Lonidamine (LND) is a drug that interferes with energy metabolism of cancer cells, principally inhibiting aerobic glycolytic activity, by its effect on mitochondrially-bound hexokinase (HK). In such way LND could... In such way LND could impair energy-requiring processes, as recovery from potentially lethal damage, induced by radiation treatment and by some cytotoxic drugs.
- Mechanism
- Curator reviewed
Lonidamine is an orally administered small molecule that inhibits glycolysis by the inactivation of hexokinase. Hexokinase is an enzyme that catalyzes glucose, the first step in glycolysis. The inhibition of hexokinase by lonidamine is well established. In addition, there is evidence that lonidamine may increase programmed cell death. This stems from the observation that mitochondria and mitochondria-bound hexokinase are crucial for induction of apoptosis; agents that directly effect mitochondria may, therefore, trigger apoptosis. Indeed, in vitro models with lonidamine exhibit the hallmarks of apoptosis, including mitochondrial membrane depolarization, release of cytochrome C, phosphatidylserine externalization, and DNA fragmentation. [PMID: 16986057]
- Primary indication
- Investigated for use/treatment in benign prostatic hyperplasia, prostate disorders, and cancer/tumors (unspecified).Curator reviewed
- Formula / weight
- C15H10Cl2N2O2 · 321.158 g/mol (avg)
- Also known as
- DICA · diclondazolic acid · Doridamina
Resolves to
WDRYRZXSPDWGEB-UHFFFAOYSA-NSMILESOC(=O)C1=NN(CC2=C(Cl)C=C(Cl)C=C2)C2=C1C=CC=C2What you can answer from here — as of February 21, 2021
Which drugs share a target with Lonidamine, and which of those have an active Phase 3 trial?
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