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Pemetrexed

培美曲塞
Mechanism of action:
Pemetrexed 是一種多靶點葉酸類抑制劑(multitarget antifolate)。Pemetrexed 進入細胞後,會被轉化為多麩胺酸化形式(polyglutamated pemetrexed),能抑制胸苷酸合成酶(thymidylate synthase)、二氫葉酸還原酶(dihydrofolate reductase)、甘氨醯胺核醣核苷酸甲醯轉移酶(glycinamide ribonucleotide formyltransferase)等,導致嘌呤與嘧啶合成受阻,讓細胞無法正常進行 DNA 和 RNA 合成。
Reference(s):
1. Rollins KD et al. (2005). Pemetrexed: a multitargeted antifolate. Clin Ther.
2. Lansiaux A et al. (2007). [Pemetrexed: from preclinic to clinic]. Bull Cancer.
3. Fuld AD et al. (2010). Pemetrexed in advanced non-small-cell lung cancer. Expert Opin Pharmacother.
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