Drug intelligence / Profile preview

lobaplatin + 5-fluorouracil + leucovorin

Development stage
Unknown
Lead developer
Degussa
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

The combination of lobaplatin, 5-fluorouracil (5-FU), and leucovorin is a chemotherapy regimen that has been studied for various cancer types. This combination leverages the synergistic effects of these three agents to enhance anti-tumor activity. It has shown promising anti-tumor activity with tolerable toxicity when used as a first-line treatment strategy in patients with locally advanced nasopharyngeal carcinoma (LA-NPC). In a study involving 59 patients with stage III-IVa-b NPC, this combination achieved objective response rates of 88.1% after induction chemotherapy and 100% after concurrent chemoradiotherapy. With a median follow-up period of 44 months, the 3-year estimated progression-free survival and overall survival were 86.4% and 94.9%, respectively. The regimen typically involves doses of lobaplatin (e.g., 30 mg/m² on days 1 and 22, and 50 mg/m² on days 43 and 64) combined with continuous intravenous 5-fluorouracil (e.g., 4 g/m² over 120 hours), often administered alongside radiation therapy. The most common grade 3-4 toxicities observed were neutropenia and thrombocytopenia. Lobaplatin itself is noted for potent antineoplastic activities with advantages like no significant nephrotoxicity or neurotoxicity and no cross-resistance with cisplatin.

02

Targets

DNATS (Thymidylate synthase)

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