Drug intelligence / Profile preview

pegliposomal doxorubicin + 5-fluorouracil

Development stage
Unknown
Lead developer
The Sixth Affiliated Hospital of Sun Yat-Sen University
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

pegliposomal doxorubicin + 5-fluorouracil is a combination chemotherapy regimen investigated by the Sixth Affiliated Hospital, Sun Yat-sen University, for the second-line treatment of metastatic gastric cancer. This regimen pairs pegylated liposomal doxorubicin (PLD)—an anthracycline formulation designed to enhance drug delivery to tumor tissues while minimizing cardiotoxicity—with 5-fluorouracil (5-FU), a well-established pyrimidine antimetabolite. Doxorubicin functions by intercalating into DNA and inhibiting DNA topoisomerase II, leading to double-strand breaks and apoptosis, while 5-FU inhibits thymidylate synthase, thereby depleting the nucleotide pools required for DNA synthesis. The combination was evaluated in a Phase II clinical trial (NCT02145559) as a potentially more tolerable and effective alternative to standard second-line agents like irinotecan in patients who have progressed on first-line therapy.

Other names
Pegylated liposomal doxorubicin + 5-fluorouracilPLD + 5-fluorouracil
02

Targets

TOP2A (DNA topoisomerase II)DNATS (Thymidylate synthase)

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