Table 4 Drugs that target production and transport of lactate

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