Agasti 2021: Belzutifan (Welireg, Merck), i-hypoxia-inducible factor inhibitor, ivunyelwe yi-Food and Drug Administration yeziguli ezindala ezinesifo se-von Hippel-Lindau esidinga ukwelashwa kwe-renal cell carcinoma (RCC), i-central nervous system (CNS) i-hemangioblastomas, noma i-pancreatic neuroendocrine tumors (pNET) kepha ayidingi ukuhlinzwa ngokushesha.
UBelzutifan wafundwa ezigulini ezingama-61 ezine-RHL ehambisana ne-VHL (VHL-RCC) etholwe ngokuya ngoshintsho lwe-VHL lwe-germline futhi okungenani isimila esisodwa esitholakalayo esivalelwe ensozini ku-Study 004 (NCT03401788) eqhubekayo, uphenyo lomtholampilo oluvulekile. Iziguli ezinamanye amakhemikhali ahlobene ne-VHL, njenge-CNS hemangioblastomas ne-pNET, zabhaliswa. I-Belzutifan 120 mg yanikezwa iziguli kanye ngosuku kuze kube ukuqhubekela phambili kwezifo noma ubuthi obungabekezeleleki.
Izinga lokuphendula lilonke (i-ORR) laliyisiphetho sokusebenza okuyisisekelo, njengoba kuchaziwe ngokuhlolwa kwemisebe futhi kwahlolwa yikomidi elizimele lokubuyekeza lisebenzisa i-RECIST v1.1. Isikhathi sokuphendula (i-DoR) nesikhathi sokuphendula kwakungezinye izinhloso ezimbili zokusebenza (TTR). Kubantu abane-RCC ehambisana ne-VHL, i-ORR ye-49% (95% CI: 36, 62) itholakele. Zonke iziguli ezine-VHL-RCC ezinempendulo zilandelwe okungenani izinyanga eziyi-18 ngemuva kokuqala ukwelashwa. I-DoR yasemkhatsini ayizange ihlangatshezwe; Ama-56% wabaphenduli babene-DoR engaphansi kwezinyanga eziyi-12 kanye ne-TTR emaphakathi yezinyanga eziyi-8. Iziguli ezingama-24 ezinokulinganiswa kwe-CNS hemangioblastomas zine-ORR yamaphesenti angama-63, kanti iziguli eziyi-12 ezine-pNET elinganisekayo zine-ORR yamaphesenti angama-83 ezigulini ezinamanye amakhemikhali angahlobene ne-VHL ahlobene ne-VHL. Okwe-CNS hemangioblastomas ne-pNET, i-median DoR ayihlangatshezwanga, ngezikhathi zokuphendula ezingaphansi kwezinyanga eziyi-12 kumaphesenti angama-73 namaphesenti weziguli ezingama-50, ngokulandelana.
Reduced haemoglobin, anaemia, fatigue, increased creatinine, headache, dizziness, elevated hyperglycemia, and nausea were the most prevalent adverse effects, including laboratory abnormalities, reported in almost 20% of patients who took i-belzutifan. Belzutifan usage can cause severe anaemia and hypoxia. Anemia was seen in 90% of participants in Study 004, with 7% having Grade 3 anaemia. Patients should be transfused as needed by their doctors. In individuals on belzutifan, the use of erythropoiesis stimulating drugs to treat anaemia is not suggested. Hypoxia occurred in 1.6 percent of patients in Study 004. Belzutifan can make some hormonal contraceptives ineffective, and it can harm an embryo or foetus if taken during pregnancy.
I-Belzutifan kufanele ithathwe kanye ngosuku, noma ngaphandle kokudla, kumthamo we-120 mg.
Izikhombo: https://www.fda.gov/
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