Table 4.

Drugs that target production and transport of lactate

Molecule	Target	Mechanism	Condition	Clinical trial
AZD3965	Lactate transporters	Inhibits MCT1/2	Malignant tumor	Phase I Trial
α-Cyano-4-hydroxycinnamate	Lactate transporters	Inhibits MCT1/2	Hyperglycolytic malignancies	N/A
AR-C155858	Lactate transporters	Inhibits MCT1/2	Hyperglycolytic malignancies	N/A
Syrosingopine	Lactate transporters	Inhibits MCT1/4	Malignant tumor	N/A
Meplazumab	CD147	Inhibits the distribution of MCT1/4 on cell membrane	Malignant tumor, COVID-19	Phase I Trial
Stiripentol	LDH	Inhibits LDH	Epilepsy, Dravet Syndrome	Approved by FDA
Galloflavin	LDH	Binds the free enzyme	Malignant tumor	N/A
N-hydroxyindoles	LDH	Compete with pyruvate and NADH	N/A	N/A
AT-101 (gossypol)	LDH	Inhibits LDH	Malignant tumor	Phase II Trial
FX-11	LDH	Inhibits LDH-A	Pancreatic cancer	N/A
GSK2837808A	LDH	Inhibits LDH-A	N/A	N/A
Vitamin C	LDH	Inhibits LDH-A	Breast cancer	N/A
2-DG	HK	Inhibits glycolysis by competing with glucose	Malignant tumor	Dose Escalation Trial, Phase I/II Trial
DCA	PDK	Increases glucose uptake into mitochondria	Malignant tumor, Lactic acidosis	Phase I/II Trial
Lonidamine	HK	Inhibits glycolysis	Malignant tumor	Phase II Trial

Notes: N/A not available