye izizukulwane zokuqala ezivunyelwe yi-FDA noma ezihlolwe ngokwezokwelapha (i-larotrectinib) kanye nezizukulwane ezilandelayo (i-selitrectinib kanye ne-repotrectinib) TRK inhibitors ngokumelene nezinhlobo eziningi zokuguqulwa kokumelana kwe-TRK inhibitors. Ngokufanayo, i-zurletrectinib (1 mg/kg BID) yavimbela ukukhula kwesimila kumamodeli e-xenograft atholakala kumaseli e-NTRK fusion-positive ngesilinganiso esiphansi ngokuphindwe ka-30 uma kuqhathaniswa ne-selitrectinib.
Leli phepha liphinde labonisa ukuthi, ocwaningweni lwe-CNS penetrant pharmacokinetic kumagundane e-SD, i-zurletrectinib ibonise ikhono elithuthukisiwe lokungena emgodleni wegazi nobuchopho, ifinyelela ebuchosheni ngempumelelo kakhulu kune-selitrectinib kanye ne-repotrectinib. Ukungena kobuchopho okwandisiwe kwe-Zurletrectinib nakho kwahunyushwa kwaba umsebenzi othuthukisiwe wokulwa nomdlavuza. Kumodeli ye-xenograft yegundane le-orthotopic glioma ephethe ukuguqulwa kokumelana kwe-TRKA G598R/G670A, i-zurletrectinib (15 mg/kg) ithuthukise kakhulu ukusinda kwamagundane aphethe i-orthotopic NTRK fusion-positive, TRK-mutant gliomas (ukusinda okumaphakathi = izinsuku ezingu-41.5, 66.5, kanye nezinsuku ezingu-104 ze-selitrectinib, repotrectinib, kanye ne-zurletrectinib ngokulandelana; P < 0.05), okubonisa ukusebenza kahle okuphezulu uma kuqhathaniswa ne-repotrectinib (15 mg/kg) kanye ne-selitrectinib (30 mg/kg) (P=0.0384 kanye no-0.0022, ngokulandelana), enephrofayili yokuphepha enhle kakhulu.
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.
Inombolo yocingo: 4008803716
Email：myimmnet@163.com
Isikhathi sokuthunyelwe: Ephreli-17-2025