Table 1.
Diverse drugs that target LDHA
| Mechanism of action | LDHA inhibitor | Cancer | Clinical trials | Drawbacks | References |
|---|---|---|---|---|---|
| Pyruvate‐competitive | Oxamate | Gastric cancer; cervical cancer | No | Limited membrane permeability | 110, 111 |
| NADH‐competitive | Gossypol | Melanoma; lung cancer; breast cancer; cervical cancer; leukemia; glioma; adrenal cancer | Yes | Non‐specific toxicity | 112, 113, 114, 115, 116, 117, 118 |
| FX11 | B‐lymphoma; pancreatic cancer | No | Highly reactive catechol portion of this molecule | 3, 5, 120 | |
| Quinoline 3‐sulfonamides | Hepatocellular carcinoma | No | Low clearance in the body and incompatible with oral bioavailability | 55 | |
| Pyruvate and NADH competitive | NHI | Pancreatic ductal adenocarcinoma; cervical cancer | Unknown | Unknown | 9, 120, 121 |
| Binding the free enzyme | Galloflavin | Breast cancer; hepatocellular carcinoma | Unknown | Unknown | 122, 123, 124 |