Table 2 Onco-therapeutic drugs targeting lactate metabolism/lactylation

From: Lactate and lactylation in cancer

Target	Drug name	Reserch status	Applications	Mechanism	Ref/Trial No.
LDHA	AT-101(Gossypol) and its derivative e.g., FX-11	Preclinical	Pancreatic cancer, breast cancer, adrenocortical carcinoma, and lymphoma	Lactate anabolism	^{26,34,188,382,383,498}
LDHA	oxamate	Preclinical	NSCLC, melanoma	Lactate anabolism	^190,389,391
LDHA	GSK2837808A	Preclinical	Melanoma	Lactate anabolism	³⁹²
LDHA	GNE-140	Preclinical	Pancreatic cancer	Lactate anabolism	³⁸⁵
LDHA	Zinc	Preclinical	Melanoma	Lactate anabolism	³⁹⁴
LDHA	NHI-Glc-2	Preclinical	NSCLC and gastric cancer	Lactate anabolism	³³⁴
LDHA	LncRNA GLTC	Preclinical	PTC	Lactate anabolism	³⁹³
LDHA/B	NCI-006	Preclinical	Pancreatic cancer	Lactate anabolism	³⁸⁶
LDHA/B	MS6105	Preclinical	Pancreatic cancer	Lactate anabolism	³⁸⁷
MCT	CHC	Preclinical	Breast cancers	Lactate anabolism	^342,343,344
MCT1/2	AR-C155858 (SR13801)	Preclinical	Breast cancers, B-cell lymphoma	Lactate anabolism	^397,398,499
MCT1/2	AZD3965	Clinical trial	Advanced solid cancers (NSCLC, SCLC, prostate, gastric, breast cancers), Burkitt’s lymphoma and diffuse large B-cell lymphoma	Lactate excretion	NCT01791595^{76,79,178,334,344,398,496}
MCT1	AZ3965	Preclinical	CRC, melanoma	Lactate excretion	⁴⁰⁰
MCT1	AR-C122982 (SR13800)	Preclinical	Burkitt lymphoma cell, neuroblastoma	Lactate excretion	^399,500
MCT1	BAY8002	Preclinical	HCC, some solid cancers	Lactate excretion	⁴⁰⁰
MCT4	AZ93	Preclinical	CRC, melanoma	Lactate excretion	⁴¹⁰
MCT4	ALK-04	Preclinical	Melanoma	Lactate excretion	⁴⁹²
MCT1/4	Syrosingopine	Preclinical	HCC, lung cancer, hematologic malignancies, breast cancer	Lactate excretion	^166,501,502
MCT1/4	7ACCs	Preclinical	Cervix cancer, breast cancer, CRC	Lactate excretion	^102,503
CD147	AC-73	Preclinical	HCC, AML	CD147-MCT interaction	^413,504
CD147	metuzumab	Preclinical	LUAD, NSCLC	CD147-MCT interaction	⁴¹⁴
Lactate	LOx	Preclinical	Breast cancer, melanoma, GBM, HCC	Lactate catabolism	^{418,419,420,421,422,423,424,425,428,429,430,431,495}
Lactate	NaHCO₃	Preclinical	NSCLC, breast cancer	Lactate catabolism	^434,494
Lactate	nanoCaCO₃	Preclinical	Βreast cancer	Lactate catabolism	⁴³⁵
Lactate	CoMnFe-LDO	Preclinical	UM	Lactate catabolism	⁴⁹³
GLUT1	BAY876	Preclinical	Breast cancer, GBM	Lactate anabolism	^432,505
Pyruvate	UK5099. POx	Preclinical	Breast cancer	Pyruvate catabolism	⁴³³
Lactylation	BML	Preclinical	HCC	Histone modification	²²⁵
Lactylation	RJA	Preclinical	HCC	Histone modification	²²⁶
Lactylation	K673-pe	Preclinical	CRC	Non-histone modification	²⁴³
Lactylation	D34-919	Preclinical	GBM	Non-histone modification	^244,436
Lactylation	anti-APOC2^K70-lac antibody	Preclinical	NSCLC	Non-histone modification	¹⁸¹
Lactylation	β-alanine	Preclinical	CRC	Non-histone modification	²³⁹
Lactylation	MG149	Preclinical	CRC	Non-histone modification	²⁴⁰

AML acute myeloid leukemia, CD147 cluster of differentiation 147, CRC colorectal cancer, GBM glioblastoma, GLUT1 glucose transporter 1, HCC hepatocellular carcinoma, LDHA lactate dehydrogenase A, LUAD lung adenocarcinoma, MCT monocarboxylate transporters, MCT1 monocarboxylate transporter 1, MCT2 monocarboxylate transporter 2, MCT4 monocarboxylate transporter 4, NSCLC non-small cell lung cancer, SCLC small cell lung cancer, UM uveal melanoma

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Table 2 Onco-therapeutic drugs targeting lactate metabolism/lactylation

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