Drug intelligence / Profile preview

cyclophosphamide + doxorubicin + lomustine + lonidamine + methotrexate

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of five agents: - Cyclophosphamide (an alkylating agent) - Doxorubicin (an anthracycline antibiotic) - Lomustine (a nitrosourea alkylating agent, also known as CCNU) - Lonidamine (an antineoplastic that inhibits energy metabolism in tumor cells) - Methotrexate (an antimetabolite and antifolate) The combination has been studied primarily for the treatment of advanced non-small cell lung cancer. The rationale is to combine multiple cytotoxic mechanisms with the metabolic inhibition provided by lonidamine, which may potentiate anticancer activity without significantly increasing toxicity. Each component acts via a distinct mechanism to inhibit DNA synthesis or function, disrupt cell division, or impair tumor cell metabolism. Toxicities are generally predictable based on the individual drugs and include gastrointestinal, hematologic, oral mucosal, renal, cardiac effects from the cytotoxics; and myalgia, asthenia, testicular pain and mild visual/gastric intolerance from lonidamine[1][3].

Other names
MACC plus lonidamine
02

Targets

DNATOP2A (DNA topoisomerase II)DHFR (Dihydrofolate reductase)

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