Uji Preklinis 177Lu-DOTA-Trastuzumab: Radiofarmaseutika Potensial untuk Terapi Kanker Payudara HER-2 Positif

  • MARTALENA RAMLI NATIONAL NUCLEAR ENERGY OF INDONESIA
  • BASUKI HIDAYAT DR. HASAN SADIKIN GENERAL HOSPITAL
  • SRI AGUSWARINI NATIONAL NUCLEAR ENERGY OF INDONESIA
  • KARYADI KARYADI NATIONAL NUCLEAR ENERGY OF INDONESIA
  • CAHYA NOVA ARDIYATNO NATIONAL NUCLEAR ENERGY OF INDONESIA
  • HAMMAD SUBUR NATIONAL NUCLEAR ENERGY OF INDONESIA
  • TITIS SEKAR HUMANI NATIONAL NUCLEAR ENERGY OF INDONESIA
  • RIEN RITAWIDYA NATIONAL NUCLEAR ENERGY OF INDONESIA
  • ABDUL MUTALIB NATIONAL NUCLEAR ENERGY OF INDONESIA
  • JOHAN MASJHUR DR. HASAN SADIKIN GENERAL HOSPITAL

Abstrak

Radiofarmaka 177Lu-(1,4,7,10-tetraazacyclododecane-N,N’,N”,N”’-tetra acetic acid)-trastuzumab (177Lu-DOTA-trastuzumab), berbasis antihuman epithelial receptor type 2 (HER-2) antibodi monoklonal, yang diharapkan potensial untuk diagnosis dan terapi kanker payudara positif HER-2, dengan kemurnian radiokimia besar dari 99% telah berhasil dipreparasi. Uji preklinis yang dimaksudkan untuk mendapatkan data dasar sebelum pelaksanaan uji klinis dan khususnya untuk melihat efektifitas 177Lu-DOTA-trastuzumab dalam membunuh sel kanker yang mengekspresikan HER-2, telah berhasil dilakukan. Data dasar tersebut diantaranya adalah data clearance, citra dengan gamma kamera dan data hasil uji sitoksisitas. Hasil uji clearance memperlihatkan bahwa ekskresi radioaktif setelah pemberian 177Lu-DOTA-trastuzumab pada tikus sehat lebih cepat melalui urin dibandingkan dengan eksresi melalui feses. Hasil pencitraan dengan kamera gamma pada tikus normal 144 jam setelah pemberian 177Lu-DOTA-trastuzumab memperlihat adanya residu radioaktif di daerah hati (< 5%, berdasarkan hasil uji biodistribusi). Residu ini lebih rendah jika dibandingkan dengan residu radioaktif pada hati yang dilaporkan untuk 111In-NSL-trastuzumab. Walaupun residu radioaktif ini relatif rendah, tetapi harus tetap menjadi perhatian yang serius pada saat 177Lu-DOTA-trastuzumab akan digunakan pada pasien penderita kanker. Uji sitotoksisitas memperlihatkan 177Lu-DOTA-trastuzumab jauh lebih efektif dalam membunuh sel kanker positif HER-2 (SKOV-3 cell lines) dibandingkan dengan trastuzumab tidak bertanda.

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Diterbitkan
2013-09-30
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RAMLI, MARTALENA et al. Uji Preklinis 177Lu-DOTA-Trastuzumab: Radiofarmaseutika Potensial untuk Terapi Kanker Payudara HER-2 Positif. JURNAL ILMU KEFARMASIAN INDONESIA, [S.l.], v. 11, n. 2, p. 116-122, sep. 2013. ISSN 2614-6495. Tersedia pada: <http://jifi.farmasi.univpancasila.ac.id/index.php/jifi/article/view/203>. Tanggal Akses: 02 apr. 2025
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