Table 3.
Summary of targeted therapies and their current developmental status in cancer treatment
| Cancer Type | Study model | Targeted Drug | Therapeutic Target Classification | Primary Target | Combination Strategy | Mechanism | Research Status | Refs. |
|---|---|---|---|---|---|---|---|---|
| Colorectal Cancer | MC38 | STM2457 (METTL3 inhibitor) | RNA Modification Modulator | METTL3 | Monotherapy (pre-treated BM-Mf and BM-MDSCs) | Epigenetic modulation | In vivo | [72] |
| SW480, HT29; AOM/DSS mouse | Nsun2-i4 (NSUN2 inhibitor) | RNA Modification Modulator | NSUN2 | Monotherapy or combination with anti-PD-1 therapy | Epigenetic modulation | In vitro and in vivo | [64] | |
| BALB/c; C57BL/6 mice; xenografts of HCT-116, RKO, and MC38 | METTL1-WDR4-IN-1, Shikonin (PKM2 inhibitor) | Combination Therapy | METTL1, PKM2, CD155 | Monotherapy or combination of METTL1-WDR4-IN-1 and Shikonin | Epigenetic & metabolic inhibition | In vivo | [77] | |
| HCT-116/5-FU, SW480/5-FU, SW620/5-FU; xenograft models | FX11 (LDHA inhibitor) | Metabolic Inhibitor | METTL3, LDHA | Monotherapy or combination of sh-METTL3 and FX11 | Epigenetic & metabolic inhibition | In vitro and in vivo | [81] | |
| HCT116, DLD1; CRC organoids, HCT116 xenografts, ApcMin/+ mice | Sirolimus (Rapamune ®), Temsirolimus (Torisel®, mTORC1 inhibitors) | Combination Therapy | METTL3, mTORC1 | Monotherapy or combination with sh-METTL3 | Epigenetic & signaling inhibition | In vitro and in vivo | [112] | |
| HCT116, DLD1; nude mice xenografts |
DAA (pan-methylation inhibitor) |
RNA Modification Modulator | METTL3 | Monotherapy | Epigenetic modulation | In vitro and in vivo | [86] | |
| Ocular Melanoma | 92.1, CRMM1 | Oxamate, 2-DG | Metabolic Inhibitor | Histone lactylation | Monotherapy | Metabolic inhibition | In vitro | [70] |
| OCM1, CRMM1, orthotopic xenograft mouse | 2-DG, Oxamate, LDHA/B siRNAs | Metabolic Inhibitor | Histone lactylation | Monotherapy | Metabolic inhibition | In vitro and in vivo | [17] | |
| HCC | Huh-7, HepG2 | C646 (p300 inhibitor) | Lactylation Inhibitor | Histone lactylation, p300 | Monotherapy | Epigenetic modulation | In vitro | [66] |
| Post-treatment surgical HCC samples; orthotopic xenograft | 2-DG, siIGF2BP3-loaded liposomes (si-LNPs) | Combination Therapy | IGF2BP3 | Combination of lenvatinib with 2-DG or siIGF2BP3-LNPs | Epigenetic & Post-translational Regulation | In vivo and clinical sample analysis | [74] | |
| HepG2, HCC-PDX mouse model | Cpd-5 (ALDOA inhibitor) | Metabolic Inhibitor | ALDOA | Monotherapy | Metabolic inhibition. | In vitro and in vivo | [79] | |
| ESCC | KYSE30 cell, KYSE30 xenograft | Stiripentol (Diacomit®, LDHA inhibitor), Elesclomol (copper ionophore) | Lactylation Inhibitor | LDHA, NUDT21, FDX1 | Combination of Stiripentol with Elesclomol | Post-translational Regulation | In vitro and in vivo | [75] |
| APL | NB4-R1, NB4-R2; BALB/c nude mouse xenograft model | GRh2 (histone deacetylase inhibitor) | Lactylation Inhibitor | Histone lactylation | Monotherapy or combination with ATRA | Epigenetic modulation | In vitro and in vivo | [116] |
| Gastric Cancer | HGC-27; xenograft mouse model | Elesclomol (cuproptosis inducer), AGK2 (SIRT2 inhibitor) | Delactylation Inhibitor | METTL16 | Combination of elesclomol and AGK2 | Post-translational Regulation | In vitro and in vivo | [73] |
| LUAD | CDX models, PDX models, and KPE mouse model |
DAA (pan-methylation inhibitor), 2-DG, ENOblock (ENO inhibitor) |
Combination Therapy | m6A, ENO1 | Monotherapy | Epigenetic & metabolic inhibition | In vivo | [100] |
| Leukemia | NOMO-1, U937 | R-2HG | RNA Modification Modulator | FTO | Monotherapy | Metabolic inhibition | In vitro | [99] |
| TNBC | 4T1 tumor-bearing mice |
Remodelin (NAT10 inhibitor) |
RNA Modification Modulator | NAT10 | Monotherapy or combination with anti-CTLA-4 | Epigenetic modulation | In vivo | [111] |
| ICC | HCCC-9810, HuCC-T1; HuCC-T1 allografts in nude mice | STM2457 (METTL3 inhibitor) | RNA Modification Modulator | METTL3 | Monotherapy or combination with Gemcitabine | Epigenetic modulation | In vitro and in vivo | [113] |
| Melanoma | B16 cells; B16 mouse | ALK-04 (ALKBH5 inhibitor) | RNA Modification Modulator | ALKBH5 | Monotherapy or combination with GVAX and anti-PD-1 | Epigenetic modulation | In vitro and in vivo | [88] |