Repositioning Candidate Details
| Candidate ID: | R0964 |
| Source ID: | DB06266 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Lonidamine |
| Synonyms: | 1-(2,4-dichlorbenzyl)-indazole-3-carboxylic acid; DICA; diclondazolic acid; Doridamina; Lonidamine |
| Molecular Formula: | C15H10Cl2N2O2 |
| SMILES: | OC(=O)C1=NN(CC2=C(Cl)C=C(Cl)C=C2)C2=C1C=CC=C2 |
| Structure: |
|
| DrugBank Description: | 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 impair energy-requiring processes, as recovery from potentially lethal damage, induced by radiation treatment and by some cytotoxic drugs. |
| CAS Number: | 50264-69-2 |
| Molecular Weight: | 321.158 |
| DrugBank Indication: | Investigated for use/treatment in benign prostatic hyperplasia, prostate disorders, and cancer/tumors (unspecified). |
| DrugBank Pharmacology: | -- |
| DrugBank MoA: | 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. |
| Targets: | Cystic fibrosis transmembrane conductance regulator; Hexokinase-1 |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S03 | Anti-fibrosis | fibrosis | Angiotensin Receptor Blocker (ARB); CCR2/CCR5 antagonist; Thyroid receptor β agonist; PEGylated human FGF21 analogue; Monoclonal antibody to lysyl oxidase-like 2 (LOXL2); Galectin-3 inhibitor; FGF19 variant | Losartan; Cenicriviroc; VK-2809; MGL-3196; Pegbelfermin; Simtuzumab; GR-MD-02; NGM282 | Details |
| S13 | Anti-apoptosis | hepatocyte apoptosis; hepatic autophagy; apoptosis | Pan-caspase inhibitor | Emricasan | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class |
|---|