Table 5 Metabolism-targeted drugs
From: TGF-β signaling in the tumor metabolic microenvironment and targeted therapies
Strategy | Agent | Experiment status | Application | Cancer biological behavior | Clinical trial/Ref. |
|---|---|---|---|---|---|
GLUTs inhibitor | Silybin | Phase II; In vivo mouse model | Prostate cancer | Suppressed cancer growth | NCT00487721 [271] |
Rapaglutin A | In vivo mouse model; in vitro human cell culture | Breast cancer | Suppressed cancer growth | [272] | |
HK II inhibitor | Metformin | Phase II | Breast cancer | Inhibited cancer cell proliferation | NCT01266486 [273] |
2-deoxyglucose | Phase I/II | Prostate cancer | Inhibited cancer growth | NCT00633087 [274] | |
3-Bromopyruvate | In vitro human cell culture | Liver cancer | Inhibited cancer growth | [275] | |
CAV-1 inhibitor | Methyl-β-cyclodextrin | In vitro human cell culture | Colorectal cancer | Increased the BITC-induced anti-cancer effect | |
MCT-1 inhibitor | AZD3965 | Phase I | Lymphoma | Inhibited cancer growth | NCT01791595 [277] |
PDK inhibitor | Dichloroacetate | Phase I; In vitro human cell culture | Advanced solid tumor | Reduced tumor growth and enhanced Adriamycin cytotoxicity | |
Hordenine | In vitro human cell culture | Lung cancer | Decreased cancer cell proliferation | [280] | |
IDH inhibitor | Ivosidenib (AG-120) | Phase I | Brain cancer | Inhibited tumorigenesis | NCT02073994 [281] |
Ivosidenib (AG-120) | Phase III | Cholangiocarcinoma | Reduced tumor growth | NCT02989857 [282] | |
Enasidenib | Phase I/II | Leukemia | Inhibited cancer growth | ||
Olutasidenib (FT-2102) | Phase I/II | AML | Suppressed tumor growth | ||
Vorasidenib (AG-881) | Phase I | Glioma | Acquired complete remission | NCT02481154 [287] | |
HIF-1α inhibition | Apigenin | Phase I | Ovarian, prostate and breast cancer | Downregulated tumor angiogenesis | |
Semaxanib (SU5416) | Phase II | Metastatic melanoma | Reduced tumor metastasis | NCT00017316 [293] | |
2-Methoxyestradiol | Phase I; Phase II | Prostate, breast, brain, head and neck cancer and liver cancer | Inhibited tumor growth and angiogenesis | ||
PX-478 | Phase I | Solid tumors and Lymphoma | Enhanced radiosensitivity and suppressed tumor growth | ||
BAY 87-2243 | Phase I | Neoplasms | Impaired OXPHOS and reduced cancers growth | ||
OXPHOS inhibition | Lonidamine | Phase II; In vivo mouse model | Glioma | Limited tumor growth | |
G6PD inhibitor | Dehydroepiandrosterone | Phase I | Breast cancer | Increased the number of monocytes and NK cells | NCT00972023 [305] |
Polydatin | In vitro human cell culture | Breast cancer | Increased cancer cell autophagy and lapatinib effect on breast cancer cells | [306] | |
GSK-3 inhibitor | Lithium chloride | In vivo mouse model; in vitro human cell culture | Pancreatic and breast cancers | Enhanced autophagy and apoptosis in cancer cells and reduced cancer growth | [307] |
PGAM1 inhibitor | HKB99 | In vivo mouse model | NSCLC | Suppressed tumor growth and metastasis | [308] |
PGMI-004A | In vivo mouse model | NSCLC | Attenuated cell proliferation and tumor growth | [309] | |
ACSLs inhibition | Triacsin C | In vitro human cell culture | Colon and breast cancers | Decreased cell proliferation and chemotherapy resistance | |
ACAT-1 | Avasimibe | In vitro human cell culture | Ovarian cancer | Enhanced chemosensitivity to cisplatin treatment | [312] |
FASN inhibitor | C75 | FDA approved | NSCLC | Reduced tumor growth | |
TVB-2640 | Phase II | NSCLC, ovarian, and breast cancer | Inhibited cancer growth | NCT02223247 [315] | |
Cerulenin | In vitro human cell culture | Lung cancers | Blocked cancer cell proliferation | [316] | |
HMGCR inhibitor | Fluvastatin | In vivo mouse model | NSCLC | Inhibited cancer growth | [317] |
GLS inhibitor | Telaglenastat (CB-839) | In vivo mouse model | Melanoma | Improvement in tumor growth inhibition with anti-PD1 and anti-CTLA4 antibodies | [318] |
Withangulatin A derivative 7 | In vivo mouse model | Breast cancer | Inhibited cancer growth | [319] |